CA2131495C	Double-layered oxcarbazepine tablets	The invention relates to colour-stable tablets for the therapeutic drug oxcarbazepine, which tablets are provided with a hydrophilic, permeable layer containing white pigments and a hydrophilic, permeable outer layer containing white pigments in combination with iron(II) oxide pigments.
CA2166003C	Method for providing nutrition to the elderly patients	The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
CA2180008C	Cyclopentane(ene) heptenoic or heptanoic acids and derivatives thereof useful as therapeutic agents	The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group.  The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
CA2278056C	Gemcitabine derivatives	The invention provides Gemcitabine esters or amides in which the 3'- and/or 5'-OH group and/or the N4-amino group is derivatised with a C18- and/or C20- saturated or mono-unsaturated aryl group, preferably an acyl group selected from oleoyl, elaidoyl, cis-icosenoyl and trans-eicosenoyl. The Gemcitabine esters and amides are useful as anti-cancer and anti-viral agents.
CA2315829C	Angiostatic agents and compositions for controlling ocular hypertension	Compositions of angiostatic agents for treating GLC1A glaucoma and methods for their use are disclosed.
CA2362082C	2-n-substituted or unsubstituted-2-amino-5-methylpiperidine-3,4-diols and process for the preparation thereof	This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): (see formula I) wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower .omega.-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof.   Said compound can be prepared from a (2S,3S,4R)-5-N--protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.
CA2601963A1	Method of enriching glucoraphanin in radish seed preparations	The present invention relates to chemoprotective compounds and a method for producing chemoprotectant precursor-enriched extracts from crucifer seeds. More particularly, a method is provided for producing chemoprotectant precursor-enriched extracts from radish seeds with increased ratio of glucoraphanin to glucoraphenin. The general method comprises preparing an aqueous extract, contacting the aqueous extract with an adsorbent, removing the adsorbent to obtain a glucosinolate-containing extract, drying the glucosinolate-containing extract to obtain a dried glucosinolate-containing extract, mixing at least a portion of the dried glucosinolate-containing extract with a solvent to form a glucosinolate-containing suspension, clarifying the glucosinolate-containing suspension, contacting the glucosinolate-containing suspension with a catalyst, and introducing hydrogen for a time sufficient to obtain a chemoprotectant precursor-enriched extract. The chemoprotectant precursor-enriched extracts may be further processed to form a chemoprotectant precursor-enriched isolate or processed for use in various applications, including incorporation into a variety of food products and pharmaceuticals.
CA2605854C	Novel pyridine derivative and pyrimidine derivative (3)	A compound represented by the general formula: (I) (wherein R1 means a 3- to 10-membered nonaromatic heterocyclic group or the like; R2 and R3 mean a hydrogen atom; R4, R5, R6 and R7 are the same or different and mean a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like; R8 means a hydrogen atom or the like; R9 means a 3- to 10-membered nonaromatic heterocyclic group or the like; n means an integer of 1 to 2; and X means a group represented by the formula -CH= or a nitrogen atom), a salt thereof or a hydrate thereof has an excellent hepatocyte growth factor receptor (HGFR) inhibitory action, and exhibits an anti-tumor action, angiogenesis inhibitory action or cancer metastasis inhibitory action.
CA2647981A1	19-nor-vitamin d analogs with 1,2,or 3,2 heterocyclic ring	19-nor-vitamin D analogs having an additional heterocyclic ring connecting the 3.beta.-oxygen and carbon-2 or the 1.alpha.-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit significant activity in mobilization of bone, making them therapeutic agents for the treatment or prophylaxis of osteoporosis, osteomalacia, osteopenia, renal osteodystrophy and hypoparathyroidism.
CA2711839A1	Method of treatment with potentised stereoisomer of glutamate	The present invention relates to a method of treatment, in particular to a method of treating an effect of glutamate or glutamic acid by administering a dilution or an ultra-high dilution or potentised preparation of glutamic acid or glutamate.
CA2755954A1	Quaternary quinuclidine derivatives and their use as muscarinic receptor antagonists	Compounds of formula I   (see formula I) and pharmaceutical compositions comprising same are disclosed. The compounds of the invention are muscarinic acetylcholine receptor antogonists which can be used in the treatment of a muscarinic acetylcholine receptor mediated disease.
CA2783468A1	Ppar-sparing thiazolidinedione salts for the treatment of metabolic diseases	The present invention relates to novel salts of thiazolidinediones of compounds of formula I and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).
CA2804173A1	Sulfonamide nav1.7 inhibitors	The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
CA2851513A1	Method for treating acute kidney injury	The present invention provides methods for treating acute kidney injury through introduction of one or more drag reducing polymers, oligomers, and/or monomers, as well as compositions that include therapeutic amounts of one or more of these drag reducing polymers, oligomers, and/or monomers. These compositions may also include additional components that enhance at least one of the stability, effectiveness, or administerability of the polymers, oligomers, and/or monomers - such as buffers, anti¬ oxidants, and enzyme inhibitors.
CN101199499A	Active controlled-release contraceptive emulsion	The invention discloses available sustained release contraceptive film, which selects nonoxynol-9 as the effective component to prepare multilayer compound herbal membrane. The invention has the characteristics of fast percutaneous absorption, good permeability and gradually drug releasing with double functions of availability and sustained releasing. The invention does not cause the skin to be allergic with advantages of long effect, absorption by the skin and convenient carrying and using.
CN101209250A	Compound lignocaine emulsifiable paste and preparing technique	The invention provides a compound lidocaine cream and the preparation technique. The invention selects a new cream formulation and technique. The product which is prepared by the technique has stable quality, the formulation and the technique are reasonable and stable, and the method overcomes the shortcomings of the original technique and can meet the needs of industrial large-scale production. The product of the invention can shorten the anesthesia time when in clinical use, thus greatly reducing the waiting time of the patients and being much easier to be accepted by the patients.
CN101301396A	Medicament for treating oral ulcer of children and preparation thereof	The invention discloses a medicine for treating children stomatocace and a method for preparing the same. The medicine is mainly prepared by the following components of the yellow-corktree bark, the dried rehmannia root, the figwort root, the honeysuckle, the fiveleaf akebia, the Chinese goldthread and the root-bark of tree peony according to a certain proportioning by weight. The medicine of the invention has the functions of resolving heat, removing toxins, diminishing inflammation, killing bacteria, cooling blood and promoting wound healing and is mainly used to treat the children stomatocace with fast effect and high cure rate.
CN101397132A	Water-soluble fullerenes derivates, composition and application thereof in preparation of medicament for inhibiting tumor growth and metastasis	The invention provides a water-soluble fullerene derivative, composite and the applications in the preparation process of medicament used for inhibiting growth and transfer of tumor; the derivative is fullerols presented by a general formula: C60OxHy; wherein, y is more than 10 and less than or equal to x; x is less than 50 and more than or equal to y; alternatively, the derivative is fullerene carboxyl derivative presented by the general formula C60(C(COOH)2)n; wherein, n is equal to 1-3; the tumor inhibiting composite comprises the grains of the water-soluble fullerene derivative and pharmaceutically acceptable carrier. The invention has the advantages that: compared with cyclophosphamide, cisplatin, paclitaxel, and the like, which are generally applied to clinic at present; the fullerols and carboxylic fullerene nano grains have small dosage, low toxicity and can inhibite the growth and transfer of the tumor.
CN101422445A	Preparation method and use of pidotimod effervescent tablets	The invention discloses a preparation method of an effervescent tablet containing pidotimod, as well as application thereof. The invention belongs to the new technical field of medicament and relates to a new preparation formulation of pidotimod, which is used for curing (1) recurrent upper and lower respiratory infection (pharyngitis, tracheitis, bronchitis and amygdalitis); (2) recurrent infection in otorhinolaryngology (rhinitis, nasosinusitis and otitis); (3) urinary system infection; (4) gynae infection; and (5) the clinic patients with weakened cellular immune function after chemo-treatment. The invention is used for reducing the times of acute attack, shortening the course of disease and lightening the attack degree; moreover, the invention can also be used for the auxiliary treatment of antibiotics during acute infection. The new preparation formulation is characterized in that the product is the effervescent tablet, which contains sodium bicarbonate and organic acid and can generate gas when meeting water to become effervescent.
CN101485813B	Soft capsule for beauty treatment and preparation method thereof	The invention mainly relates to a soft capsule for cosmetology and a method for preparing the same. The soft capsule for the cosmetology has main characteristics that the soft capsule comprises the following raw materials in portion by weight: 360 to 460 weight portions of siritch, 20 to 25 weight portions of red deer blood meal, 15 to 20 weight portions of aloe, 5 to 10 weight portions of red deer fetus, 15 to 20 weight portions of safflower, and 0.7 to 1 weight portion of lycopene. The soft capsule adopts a compound form, elaborately selects materials, has a precise formulation, pursuits the whole to improve human condition, and fully regulates physical condition in terms of improving immunity, replenishing and activating blood, improving cardiovascular function, loosening bowel to relieve constipation, resisting oxidation, balancing nutrition, and the like. With the soft capsule, the human body has smooth qi and blood circulation, normal metabolism, and balance between yin and yang; therefore, beauty can be endowed on shape. People strives to shape beauty in health, the soft capsule makes people vigorous and full of energy, makes skin whitening and fine, and makes people full of confidence and have elegant quality so as to achieve harmony and unity of soul and external beauty. The red deer blood and the red deer fetus strengthen immunity, tonify qi, replenish blood, and strengthen tendon and bones; the safflower and the siritch active blood, remove blood stasis, soften blood vessels, and protect heart; the aloe and the lycopene shield sun, eliminate inflammation, fade brown, resist oxidation, purge bowel and defaecate; the aloe cal also balance the dryness of the red deer blood and the red deer fetus; pollen, pearl and radix angelicae formosanae improve nutrition balance, whiten skin, increase skin moisture and are natural cosmetic excellent products; and a formulation improves physical condition on the whole and shapes healthy beauty consistent with inside and.
CN101703672A	Yellow wine capable of clearing heat, resolving toxin, and preventing and treating cold and production method thereof	The invention discloses yellow wine capable of clearing heat, resolving toxin, and preventing and treating cold and a production method thereof. The yellow wine consists of the following raw materials: garlic, vitamin C, Mongolian dandelion herb, perilla leaf, raw licorice root, brown sugar and yellow wine. In the production method, the yellow wine is prepared according to the components and processes.
CN101732718A	Pharmaceutical composition containing NCX inhibitors	The invention relates to a pharmaceutical composition which contains NCX inhibitors, at least one medicine for treating cardiovascular and cerebrovascular diseases and a pharmaceutically acceptable carrier. The invention also relates to a medicine box containing the active matter. The pharmaceutical composition or the medicine box is used for preventing, delaying or treating the following diseases or symptoms of hypertension, salt-sensitive hypertension, renal hypertension, essential hypertension, pregnancy induced hypertension, hypertension complications, diabetes, diabetic complications, dyslipidemia, ischemic diseases, coronary heart disease, angina, congestive heart failure, arrhythmia, cerebral apoplexy, arteriosclerosis, cerebral infarction, cerebrovascular diseases, cardiovascular diseases, coronary artery diseases, sexual dysfunction, cognitive dysfunction, ventricular dysfunction, pulmonary vascular diseases and renal vascular diseases, lowering the morbidity and/or the mortality of cardiovascular and cerebrovascular diseases, reducing the adverse reactions and simultaneously improving the medicine taking compliance of patients.
CN101804058A	Medicament for preventing mammitis of dairy cattle during nonlactating and preparation method thereof	The invention discloses a breast injection medicament for preventing mammitis of dairy cattle during nonlactating and a preparation method thereof. The medicament comprises procaine benzylpenicillin, norfloxacin, trimethoprim, Span 89, polyglycerol esters of fatty acids, proply gallate, Vaseline and medical plant oil.
CN101810695A	Pilatory for preventing trichomadesis	The invention discloses a pilatory for preventing trichomadesis. The pilatory comprises the following components in parts by weight: 2-4 quinine sulfate, 5-10 linalool, 4-6 phenethyl alcohol, 1-3 cinnamyl alcohol, 3-6 geraniol, 30-40 glycerol, 30-40 otto, 10-20 eugenol, 23,00-25,00 ethanol and 80-100 distilled water. The invention has favorable using effects of remarkably controlling the trichomadesis, promoting the metabolism and the circulation of hairs, enhancing the vitality of the hairs, supplementing the nutrient, recovering the growth speed of the hairs, firming hair roots, deepening hair follicle to remove grease, inhibiting sebaceous gland, allowing the hairs to newly grow and enabling people to feel cool during use; in addition, the invention has favorable therapeutic effects for seborrheic alopecia, alopecia areata, mixed trichomadesis, postpartum alopecia and the like.
CN101822637A	Beta-lactam antibiotics-containing suspension injection	The invention discloses a beta-lactam antibiotics-containing suspension injection and a preparation process thereof. In the preparation process, the beta-lactam antibiotics are uniformly mixed and suspended in a solvent by a special process; and the beta-lactam antibiotics-containing suspension injection has good dispersibility and high bioavailability, and provides a feasible path for the expanded production.
