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05th week of 2011 patent applcation highlights part 49
Patent application numberTitlePublished
20110028416NUTRITIONAL COMPOSITIONS FOR PROMOTION OF BONE GROWTH AND MAINTENANCE OF BONE HEALTH COMPRISING EXTRACTS OF FOR EXAMPLE ROSEMARY OR CARAWAY - Compositions and methods for maintenance of bone health or prevention, alleviation and/or treatment of bone disorders are presented. The present invention also provides the manufacture of a nutritional product, a supplement or a medicament for promoting bone growth or for the maintenance of bone health and methods regarding same. In an embodiment, the present invention provides a composition comprising an active ingredient having an effective amount of a plant or plant extract containing at least one phytochemical having the ability to induce bone morphogenic protein expression.2011-02-03
20110028417Macrocyclic Compounds and Methods of Use Thereof - The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.2011-02-03
20110028418USE OF GABBA RECEPTOR ANTAGONISTS FOR THE TREATMENT OF EXCESSIVE SLEEPINESS AND DISORDERS ASSOCIATED WITH EXCESSIVE SLEEPINESS2011-02-03
20110028419FUNGICIDE COMPOSITION FOR AGRICULTURE AND HORTICULTURE AND METHOD FOR PREVENTING PLANT DISEASES - The present invention provides a composition in which a fungicidal effect against a cultivated crop infected by a plant disease is stable and highly active. An excellent agricultural or horticultural fungicide composition for controlling a plant disease is provided by using (a) at least one imidazole compound represented by formula (I):2011-02-03
20110028420Regression of Established Atherosclerotic Plaques, and Treating Sudden-Onset Asthma Attacks, using PARP Inhibitors - A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.2011-02-03
20110028421Use of alkylphosphocholines in combination with antimetabolites for the treatment of benign and malignant oncoses in humans and mammals - The invention relates to the use of alkylphosphocholines in combination with antimetabolites for the treatment of multiple myeloma, colon cancer or renal cancer. Preferred alkylphosphocholines are described by the Formula II.2011-02-03
20110028422COMBINATION OF NILOTINIB AND A NITROGEN MUSTARD ANALOGUE FOR THE TREATMENT OF CHRONIC LYMPHOCYTIC LEUKEMIA - The invention relates to a combination which comprises (a) a DNA damaging agent; and (b) 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide (“nilotinib”); a pharmaceutical composition comprising such a combination and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the treatment chronic lymphocytic leukemia (CLL); the use of such a combination for the preparation of a medicament for the treatment of CLL; a commercial package or product comprising such a combination; and to a method of treatment of a warm-blooded animal, especially a human.2011-02-03
20110028423AGENT THAT MODULATES PHYSIOLOGICAL CONDITION OF PESTS, INVOLVED IN INSECT CHOLINE ACETYLTRANSFERASE ACTIVITY - The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect choline acetyltransferase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a choline acetyltransferase in a reaction system in which the choline acetyltransferase contacts with a test substance, and the like.2011-02-03
20110028424OIL-IN-WATER MICROEMULSION CARRYING LARGE AMOUNT OF OIL - An oil-in-water microemulsion is provided, which includes, on the basis of its total weight, the following components of A) 55-95 wt % of a water phase; B) 0.1-20 wt % of an oil phase, wherein the oil phase comprises at least one oil/fat component containing polyoxypropylene chains; and C) 1-25 wt % of an oil-in-water nonionic emulsifier, wherein the emulsifier is selected from the following group of: hydrophilic nonionic surfactants with polyoxyethylene chains as hydrophilic groups, polyglycerol fatty acid esters, polyglycerol fatty alcohol ethers, sucrose fatty acid esters, and hydrocarbyl polyglycosides. The oil-in-water microemulsion carries a large amount of oil. In addition, the use of an oil/fat containing polyoxypropylene chains is disclosed for increasing the amount of oil carried in an oil-in-water microemulsion.2011-02-03
20110028425Vesicle And Cosmetic Containing The Same - A vesicle according to the present invention is characterized in that it comprises a sucrose fatty acid diester and an acyl methyl taurate in an amount of 5 to 30 wt % relative to the diester and that the sucrose fatty acid diester is contained as a main component of membrane, and has excellent dispersion stability. Also the present invention includes a cosmetic comprising the vesicle and a lotion in which the vesicle is dispersed in a solvent containing alcohol.2011-02-03
