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37th week of 2010 patent applcation highlights part 52
Patent application numberTitlePublished
20100234372SUBSTITUTED 2-MERCAPTOQUINOLINE-3-CARBOXAMIDES AS KCNQ2/3 MODULATORS - The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.2010-09-16
20100234373BIS-ARYL AMIDE COMPOUNDS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I2010-09-16
20100234374Heterocycle Substituted Ketone Derivatives as Histone Deacetylase (HDAC) Inhibitors - The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.2010-09-16
20100234375HIV INHIBITING 5-(HYDROXYMETHYLENE AND AMINOMETHYLENE) SUBSTITUTED PYRIMIDINES - This invention concerns 5-(hydroxymethylene and aminomethylene)pyrimidine derivatives having HIV (Human Immunodeficiency Virus) replication inhibiting properties, to the preparation thereof and to pharmaceutical compositions comprising these compounds.2010-09-16
20100234376[4,5']Bipyrimidinyl-6,4'-Diamine Deriviatives as Protein Kinase Inhibitors - The invention provides a novel class of compounds of the Formula I:2010-09-16
20100234377PIPERAZINE COMPOUNDS FOR THE INHIBITION OF HAEMATOPOIETIC PROSTAGLANDIN D SYNTHASE - The present invention relates to compounds of general formula (I):2010-09-16
20100234378ALKYLSULFONAMIDE-SUBSTITUTED TRIAZOLES AS MATRIX METALLOPROTEASE INHIBITORS - Provided are MMP-2, MMP-3, MMP-9, MMP-12 and/or MMP-13 inhibitors having the Formula (I): wherein R2010-09-16
20100234379Dual modulation of endocannabinoid transport and fatty-acid amide hydrolase for treatment of excitotoxicity - The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury.2010-09-16
20100234380CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PHENYL-PYRAZOLES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR - The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2010-09-16
20100234381BIOMARKERS AND METHODS FOR DETERMINING SENSITIVITY TO VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2 MODULATORS - A method for predicting the likelihood a mammal will respond therapeutically to a method of treating cancer comprising administering a VEGFR-2 modulator or a dual VEGFR-2/FGFR-1 modulator wherein the method comprises: (a) measuring in the mammal the level of FGF2; (b) either comparing the level of FGF2 in the sample relative to a standard to permit assignment of the sample to either being a member of an FGF2 positive class or an FGF2 negative class, or comparing the level of FGF2 in the sample relative to a standard, wherein assignment of the mammal to the FGF2 positive sample class or a determination that the mammal has an elevated level of FGF2, indicates an increased likelihood the patient will respond therapeutically to the cancer treatment. Methods of predicting whether a mammal has received an efficacious dose of a VEGFR-2 modulator or a dual VEGFR-2/FGFR-1 modulator is also disclosed, in addition to kits comprising these methods.2010-09-16
20100234382COMPOSITION COMPRISING A PDE4 INHIBITOR AND A PDE5 INHIBITOR - The invention relates to the combined administration of a PDE4 inhibitor and a PDE5 inhibitor for the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.2010-09-16
20100234383TREATING, PREVENTING OR AMELIORATING A HYPERPROLIFERATIVE DISEASE/DISORDER - The invention provides a method for treating, preventing or ameliorating a hyperproliferative disease and/or disorder such as cancer (e.g. leukemia) in a mammal comprising administering a therapeutically effective amount of one or more compounds selected from the group consisting of compounds of Formula (I), quinolones and fluoroquinolones; or a pharmaceutically acceptable salt thereof to said mammal:2010-09-16
201002343843, 9-DIAZABICYCLO(3.3.1)NON-3-YL-ARYL METHANONE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.2010-09-16
20100234385Compsition Containing Biopterin and Method for Using The Same - It is thought that applications and use of tetrahydrobiopterin (BH4), which is used as a pharmaceutical, will expand due to its superior efficacy. However, in addition to BH4 being extremely expensive, since it is unstable with respect to oxidation, applications other than pharmaceuticals are considered to be difficult. Further, it is difficult for BH4 to permeate through a blood-brain barrier, so that BH4 concentrations in the brain tend not to increase under the present conditions. Biopterins are oxidized form of BH4, stable to oxidation, easy to handle, and can be produced inexpensively. The inventors found that administration of biopterin can be expected to demonstrate effects equal to or greater than those of administration of BH4. On the basis of the result, it was first clarified that administration of a composition containing biopterin causes increase in BH4 concentration in the body (especially BH4 concentration in the brain, which is difficult to be increased by BH4 administration) to demonstrate sufficient actions.2010-09-16