CN101843632A	Application of miR-145 in preparing medicament for treating inflammation	The invention belongs to the field of biomedicine and relates to application of micromolecule RNA (Ribonucleic Acid) in preparing a medicament, in particular to action of miR-145 for treating inflammatory metabolic diseases including diabetes. Proved by a test, in the invention, under the conditions of high glucose and high fat, micro RNA participates in generation and development of inflammation lesions of metabolic diseases including diabetic vascular lesions and can be used for preparing a medicament for treating inflammation, in particular to preparing a medicament for treating the inflammatory metabolic diseases including the diabetes and a preparation for detecting the diabetes. The miR-145 can be used as a detection index of a diabetics and as a treatment target spot of inflammatory diseases including diabetic macroangiopathy.
CN101897685A	Composition containing sibutramine and fibrate lipid-lowering drugs	The invention relates to a drug composition containing sibutramine hydrochloride, fibrate lipid-lowering drugs and a pharmaceutically acceptable carrier. The invention also relates to application of the drug composition to preparing the drugs for treating obesity associated with hyperlipidemia. The invention belongs to the pharmaceutical field.
CN101921182A	Method for extracting and purifying 5-O-methyl-myo-inositol in plants	The invention relates to a new method for extracting and purifying 5-O-methyl-myo-inositol and has the advantages of short course, low cost, simple and convenient operation, high efficiency and the like. The method is suitable for large-scale industrialized production.
CN101966155A	Preparation of hollow liquid crystal microspheres of psoralen	The invention relates to a preparation method of pharmaceutical carriers, which is mainly used in pharmacotherapy of stomach tissue diseases. A preparation method comprises the following steps of: firstly, preparing hollow microspheres: dissolving the medicaments and other materials in a solvent system consisting of ethanol and dichloromethane, uniformly mixing and adding into a PVA (Polyvinyl Alcohol) solution with a certain concentration, mixing for a certain time, collecting the microspheres and performing vacuum drying; then coating the hollow microspheres prepared: dissolving a coating material of glyceryl monooleate (GMO) in petroleum ether or ethanol; then performing fluidized bed coating for the hollow microspheres or adding the hollow microspheres into an organic solvent to stir for a certain time, filtering and performing vacuum drying; and then obtaining the hollow liquid crystal microspheres. The hollow liquid crystal microspheres prepared has good floating property and adhesivity. The preparation method is simple and easy to operate and the organic solvent is easy to volatilize, thereby the preparation method is suitable for the demand of industrial production.
CN101966199A	Application of campanumoea polysaccharide in preparation of medicament and health care food	The invention discloses application of campanumoea polysaccharide in preparation of medicament and health care food, which relates to the technical field of medicine and health care. The campanumoea polysaccharide is characterized by being used for preparing medicament and medicinal preparation for promoting functional recovery after various medical, surgical and obstetric operations and during tumor chemotherapy and burn/scald treatment, and preparing health care food or health care additives with health care effect on metabolism reduction, valetudinarianism, gastrointestinal function decline, inappetence and low immunity. Moreover, the prepared medicament and food have the characteristics of high efficiency, no toxicity and high safety.
CN101979002A	Process for preparing quick-response cough-relieving capsules	The invention discloses a process for preparing quick-response cough-relieving capsules. The process comprises the following steps of: adding 75 percent ethanol in an amount which is 10 times that of poppy shells; soaking for 0.5 hour; refluxing and extracting for 1.5 hours twice; filtering and merging filtrate; recovering the ethanol; concentrating under a reduced pressure to obtain thick paste with the relative density of 1.25 to 1.28 (80 DEG C); adding water into decoction dregs of the poppy shells and other six medicaments such as ephedra, bitter apricot seed and the like to obtain a mixture; decocting the mixture for three times, namely adding the water in an amount which is 10 times that of the mixture for the first time, soaking for 2 hours and decocting for 1.5 hours; adding the water in an amount which is 8 times that of the mixture for the second time, and decocting for 1.5 hours; adding the water in an amount which is 8 times that of the mixture for the third time, and decocting for 1 hour; filtering and merging the filtrate; concentrating the filtrate under the reduced pressure to obtain the thick paste with the relative density of 1.25 to 1.28 (80 DEG C); merging the thick paste; drying under the reduced pressure at the temperature of 50+/-5 DEG C; crushing and screening by using a VI screen; granulating by using 95 percent ethanol; drying; blending in batches; and filling into size-zero capsules to obtain the quick-response cough-relieving capsules. The process has easily controlled production conditions and is suitable for industrial production.
CN102008439B	Curcumin coated liposome preparation and preparation method thereof	The invention relates to a curcumin coated liposome preparation and a preparation method thereof. The curcumin coated liposome preparation consists of curcumin, phospholipids, cholesterol, water-soluble vitamin E and trimethyl chitosan, and can be prepared into freeze-dried powder applied to oral administration. The gastrointestinal absorption efficiency of the curcumin coated liposome is significantly higher than that of the traditional curcumin liposome preparation, so the curcumin coated liposome further improves the oral absorption of the curcumin and improve the oral bioavailability.
CN102068415A	Carbazole sulfonamide anti-tumor medicine dispersible tablets and preparation method thereof	The invention belongs to the field of pharmaceutic preparation and relates to a method for preparing anti-tumor preparations, in particular to carbazole sulfamide-derived anti-tumor medicine dispersible tablets and a preparation method thereof. The invention is characterized in that lactose and beta-cyclodextrin are mixed with a carbazole sulfamide-derived medicine such as N-(2, 6-dimethoxypyridine-3-substituted)-9-methyl carbazole-3-sulfamide, for mixing, and the mixture is ground to micro powder and prepared into the dispersible tablets. Therefore, the dissolution rate of the dispersible tablets can be increased.
CN102210701A	Application of hydrogen-saturated normal saline in preparation of medicine for treating hyperlipidemia disease	The invention relates to application of hydrogen-saturated normal saline in preparation of a medicine for treating a hyperlipidemia disease, and further provides application of a hydrogen-containing oral solution in preparation of a blood fat lowering health care product. The invention develops a new usage of the saturated normal saline, wherein a hyperlipidemia mesocricitus auratus model is employed; after the saturated normal saline is injected to an abdominal cavity for four weeks, blood is taken to detect content of plasma cholesterol; a result of experiments shows that a hydrogen treatment group is obviously reduced in both plasma TC (Total Cholesterol) and LDL-C (Low Density Lipoprotein Cholesterin). The hydrogen normal saline is simple in preparation, high in injection density, convenient for use and free from explosion risk, very low in cost, and free from side effects; and a result of animal experiments shows that the hydrogen-saturated normal saline has excellent treatment advantage and can greatly reduce side effect risk of hyperlipidemia patients and greatly lower medical cost.
CN102311423A	Preparation method and application of novel antibacterial and anticancer compounds	The invention discloses novel antibacterial and anticancer compounds shown in formulas (I), (II) and (II'), derivatives or pharmaceutically-acceptable salt or solvate thereof, and also discloses a preparation method, a medicinal composition and bioactivity thereof.
CN102389429A	Compound retinoic acid oil phase preparation	The invention provides a compound retinoic acid oil phase preparation. Medicine active ingredients in the preparation consist of retinoic acid and tetrodotoxin. The leukemia cells or cancer cells are induced to be differentiated through multiple targets, new targets, molecular targeted and signal network mechanisms, and the malignant cell proliferation is prevented, so the malignant cells are naturally reduced or died. The preparation has the advantages that the toxic and side effect is smaller than that of the retinoic acid, the retinoic acid syndrome (RAS) can not be caused, the harm to human bodies caused by chemotherapy and radiotherapy can be relieved, and the effects of treating psoriasis and stubborn skin disease and relieving the paint are realized.
CN102429881A	Method for preparing benzbromarone tablets	The invention discloses a method for preparing benzbromarone tablets. By the method, the dissolution of the benzbromarone tablets can be obviously improved. The method comprises the following steps of: treating a benzbromarone raw material by a jet milling method until the particle size D50 is 5mu m; combining part of dodecyl sodium sulfate and Tween-80 in a prescription with the micronized raw material through a fluidized bed; and pelletizing and tabletting the obtained material and other auxiliary materials. The dissolution of the prepared tablets is obviously improved.
CN102526037A	Telmisartan medicinal composition, telmisartan medicinal composition tablets and preparation method for telmisartan medicinal composition tablets	The invention provides a telmisartan medicinal composition, telmisartan medicinal composition tablets and a preparation method for the telmisartan medicinal composition tablets. The composition consists of the following components: telmisartan sodium salt, sorbitol, polacrilin potassium, anhydrous calcium phosphate, lactose, microcrystalline cellulose and magnesium stearate. The invention provides a preparation method for the telmisartan sodium salt, reaction conditions are mild, few side reactions are performed, and the generated sodium salt has higher water solubility; meanwhile, the sorbitol in the medicine has a diuresis effect, and has a synergistic antihypertensive effect with telmisartan in human bodies, so that the therapeutic effect of the product is strengthened; and after the telmisartan is taken, the urinary albumin excretion rate (UAER) of patients with early diabetic nephropathy is remarkably reduced, so the telmisartan has a kidney protection effect.
CN102579488A	Cell nutrient mineral bath material	The invention discloses a cell nutrient mineral bath material, which is in a state of liquid or dry powder and comprises multiple microelements and a transdermal agent. The cell nutrient mineral bath material consists of the multiple natural microelements, wherein the transdermal agent which has no toxic or side effect to a human body is also comprised, so that the absorption and utilization of the microelements by the human body are increased. When the cell nutrient mineral bath material is sprayed on the surface of the human body, various elements tightly contact the human body skin and perform an action equivalent to hot spring mineral matter actions to the human body by utilizing the microelement actions, namely the human body undergoes a hot spring bath, and the cell nutrient mineral bath material has more comprehensive actions than a common hot spring bath, so that the functions of improving the human body internal environment, adjusting the human body functions, treating diseases and easing symptoms are realized.
CN102614294A	Compound amoxicillin suspension injection and preparation method thereof	The invention relates to a compound amoxicillin suspension injection. The injection is prepared from 5-20% of amoxicillin, 5-15% of Herba Houttuyniae oil, 2-5% of a suspending aid, 1-3% of a dispersant, 0.1-0.5% of an antioxidant, and the balance vegetable oil for injection. The injection has a wide antimicrobial spectrum and stable physical and chemical properties. After intramuscular injection, the Herba Houttuyniae oil rapidly reaches an effective plasma concentration after absorption and performs effects, and amoxicillin forms small storage reservoirs in the body in a particle state, the slow and continuous release guarantees the long-term above effective plasma concentration of above medicine in the body fluid, so the half life of the medicine is prolonged, the biological utilization degree is improved, the medicine resistance of bacteria to amoxicillin is reduced, and the body resistance is enhanced, thereby the injection has effects of simultaneous treatment of principal and subordinate symptoms on the control of clinical livestock and poultry diseases.
CN102631684A	Stable cephalosporin composition	The invention relates to a stable cephalosporin composition and a preparation method thereof. The cephalosporin is selected from one of cefaclor, cefixime, cefalexin and cefradine. The preparation method is characterized by comprising the steps of: inclusion of the cephalosporin by using dextrin; and then preparation according to the normal method in the industry. According to the invention, the stability problem of the cephalosporin composition at the normal temperature in summer, namely, the problem of content decreasing of main drugs in a storage process is solved; and the cephalosporin composition with stable quality is provided.
CN102657615A	Vincamine sustained-release pellet preparation and preparation method thereof	The invention discloses a vincamine sustained-release pellet preparation, which comprises main medicines of vincamine, acid blank pellet cores, an adhesive and a diluent in a weight ratio of (1-10): (10-20): (1-10): (20-200), wherein the acid blank pellet cores consist of blank pellet cores and an organic acid covered on the blank pellet cores. The invention provides the vincamine preparation which can be stably released under the pH of 1.5-7.4, the release pH dependency of the conventional vincamine sustained-release preparation is solved, the vincamine preparation can be released stably and slowly in stomach and intestinal tracts, and the pharmaceutical effect is lasting. Moreover, the invention also discloses a preparation method for the vincamine sustained-release pellet preparation. The preparation method is simple, good in repeatability, high in production efficiency and suitable for industrialized mass production. The prepared medicine-carrying pellets are smooth and round, are released uniformly under the pH of 1.5-7.4, and are high in stability.
CN102657655A	Application of pyrilamine compounds to preparation of acetylcholinesterase inhibitor	The invention relates to application of pyrilamine compounds to the preparation of an acetylcholinesterase inhibitor. The pyrilamine compounds have a structure of a general formula I, wherein in the general formula I, S1 is selected from O, S, -CH2- and -NH-; S2 is selected from O, S, -N(CH3)-, -NH- and -(CH2)n-, and n is an integral number of 1 to 6; Q1 is selected from hydrogen, halogens, straight chain or branched chain alkyl, cycloalkyl, trihaloalkyl and alkoxy; Q2 and Q3 are selected from the hydrogen, the halogens, the straight chain or branched chain alkyl, the cycloalkyl, the trihaloalkyl, the alkoxy, aryl, heteroaryl, -(CO)R1 and -S(O2)R2 independently and respectively; R1 and R2 are selected from straight chain or branched chain alkyl having 1 to 4 carbon atoms and amino independently and respectively; and X1 and X2 are respectively selected from H, the straight chain or branched chain alkyl having 1 to 4 carbon atoms and haloalkyl having 1 to 4 carbon atoms independently.