20110028426DEWATERING BIOMASS MATERIAL COMPRISING POLYSACCHARIDE, METHOD FOR EXTRACTING POLYSACCHARIDE FROM BIOMASS MATERIAL, AND DEWATERED BIOMASS MATERIAL - A process for dewatering biomass material comprising polysaccharide and water. The process comprises wetting the biomass material with a wetting composition comprising an alcohol to form a biomass slurry comprising wetted biomass material and a liquid component, mechanically separating a portion of the liquid component from the biomass slurry, and mechanically separating at least a portion of the water from the wetted biomass material. A process for extracting polysaccharide from the biomass material and a dewatered biomass material are also disclosed.2011-02-03
20110028427DIETARY FIBER AND METHOD FOR PREPARING DIETARY FIBER - The invention relates to a soluble antioxidant dietary fiber obtained from pineapple and a method of processing pineapple pulp to provide a soluble antioxidant fiber.2011-02-03
20110028428HIRSUTELLA SINENSIS MYCELIA COMPOSITIONS AND METHODS FOR TREATING SEPSIS AND RELATED INFLAMMATORY RESPONSES - Compositions comprising 2011-02-03
20110028429COMBINATION OF POLYCHITOSAMINE AND HMG-COA REDUCTASE INHIBITOR FOR HYPERLIPIDEMIA - Combinations of therapeutic compounds for prophylaxis or treatment of hyperlipidemia and hyperlipidemia related disorders, such as hypercholesterolemia and the resultant atherosclerosis in a mammal. The combinations are useful for reducing serum cholesterol, and/or cholesteryl ester, triglycerides, phospholipids and fatty acids in a mammal. The methods of the preferred embodiments comprise administering to a mammal a first amount of polychitosamine and a second amount of an HMG-CoA reductase inhibitor (statin).2011-02-03
20110028430INJECTABLE VISCOUS MEDICINAL PREPARATION COMPRISING ETHANOL AND AN X-RAY OPAQUE FAT-SOLUBLE COMPOUND - An injectable medicinal preparation is including ethanol and at least one at least partially X-ray opaque, fat-soluble compound, characterized in that it further comprises an ethanol-soluble compound which, when dissolved, has a viscosity ranging from 10 to 700 cP and preferably from 90 to 350 cP at 25° C., so as to provide an embolizing effect-inducing gel, and, in that the ethanol has a purity ranging from 70 to 99% vol., preferably from 90 to 99% vol., so as to provide a sclerosing effect. The preparation is particularly useful for treating venous malformations such as venous angiomas.2011-02-03
20110028431ORAL MUCOADHESIVE DOSAGE FORM - A direct compression formulation suitable for preparing buccal and/or sublingual and dosage forms incorporates a combination of a non-ionic polymeric solubility enhancer, a mucoadhesive polymer, a filler, a disintegrant, and a pharmaceutically active agent. Cannabinoid-cyclodextrin complexes exhibiting an improved property selected from improved stability, higher product yield and improved product uniformity may be obtained by complexing the cannabinoid with the cyclodextrin in a liquid medium containing an antioxidant. To enhance stability, product yield and/or product uniformity, complexing may be done while the liquid medium is in contact with an atmosphere having a very low oxygen content. The resulting complexes may be combined with decomplexing agents and/or dispersed in a matrix material comprised of a hydrogel-forming polymer to provide enhanced absorption of the cannabinoid through oral mucosa and reduced ingestion of the cannabinoid as compared with known commercially available cannabinoid-containing oral dosage forms.2011-02-03
20110028432USE 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.2011-02-03
20110028433QUINAZOLINONE DERIVATIVES AS TUBULIN POLYMERIZATION INHIBITORS - The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I)2011-02-03
20110028434LONG-CHAIN POLYUNSATURATED FATTY ACIDS (LC-PUFA) IN MATERNAL NUTRITION DURING PREGNANCY AND LACTATION - The present invention relates in general to maternal food compositions. In particular, the present invention relates to maternal food compositions comprising LC-PUFA and their uses. Embodiments of the present invention relate to maternal food compositions comprising a source of lipids, wherein the source of lipids includes at least one LC-PUFA in the form selected from the group consisting of phospholipids (PL), phosphotidylcholine (PC), phosphatidylethanolamine (PE), N-Acylphosphatidylethanolamine (NAPE), phosphatidylinositol (Pl), phosphatidylserine (PS) or their lyso derivatives and their uses in brain development and eye development of neonates.2011-02-03