20100234386QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.2010-09-16
20100234387Sulfonylated Tetrahydroazolopyrazines and their Use as Pharmaceuticals - Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I2010-09-16
20100234388SUBSTITUTED PDE5 INHIBITORS - Provided herein are substituted PDE5 inhibitors of Formula (1), and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function. The compounds are deuterated tadalafil derivatives.2010-09-16
20100234389AMIDE COMPOUND - An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic.2010-09-16
20100234390NOVEL COMPOUND AND THEIR USE - The present invention provides novel compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The novel compounds are useful as antibacterial agents in the treatment of conditions such as nosocomial pneumonia, community acquired pneumonia, infections caused by vancomycin resistant enterococci (VRE), methicillin resistant 2010-09-16
20100234391N-SUBSTITUTED PIPERAZINES - Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I)2010-09-16
201002343924-SULFONYLPIPERIDINE DERIVATIVES - [Problems] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases.2010-09-16
20100234393USE OF A VASOPEPTIDASE INHIBITOR FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - The present invention relates to the use of a vasopeptidase inhibitor for the preparation of a medicament for use in the treatment and/or prevention of PAH.2010-09-16
20100234394SUBSTITUTED BENZIMIDAZOLES AND METHODS OF THEIR USE - New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.2010-09-16
20100234395UREIDE DERIVATIVE AND PHARMACEUTICAL APPLICATION THEREOF - Discloses is a pharmaceutical agent comprising an ureide derivative represented by the formula: or a pharmaceutically acceptable salt thereof as an active ingredient. The ureide derivative or the pharmaceutically acceptable salt thereof is useful for the relief of a pain or the treatment or prevention of neurogenic pain.2010-09-16
20100234396Tetrhydropyridoindole 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.2010-09-16
20100234397ENZYME INHIBITORS - There is disclosed herein methods for using compounds of formula (I),2010-09-16
20100234398INSECTICIDAL N-SUBSTITUTED (HETEROARYL)ALKYL SULFILIMINES - N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.2010-09-16
20100234399AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT - An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.2010-09-16
20100234400COMPOUNDS THAT MAINTAIN PLURIPOTENCY OF EMBRYONIC STEM CELLS - The present invention relates to methods and compositions for culturing embryonic stem (ES) cells. The methods relate to growing the ES cells in the presence of small molecules of formula (I) that maintain the pluripotency/self-renewal of the cells without feeder cells and LIF in serum-free conditions. These methods in part facilitate much more consistency in embryonic stem cell production, providing, for example, new avenues in the practical applications of embryonic stem cells in regenerative medicine.2010-09-16
201002344016,9-Disubstituted Purine Derivatives and Their Use For Treating Skin - The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.2010-09-16
20100234402METHODS AND COMPOSITIONS FOR TREATING SPINAL MUSCULAR ATROPHY - This invention provides methods of treating and abrogating spinal muscular atrophy by administering an antioxidant. Additionally, the invention provides a method of protecting the SMN protein by administering an antioxidant.2010-09-16
20100234403Aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.2010-09-16
20100234404P-38 Kinase Inhibitors - Compounds and compositions for modulating the activity of p38 kinases are provided, including p38α, and p38β kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.2010-09-16
20100234405PYRIMIDINE NUCLEOSIDE DERIVATIVES AND SALTS THEREOF - A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have excellent antiviral properties and are useful as antiviral therapeutic agents:2010-09-16
20100234406COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.2010-09-16