CN102665738A	Prophylactic composition for influenza infection	It was clarified that a culture of a propionic acid bacterium exhibited a prophylactic effect on influenza infection. Disclosed is a composition comprising a culture of a propionic acid bacterium which is capable of potentiating the induction of a neutralizing antibody in an animal that has been inoculated with an influenza vaccine. The fact that the component constituting the aforesaid composition has been eaten by humans over a long time assures the high safety and good taste thereof and, therefore, said composition can be taken over a long period of time. In addition, the aforesaid composition can contain, as optional components, a milk fermentation product and an oligosaccharide. It can be also expected that another effect of controlling the functions of the intestines is achieved by administering the aforesaid composition.
CN102702259A	Pyrazol methyl amino phosphonate compound, preparation and application thereof in resisting cancer	The invention discloses a pyrazol methyl amino phosphonate compound, a preparation and an application of the pyrazol methyl amino phosphonate compound in resisting cancer. The invention has the advantages that the pyrazol methyl amino phosphonate compound has notable inhibition function for human breast cancer cells (MCF-7), so that the pyrazol methyl amino phosphonate compound can be used as potential anti-tumor drug.
CN102827210A	Naphthol aldehyde Schiff alkali cobalt coordination polymer and preparation method and application thereof	The invention discloses a naphthol aldehyde Schiff alkali cobalt coordination polymer. A preparation method of the naphthol aldehyde Schiff alkali cobalt coordination polymer comprises the following steps of: (1) enabling raw materials including 2-amino group-2-ethyl-1, 3-propylene glycol and 2-oxhydryl-1-naphthaldehyde to react in solvent carbinol for 3-5h, steaming out the solvent, and drying after freezing, so that 2-oxhydryl-1-naphthaldehyde-2-amino group-2-ethyl-1, 3-propylene glycol Schiff alkali ligand can be obtained; and (2) under room-temperature condition, enabling raw materials including Co(CH3COO)2.4H2O and 2-oxhydryl-1-naphthaldehyde-2-amino group-2-ethyl-1, 3-propylene glycol Schiff alkali ligand to react in solvent carbinol for 4-6h, filtering to obtain solid matter, dissolving in ethanol, and standing and volatilizing solution, thus obtaining a brick-red blocky crystal, i.e. the naphthol aldehyde Schiff alkali cobalt coordination polymer provided by the invention. The coordination polymer is higher in antitumor activity, and can be taken as the raw material to prepare the drug for curing human pulmonary adenocarcinoma and human chronic granulocytic leukemia erythroleukemia pathological change. Compared with the common-used cis-platinum anticancer drugs, the naphthol aldehyde Schiff alkali cobalt coordination polymer has the characteristics of being high in antitumor activity, stability, and the like.
CN102871974A	Paclitaxel magnetic nanoparticle as well as preparation method and purpose of paclitaxel magnetic nanoparticle	The invention discloses a paclitaxel magnetic nanoparticle as well as a preparation method and a purpose of the paclitaxel magnetic nanoparticle. The form of the paclitaxel magnetic nanoparticle is in a sphere shape, the particle size is 50 to 200nm, and the paclitaxel magnetic nanoparticle comprises the following ingredients in percentage by weight: 0.1 to 10 percent of paclitaxel, 0.5 to 20 percent of ferroferric oxide nanoparticle, 45 to 65 percent of surfactants and 25 to 45 percent of freeze-drying protecting agents. The paclitaxel magnetic nanoparticle has the characteristics that the paclitaxel is prepared into magnetic nanoparticle solution and is then freeze-dried, the targeting of the paclitaxel is improved, in addition, medicine is prevented from being gathered and separated out, and the paclitaxel magnetic nanoparticle has the advantages that long-term and stable effects are realized, the storage and the transportation are convenient, and the like. The preparation process is simple and is suitable for industrial production.
CN102988339A	Preparation method and application of fenofibrate nano-crystal powder	The invention provides a preparation method of fenofibrate nano-crystal powder and application of the fenofibrate nano-crystal powder in preparation of oral solid medicaments, and belongs to the field of pharmaceutical preparations. The fenofibrate nano-crystal powder is prepared by adding a hydrophilic auxiliary material and a surface active agent serving as a spray drying supporting agent into a drug-containing nano mixed suspension, and adopting a spray drying method. The mass percent of the spray drying supporting agent to fenofibrate is (1:10) to (10:1). The spray drying supporting agent is preferably a mixture of mannitol and lauryl sodium sulfate, and the ratio of the mannitol to the lauryl sodium sulfate is (15:1) to (5:1). The average particle diameter of the prepared spray-dried powder which is re-dispersed in water is smaller than 1,000 nm. The preparation method can be used for industrial production and has an industrialization production prospect. The spray-dried powder and the pharmaceutically acceptable drug auxiliary material are used for preparing a solid oral preparation, so that the in-vitro dissolution and the in-vivo bioavailability of the fenofibrate can be significantly improved.
CN103040829A	Pharmaceutical composition containing lappaconitine and oxycodone	The invention relates to a pharmaceutical composition containing lappaconitine and oxycodone for treating pain. The pharmaceutical composition contains a treatment effective quantity of lappaconitine or a pharmaceutically acceptable salt thereof or a solvate thereof, a treatment effective quantity of oxycodone or a pharmaceutically acceptable salt thereof and an optional pharmaceutically acceptable carrier. The invention further relates to a use of the composition containing the treatment effective quantity of lappaconitine or the pharmaceutically acceptable salt thereof or the solvate thereof and the treatment effective quantity of oxycodone or the pharmaceutically acceptable salt thereof in the preparation of medicines for relieving pain. The pharmaceutical composition and the use, disclosed by the invention, have the beneficial effects as described in the specification.
CN103083677A	Permeation accelerator and application thereof to permeation acceleration	The invention discloses a permeation accelerator. An effective component of the permeation accelerator is a natural extractive. The invention further provides the application of the permeation accelerator to permeation acceleration. The permeation accelerator disclosed by the invention has the beneficial effects that the permeation accelerator and the application of the permeation accelerator disclosed by the invention have good permeation acceleration effect; and the natural extractive is used so that the toxic side effect is low, the irritation is low and the market prospect is good.
CN103083682A	Folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as preparation method and application thereof	The invention belongs to the technical field of medicines and specifically provides a folic acid modified chitosan quaternary ammonium salt-taxol polymer medicine, as well as a preparation method and an application of the polymer medicine. The polymer medicine provided by the invention is formed by connecting taxol to chitosan quaternary ammonium salt in the form of covalent linkage by succinyl ester and connecting tumor target ligand folic acid. The preparation method comprises the following steps of: connecting succinic anhydride open loop with taxol to synthesize succinyl taxol, modifying chitosan by quaternization to obtain chitosan quaternary ammonium salt; and under the action of a catalyst, connecting succinyl taxol to chitosan quaternary ammonium salt in the form of covalent linkage, and introducing target ligand folic acid. The polymer medicine can be assembled automatically in water to form nanoparticles, wherein hydrophobic medicine is used as the inner core and chitosan quaternary ammonium salt is used as a hydrophilic shell. The polymer medicine is simple in preparation method, excellent in repeatability and security, and can enhance the targeting and tumor inhibiting effect of taxol by two administration routes consisting of oral taking and intravenous injection.
CN103087254A	Preparation method and applications of amphiphilic co-network resin	The present invention relates to a preparation method and applications of an amphiphilic co-network resin, wherein a hydrophilic poly(ethylene glycol) diacrylate and a hydrophobic alkene monomer (stearyl methylacrylate) are subjected to a copolymerization reaction in an ethanol solution to obtain the amphiphilic co-network resin. The resin is characterized in that the structure comprises a hydrophobic chain segment portion and a hydrophilic chain segment portion, and the structure formed by the two types of the chain segments is different from an interpenetrating network, is further different from a blending structure, and is a uniformly-distributed co-network structure formed through covalent bonding of the two chain segments. The resin can be subjected to swelling in water and a plurality of organic solvents, and absorb water and organic solvents. According to hydrophilic and oleophylic properties of the resin, the product can be used as a drug carrier to swell an entrapped drug so as to control release.
CN103159754A	Amino propyl replacing tropane amine compound, medical composition thereof, preparation method and purpose thereof	The invention belongs to the medicinal chemistry field, and discloses an 8-(3-amino propyl)-3-outer direction-8-azabicyclo [3.2.1] octane-3-amino acid amide compound showed in the following general formula (I), a medical composition thereof, and a purpose thereof. The compound or acceptable salt in pharmacy can be CCR5 antagonism agents which are used for preparing medicines for treating a disease which is mediated by the CCR5, so that used for preparing medicines for treating human immunodeficiency virus (HIV) infection, asthma, chronic infectious arthritis, an autoimmunity diseases and a chronic obstructive pulmonary disease (COPO).
CN103181909A	Daphnetin slow-release composition and preparation method thereof	The invention relates to a daphnetin slow-release composition and a preparation method thereof. The slow-release composition is a matrix tablet. The matrix tablet comprises daphnetin, filler, a matrix material, a bonding agent and a lubricating agent. The matrix material is a high-viscosity hydrophilic matrix material or a soluble matrix material. The daphnetin slow-release tablet prepared with the method has a good slow-release effect and is long in action time, low in dosage, low in frequency of taking and high in bioavailability in comparison with a capsule on the market. The process is simple in operation, low in cost and easy to control, and is suitable for industrial mass production.
CN103191136A	Compound preparation containing aspirin and ilaprazole sodium and preparation method thereof	The invention discloses a compound preparation containing aspirin and ilaprazole sodium. The compound preparation comprises active ingredients 50 to 400mg of aspirin and 5 to 10mg of ilaprazole sodium, as well as pharmaceutically acceptable auxiliaries. The formulation of the compound preparation can be double-layer tablets, granules and capsules, and optimally enteric-pellets capsules. The compound preparation can be used for preventing or treating diseases induced by platelet aggregation, wherein the diseases mainly comprise thrombotic diseases and cardiovascular diseases induced by the thrombotic diseases. According to the compound preparation, aspirin and proton pump inhibitor are combined to prepare a medical preparation, aspirin can be used for treating thrombotic diseases when a patient uses the preparation, and the preparation can be used for preventing and treating gastrointestinal toxic and side effects caused by aspirin.
CN103371975A	Targeted long-circulation liposome preparation and preparation method thereof	The invention provides a targeted long-circulation liposome preparation and a preparation method thereof. Adriamycin as an anti-tumor drug is carried in a targeted long-circulation liposome modified by a hydrophilic polymer polyethylene glycol and targeted ligand cyclic RGD (Arginine-Glycine-Aspartic Acid) peptides, and the liposome can be used for prolonging the circulation time of the drug in vivo and achieving the effects of targeting a tumor, improving the curative effect and reducing the toxic and side effects.
CN103417598A	Sterile and detumescent external medicine for treating local pain and preparation method thereof	The invention relates to a medicine, in particular to a sterile and detumescent external medicine for treating local pain and a preparation method thereof. The sterile and detumescent external medicine adopts the raw materials of realgar, mothball, frankincense, myrrhic, common clubmoss herb, paniculate swallowwort root, borneol and 500 mL 75% medical alcohol, through seven steps, the third-time obtained liquor is bottled, sealed and stilled, and then the supernatant fluid is taken. The pain part is heated after the sterile and detumescent external medicine is applied, so that blood circulation is sped up. Therefore, the purposes of dispelling wind and cold, stretching the muscles and smoothing the vein, activating blood circulation to dissipate blood stasis, softening hardness to dissipate stagnation and relieve swelling and pain are achieved.
CN103450209A	Isoflavonoid compound in ficus auriculata, as well as preparation method and application thereof	The invention provides an isoflavonoid compound in ficus auriculata. The structural formula is shown in the specification. The invention further provides a preparation method of the compound and an application of the isoflavonoid compound in the ficus auriculata in preparation of medicaments for treating osteoporosis. The isoflavonoid compound in the ficus auriculata, provided by the invention, has the advantages of simple preparation process, low cost and extensive raw material sources, and the extracted isoflavonoid compound has a great treatment effect against the osteoporosis, and has natural sources and few side effects.
CN103462907A	Omeprazole sodium freeze-dried powder injection for injection and preparation method thereof	The invention discloses an omeprazole sodium freeze-dried powder injection for injection. The admixture in the freeze-dried powder injection comprises tromethamine; and the tromethamine is prepared into liquor and freeze-dried to obtain the freeze-dried powder injection. The freeze-dried powder disclosed by the invention has the advantages of high stability, fewer varieties of adjuvants and higher preparation safety; and the technique is simple and suitable for the requirements of mass production.
CN103463023A	Application of Lycojaponicumin B in helicobacter pylori resistant medicine	In-vitro activity experiments show that Lycojaponicumin B has strong helicobacter pylori (Hp) resistant activity. The Lycojaponicumin B can be applied to treatment of diseases, such as acute and chronic gastritis and gastric and duodenal ulcer, and preparation of medicines for treating the acute and chronic gastritis and the gastric and duodenal ulcer. The application of the Lycojaponicumin B in preparation of the Hp resistant medicine is disclosed for the first time. The skeleton type of the Lycojaponicumin B belongs to a brand-new skeleton type, and the inhibiting activity of the Lycojaponicumin B on the Hp is unexpectedly strong, so that no possibility for providing any inspiration by other compounds exists. The Lycojaponicumin B has predominant substantial characteristics and obviously has a remarkable progress in prevention and treatment of Hp infection.