20110028435CRYSTALLIZATION METHOD AND BIOAVAILABILITY - Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.2011-02-03
20110028436ORAL COMBINATION OF VITAMINS - This invention provides compositions for treating and preventing nausea and other disorders, the compositions comprising vitamins as active ingredients, including vitamin B6, vitamin K, and vitamin C, and a method for treating nausea or morning sickness with the oral compositions.2011-02-03
20110028437PHOSPHORYLATED PYRONE ANALOGS AND METHODS - The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.2011-02-03
20110028438MEDICAL USE OF 3-2,2,2-TRIMETHYLHYDRAZINIUM PROPIONATE SALTS. - The present invention relates to highly effective treatment of ischemic heart disease with 3-(2,2,2-trimethylhydrazinium) propionate hydrogen fumarate, and 3-(2,2,2-trimethylhydrazinium) propionate dihydrogen phosphate.2011-02-03
20110028439Combination hormone replacement therapy (HRT) and melatonin to prevent and treat mammary cancer - A combination hormone and melatonin therapy is provided to reduce the risk of developing, or to reduce the severity of, breast cancer by administering at least one estrogen hormone and optionally at least one progesterone-receptor-binding compound or composition and melatonin together, preferably at normal bed time.2011-02-03
20110028440Simultaneous Method for the Preparation of a Mixture of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene and 3-acetoxy-2'-chloro-5-androsteno[17,16-b]pyridine - The present invention relates to preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene (4) and 3-acetoxy2′-chloro-5-androsteno[17,16-b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole, a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC2011-02-03
20110028441NOVEL PHENYL-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES - The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO2011-02-03
20110028442DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL) PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR - The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.2011-02-03
20110028443LIGANDS FOR NEMATODE NUCLEAR RECEPTORS AND USES THEREOF - An effective anti-nematode methodology entails contacting nematodes with a biologically effective amount of at least one compound according to formula I:2011-02-03
20110028444PHARMACEUTICALLY ACCEPTABLE SALTS OF ANTI-INFECTION QUINOLONE COMPOUNDS - The invention discloses the pharmaceutically acceptable salts of an optically active quinolone compound useful against infection, specifically the pharmaceutically acceptable salts of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. The pharmaceutically acceptable salts of the present invention are stable and have improved water solubility. They possess higher biological activity, less toxicity for kidney and no irritation to skin and muscle.2011-02-03
20110028445Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use - The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim 2011-02-03
20110028446ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I):2011-02-03
20110028447INDAZOLE DERIVATIVES - This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R2011-02-03
20110028448PYRIDINE COMPOUNDS - The invention relates to pyridine compounds, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.2011-02-03
20110028449NOVEL AMINOMETHYL BENZENE DERIVATIVES - The invention relates to novel aminomethyl benzene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.2011-02-03
20110028450Ring-annulated dihydropyrrolo[2,1-alpha]isoquinolines - The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I2011-02-03
20110028451Dihydrobenzoindazoles - The invention relates to benzoindazole derivatives according to general Formula I2011-02-03
20110028452PYRIDO[4,3-d]PYRIMIDIN-4(3H)-ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS - The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I2011-02-03
20110028453Treating Negative Symptoms of Schizophrenia Associated with Defective Neuregulin 1 - Use of a compound that is a serotonin transporter inhibitor, a selective norepinephrine reuptake inhibitor, or a 5-HT2011-02-03