20100234407PREVENTIVES/REMEDIES FOR MYELOMA TUMOR AND METHOD FOR DIAGNOSING THE SAME - The present invention provides a preventive or therapeutic drug for a myeloma tumor and osteoclastic bone loss associating therewith, the drug containing as an active ingredient an osteopontin-production regulator or inhibitor; a screening method for a preventive or therapeutic drug for a myeloma tumor, characterized by determining osteopontin production regulatory or inhibitory effect; as well as a diagnostic kit for a myeloma tumor, characterized by including a reagent for measuring blood osteopontin level, and a diagnostic method.2010-09-16
20100234408PYRIMIDYLAMINOBENZAMIDE DERIVATIVES FOR THE TREATMENT OF NEUROFIBROMATOSIS - The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF.2010-09-16
20100234409Amino cyclopentyl heterocyclic and carbocyclic modulators of chemokine receptor activity - Compounds of the formulae (I) and (II): (wherein Q, X, E, G2010-09-16
20100234410HYDRATE FOR MEDICAL PURPOSES - The present invention relates to [7-[(7S)-7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hemihydrate. This hemihydrate is stable and easy to prepare, and has excellent properties for a pharmaceutical bulk powder.2010-09-16
20100234411New Combination for the Treatment of Respiratory Diseases - The present invention relates to novel pharmaceutical compositions based on telmisartan 1 and anticholinergics 2 processes for preparing them and their use for the treatment of respiratory diseases.2010-09-16
20100234412Buprenorphine Derivatives and Uses Thereof - Ester derivatives of the phenolic hydroxyl group of buprenorphine can be used in the treatment of opiate dependency and/or moderate to severe pain. The esters have an enhanced bioavailability, an enhanced duration of action, and a reduced abuse potential.2010-09-16
20100234413COMPOSITIONS AND METHODS FOR PROPHYLAXIS AND TREATMENT OF ADDICTIONS - The present invention relates to methods of treating or preventing addiction and relapse use of addictive agents, and treating or preventing addictive or compulsive behaviour and relapse practice of an addictive behaviour or compulsion, by administering a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, alone or in combination with another therapeutic agent, such as, for example, an opioid receptor antagonist or an antidepressant, or an addictive agent, such as, for example, an opioid agonist. The present invention also includes pharmaceutical compositions for treating or preventing addiction or relapse that include a PPARγ agonist and one or more other therapeutic or addictive agents, as well as unit dosage forms of such pharmaceutical compositions, which contain a dosage effective in treating or preventing addiction or relapse. The methods and compositions of the invention are useful in the treatment or prevention of addiction to any agent, including alcohol, nicotine, marijuana, cocaine, and amphetamines, as well as compulsive and addictive behaviours, including pathological gambling and pathological overeating.2010-09-16
20100234414Use of Loratadine 10mg for the prevention of upper respiratory inflammation/sinus infections caused from exposure to bacteria and viruses on airplane flights - The invention relates to the use of Loratadine 10 mg prior to flying to prevent upper respiratory inflammation and sinus infections caused from exposure to bacteria and viruses while flying. People are packed together in airplanes, which has dry and polluted air. Flying is one of the more common places to pick up cold viruses and airborne bacteria. Use of Loratadine 10 mg before the plane takes off to shrink the nasal lining helps prevent susceptibility to bacteria and viruses.2010-09-16
20100234415INDOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS - Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.2010-09-16
20100234416USE OF HUPERZINE FOR DISORDERS - Methods and compositions containing huperzine are used to prevent and alleviate neuropathic pain. The invention is also directed to methods and compositions for using huperzine for the prevention and/or treatment of neuropathic pain and orthostatic hypotension.2010-09-16
20100234417THYROTROPIN RELEASING HORMONE RECEPTOR-OREXIN RECEPTOR HETERO-DIMERS/-OLIGOMERS - A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.2010-09-16
20100234418COMPOUNDS AND USES THEREOF - N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, N-[3-(4-ethynyl-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including pain and polycystic kidney disease.2010-09-16