CN103463221A	External use analgesic liquid capable of activating blood, dissolving stasis and relieving swelling and pain and preparing method thereof	The invention relates to an external use health-care product, in particular to external use analgesic liquid capable of activating blood, dissolving stasis and relieving swelling and pain and a preparing method thereof. The external use analgesic liquid comprises corydalis tuber, caulis spatholobi, radix clematidis, eucommia ulmoides, radix saposhnikoviae, cassia twig, carthamus tinctorius, camphor, borneol, menthol and muscone. The preparing method comprises the step of smashing the corydalis tuber, the caulis spatholobi, the radix clematidis, the eucommia ulmoides, the radix saposhnikoviae and the cassia twig into coarse powder to be mixed with the carthamus tinctorius, the step of adding 60% ethyl alcohol for immersing for 24 hours, percolating for 24 hours, collecting the percolated liquid, stopping percolating, squeezing dregs of decoction, mixing the pressed liquid and the percolated liquid for standby application, the step of adding the smashed muscone, the camphor, the borneol and the menthol fin powder into the percolated liquid, stirring for 15 minutes, standing for 24 hours, filtering, collecting the filter liquid and adding 1000ml-solution to enable the alcohol content to be 45-55%. The external use analgesic liquid has the healthcare function of relieving pains. The external use analgesic liquid is suitable for being used by people who are suffered from pains caused by rheumatism, cold and cool, strain, injuries from falling, herniation of intervertebral disc, arthrocele pains, sciatica, cervical vertebra pains, osteoproliferation and the like.
CN103492390A	Fluorophenyl bicyclic heteroaryl compounds	The present invention provides a compound of formula (I), a method for manufacturing the compounds of the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
CN103565772A	Glipizide controlled release composition and preparation method thereof	The invention relates to a glipizide controlled release composition which consists of a double-layered tablet core and a semipermeable membrane controlled release coating film. The double-layered tablet core consists of a medicine containing layer and a boosting layer. The coating film is prepared by intermittently spraying a coating liquid. The method specifically comprises the following steps: (1) preparing the coating liquid; (2) spraying the coating liquid; (3) spraying water; (4) drying to remove water; and (4) repeating operation of the steps (2) to (4) till weight increment of the coating film satisfies the demand. The invention further relates to a preparation method of the glipizide controlled release composition. The preparation method comprises the following steps: pelletizing the medicine containing layer; pelletizing the boosting layer; preparing the double-layered tablet core; coating; and carrying out laser punching. The coating process is intermittently spraying coating. According to the invention, the effect of low residue of organic solvents and high transparency in appearance of the coating film is realized by controlling the content of a film forming material of the coating liquid and the contents of water and acetone in a solvent and by means of a coating technical method. The preparation method is simple and feasible, thereby facilitating industrialized application.
CN103588830A	New benzyl alcohol ester glycoside compound in gastrodia elata and application thereof	The invention relates to the field of medical technology, and discloses a new benzyl alcohol ester glycoside compound separated from gastrodia elata by extraction, and an application thereof in the aspect of preparation of medicines related to senile dementia, hypomnesis and the like caused by cerebral vessel ischemia. The new benzyl alcohol ester glycoside compound has the structure general formula as shown in the specification. Pharmacological research indicates that the new benzyl alcohol ester glycoside compound can obviously reduce reaction time, prolong latent time, decrease error count and reduce escape latent period and escape distance, and shows that the new benzyl alcohol ester glycoside compound can improve learning and memory ability of mice with vascular dementia caused by cerebral ischemia-reperfusion and has a certain improvement to vascular dementia. The new benzyl alcohol ester glycoside compound can obviously improve learning and memory ability (P is less than 0.05) of multi-infarct dementia rats, and can remarkably reduce brain tissue AchE (acetylcholinesterase) content of the multi-infarct dementia rats and increase CHAT (choline acetyl transferase), NE (norepinephrine), 5-HT (5-hydroxytryptamine) and GSH-Px (glutathione peroxidase) (P is less than 0.05-0.01) content of brain tissue.
CN1594298A	Pyridine ring containing oxazolidinone compounds and preparation process and application thereof	The invention discloses oxazolidinone group compounds having a formula (I) described in the specification and their salts, wherein X is CH or N atom, R1 is H atom or F atom, R2 is substituted alkyl sulfonyl, substituted aryl sulfonyl, substituted aromatic nucleus sulfonyl, substituted alkyl-carbamic ester or substituted aryl-carbamic acid ester.
CN1637009A	Extraction process of total rehmannioside	The present invention is extraction process of total rehmannioside. The extraction process includes active carbon adsorption of water solution of rehmannia extractive, washing out the acid component with alkali solution, water washing to neutrality, eluting saccharide and other impurity with low concentration aqua of water soluble organic solvent, eluting with high concentration aqua of water soluble organic solvent, concentrating the eluted liquid, adding ethanol to produce precipitate, taking supernatant, decompression concentrating to dry to obtain the total rehmannioside extractive. The total rehmannioside extractive has iridoid glycoside as its main component.
CN1640397A	Kurarinol drop pill and its preparing method	The present invention relates to a medicine kurarinone dripping pills and its preparation method. It is made up by using kurarinone as raw material and adding matrixes of surfactant polyoxyethylene (40) monostearate, etc. according to a certain ratio, uniformly mixing them, heating to make them be molten, uniformly stirring them and placing them into dripping pills machine to obtain the invention kurarinone dripping pills, then making them into coated preparation.
CN1683366A	Fatty chain end group diamine substituted hypocrellin derivative and its preparing method and use	The present invention discloses fatty chain end group diamine substituted hypocrellin derivatives, including 2-site amino substituted hypocrellin A, 2-site amino substituted hypocrellin B, and Schiff base formed with hypocrellin A or hypocrellin B with diamine in the site-17. Compared with hypocrellin A and hypocrellin B, the products of the present invention has stronger absorption in phototherapeutic window of 600-900 nm, can produce active oxygen in photosensitive condition, and has powerful photodynamic effect and low dark toxicity. The present invention also discloses the preparation process and the use in preparing medicine for treating cancer and AIDS.
CN1732905A	Directly tabletting xylitol powder and its production method	The invention relates to a directly tabletted xylitol powder and its production method, which comprises using xylitol as main ingredient, charging right adhesive and polyatomic alcohol compounds, mixing, palletizing and drying. The prepared particles capable of tabletting directly have good stability, good taste and dental caries prevention effect.
CN1875976A	Use of tanshinone compound in preparation of medicine for treating prostate hyperplasia	The invention discloses the use of tanshinone compounds in preparing medicaments for treating prostate gland hyperplasia. Plenty of animal and human body tests shows that, tanshinone compounds have evident actions for treating and improving prostate gland hyperplasia.
CN1875985A	Externally applied medicine for treating hicismus and processing method thereof	The invention relates to an externally-used medicament for treating tragomaschalia and its processing method, wherein the medicament comprises the following constituents (by weight portions): red mercuric oxide 20-260 parts, allume 20-80 parts, clove 10-180 parts, calcium sulphate 300-500 parts, dragon's bone 30-100 parts. The preparing process consists of grinding, sieving, drying and mixing.
CN1907284A	Pharmaceutical composition containing pemetrexed	The invention discloses a drug composition with Peimeiqusai and stabilizer at 5: 2-7, wherein the weight rate of Peimeiqusai and shaping agent is 0.5-1: 1. The invention is stable for light and heat, which can be reserved at normal temperature.
CN1965843A	Use of statin and aspirin in preparation of medicine for treating blood high viscosity syndrome	The invention provides a method for treating hyperviscosemia, in particular the use of statins antihyperglycemic medicaments and aspirin in preparing medicament for the treatment of hyperviscosemia, wherein the content of aspirin is 25-250mg, the statins antihyperglycemic medicament is selected from simvastatin, pravastatin, lovastatin, fluvastatin, atorvastatin, rosuvastatin and pitavastatin.
CN1995056A	Curcumenol glucoside compound and its preparation method and uses	The invention discloses a new curcumenol glycoside compound and making method and application to treat cancer, bacteria and virus, which is characterized by the following: decorating curcumenol through glycoside; possessing excellent tumour resistant and virus resistant activity.
EP1073638B1	Heterocyclically substituted amides, their production and their use	The invention relates to amides of the general formula (I) and their tautomeric and isomeric forms, their possible enantiomeric and diastereomeric forms and possible physiologically compatible salts, where the variables have the meanings given in the description. The invention also relates to their production and their use as calpain inhibitors.
EP1087981B1	Prenyl transferase inhibitors	A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by five formulas (I), (II), (III), (IV), (V). Each of the R groups is defined in the disclosure.
EP1098647B1	Compounds and compositions for treating tissue ischemia	There is disclosed a genus of compounds and pharmaceutical compositions that are protective for mitigating damage associated with tissue ischemia, particularly stroke (CNS ischemia), and ischemia of the myocardium. The present invention further provides a method for treating tissue damage caused by ischemia. Lastly, the present invention provides a method for treating tissue damage caused by providing a compound that inhibits the cytotoxic activity of 3-aminopropanal.
EP1200067B1	Method for the preparation of microparticles comprising biological material	The present invention relates to a composition and method for delivery of biological material, especially nucleic acids into target cells and into the nucleus.
EP1212058B1	Topical treatment for prevention of ocular infections	The topical application of an oxazolidinone antibiotic in a polymeric suspension or aqueous composition to the eye is useful in treating or preventing ocular infections. Preferred oxazolidinone antibiotic compositions comprise the compound of formula (IV), and are represented by formula (IV), and the pharmaceutically acceptable salts thereof.
EP1363637B1	Pyrimidine compounds and methods for their preparation	This invention discloses compounds, and pharmaceutically acceptable salts, solvates and prodrugs thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii, Toxoplasma gondii, Mycobacterium tuberculosis, and Mycobacterium avium. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. The compounds include 5-thiapyrimidines.
EP1370254B1	Copper chelators for treating ocular inflammation	In various aspects, the invention provides methods for treating ocular inflammation using copper chelating compounds, such as compounds other than D-penicillamine. In some embodiments, such compounds may be polyamines, such as triethylenetetramine or tetraethylenepentamine. For example, the present invention provides methods for treating inflammation secondary to ocular laser therapy.
EP1496920A1	Pharmaceutical composition containing an extract from barleria prionitis linn and its process of preparation	The present invention provides a synergistic composition of bioactive fraction essentially constituting iridoid glucosides, acetyl barlerin and shanzhiside methyl ester isolated from a plant source Barleria prionitis linn along with a process for the isolation of the bioactive fraction, the present invention also relates to a use of treating mammals for hepatotoxicity, stress and immuno-deficiency with the synergistic bioactive composition.
EP1497287B1	Quinoline derivatives in combination with 5-FU or CPT-11 for use in the treatment of cancer	Organic compounds having the formulas (I) and (II) are provided where the variables have the values described herein. Medicaments include an anti-cancer drug selected from 5-FU or CPT 11 and a compound of formula (I) or formula (II), a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable salt of the tautomer in treatin along with an anti-cancer drug selected from 5-FU or CPT-11. The medicaments may be used in treating cancer. The use of a compound of formula (I) or formula (II), a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable salt of the tautomer in treating cancer in conjunction with an anti-cancer drug selected from 5-FU or CPT-11 is also provided.
EP1522313A1	Combination therapy of radiation and valdecoxib for the treatment of neoplasia	The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of radiation therapy and a cyclooxygenase-2 inhibitor.
EP1546150B1	Pyrrole derivatives as inhibitors of cyteine proteases	Compounds of general formula (I) wherein: Z = CR3R4, where R3 and R4 are independently chosen from CO-7-alkyl P1 = CR5R6, P2 = O, CR7R8 or NR9, Y = CR10R11-C(O) or CR10R11-C(S) or CR10R11-S(O) or CR10R11-SO2 (X)o=.CR16R17 (W)n = 0, S, C(O), S(O) or S(O)2-or NR18 (V)m = C(O), C(S), S(O), S(O)2, S(O)2NH, OC(O), NHC(O), NHS(O), NHS(O)2, OC(O)NH, C(O)NH or CR19R20, C=N-C(O)-OR19 or C=N-C(O)-NHR19, U = a stable. 5- to 7-membered monocyclic or a stable 8- to 11-membered bicyclic ring which is either saturated or unsaturated, and which includes zero to four heteroatoms and their salts, hydrates, solvates, complexes and prodrugs are inhibitors of cathepsin K and other cysteine protease inhibitors and are useful as therapeutic agents, .for example in osteoporosis, Paget's disease gingival diseases such as gingivitis and periodontitis, hypercalaemia of malignancy, metabolic bone disease, diseases involving matrix or cartilage degradation, in particular osteoarthritis and rheumatoid arthritis and neoplastic diseases. The compounds are also useful for validating therapeutic target compounds.
EP1617873B1	Treatment of multi-drug resistant tumours by a conjugate of mitomycin C	Methods for administering mitomycin C to a multi-drug resistant cell and for reducing the toxicity of the compound are described. In the methods, mitomycin C is provided in the form of a prodrug conjugate, where the drug is linked to a hydrophobic moiety, such as a lipid, through a cleavable dithiobenzyl linkage. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of mitomycin C in its original form. The linkage is stable under non reducing conditions. The prodrug conjugate can be incorporated into liposomes for administration in vivo reducing conditions or in response to administration of an exogenous reducing agent.