20110028454DEUTERIUM-ENRICHED BAZEDOXIFENE - The present application describes deuterium-enriched bazedoxifene, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.2011-02-03
20110028455Indole-substituted 3-cyanopyridines As Kinase Inhibitors - Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is —O—, —N(R2011-02-03
20110028456Solid Pharmaceutical Dosage Form - A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid/sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and/or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.2011-02-03
20110028457PHARMACEUTICAL PREPARATION COMPRISING PERMETHYLATED CYCLODEXTRIN - The invention relates to a pharmaceutical preparation for applying a pharmaceutical agent. According to the invention, the preparation contains: a) a pharmaceutical agent which has an aromatic group or an aromatic part and the molecule of which has a maximum diameter of ≦2 nm; b) a permethylated cyclodextrin having a degree of substitution of 3 methyl groups per glucopyranose unit. The permethylated cyclodextrin and the pharmaceutical agent form a complex.2011-02-03
20110028458INHIBITION OF CELL MIGRATION BY A FARNESYLATED DIBENZODIAZEPINONE - The invention relates to the discovery that dibenzodiazepinone analogues have cell migration inhibiting activities on neoplastic and endothelial cells. The migration of neoplastic cells from various tumor types, such as a glioma tumor that may comprise an EGF and/or PTEN mutation, or a Ras-, Raf, or EGFR-mediated tumor, may be inhibited when contacted by the dibenzodiazepinone analogues of the present invention. The invention includes methods for inhibiting migration of a cell in a subject, by contacting a cell with a dibenzodiazepinone analogue of the present invention.2011-02-03
20110028459Wound Healing - A phenothiazinium compound, compositions and medicaments for use in promoting wound healing and a method for promoting wound healing or cosmetic use by applying or administering a phenothiazinium compound to a wound site or the skin, and optionally exposing the wound site or skin to light.2011-02-03
20110028460TOPICAL FORMULATION - It has been discovered that certain combinations compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.2011-02-03
20110028461HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.2011-02-03
20110028462Niacin Receptor Agonists, compositions Containing Such Compounds and Methods of Treatment - A method of treating atherosclerosis and related conditions using compounds of formula I: as well as pharmaceutically acceptable salts and solvates is disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels.2011-02-03
20110028463AMIDE COMPOUNDS - [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. 2011-02-03
20110028464INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of formula I: wherein c, R2011-02-03
20110028465AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following:2011-02-03
20110028466NITROIMIDAZOOXAZINE AND NITROIMIDAZOOXAZOLE ANALOGUES AND THEIR USES - The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for 2011-02-03
20110028467HETEROCYCLIC DERIVATIVES - The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid.2011-02-03
20110028468COMPOUNDS HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY - This invention provides a compound of the formula (I):2011-02-03
20110028469Thiphene-2-Carboxamide Derivatives As Modulators of CCR9 Receptor - Provided are compounds of Formula (I) or of Formula (II) that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or amelioratin diseases associated with modulation of CCR9 receptor activity.2011-02-03
20110028470Detection and Treatment of Schizophrenia - The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.2011-02-03
20110028471COMBINATION THERAPY 238 - There is provided a combination product comprising a VEGFR tyrosine kinase inhibitor and a m TOR-selective kinase inhibitor, and methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient.2011-02-03
20110028472THIENOPYRIMIDINES - Novel thienopyrimidines of the formula (I), in which R2011-02-03
20110028473METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS BY ADMINISTERING 6,7-DIALKOXY QUINAZOLINE DERIVATIVES - Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.2011-02-03
20110028474PROTEIN KINASE AND PHOSPHATASE INHIBITORS - The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.2011-02-03
20110028475TETRAHYDROISOQUINOLINE SULFONAMIDE DERIVATIVES, THE PREPARATION THEREOF, AND THE USE OF THE SAME IN THERAPEUTICS - The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I:2011-02-03