20100234419SUBSTITUTED 3-AMINOISOXAZOLOPYRIDINES AS KCNQ2/3 MODULATORS - The invention relates to substituted 3-aminoisoxazolopyridines, to processes for their preparation, to medicaments containing these compounds and to the use of these compounds in the preparation of medicaments.2010-09-16
20100234420TETRAHYDROQUINOLINE DERIVATIVES FOR TREATING POST-TRAUMATIC STRESS DISORDERS - The invention relates to methods of treating, reducing the symptoms of, or preventing a post-traumatic stress syndrome by administration of tetrahydroquinoline derivatives of formula I2010-09-16
20100234421SUBSTITUTED 3-AMINO-2-MERCAPTOQUINOLINES AS KCNQ2/3 MODULATORS - The invention relates to substituted 3-amino-2-mercaptoquinolines, to processes for their preparation, to medicaments containing these compounds and to the use of these compounds in the preparation of medicaments.2010-09-16
20100234422Sulfonylated Heterocycles Useful for Modulation of the Progesterone Receptor - Compounds of the following structure are provided, wherein n, R2010-09-16
20100234423TRIAZOLOTHIADIAZOLE INHIBITOR OF C-MET PROTEIN KINASE - The present invention relates to compound 1, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising Compound 1 and methods of using the compositions in the treatment of proliferative disorders.2010-09-16
20100234424DERIVATIVES OF N-PHENYL(PIPERIDINE-2-YL) METHYL BENZAMIDE PREPARATION METHOD THEREOF AND APPLICATIONS OF SAME IN THERAPEUTICS - Compounds of formula (I) as defined herein:2010-09-16
201002344252-SUBSTITUTED-1H-BENZIMIDAZOLE-4-CARBOXAMIDES ARE PARP INHIBITORS - Compounds of Formula (I)2010-09-16
20100234426Phenylpropionamide Compounds and the Use Thereof - The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R2010-09-16
201002344271-PHENETHYLPIPERIDINE DERIVATIVES AND THEIR USE AS OPIOID RECEPTOR LIGANDS - This invention relates to novel 1-phenethylpiperidine derivatives useful as opioid receptor ligands. More specifically, the invention provides compounds useful as μ opioid receptor ligands.2010-09-16
20100234428SUBSTITUTED 2-MERCAPTO-3-AMINOPYRIDINES AS KCNQ2/3 MODULATORS - The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.2010-09-16
20100234429SUBSTITUTED NICOTINAMIDES AS KCNQ2/3 MODULATORS - The invention relates to substituted nicotinamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.2010-09-16
20100234430METHODS AND PHARMACEUTICAL FORMULATIONS FOR PROTECTING PHARMACEUTICAL COMPOUNDS FROM ACIDIC ENVIRONMENTS - Methods and pharmaceutical compositions for protecting pharmaceutical compounds (or drugs) in acidic environments are provided. Methods of treatment using formulations capable of protecting pharmaceutical compounds in acidic environments are also provided. Formulations provided generally comprise a therapeutically effective amount of at least one pharmaceutical compound, and a pharmaceutically acceptable protectant. The pharmaceutically acceptable protectant of the invention generally comprises a water-soluble acid neutralizer, and a water-insoluble acid neutralizer.2010-09-16
20100234431PYRROLIDINE COMPOUNDS - A compound of the following formula:2010-09-16
20100234432Substituted 6-phenylnicotinic acids and their use - The present application relates to novel substituted 6-phenylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, in particular dyslipidaemias, arteriosclerosis and heart failure.2010-09-16
20100234433GLYCOGEN PHOSPHORYLASE INHIBITOR COMPOUND AND PHARMACEUTICAL COMPOSITION THEREOF - This invention relates to a novel compound which is a glycogen phosphorylase inhibitor and its use in the treatment of diabetes and other conditions associated therewith. The invention further relates to a pharmaceutical composition containing the compound and to processes for preparing the compound and pharmaceutical composition.2010-09-16
20100234434FLAVIVIRUS INHIBITION BY SULTAMS AND RELATED COMPOUNDS - Disclosed herein are compounds, compositions and methods for treating or ameliorating flavivirus infections. This is particularly important because the present disclosure provides methods for treating flavivirus infections for which there is no effective vaccine.2010-09-16
20100234435CYCLOALKYLAMINO ACID DERIVATIVES - The invention relates to compounds of formula I2010-09-16