EP1649054A1	Method for diagnosing colorectal cancers	Objective methods for detecting and diagnosing colorectal cancer (CRC) are described herein. In one embodiment, the diagnostic method involves determining an expression level of FGF18 that discriminate between CRC and normal cell. The present invention further provides methods of screening for therapeutic agents useful in the treatment of CRC, methods of treating CRC, and method of vaccinating a subject against CRC.
EP1759701A2	Buproprion Metabolites and Methods of Their Synthesis and Use.	Methods and compositions are disclosed which utilize metabolites of bubropion for treating disorders ameliorated by inhibition of neuronal monoamine reuptake. Such disorders include, but are not limited to, erectile dysfunction, affective disorders, cerebral function disorders, cigarette smoking, and incontinence. The invention further discloses methods of making optically pure bupropion metabolites.
EP1976494A1	Adenosine a3 receptor agonists for the treatment of dry eye disorders	The present invention concerns methods and compositions for treating dry eye. The method comprises providing an individual exhibiting ophthalmologic clinical symptoms and signs of dry eye with an A3 adenosine receptor (A3AR) agonist. The A3AR agonist is preferably administered to the subject either topically or orally.
EP2146971A1	Novel benzamidine derivatives useful as potassium channel modulators	This invention relates to novel benzamidine derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. A stereoisomer or a mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically-acceptable addition salt thereof, wherein B may be absent (i.e. no heterocyclic ring is formed); and when absent, the nitrogen next to B holds a hydrogen (i.e. 'NH'), and A represents NH2 or OH; or B may be present (i.e. forms part of a heterocyclic ring); and when present, B represents C=O or C=S; and A represents NH or O; and wherein the rest of variables are as specified in claim 1.
EP2200985A1	1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones	The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I), wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
EP2440065A1	Copepod oil composition, formulations comprising the oil composition, and the use thereof to reduce accumulation of visceral fat, improve glucose tolerance, and prevent or treat obesity related diseases and disorders	This invention relates to an oil composition, preferably obtained from a copepod, and the use thereof to reduce accumulation of visceral fat and counteract impairment of heart function caused by obesity inducing Western diets. The oil composition of the present invention can thus be used to reduce abdominal obesity and improve glucose tolerance and thus to reduce the risk of obesity related diseases such as but not limited to type 2 diabetes or cardiovascular disease, or to prevent or treat such diseases.
EP2496239A2	Copper salts of ion exchange materials for use in the treatment and prevention of infections	Copper salts of ion exchange materials provide copper ions at levels suitable for use as an anti-infective agent. The copper salts of ion exchange materials may be formed using ether and ester derivatives of cellulose, such as carboxymethyl cellulose (CMC), ethylcellulose (EC), methylcellulose (MC), hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), hydroxyethyl methyl cellulose (HEMC), cellulose acetate, and cellulose triacetate. Wound dressings having copper salts of ion exchange materials incorporated therein are also provided, and may be used to reduce the incidence of infection in wounds. The wound dressings may also be used to prevent infections in long-term wounds, such as those formed at wound drain, catheter, and ostomy entry sites. Copper salts of ion exchange materials may be used to kill microorganisms, and may optionally be used with additional anti-infective agents.
EP2734211A1	Adenine derivatives having immunomodulating anti-inflammatory and analgesic activity	The compound 2-[l-(6-aminopurin-9-yl)-2-oxoethoxy]prop-2-enal of formula (I), its monohydrate of formula (II), or its corresponding cyclic monohydrate of formula (III), in which the stereochemical chiral centre indicated with an asterisk can be R (Rectus), S (Sinister) or racemic, including the tautomers of the adenine ring and the pharmaceutically acceptable salts, for use in the treatment of inflammatory disorders or of pain disorders.
US20050090527	H1 antagonists used include loratadine, desloratadine, cetirizine and fexofenadine; H3 antagonists used include thioperamide, impromidine, burimamide, clobenpropit, impentamine, and mifetidine; and H4 antagonists used include dual H3/H4 antagonists	The present invention includes methods for treating allergic conditions involving the airway by administering histamine receptor antagonists.
US20050101595	N-containing cycloalkyl-substituted amino-thiazole derivatives and pharmaceutical compositions for inhibiting cell proliferation and methods for their use	Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, pharmaceutically active metabolite or pharmaceutically acceptable salt of said compound, or metabolite thereof, modulate and/or inhibit the cell proliferation and activity of protein kinases.                The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating malignancies and other disorders by administering effective amounts of such compounds.
US20050112197	Celecoxib dissolving in polyethylene glycol; antiinflammatory agents, osteoporosis, respiratory system disorders, antitumor agents, analgesics	An orally deliverable pharmaceutical composition is provided comprising an aminosulfonyl-comprising drug, for example a selective cyclooxygenase-2 inhibitory drug such as celecoxib, and a solvent liquid comprising a polyethylene glycol and one or more free radical-scavenging antioxidants. At least a substantial part of the drug is in dissolved form in the solvent liquid. The composition has rapid-onset properties and is useful in treatment of cyclooxygenase-2 mediated conditions and disorders.
US20050209329	Potentiation of therapeutic effects of fatty acids	The oral administration of an essential fatty acid, preferably eicosapentaenoic acid, at a defined purity together with an inhibitor of COX-1 or COX-2 or LOX or one or more of the FACL enzymes gives improved therapeutic results over administration of the fatty acid alone.
US20050245609	Method of using pyruvate and/or its derivatives for the treatment of cytokine-mediated inflammatory conditions	This invention is directed to a method of using a therapeutic composition comprising an ester of an alpha-ketoalkanoic acid for the treatment of cytokine-mediated inflammatory conditions. The cytokine-mediated inflammatory conditions are mediated by, for example, Tumor Necrosis Factor (TNF), interleukin-1β (IL-1β)) or High Mobility Group B-1 (HMGB-1) mediator of inflammation. Exemplary cytokine-mediated inflammatory conditions include, but are not limited to, rheumatoid spondylitis, osteoarthritis, gouty arthritis, endotoxic shock, cerebral malaria, silicosis, pulmonary sarcoidosis, bone resorption disease, graft versus host disease, allograft rejections, fever and myalgia due to infection, AIDS related complex (ARC), Crohn's disease, rheumatoid arthritis, cachexia and septic shock.
US20050260601	Recombinant mutants of rhabdovirus and methods of use thereof	The present invention relates to recombinant Rhabdoviridae, isolated nucleic acids, vectors, cells and compositions comprising same. The recombinant Rhabdoviridae, isolated nucleic acids, vectors, cells and compositions express Rhabdoviral proteins including a mutated matrix protein (M) and/or a mutated glycoprotein (G), in addition to expression of at least one foreign nucleic acid. The present invention also relates to methods of use thereof, including their use in vivo, in anti-cancer applications, such as in the treatment of gliomas. The recombinant Rhabdoviridae of the present invention are also useful in gene therapy and vaccine applications.
US20060079464	Peritoneal dialysate containing taurine	[Purpose] It is an objective of the present invention to provide a stable neutral peritoneal dialysate that contains a substance other than glucose to serve as an osmotic agent. [Means to solve the problem] The peritoneal dialysate of the present invention is stable and can be provided in the form of a single solution in one-compartment containers.
US20060154878	for treating bacterial infections; intermediates for the synthesis of other macrolide antibiotics	The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.
US20060178359	Tricyclic compound, process for producing the same, and use	A compound of the formula:                 wherein R1 is a 5- or 6-membered ring;     Z1 is a 5- or 6-membered aromatic ring;  Z2 is a group -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain;   W is a group represented by                 wherein R3 and R3′ are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n′ are each an integer of 0 or 1 to 4; m and m′ are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and   R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide; or a salt thereof. The compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.
US20070048390	Combination of a lanthanum compound and bone enhancing agent for the treatment of bone diseases	The invention provides a method for enhancing bone formation, inhibiting osteoclastic differentiation and/or activating osteoblastic differentiation whereby to manage, treat or achieve prophylaxis of bone disease which comprises administering to a human or animal subject suffering from, or susceptible to bone disease a therapeutically or prophylactically effective amount of a lanthanum compound and a bone enhancing agent, such as vitamin D.
US20080107693	Hybrid or chimeric polynucleotides, proteins, and compositions comprising hepatitis B virus sequences	H-2 class I negative, HLA-A2.1 transgenic HHD mice were used for a comparative evaluation of the immunogenicity of HLA-A2.1 restricted human tumor-associated CTL epitopes. A hierarchy was established among these epitopic peptides injected into mice in IFA which correlates globally with their capacity to bind and stabilize HLA-A2.1 molecules. Co-injection of a helper peptide enhanced most CTL responses. In contrast, classical HLA class I transgenic mice which still express their own class I molecules did not, in most cases, develop H.A.-A2.1-restricted CTL responses under the same experimental conditions. Different monoepitopic immunization strategies of acceptable clinical usage were compared in HHD mice. Recombinant Ty-virus-like particles, or DNA encoding epitopes fused to the hepatitis B virus middle envelope protein gave the best results. Using this latter approach and a melanoma-based polyepitope construct, CTL responses against five distinct epitopes could be elicited simultaneously in a single animal. Thus, HHD mice provide a versatile animal model for preclinical evaluation of peptide-based cancer immunotherapy.
US20080108694	Inhibit the growth of or kill Rb negative cancer cells; inhibit the activity of Heat shock protein 90; antibiotics, antimalarial agents, anticancer agents, antitumor agents; cytotoxicity; to treat glioblastoma, lung cancer and retinoblastoma	The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof)                                              wherein Ro-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
US20080226605	Methods and Compositions Facilitating Entry of Compounds Into Cells	Disclosed are methods and compositions for facilitating entry of compounds to cells. In some forms, the compositions comprise one or more aminoglycosides and one or more lipids. The disclosed compositions can also comprise one or more compounds or compositions. It was discovered that the disclosed compositions increase the efficiency of delivery of compounds into cells. The disclosed compositions and methods increase both delivery into cells and the activity of compounds once delivered into cells. For example, the disclosed methods and compositions can be used to deliver nucleic acids to cells and to thereby increase the activity of such nucleic acids delivered to cells. The disclosed compositions can be used to deliver compounds and compositions to cells in vitro, ex vivo and in vivo. Delivery can be, for example, non-specific, non-directed, non-targeted, specific, directed or targeted.
US20080234376	Prostaglandin E1, a phospholipid with a high purity and a non-proton-providing surfactant;  hypertension, thrombosis, asthma, gastric and intestinal ulcers	An emulsion composition includes prostaglandin E1 (PGE1), a phospholipid with a high purity and a non-proton-providing surfactant that improves stability of PGE1. Embodiments of the emulsion composition include an effective amount of PGE1, about 1% to about 30% (w/w) of a pharmaceutically acceptable oil as an oil base based on the weight of the emulsion composition, about 1% to about 30% (w/w) of a phospholipid with a high purity based on the weight of the oil base, about 1.6% to about 40% (w/w) of a non-proton-providing surfactant based on the weight of the oil base, and the balance of the emulsion composition being water.
US20080249044	Nucleic acid external skin formulation	The present invention provides a nucleic acid external skin formulation having high skin permeability, which is prepared from a polymeric nucleic acid which has high molecular weight and sodium alginate. The nucleic acid external skin formulation is highly skin permeable and delivers its active ingredient nucleic acid to the affected area efficiently. The nucleic acid used may be smaller in amount, and thus, the formulation is also superior in safety and cost. The working mechanism thereof is different from that of the low-molecular weight compounds currently used as an active ingredient for skin anti-inflammatory agents, and thus, the formulation may be applicable to cases where such low-molecular weight medicines are less effective.
US20080287481	Process for the preparation of desloratadine polymorph mixtures	The present application provides a process for the preparation of mixture of polymorphic Form I and Form II of desloratadine in any desired ratio.
US20090018101	S-adenosyl-l-methionine analogs with extended activated groups for transfer by methyltransferases	S-Adenosyl-L-methionine analogs of formula (I)                                      wherein R comprises a carbon-carbon double bond, carbon-oxygen double bond, carbon-sulfur double bond, carbon-nitrogen double bond, a carbon-carbon triple bond, carbon-nitrogen triple bond or an aromatic carbocyclic or heterocyclic system in β-position to the sulfonium center,  X— is an organic or inorganic anion carrying one or more negative charges, Z is —CR1R2—, —O—, —S— or —NR3— and R1, R2 and R3 are independently selected from H, D and C1-C12 alkyl. Also disclosed are complexes of the compound with a methyltransferase, pharmaceutical compositions comprising the same, methods for modifying biomolecule using the compound, and methods for detecting sequences specific methylation of biomolecules using the compound.
US20090076050	Synergistic tumor-killing effect of radiation and berberine combined treatment in lung cancer	A method for treating a subject suffering cancer, comprising administering an effective amount of berberine or its acid or ester derivates to the subject in need of such treatment, and radiating the cancer of the subject.
US20090118208	Composition and methods of RNAI therapeutics for treatment of cancer and other neovascularization diseases	Compositions and methods are provided for treatment of diseases involving unwanted neovascularization (NV). The invention provides treatments that control NV through selective inhibition of pro-angiogenic biochemical pathways, including inhibition of the VEGF pathway gene expression and inhibition localized at pathological NV tissues. Tissue targeted nanoparticle compositions comprising polymer conjugates and nucleic acid molecules that induce RNA interference (RNAi) are provided. The nanoparticle compositions of the invention can be used alone or in combination with other therapeutic agents such as VEGF pathway antagonists. The compositions and methods can be used for the treatment of NV diseases such as cancer, ocular disease, arthritis, and inflammatory diseases.