20110028476PROTON PUMP INHIBITORS - A proton pump inhibitor containing a compound represented by the formula (I)2011-02-03
20110028477STABLE OPHTHALMIC FORMULATIONS - Disclosed herein are stable formulations suitable for the treatment of glaucoma and ocular hypertension.2011-02-03
20110028478ISOXAZOLINES AS INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides isoxazoline FAAH inhibitors of the formula (I):2011-02-03
20110028479SUBSTITUTED PYRROLOTRIAZINES AND THEIR USE - The present application relates to new, substituted pyrrolo[2,1-f][1,2,4]triazine derivatives of the formula (I) as prostacyclin (PGI2011-02-03
20110028480ORODISPERSABLE FORMULATIONS OF PHOSPHODIESTERASE-5 (PDE-5) INHIBITORS - Orodisperable formulations of phosphodiesterase-5 (PDE-5) inhibitors and methods of manufacturing such are provided. Further, an improved dosage form and method of treating sexual dysfunction are provided.2011-02-03
20110028481HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.2011-02-03
20110028482ISOXAZOLINES AS INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides isoxazoline FAAH inhibitors of the formula (I):2011-02-03
20110028483INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.2011-02-03
201100284842-PHENYL-4-CYCLOPROPYL-PYRIMIDINE DERIVATIVES - The present invention relates to 2-phenyl-4-cyclopropyl-pyrimidine derivatives and their use as P2Y2011-02-03
201100284851,5-DIPHENYLPYRAZOLES II AS HSP90 INHIBITORS - Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R2011-02-03
20110028486INDOLES AS MODULATORS OF NICOTICIC ACETYLCHOLINE RECEPTOR SUBTYPE ALPHA-7 - The present invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-5-(trifluoromethyl)-2-pyrimidinecarboxamide.2011-02-03
20110028487IMIDAZOPYRIMIDINES AND USES THEREOF - The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.2011-02-03
20110028488COMBINATION PRODUCT COMPRISING SRC KINASE INHIBITOR AZDO530 AND AN ANTIOESTROGEN OR EGFR-TK-INHIBITOR - The invention relates to a combination for use in the synergistic treatment of breast cancer comprising an antioestrogen and the Src kinase inhibitor AZD0530, a combination for the synergistic treatment of cancer comprising an EGFR TKI and the Src kinase inhibitor AZD0530 and a triple combination for the synergistic treatment of breast cancer comprising an antioestrogen, an EGFR TKI and the Src kinase inhibitor AZD0530.2011-02-03
20110028489Pyrimidine Derivatives and Their Use for Treating Bone-Related Disorders - The present invention relates to a new use of pyrimidine derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof in the manufacture of a medicament in the treatment and/or prophylaxis of Alzheimer's Disease:2011-02-03
201100284904-PHENYL-PIPERAZIN-1-YL-ALKYL-BENZOIMIDAZOL-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE IN-HIBITORS - This invention relates to novel 4-phenyl-piperazin-1-yl-alkyl-benzoimidazol-2-one derivatives of structure (I) useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.2011-02-03
20110028491APOPTOSIS INHIBITOR - It is directed to provide a novel apoptosis inhibitor. Specifically directed is an apoptosis inhibitor containing a biphenylcarboxamide compound represented by the following formula (1) as an active ingredient, wherein R2011-02-03
20110028492Heteroaryl Compounds and Their Uses - The present invention provides a compound of formula (I):2011-02-03
20110028493HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like.2011-02-03
20110028494HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.2011-02-03
20110028495THE USE OF 6-HALOGENO-[1,2,4]-TRIAZOLO-[1,5-a]-PYRIMIDINE COMPOUNDS FOR COMBATING PESTS IN AND ON ANIMALS - The present invention relates to the use of 6-halogeno-[1,2,4]-triazolo[1,5-a]-pyrimidine compounds of the general formula I2011-02-03
20110028496Deuterium-enriched pyrimidine compounds and derivatives - The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof2011-02-03
20110028497NOVEL DERIVATIVES OF PURINIC AND PYRIMIDINIC ANTIVIRAL AGENTS AND USE THEREOF AS POTENT ANTICANCER AGENTS - Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.2011-02-03
20110028498METHOD FOR EVALUATING PATIENTS FOR TREATMENT WITH DRUGS TARGETING RET RECEPTOR TYROSINE KINASE - The present invention provides a method of selection of a patient, who is a candidate for treatment with a RET drug, whereby to predict an increased likelihood of response to a RET drug. The invention provides a method for determining the sequence of RET. The method provides ARMS primers optimised for determining the sequence of RET. The invention also provides a diagnostic kit, comprising an ARMS primer.2011-02-03