20100234436Pest control agent in form of stable suspension - Disclosed is a pest control agent in the form of a suspension, which exhibits excellent dispersion stability for a long time without forming a hard cake due to settling and separation of solid particles or without losing fluidity due to gelation even when a cationic pest control active ingredient and/or an acid is used. Specifically disclosed is a pest control agent in the form of a suspension, which contains (a) a cationic pest control active ingredient and/or an acid, (b) a nonionic thickening agent, (c) a nonionic surface active agent, (d) a solid active ingredient and (e) water.2010-09-16
20100234437PESTICIDE COMPOSITIONS - This invention is related to the field of compositions useful in the control of pests that eat cellulose, such as, termites, where said composition is compacted and where said composition comprises alpha-cellulose, water, and a pesticide.2010-09-16
20100234438THERAPEUTIC AGENTS - The present invention relates to a 1,5-diphenylpyrazole compound and its use in the treatment of obesity, psychiatric and neurological disorders, to methods for the its therapeutic use and to pharmaceutical compositions containing them.2010-09-16
20100234439THERAPEUTIC AGENTS - The present invention relates to a 1,5-diphenylpyrazole compound and its use in the treatment of obesity, psychiatric and neurological disorders, to methods for the its therapeutic use and to pharmaceutical compositions containing them.2010-09-16
20100234440NOVEL CRYSTAL OF SUBSTITUTED PHENYLALKANOIC ACID ESTER AND PROCESS FOR PRODUCING THE SAME - [Object] In the case of using 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophenyl]propionate, or methyl 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phenyl]propionate as a medicine, more preferable aspects or improved methods are provided.2010-09-16
20100234441NOVEL COMPOUNDS - The present invention provides compounds of formula (I):2010-09-16
20100234442Compositions and Methods for Treatment and Prevention of Cardiovascular Disease - The present invention is in the fields of medicine, pharmaceuticals, neutraceuticals and cardiology. In one aspect, the invention provides compositions comprising enalapril and simvastatin for use in methods for the treatment and/or prevention of cardiovascular disease, and to the use of such compositions in the manufacture of products for such treatment and/or prevention. In another aspect, the invention provides methods for the treatment and/or prevention of cardiovascular disease using compositions comprising enalapril, simvastatin and acetylsalicylic acid. The compositions and methods of the invention are useful in the treatment and prevention of cardiovascular disease in a variety of animals, particularly humans.2010-09-16
20100234443Combinations of statins and anti-obesity agent - Co-therapy of an anti-obesity agent, a statin, is disclosed along with fixed combinations thereof. Atorvastatin and orlistat are preferred as the various components.2010-09-16
20100234444HINDERED ESTER-BASED BIODEGRADABLE LINKERS FOR OLIGONUCLEOTIDE DELIVERY - The invention provides hindered ester-based biodegradable linkers for the delivery of oligonucleotides in vivo, as well as method of making and using the same.2010-09-16
20100234445Patterns of known and novel small RNAS in human cervical cancer - Small RNA sequences that are differentially expressed in SCCC cells are provided. The sequences find use in diagnosis of cancer, and classification of cancer cells according to expression profiles. The methods are useful for detecting cervical cancer cells, facilitating diagnosis of cervical cancer and the severity of the cancer (e.g., tumor grade, tumor burden, and the like) in a subject, facilitating a determination of the prognosis of a subject, and assessing the responsiveness of the subject to therapy.2010-09-16
20100234446RNAi Modulation of the BCR-ABL Fusion Gene and Uses Thereof - The invention relates to compositions and methods for modulating the expression of Bcr-Abl, and more particularly to the down-regulation of Bcr-Abl mRNA and Bcr-Abl protein levels by oligonucleotides via RNA interference, e.g., chemically modified oligonucleotides.2010-09-16
20100234447MODULATION OF GLUCAGON RECEPTOR EXPRESSION - Compounds, compositions and methods are provided for modulating the expression of glucagon receptor. The compositions comprise oligonucleotides, targeted to nucleic acid encoding glucagon receptor. Methods of using these compounds for modulation of glucagon receptor expression and for diagnosis and treatment of disease associated with expression of glucagon receptor are provided.2010-09-16