US20090143456	Polyamine Analogs as Modulators of Cell Migration and Cell Motility	This disclosure relates to methods of inhibiting cell motility or cell migration, and of treating diseases involving cell migration or cell motility, using polyamine analogs, such as conformationally restricted polyamine analogs. The diseases to be treated include immune disorders, inflammatory conditions, infection, abnormal immune responses, undesired angiogenesis, tumor cell metastasis or invasion, atherosclerosis, vascular graft occlusion, transplant rejection, other complications of transplants, glomerulonephritis, arthritis, inflammatory responses subsequent to stroke or ischemia, and asthma.
US20090274671	Vector encoding human globin gene and use thereof in treatment of hemoglobinopathies	Recombinant lentiviral vectors having a region encoding a functional β-globin gene; and large portions of the β-globin locus control regions which include DNase I hypersensitive sites HS2, HS3 and HS4 provides expression of β-globin when introduced into a mammal, for example a human, in vivo. Optionally, the vector further includes a region encoding a dihydrofolate reductase. The vector may be used in treatment of hemoglobinopathies, including β-thalessemia and sickle-cell disease. For example, hematopoietic progenitor or stem cells may be transformed ex vivo and then restored to the patient. Selection processes may be used to increase the percentage of transformed cells in the returned population. For example, a selection marker which makes transformed cells more drug resistant than untransformed cells allows selection by treatment of the cells with the corresponding drug.
US20090312385	Cannabinoid receptor modulators for treating non-immediate type allergic diseases	The present invention relates to the use of cannabinoid receptor modulators, particularly selective CB2 receptor agonists, for treating non-immediate type allergic diseases in mammals. The invention further relates to a pharmaceutical composition for non-immediate type allergic diseases.
US20100021467	Method of detecting a cancer cell by aberrant expression of a human k+ ion channel	The present invention relates to a novel human K+ ion channel, to nucleic acid molecules encoding the same and to vectors comprising said nucleic acid molecules. The invention additionally relates to antibodies specifically directed to the novel K+ ion channel and to pharmaceutical compositions and diagnostic kits containing at least one of the above-mentioned components. Furthermore, the present invention relates to methods of treating a disease caused by malfunction of the polypeptide of the present invention or by the (over)expression of the nucleic acid molecule of the invention comprising administering an inhibitor of said (over)expression or of ion channel function or an inhibitor abolishing said malfunction to a patient in need thereof. Methods of devising drugs for treating or preventing the above-mentioned disease, methods of inhibiting cell proliferation and methods of prognosing cancer are additional embodiments comprised by the present invention. The invention also envisages specific antisense or gene therapies on the basis of the nucleic acid molecule of the invention for inhibiting undesired cellular proliferation, for example, in connection with cancer or in neurodegenerative diseases.
US20100021555	Compositions containing high omega-3 and low saturated fatty acid levels	Food products and supplements comprising the essential unsaturated fatty acids EPA or DHA at high concentrations relative to other n-3 HUFAs and with relatively low levels of saturated fatty acids (myristic and palmitic acids) are provided. These compositions can be made in commercial quantities in a cost effective manner by culture of selected microorganisms. The food products and supplements are suited to human health needs which are unable to be met from fish oil origins. Also provided are EPA containing food products obtained from animals.
US20100068276	Multiparticulates of spray-coated drug and polymer on a meltable core	A pharmaceutical composition comprises multiparticulates comprising a melt-congeal core and a solid amorphous dispersion layer of a poorly water soluble drug and polymer. The multiparticulates are suitable for improving bioavailability of poorly water soluble drugs. The melt-congeal cores facilitate application of the solid amorphous dispersion layer, and allow incorporation of additional optional components to the core so as to adjust the release of drug from the multiparticulate.
US20100069422	Methods and compositions for promoting bone and joint health	Methods and compositions that can be used to promote bone and joint health through amelioration, stabilization and repair of damage associated with various pathophysiological conditions are disclosed.
US20100087458	Method of treating melanoma	Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a cytotoxic agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating melanoma.
US20100087525	Stereoselective enzymatic synthesis of (s) or (r)-iso-butyl-glutaric ester	The present invention relates to a stereoselective enzymatic synthesis of (S) or (R)-iso-butyl-glutaric ester, an intermediate of S-Pregabalin.
US20100166675	Pharmaceutical Composition for the Treatment of Type 1-Diabetes	A composition for the prevention or treatment of type I diabetes in a subject, said composition comprising a GABAergic and incretin exemplified by GABA and GLP-1/Ex4. These are optionally provided together in a single composition to promote beta-cell regeneration prevent beta-cell apoptosis and control autoimmunity for the prevention and treatment of T1D in mammals.
US20100183597	Drak2 expression is associated with diabetes	Drak2 is a member of the death-associated protein family and a serine threonine kinase. In this study, we investigated its role in beta-cell survival and diabetes. Drak2 mRNA and protein were rapidly induced in islet beta-cells after stimulation by inflammatory cytokines known to be present in type 1 diabetes. Drak2 upregulation was accompanied by increased beta-cell apoptosis, beta-cell apoptosis caused by the said stimuli was inhibited by Drak2 knockdown using siRNA. Conversely, transgenic (Tg) Drak2 overexpression led to aggravated beta-cell apoptosis triggered by the stimuli. Further in vivo experiments demonstrated that Drak2 overexpressed in Tg islets is responsible for type 1 diabetes-prone phenotype. Purified Drak2 could phosphorylate ribosomal protein S6 (p70S6) kinase in an in vitro kinase assay. Drak2 overexpression in NIT-1 cells led to enhanced p70S6 kinase phosphorylation, while Drak2 knockdown in these cells reduced it. These mechanistic studies proved that p70S6 kinase was a bona fide Drak2 substrate in vitro and in vivo.
US20100234396	Tetrhydropyridoindole Derivatives	The invention relates to tetrahydropyridoindole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions comprising one or more of those compounds and methods of treatment comprising administration of said compounds.
US20100280097	Compositions comprising hif-1 alpha sirna and methods of use thereof	The present invention provides nucleic acid molecules that inhibit HIF-1α expression. Methods of using the nucleic acid molecules are also provided.
US20100285159	Combination of unsaponifiable lipids combined with polyphenols and/or catechins for the protection, treatment and repair of cartilage in joints of humans and animals	The present invention relates to a composition and a kit for the protection, treatment and repair of cartilage in humans and animal joints. The composition or kit contains a combination of unsaponifiable lipids together with one or more of polyphenols and/or catechins. Preferably, the composition or kit contains avocado:soybean unsaponifiables (ASU) and green tea.
US20100298354	Crystalline Form Of Abacavir That Is Essentially Free Of Solvent	Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.
US20110021606	RNAi Modulation of RSV, PIV and Other Respiratory Viruses and Uses Thereof	The present invention is based on the in vivo demonstration that RSV and PIV can be inhibited through intranasal administration of RNAi agents as well as by parenteral administration of such agents. Further, it is shown that effective viral reduction can be achieved with more than one virus being treated concurrently. Based on these findings, the present invention provides general and specific compositions and methods that are useful in reducing RSV or PIV mRNA levels, RSV or PIV protein levels and viral titers in a subject, e.g., a mammal, such as a human. These findings can be applied to other respiratory viruses.
US20110077243	Triazolopyridine Compounds Useful As Kinase Inhibitors	A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I), and methods of treating conditions associated with the activity of p38 kinase.
US20110092509	Pharmaceutical Composition for Prevention or Treatment of Disease Associated with Tear Reduction	The present invention provides pharmaceutical compositions for the prevention or treatment of diseases associated with decrease in tear.     The present invention provides pharmaceutical compositions for the prevention or treatment of diseases associated with decrease in tear such as dry eye, dry disorders of cornea and conjunctiva, disorders of the keratoconjunctival epithelium, syndrome with decrease in tear secretion, xerophthalmia, dry eye due to aging, ophthalmopathy in Stevens-Johnson syndrome, ophthalmopathy in Sjögren's syndrome, keratoconjunctival ulcer, dryness in wearing of contact lens or the like, which comprises as an active ingredient a phenylethanolaminotetralin-carboxamide derivative represented by the general formula (I) wherein A represents a lower alkylene group, B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may have an oxygen atom in the ring, a carbon atom with the mark “*” represents a carbon atom of S-configuration or R-configuration, or a mixture thereof and a carbon atom with (S) represents a carbon atom of S-configuration, or a pharmaceutically acceptable salt thereof.
US20110104137	ADJUNCTS AND COMPLEXES FOR IMPROVING HMG-CoA REDUCTASE INHIBITOR (STATIN) AND SELECTIVE PHOSPHODIESTERASE 5 INHIBITOR THERAPY	Dosage forms and methods of use are disclosed for a) adjuncts administered individually or simultaneously with HMg-CoA reductase inhibitors (statins) and/or selective phosphodiesterase 5 inhibitors or, b) the administration of a conjugate consisting of the adjuncts and an HMG-CoA reductase inhibitor and/or a selective phosphodiesterase 5 inhibitor. The invention is useful in the amelioration of side effects associated with HMG-CoA reductase inhibitors and will improve their effectiveness in diseases for which these are useful. The invention will also improve the effectiveness in the of selective phosphodiesterase 5 inhibitors in patients using these medications alone or in conjunction with statins, for the treatment of erectile dysfunction.
US20110129547	Preparation for care and protection of skin with children and adults, method for obtaining thereof	Preparation for care and protection of skin with children and adults, i.e. method for obtaining thereof consists in that the zinc oxide and powder resolve in paraffin oil during 1-2 minutes up to the complete homogenization, so that these substances can be homogenized and prepared for combining merging with other substances. In the following step the water-free lano-line and white Vaseline are melted and dissolved at the same temperature of about 65% and poured into duplicate unit. Moreover in such a way melted lanoline and Vaseline, paraffin oil is added, mixture of zinc oxide and powder previously dissolved in paraffin oil and citric acid, hence the cooled mass is added. Bisabolol and bitter almond water, with constant mixing up the complete homogenization of mass, i.e. obtaining the consistency of ointment. Preparation obtained by this procedure is cooled and a slight yellowish ointment with fine almond fragrance is obtained.
US20110150767	Alpha-substituted and alpha-unsubstituted aromatic amino acid derivatives and compositions thereof for use to treat, diagnose, or monitor a medical condition	A compound represented by the general formula 1 as described, a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a radio-labeled analog thereof (i.e. 18F, 124I, 11C, etc), and mixtures of any of the foregoing, for diagnosis or monitoring of a medical condition.
US20110178145	Alpha-2 adrenergic agonist having long duration ofintraocular pressure-lowering effect	The present invention provides a method of lowering intraocular pressure which comprises administering a therapeutically effective amount of a pharmaceutical composition comprising 4-bromo-5-(2-imidazolin-2-ylamino)benzimidazole, or a salt thereof to the affected eye of a patient, as a single dose, wherein the affected eye has an intraocular pressure less than the baseline intraocular pressure for at least eight (8) hours.
US20110263684	Lipid Formulated Compositions and Methods for Inhibiting Expression of Serum Amyloid A Gene	The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a Serum Amyloid A (SAA) gene, and methods of using the dsRNA to inhibit expression of SAA.
US20120021057	Once-daily oral ir/cr pramipexole formulation	An oral once-daily pramipexole formulation, comprising an immediate-release component and a controlled-release component, is provided wherein in preferred embodiments, both the immediate-release component and the controlled-release component comprise pramipexole The formulation is preferably in the form of a coated bead A method of manufacturing said formulation is also provided.
US20120035227	Deuterium-enriched ixabepilone	The present application describes deuterium-enriched ixabepilone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
US20120040957	Novel Bicyclic Antibiotics	Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino-carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl-sulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclyl-carbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, unsubstituted or substituted phenoxy or phenylcarbonyl, unsubstituted or substituted C5-C6heterocyclyl or carboxy; A1 represents a divalent group of one of the formulae —O—(CH2)m—(CH2)—, —S—(CH2)m—(CH2)— or —(C═O)O—(CH2)m—(CH2)—, wherein the (CH2)m moiety is optionally substituted by C1-C4alkyl, C2-C4alkenyl, C3-C6cycloalkyl, C3-C6cycloalkylmethyl, morpholinomethyl, halogen, carboxy, hydroxy, C1-C4alkoxy; C1-C4alkoxyC1-C4alkyl, C1-C4alkoxy(C1-C4alkylenoxy)C1-C4alkyl, benzyloxyC1-C4alkyl, amino, mono- or di-(C1-C4alkyl)amino or acylamino, in which substituents the alkyl moieties can be further substituted by 1 or more fluoro atoms m is 0, 1 or 2, provided that the nunber of atoms in the direct chain between the two terminal valencies of A1 is at least 3, which group A1 is linked to A2 via the terminal (CH2)-moiety; A2 is a group selected from C3-C8 cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A2 is unsubstituted or substituted; R4 represents hydrogen or C1-C4 alkyl; A3 represents C1-C4 alkylene, C2-C4 alkenylene, >C═O, —C(O)C1-C3 alkylene-, —C(═O)NH—, or a group selected from —C2H4NH—, —C2H 4O—, and —C2H4S— being linked to the adjacent NR4-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and n is 0, 1 or 2; or a pharmaceutically acceptable salts, hydrates or solvates thereof are valuable antibacterial agents.