20110028499PHARMACEUTICAL COMBINATION COMPRISING VITAMIN K - It is found that compounds having PPARδ agonistic activity induced abnormal blood coagulation or muscular disorder. A pharmaceutical combination comprising vitamin K and a compound having PPARδ agonistic activity can prevent the abnormal blood coagulation. A pharmaceutical composition comprising vitamin K can prevent muscular disorder.2011-02-03
20110028500PLANT PATHOGEN INHIBITOR COMBINATIONS AND METHODS OF USE - Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity2011-02-03
20110028501SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.2011-02-03
20110028502DIHYDROPYRIMIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I:2011-02-03
20110028503COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the eye.2011-02-03
20110028504Formulation of radioprotective alpha beta unsaturated aryl sulfones - A pharmaceutical composition is provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject. An effective amount of the pharmaceutical composition provided comprising an effective amount of at least one radioprotective α, β unsaturated aryl sulfone, and at least one component selected from the group consisting of a) at least one water soluble polymer in an amount between about 0.5% and about 90% w/v, b) at least one chemically modified cyclodextrin in an amount between about 20% and about 60% w/v, and c) DMA in an amount between about 10% and about 50% w/v.2011-02-03
20110028505COMPOSITIONS AND METHODS FOR REDUCING FOOD CRAVINGS - Disclosed are compositions for reducing food cravings, comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound is an α-MSH agonist. Also disclosed are methods of reducing food cravings, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.2011-02-03
20110028506Pharmaceutical Composition For Preventintion And Treatment Of Restenosis Comprising Isoxazole Derivatives - There is provided a pharmaceutical composition for prevention and treatment of restenosis comprising isoxazole derivatives. The pharmaceutical composition includes a therapeutic effective amount of isoxazole derivatives represented by Formula 1 or pharmaceutically available salts thereof. The pharmaceutical composition may be useful to prevent and treat vascular restenosis since the pharmaceutical composition shows an anti-restenosis activity and accelerates the re-endothelization.2011-02-03
20110028507PYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIF α in a subject, modulating expression of HIF-regulated genes in a subject, treating an HIF-related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds.2011-02-03
20110028508NOVEL PROCESS FOR THE PREPARATION OF SCOPINE ESTERS - The present invention relates to novel processes for the preparation of scopine esters and their quaternary salts. In particular, the present invention relates to a process for the preparation of tiotropium bromide, pharmaceutical compositions comprising tiotropium bromide and the use of such compositions in the treatment of respiratory disorders.2011-02-03
20110028509Sulfonamides - The invention relates to compounds of formula I2011-02-03
20110028510Compositions, Methods, and Kits for Treating Influenza Viral Infections - The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus).2011-02-03
20110028511PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS - According to the present invention there are provided novel processes for the manufacture of the compound of formula 12011-02-03
20110028512BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS - Heterocyclic compounds of the general formula (I) are provided in which R, R2011-02-03
20110028513METHOD FOR TREATING NEUROLOGICAL DISORDERS WITH IMIDAZOLIUM AND IMIDAZOLINIUM COMPOUNDS - There is presently provided methods for delivering a neuroprotective agent to a neural cell. The methods comprise contacting a neural cell with an imidazolium or imidazolinium compound as described herein, including an imidazolium or imidazolinium salt.2011-02-03
20110028514Azoles as Malonyl-CoA Decarboxylase Inhibitors Useful as Metabolic Modulators - The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R2011-02-03
20110028515NEW PIPERIDINE DERIVATIVES - Compounds of formula (I)2011-02-03
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