20100234448IN VIVO PRODUCTION OF SMALL INTERFERING RNAS THAT MEDIATE GENE SILENCING - The invention provides engineered RNA precursors that when expressed in a cell are processed by the cell to produce targeted small interfering RNAs (siRNAs) that selectively silence targeted genes (by cleaving specific mRNAs) using the cell's own RNA interference (RNAi) pathway. By introducing nucleic acid molecules that encode these engineered RNA precursors into cells in vivo with appropriate regulatory sequences, expression of the engineered RNA precursors can be selectively controlled both temporally and spatially, i.e., at particular times and/or in particular tissues, organs, or cells.2010-09-16
20100234449Immunostimulatory Method - The present invention makes it possible to enhance steroid efficacy in a steroid refractory or dependent patient afflicted with an inflammatory condition not responding or responding poorly or inadequately to anti-inflammatory treatment, by administering an oligonucleotide having the sequence 5 5′-Xm-CG-Yn-3′ in an effective amount to said patient and wherein X is A, T, C or G, Y is A, T, C, or G, m=1-100, n=1-100 and wherein at least one CG dinucleotide is ummethylated. The invention also encompasses the use of said oligonucleotide for the manufacture of pharmaceuticals.2010-09-16
20100234450Molecular targeting agents - The present invention relates to aptamer conjugates comprising a metal chelating group and to methods of using these aptamers.2010-09-16
20100234451LNA ANTAGONISTS TARGETING THE ANDROGEN RECEPTOR - The invention relates to oligonucleotide compounds (oligomers), which target androgen receptor mRNA in a cell, leading to reduced expression of the androgen receptor. Reduction of the androgen receptor expression is beneficial for the treatment of certain disorders, such as a hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of androgen receptor using said oligomers, including methods of treatment.2010-09-16
20100234452Anti-Inflammatory and Antioxidant Conjugates Useful for Treating Metabolic Disorders - The present invention is directed to methods for treating metabolic disorders with compounds that are conjugates. The conjugates of the present invention are comprised of salicylic acid, triflusal, diflusinal, salsalate, IMD-0354, ibuprofen, diclofenac, licofelone, or HTB, and one or more antioxidants.2010-09-16
20100234453PHARMACEUTICAL COMPOSITION CONTAINING PHENANTHRENEQUINONE-BASED COMPOUND FOR INTESTINE DELIVERY SYSTEM - Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular phenanthrenequinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.2010-09-16
20100234454TREATMENT OF CNIDARIA INTOXICATION - The present invention relates to the use of vanilloid receptor (VR) antagonists, and more particularly vanilloid receptor 1 (VR1) antagonist, as analgesics in the treatment and/or prohylaxis of cnidaria envenomations.2010-09-16
20100234455Histone Deacetylase Inhibitors - Hormone refractory metastatic disease can be treated with an oxyamide-containing compound through the inhibition of HDAC1 or HDAC2.2010-09-16
20100234456APOPTOSIS PROMOTERS - Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds and methods of treating diseases during which are expressed the Mcl-1 protein are disclosed.2010-09-16
20100234457Aqueous microemulsions containing organic insecticide compounds - The present invention relates to new aqueous microemulsions containing one or more organic insecticide compounds and to their use for plant protection, including seed and crop protection, and protection of non-living material. The formulation according to the invention comprises: 2010-09-16
20100234458Process for the Production of Fatty Acid Alkyl Esters - Disclosed is an improved process for the production of fatty acid lower alkyl esters according to formula (I)2010-09-16
20100234459MEDICALL USE OF 3-(2,2,2,-TRIMETHYLYHDRAZINIUM) PROPIONATE HDROGEN FUMARATE AND DIHYDROGEN PHOSEPHATE - Novel medical use of 3-(2,2,2-trimethylhydrazinium) propionate salts for the manufacture of a medicament for prevention and therapy of atherosclerosis.2010-09-16
20100234460Compositions Comprising A C2-C14 Carboxylic Acid And A Surfactant For Treating Hoof Diseases - Germicidal compositions containing at least one carboxylic acid combined with at least one nonionic or anionic surfactant, and methods of using the compositions for treatment or prevention of infectious hoof diseases are disclosed. The germicidal compositions remain active in the presence of manure, which eliminates the need to pre-clean the hooves before use. The compositions have particular utility for treating or preventing papillomatous digital dermatitis, interdigital phlegmon, interdigital dermatitis, laminitis, white line disease, heel erosion and other hoof diseases.2010-09-16