US20120108545	Trioxane Monomers and Dimers	Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
US20120122896	2,1,3-benzoxadiazol derivatives for the inhibition of influenza a and b virus and respiratory syncytial virus replication	A 2,1,3-benzoxadiazole compound as a medicament according to the invention is one of the following compounds: 4-[(4-methoxybenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl 4-methoxybenzene-1-sulfonate, 4-[(4-methylphenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(2,4-dichlorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethan-1-ol, 4-[(4-methylbenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(4-fluorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(3-chlorophenyl)-thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl-4-methoxy-benzoate, 5-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,1,3-benzoxadiazole, N-benzyl-4-nitro-2,1,3-benzoxadiazol-5-amine, 4-nitro-7-(phenylmethylsulfanyl)-2,1,3-benzoxadiazole, 4-nitro-7-(phenylmethylsulfonyl)-2,1,3-benzoxadiazole, 2-(hydroxymethyl)-5-[6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]oxolane-3,4-diole, or 2-[2-amino-6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol; or a physiologically tolerable salt, solvate, or physiologically functional derivative thereof. Said compounds are particularly advantageous for treating and/or preventing influenza type A and/or influenza type B infections in humans, mammals and/or birds, and for treating and/or preventing respiratory syncytial virus infections in humans, mammals and/or birds.
US20120157398	Materials and methods for treating diseases caused by genetic disorders using aminoglycosides and derivatives thereof which exhibit low nephrotoxicity	Various aspects related to the preparation of congeners of the aminoglycosides gentamicin such as the congener C2 and using this compound or derivatives thereof and pharmaceutically active salts to treat diseases that involve genetic mutations which introduce a missense or premature stop codon into a gene. Still other aspects include treating human or animal patients with the gentamicin congener C2 and derivatives and pharmaceutical salt thereof to overcome, or to at least mitigate, the symptoms of disease and disorders such as some forms of Becker's or Duchenne muscular dystrophy, Hurler's Syndrome and Cystic Fibrosis that have as their etiology the presence of a premature stop codon in a gene whose proper expression is necessary for good health.
US20120189719	Schisandrae fructus extracts for inhibition or prevention of h1n1 influenza virus infection and its application thereof	Disclosed are an Schisandrae fructus extract for inhibition or prevention of influenza and its application, wherein the Schisandrae fructus extract is obtained by water, methanol, or ethanol extraction process and the extract comprises compounds such as schisandrone, benzoylgomisin P, wulignan A1, epigomisin O, epiwulignan A1, and tigloylgomisin P. The extracts and purified compounds of Schisandrae fructus has anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities, therefore the extracts and the purified compounds of Schisandrae fructus can be applied as an inhitibory agent of a pharmaceutical composition for treatment or prevention agent for influenza infection.
US20120197221	Transepidermal drug delivery system containing rivastigmine	Disclosed is a pharmaceutical composition containing rivastigmine. Specifically, disclosed is a transepidermal drug delivery system including a rivastigmine-containing drug layer and a supporter adhered to one surface of the drug layer to support the drug layer, wherein the drug layer contains 10 to 40 parts by weight of a rubber, 20 to 80 parts by weight of a rosin ester resin and 0.1 to 10 parts by weight of an acrylic adhesive and the drug layer has a thickness of 40 μm to 100 μm.
US20120231002	Treatment of vasculoproliferative conditions	This invention relates to the field of molecular physiology. Specifically, this invention relates to the prevention and/or treatment of vasculoproliferative conditions, especially those of the eye and in the treatment of tumours that exhibit vascular proliferation. Levels of leucine-rich alpha-2-glycoprotein (Lrg1) have been demonstrated to be increased in patients suffering from such conditions and animal models of such conditions. Antagonists of Lrg1 can be used to prevent and/or treat vasculoproliferative conditions.
US20120252894	Compounds for alleviating pain and stress in fetus and newborn	The invention relates to a compound which inhibits the importation of chloride into neurons or a compound which improve the outflow of chloride from neurons thereby promoting the inhibitory actions of GABA and alleviating pain and stress of the fetus during delivery and the newborn. The invention also relates to a pharmaceutical composition for use in a method for alleviating pain and stress of the fetus during delivery and the newborn comprising a compound according to the invention and a pharmaceutically acceptable carrier.
US20120309765	5-anilinoimidazopyridines and methods of use	The invention relates to a method of inhibiting abnormal cell growth or treating a hyperproliferative disorder in a mammal comprising administering to said mammal a therapeutically effective amount of an imidazopyridine of formula I with anti-hyperproliferative activity.
US6855843	Antihistamines; rheumatic diseases; antidiabetic agents; inflammatory bowel disorders	The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH═CH—, —NH— or —N═CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.; or a pharmaceutically acceptable salt thereof.
US6878734	Gastrin and cholecystokinin receptor ligands(II)	Ligands for the gastrin and cholecystokinin (CCK) receptors are provided, together with methods for preparing such ligands, and compounds which are useful intermediates in such methods. Pharmaceutical compositions comprising such ligands, methods for preparing such pharmaceutical compositions, and methods of treatment using these compositions also are provided. The ligands have the formula (I):                where n is from 1 to 3;  X and Y are independently ═N— or —N(R5)— where R5 is selected from the group consisting of H, Me, Et, Pr, Bn, —OH and —CH2COOR6, where R6 represents H, Me, Et, Pr or Bn; R1 is H or a C1-C15 saturated carbocylic ring optionally substituted with OMe, NMe2, CF3, Me, F, Cl, Br or I where up to three H atoms may optionally be replaced by halogen atoms; R2 is selected from H, Me, Et, Pr and OH, each R2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R3 is selected from the group consisting of H, Me, Et and Pr when n is 1; or, when n is greater than 1, each R3 is independently selected from the group consisting of H, Me, Et and Pr, or two R3 groups on neighbouring carbon atoms are linked to form a C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an ═O group; R4 is H or a C3 to C10 alicyclic ring where up to three H atoms may optionally be replaced by halogen atoms; Z is selected from the group consisting of:                Q is a 6-membered aromatic carbocycle substituted with 1 or 2 V groups and optionally substituted with 1, 2 or 3 T groups; V is selected from the group consisting of —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —CH2OH, or a group of the formula —R7U, where U is selected from the group consisting of —COOH, tetrazolyl, —CONHOH and —SO3H; and R7 is selected from the group consisting of a bond; C1 to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)-; —SO2NR8—CHR9—; —CO—NR8—CHR9—, where R8 and R9 are independently selected from H and methyl; and —NH—(CO)c—CH2—, where c is 0 or 1.
US6900200	Tricyclic hydroxy carboxamides and derivatives thereof tocolytic oxytocin receptor antagonists	This invention provides novel substituted tricyclic carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea and endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
US7041667	CCR5 modulators	Compounds of Formula 1  [Region α]—[Region β]—[Region γ]—[Region δ]  (1)   which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.
US7056922	Acylamino cyclopropane derivatives	A compound of the formula                                                                                                                  wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R1, R2, R3, R4, R5, R6 R7 are as defined in the specification, pharmaceutical compositions thereof, and methods of use to treat diseases and as D3 receptor modulators.
US7081474	Drugs to improve synaptic transmission	Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal issues.
US7160881	Crystalline modifications of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1 λ6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide	The present invention relates to a new crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1λ6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide characterized by the following X-ray diffraction pattern obtained with a CuKα, radiation at 2θ (2Theta)=4.5, 6.4, 7.5, 7.7, 8.0, 8.2, 10.0, 10.2, 10.9, 11.1, 12.9, 13.4, 14.0, 14.5, 15.1, 15.6, 16.2, 16.5, 17.3, 17.5, 18.0, 18.9, 19.3, 19.5, 19.9, 20.1, 20.6, 21.0, 21.4, 22.7, 23.1 and 23.6 and an infrared spectrum having sharp bands at 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm−1, and wherein the extrapolated melting point (DSC) is 137.2° C.
US7192971	4-Heteroaryl-tetrahydroquinolines and their use as inhibitors of the cholesterin-ester transfer protein	Hetero-tetrahydroquinolines can be prepared either by condensing correspondingly substituted hetero-tetrahydroquinoline aldehydes with the desired substituent or by reducing the corresponding keto-substituted hetero-tetrahydroquinolines, followed by introduction of the desired substituent by customary methods. The hetero-tetrahydroquinolines are suitable for use as active compounds in medicaments, in particular in medicaments for treating artheriosclerosis and dyslipidaemias.
US7229643	Solid oral formulation coated with hydroxypropyl methylcellulose; the polymer coating is free of polyethylene glycol	The invention provides a pharmaceutically elegant solid oral formulation of olanzapine and a process for making such formulation.
US7253194	Compounds and inhibitors of phospholipases	The present invention relates generally to amino acid derivatives and to methods of making the same. In particular, the invention relates to compounds bearing a stereochemical identity, that is, the same stereochemistry, with the chiral α-carbon of D-α-amino acids and their use in methods of therapy, including the treatment of inflammatory diseases, and to compositions and enantiomeric mixtures containing them.
US7351736	Therapeutic compositions (II)	Method of producing a physiologically acceptable ketosis such as to treat a patient in need of therapy for one or more of Amylotrophic lateral sclerosis, Free Radical disease, Heart failure and Duchenne's muscular dystrophy by oral administration to the patient of a cyclic oligomer of formula (I)                    where n is an integer of 1 or more or a complex thereof with one or more cations or a salt thereof, wherein the physiologically acceptable ketosis is characterized by blood levels of (R)-3-hydroxybutyrate of from 0.5 to 20 mM.
US7498147	Modulating the activity of one or more elements in the complement/lipid pathway	Complement is recognized as an important, humoral defense system involved in the innate (nonspecific) recognition and elimination of microbial invaders, other foreign particles or molecules, and antigen-antibody complexes from the body. The present invention makes use of the surprising notion that the handling of lipids by the body, rather than its antimicrobial activity, is the primary and most ancient function of the complement system. Consequently, atherosclerosis as observed in disorders associated with disturbed lipid metabolism (familial combined hyperlipemia (FCHL), postprandial hyperlipidemia, hypertriglyceridemia with low levels of HDL cholesterol, and insulin resistance associated with type-II diabetes and obesity), is ascribed to either genetic or acquired defects in ancient (activatory and/or regulatory) complement components. Based on this new insight, novel preventive measures and treatment modalities of disturbed lipid metabolism are introduced.
US7674769	Treatment of severe pneumonia by administration of tissue factor pathway inhibitor (TFPI)	Methods for prophylactically or therapeutically treating severe pneumonia involve administration of tissue factor pathway inhibitor (TFPI) or a TFPI analog to patients suffering from or at risk of developing this condition. The methods involve the use of continuous intravenous infusion of TFPI or a TFPI analog, preferably at low doses to avoid adverse side effects.
US8337834	Methods of making enhanced, autologous fat grafts	Cells present in processed lipoaspirate tissue are used to treat patients. Methods of treating patients include processing adipose tissue to deliver a concentrated amount of stem cells obtained from the adipose tissue to a patient. The methods may be practiced in a closed system so that the stem cells are not exposed to an external environment prior to being administered to a patient. Compositions that are administered to a patient include a mixture of adipose tissue and stem cells so that the composition has a higher concentration of stem cells than when the adipose tissue was removed from the patient.
US8372430	comprises stiffening agents for ameliorating side effects associated with adminstration of lipase inhibitors (anal leakage of undigested fat or oil); for treatment of diabetes	Disclosed are compositions, methods, and kits for treating conditions including; ameliorating side effects associated with compounds such as lipase inhibitors; gastrointestinal distress; fecal urgency; obesity; hyperlipidemia; diarrhea; reducing levels of toxic substances; reducing blood cholesterol levels; inducing satiety; effecting weight loss; effecting weight control; and treating, delaying onset and/or preventing Type II diabetes. One embodiment includes compositions for administration to an animal for stiffening lipophilic substances in the gastrointestinal tract. Such stiffening agents have a complete melting point of about 33° C. or greater. Kits comprising the composition are also included. Methods of stiffening lipophilic substances present in the gastrointestinal tract of an animal are also provided. The methods comprise administering a composition comprising a safe and effective amount of a stiffening agent to an animal. The methods also comprise administering a composition comprising a safe and effective amount of a stiffening agent and a safe and effective amount of a lipase inhibitor to an animal.
US8629185	7-[3,5-dihydroxy-2- (3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-N-ethyl-hept-5-enamide (bimatoprost) in crystalline form II, methods for preparation, and methods for use thereof	The present invention provides a new crystalline form of bimatoprost, designated as crystalline form II. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystalline form II is readily prepared from crystalline form I.
WO2004054507A3	Indolizine compounds	This invention relates to compounds of Formula (I) wherein Ring A, X, Y, Z, R1, R2 and R3 are defined herein. These compounds are useful for treating and preventing cancer, inflammatory disorders, autoimmune diseases and other conditions involving PDE4 or elevated levels of cytokines. This invention also relates to pharmaceutical compositions comprising at least one compound of Formula (I) and methods for treating and preventing cancer, inflammatory disorders, autoimmune diseases and other conditions involving PDE4 or elevated levels of cytokines.