20100234461Compositions For Improved Oxidative Status In Companion - A food composition that is useful for increasing antioxidant levels in the body is provided having increased levels of sulfur-containing amino acids, such as methionine, cysteine, or mixtures thereof. Methods of using these compositions for increasing antioxidant levels in the body in mammals, especially in companion animals, are also provided.2010-09-16
20100234462TOPICAL COMPOSITION - The invention relates to beneficial topical pharmaceutical compositions comprising diclofenac sodium salt in unusually low amounts. The compositions represent opaque emulsion-gels, in which diclofenac is kept fully dissolved.2010-09-16
20100234463Method for Identifying Modulators of Gamma Secretase or Notch - The present invention relates to methods for high throughput screening to identify selective modulators of γ-secretase. Such modulators selectively block γ-secretase activity without affecting Notch cleavage and signaling. Said methods employ the use of high content screening methodologies to measure and quantify the translocation of the Notch intracellular domain (NICD) between the nucleus and cytoplasm in cells and the activation of Notch.2010-09-16
20100234464COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS - 3-(2,4-Bis(trifluoromethyl)benzyloxy)phenylacetic acid, 4-(2,6-Dimethylbenzyloxy)-phenylacetic acid, and their pharmaceutically acceptable salts are useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis.2010-09-16
20100234465Administration of Intravenous Ibuprofen - An effective dose of intravenous ibuprofen administered every 6 hours in surgery patients is a safe and effective way to reduce both pain and the need for morphine. In preferred embodiments, the administration of intravenous ibuprofen starts with the onset of anesthesia.2010-09-16
20100234466Compositions and Methods for Reducing Body Fat - The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions.2010-09-16
20100234467METHODS FOR IMPROVING BIOAVAILABILITY OF A RENIN INHIBITOR - The present invention provides a method for improving the bioavailability of a renin inhibitor, preferably, of a ε-amino-γ-hydroxy-ω-aryl-alkanoic acid derivative, which method comprises co-administering to a mammal, especially a human, in need of such treatment, a combination of a renin inhibitor, or a pharmaceutically acceptable salt thereof, and an MDR2010-09-16
20100234468NOVEL PROCESS - The present invention relates to a process for the preparation of polymorphic forms of the R- and S-enantiomers of modafinil, R-(−)-2-benzhydrylsulfinylacetamide and S-(+)-2-benzhydrylsulfinylacetamide respectively.2010-09-16
20100234469New Crystals Of A Benzoylbenzeneacetamide Derivative - The invention relates to 2-amino-3-benzoylbenzeneacetamide, i.e. nepafenac, crystals having reduced chargeability, to processes for the preparation thereof, and to the use thereof for preparing pharmaceutical formulations.2010-09-16
20100234470Instillation Administration of Capsaicinoids for the Treatment of Pain - This present invention relates to methods for treating or attenuating pain in a patient. Specifically, the invention provides a method for attenuating pain in proximity to the site of an open wound or surgical incision comprising instilling a pharmaceutical composition comprising a capsaicinoid into the wound or incision, allowing the pharmaceutical composition to dwell for a predetermined period of time, and aspirating the wound or incision to remove the pharmaceutical composition. The invention also provides a method for attenuating pain in proximity to a joint comprising intra-articularly injecting a pharmaceutical composition comprising a capsaicinoid into the joint, allowing the pharmaceutical composition to dwell for predetermined period of time, and aspirating the joint to remove the pharmaceutical composition. In certain embodiments of the invention, the capsaicinoid is capsaicin.2010-09-16
20100234471LIDOCAINE TAPE PREPARATION - The present invention discloses a novel tape preparation containing lidocaine at a high concentration. A tape preparation containing lidocaine at a high content, which has a lidocaine contant of 10 w/w % or more, can be produced by using a lactic acid salt of lidocaine, while preventing the precipitation of a crystal of lidocaine.2010-09-16