WO2006037769A1	Use of cyclodextrin for treatment and prevention of bronchial inflammatory diseases.	The invention provides the use of a cyclodextrin compound for the manufacturing of a medicament for the treatment or prevention of bronchial inflammatory diseases, particularly for asthma.
WO2006061140A2	Composition of ssao substrates and metal compounds of the vla and vlb groups of the periodic table	This invention relates to (pharmaceutical) compositions comprising a combination of SSAO substrates and pharmaceutically acceptable compounds of the Vla and Vlb group of the periodic table, i.e. selenium (VI)-, molybdenum (VI)- and tungsten (V)/(VI) compounds, etc. and to their use as insulin mimetic, i.e., to treat illness Diabetes mellitus, Obesity, or their symptoms. A here discovered synergism between the compounds of the Vla and Vlb groups of the periodic table, i.e. selenium (VI)-, molybdenum (VI)- and tungsten (V)/(VI) com­pounds, etc. and the SSAO substrates makes the effective concentration of the compounds of the Via and Vlb groups of the periodic table in the (pharmaceutical) composition one order of magnitude lower than the corresponding compound of the Vla and Vlb groups alone. Consequently the inventive (pharmaceutical) composition has much lower toxicity than the known compounds or compositions in the art alone, what is a crucial advantage of the former for its use in the treatment and/or prevention of Diabetes mellitus, particularly of Diabetes type 2, or Obesity.
WO2006083508A3	Combinations of superoxide dismutase mimetics and nonsteroidal analgesic/anti-inflammatory drugs	Combinations of synthetic low molecular weight catalysts for the dismutation of superoxide and Nonsteroidal Analgesic/Anti-Inflammatory Drugs (NSAIDs) are potent analgesics that are effective in elevating the pain threshold in hyperalgesic conditions.
WO2006106103A3	Prevention of hiv- infection with tmc278	This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.
WO2006130688A2	Compounds for inhibiting cathepsin activity	A method of treating, preventing or ameliorating one or more symptoms of hepatitis C, or inhibiting cathepsin activity, in a subject is provided, in which at least one compound (e.g., a HCV protease inhibitor) is administered in one or more discrete dosages over a twenty-four hour time interval in an asymmetric pattern as to dosage amount and/or timing of dosage, wherein the at least one compound is selected from the group consisting of compounds of Formulae I-XXVI, described herein. Methods of modulating the activity of hepatitis C virus protease in a subject are also provided. Asymmetric dosing as to amount of dose and/or timing of dose permits adjustment of dosing to accommodate variations in drug metabolism and/or viral activity caused by viral cell division or a patient's circadian rhythms, thus delivering the maximum amount of dose at the time or times it is most effective.
WO2007019078A3	Tricyclic beta-secretase inhibitors for the treatment of alzheimer's disease	The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
WO2007045151A1	Compounds and their pharmaceutical compositions for the treatment of nasal cavum hypersecretion and chronic obstructive pulmonary disease	Compounds and their pharmaceutical compositions are for the treatment of nasal cavum hypersecretion and chronic obstructive pulmonary disease. The compounds are azo biocyclo [2.2.2] octane derivatives. The pharmaceutical compositions contain the above active compounds and are in forms of aerosol, powder, nasal drop and nasal spray. The compounds and the compositions containing the compounds can be used as medicines for anti-chronic obstructive pulmonary disease and treating rhinitis.
WO2007058630A1	Novel bis(amino)-ortho-dicarbaborane cluster compounds	Bis(amino)-ortho-dicarbaboranes and bis(amino)-ortho-dicarbaborane compounds and their nido-derivates are used as boron neutron capture therapy agents. A method of synthesizing the bis(amino)-ortho-dicarbaborane clusters from corresponding bis(phthalimido)acetylenes is described as well as pharmaceutical compositions and the use of the compounds.
WO2007115947A1	Pyrrolo-quinoxalinone derivatives as antibacterials	Tricyclic nitrogen containing compounds of the following Formula (I) and their use as antibacterials.
WO2007122274A1	Acetylcholinesterase-inhibiting compounds for treating alzheimer's disease	Compounds of formula (I) and the pharmaceutically acceptable salts or solvates thereof, including any stereoisomer or mixture of stereoisomers, in which R1, R2, R3 and R4 are radicals selected independently from the group consisting of H, Cl, F, Br, CF3, (C1-C4)alkyl, (C1-C4)alkoxyl and nitro; R5, R6, R7 and R8 are radicals selected independently from the group consisting of H and (C1-C6)alkoxyl; n is an integer from 3 to 5; r is an integer from 2 to 5; s is an integer from 1 to 5 and X is a biradical selected from CO and CH2. They behave as acetylcholinesterase inhibitors with two bonding sites and are useful as active principles against Alzheimer's disease.
WO2008004698A3	Pyrazolo [1, 5-a] pyrimidine compounds as cb1 receptor antagonist	The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: -C(=O)- or -SO2-, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.
WO2008024305A2	Bis (thiohydrazide amides) for treating melanoma	Disclosed herein are methods of treating lentigo maligna, superficial spreading malignant melanoma, acral lentiginous malignant melanoma or nodular malignant melanoma with bis(thio-hydrazide amides) represented by a formula selected from Structural Formulas (I)- (IX) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these bis(thio-hydrazide amides) and compositions comprising these bis(thiohydrazide)amides and one or more anticancer agent.
WO2008052350A1	Photodynamic therapy for the treatment of hidradenitis suppurativa	Provided herein are methods for photodynamic treatment and/or prevention of hidradenitis suppurativa (HS) in a subject. The method involves the systemic administration of a hydrophobic and/or lipophilic photosensitizer to a subject having HS and subsequent exposure of the affected tissue to energy of a wavelength capable of activating the photosensitizer.
WO2008119720A8	1-(1-cyclobutyl-4-piperidinyl)-1,3-dihydro-2h-benzimidazol-2-one derivatives which have activity on the m1 receptor and their use in medicine	Compounds of formula I or a salt thereof are provided wherein R4, R5, R6, Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
WO2009004152A2	Use of a composition of oligomers of galacturonic acid as an agent for inhibiting degradation of collagen	The invention concerns use of a composition of galacturonic acid oligomers having a degree of polymerization substantially in the range of 5 to 25 as an agent for inhibiting collagen degradation. The invention also concerns the use of such a composition for the preparation of a medicine against osteoporosis, cancer, angiogenesis and the proliferation of metastases.
WO2009019721A3	Quercetin derivatives as anti-cancer agents	The present invention provides novel Quercetin derivatives of formula (I) and pharmaceutically acceptable salts, hydrates, and solvates thereof, Formula (I): wherein R1 is hydrogen, benzyl or substituted benzyl; R2 is hydrogen, benzyl or substituted benzyl, linear or branched (C1-C6) alkyl, substituted alkyl, aryl, substituted aryl, heterqcyele,and (Substituted heterocycle, useful for treatment of various disorders including cancer, multi-drug resistant cancers, viral infections etc. The invention also provides a process for the preparation of compounds of formula (I) and pharmaceutical compositions comprising the same.
WO2009026621A1	Pharmaceutical compound & composition	Particulate paliperidone, or a pharmaceutically acceptable salt thereof, having a D50 particle size of between about 1 µm and about 40 µm.
WO2009054786A1	1,2,4-triazole aryl n-oxides derivatives as modulators of mglur5	The present invention is directed to 1,2,4-triazole aryl N-oxides derivatives, their use as modulators of mGluR5 and pharmaceutical compositions comprising said compounds.
WO2009074305A1	Gold xanthogenates and medicaments comprising them	The invention relates to xanthogenate-gold compounds and to pharmaceutical formulations of these complexes, and also to medicaments which comprise these formulations for treatment of tumour, virus and autoimmune disorders influenced by activated macrophages.
WO2010004435A3	Ph specific solutions of sodium mycophenolic acid for the treatment of eye disorders	Ocular delivery of drugs to the eyes is an ongoing challenge due to the unique anatomical and physiological properties of the eye. A solution of the immunosuppressant and anti-inflammatory compound mycophenolic acid with a pH from 6.0 to 8.5 has been demonstrated to exhibit improved bioavailability when topically applied to the eye. Specifically, topical application to the eye of such a solution is effective in penetrating anterior and posterior eye structures. Said solution is effective in treating a variety of inflammatory disorders, including uveitis, allergic conjunctivits, and keratoconjunctivitis sicca.
WO2010012965A2	Combination of a tlr3 ligand and a chemotherapy agent which acts on the intrinsic “apoptosis” pathway in the treatment of cancer	The present invention relates to a medicament comprising, separately or together, (i) a TLR3 ligand and (ii) a chemotherapy agent which acts on the intrinsic apoptosis pathway, for simultaneous or sequential administration in the treatment of cancer, the chemotherapy agent being selected from topoisomerase 2 inhibitors, platinum-derived alkylating agents and PI3 kinase inhibitors.
WO2010027498A3	Compositions and methods for inducing satiety and treating non-insulin dependent diabetes emillitus, pre-diabetic symptoms, insulin resistance and related disease states and conditions	The invention provides methods of treatment that induce satiety in a subject for a period of at least around twenty- four hours by once-daily administration to the subject of a controlled release dosage form, wherein the dosage form is administered while the subject is in the fasted state and at a time of around six to around nine hours prior to the subject's next intended meal, and wherein the dosage form comprises a controlled release composition, which comprises an enterically-coated, ileum hormone-stimulating amount of a nutritional substance and releases the majority of the nutritional substance in vivo upon reaching the subject's ileum. The invention also provides a diagnostic tool for probing the health and disease state of the ileal hormones, excess or deficiencies. The invention provides a safe vehicle for targeted deliveries of chemical, pharmaceuticals, natural substances and nutrition to the ileum. The present invention also provides a method for treating noninsulin dependent diabetes mellitus, pre-diabetic symptoms, and insulin resistance, as well as a number of disease states and conditions including gastrointestinal disorders as otherwise described herein.
WO2010068181A1	11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6)1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27)j16,21,23-decaene citrate salt	The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19- dioxa-5,7,26-triaza-tetracyclo[19.3.1.1 (2,6).1 (8, 12)]heptacosa- 1 (25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions.
WO2010147138A1	Gene encoding fatty acid elongase, and use thereof	A novel fatty acid elongase is provided. Disclosed are: a fatty acid elongase involved in a fatty acid chain extension reaction; a polynucleotide encoding the fatty acid elongase; and others. Specifically disclosed are: a polynucleotide comprising the nucleotide sequence depicted in SEQ ID NO:1 or SEQ ID NO:4; a polynucleotide encoding a protein comprising the amino acid sequence depicted in SEQ ID NO:2; an expression vector and a transformant, each of which carries the polynucleotide; a process for producing a food or the like using the transformant; a food produced by the process; a method for evaluating or selecting a fat-producing bacterium of interest; and others.
WO2011056222A1	Methods of treating disorders associated with protein aggregation	The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti- protein aggregate ("APA") compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.
WO2011093831A3	Effervescent formulations comprising cefprozil as active agent	Present invention relates to pharmaceutical formulations formulated in effervescent form comprising cefprozil active agent and the process for their preparations.
WO2011115687A2	Alkylated sp-b peptoid compounds and related lung surfactant compositions	SP-B peptoid compounds, lung surfactant compositions and related surfactant replacement therapies. Such SP-B peptoids can mimic lung surfactant protein B, and can be used in conjunction with biomimetic SP-C compounds over a range of lung surfactant compositions.
WO2011115938A1	Spiro-tetracyclic ring compounds as beta - secretase modulators	The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula (I) wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
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WO2013017063A1	Stable polymorphic forms of compound as hypoxia mimetics, and uses thereof	The polymorphic forms of the compound of Formula I, the preparation thereof including the preparation of the intermediates, the pharmaceutical compositions thereof and the uses of a polymorph above in the manufacture of medicaments for treating a disease, a disorder or a condition are disclosed.
WO2013132092A1	Use of monounsaturated fatty acid compounds for controlling the body weight of a dog or a cat	Use of a compound of the general formula (I), COOH-CHR-(CH2)m-CH=CH-(CH2)n-CH3 (I), wherein R can be any group with a molecular weight from 14 to 200 Da, m and n are independently selected from an integer of 0 to 15, and the double bond is in cis or trans configuration or a mixture thereof, or a veterinary acceptable salt, ester or glyceride thereof, for controlling body weight in a pet selected from the group consisting of a dog and a cat.
WO2013169578A1	C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity	Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III:These compounds are useful for the treatment of HIV and AIDS.
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WO2014136944A1	Aqueous liquid composition including high concentration of l-histidine	The present invention addresses the problem of providing an aqueous liquid composition which is suitable for oral ingestion and includes a high concentration of histidine, a method for preparing the liquid composition, and uses, and the like, for the liquid composition. Provided are: an aqueous liquid composition which includes histidine in a concentration exceeding 20 wt%, in particular, an aqueous liquid composition which further includes a divalent or polyvalent organic acid; a preparation method for a histidine-containing composition which is characterized in that histidine is dissolved in a concentration exceeding 20 wt% in an acidic aqueous solution which includes a divalent or polyvalent organic acid; and a food or beverage product which includes the liquid composition.
WO2014144455A1	1 -phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof	Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1 -R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
