31st week of 2010 patent applcation highlights part 55 |
Patent application number | Title | Published |
20100197678 | Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof - Compounds of Formula (IA) | 2010-08-05 |
20100197679 | COMPOUNDS - Bicyclic nitrogen containing compounds and their use as antibacterials | 2010-08-05 |
20100197680 | LACTAM-SUBSTITUTED DICARBOXYLIC ACIDS AND USE THEREOF - The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders. | 2010-08-05 |
20100197681 | Triazolopyridine Compounds and Their Use as Ask Inhibitors - The present invention relates to triazolopyridine compounds according to Formula (I), their use as medicament, for treating autoimmune disorders, inflammatory diseases, cardiovascular diseases and/or neurodegenerative diseases and a process for their preparation. | 2010-08-05 |
20100197682 | Organic Compounds - Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases. | 2010-08-05 |
20100197683 | FUSED RING COMPOUND AND USE THEREOF - Provided is a novel compound represented by the following formula | 2010-08-05 |
20100197684 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): | 2010-08-05 |
20100197685 | NOVEL BENZOFURAN TYPE DERIVATIVES, A COMPOSITION COMPRISING THE SAME FOR TREATING OR PREVENTING COGNITIVE DYSFUNCTION AND THE USE THEREOF - The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder. | 2010-08-05 |
20100197686 | THERAPEUTIC COMPOUNDS - The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties. | 2010-08-05 |
20100197687 | Indoles Useful in the Treatment of Inflammation - There is provided compounds of formula I, | 2010-08-05 |
20100197688 | EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER - The present invention is directed to compounds of generic formula (I) | 2010-08-05 |
20100197689 | NOVEL PROCESSES FOR THE PREPARATION OF PIPERAZINYL AND DIAZAPANYL BENZAMIDE DERIVATIVES - The present invention is directed to novel processes for the preparation of substituted piperazinyl and diazepanyl benzamides, useful for the treatment of disorders and conditions mediated by the histamine receptor. | 2010-08-05 |
20100197690 | Pyrimidinyl Pyridazinone Derivatives - Compounds selected from the group according to Claim | 2010-08-05 |
20100197691 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included. | 2010-08-05 |
20100197692 | BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. | 2010-08-05 |
20100197693 | NOVEL BENZENESULFONAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), | 2010-08-05 |
20100197694 | Compositions and methods for treatment of diseases and conditions with increased vascular permeability - The invention provides compositions and methods for treating diseases and conditions through reducing vascular permeability, selectively inhibiting VEGF-induced postcapillary venular leakage, and/or selectively reducing spread of viral and/or bacterial pathogens. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for α-2 over α-1 adrenergic receptors. The compositions preferably comprise brimonidine and/or dexmedetomidine. | 2010-08-05 |
20100197695 | ANTITUMORAL DERIVATIVES OF ET-743 - Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula Ia.: | 2010-08-05 |
20100197696 | PESTICIDAL HETEROCYCLIC DIHALOALLYL COMPOUNDS - The invention relates to compounds of formula | 2010-08-05 |
20100197697 | PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS - The present invention relates to a compounds of formula I | 2010-08-05 |
20100197698 | 5-PHENYL-3-PYRIDAZINONE DERIVATIVE - To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): | 2010-08-05 |
20100197699 | I-OXA-3-Azaspiro (4.5) Decan-2-One And 1-OXA-3, 8-Diazaspiro (4.5) Decan-2-One Derivatives For The Treatment of Eating Disorders - The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, | 2010-08-05 |
20100197700 | 5-HT7 RECEPTOR ANTAGONISTS - The present invention provides selective 5-HT | 2010-08-05 |
20100197701 | METHOD OF TREATING DIABETES - Methods are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects. | 2010-08-05 |
20100197702 | OPHTHALMIC COMPOSITION WITH NITRIC OXIDE DONOR COMPOUND AND METHOD OF FORMING AND USING SAME - The present invention is directed to the provision of ophthalmic compositions such as multi-dose, topical, ophthalmic compositions. The compositions include a nitric oxide (NO) donor compound. | 2010-08-05 |
20100197703 | N-SULFONYL THIAZOLYLPIPERAZINE DERIVATIVES AND RELATED N-SULFONYL HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF NEURO DEGENERATIVE DISEASES - This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients. | 2010-08-05 |
20100197704 | PHARMACEUTICAL COMPOSITIONS AND METHOD FOR TREATING ACUTE MANIA - The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of acute mania. Furthermore, the present invention relates to the treatment of acute mania through the administration of (thio)-carbamoyl cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof. | 2010-08-05 |
20100197705 | Quinazolinone Derivatives Useful as Vanilloid Antagonists - There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. | 2010-08-05 |
20100197706 | DERIVATIVES OF 1-OXO-1,2-DIHYDROISOQUINOLINE-5-CARBOXAMIDES AND OF 4-OXO-3,4-DIHYDROQUINAZOLINE-8-CARBOXAMIDES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS - The present invention relates to derivatives of 1-oxo-1,2-dihydroisoquinoline-5-carboxamides and of 1-oxo-3,4-dihydroquinazoline-8-carboxamides, to the preparation thereof and to the therapeutic use thereof. | 2010-08-05 |
20100197707 | Platelet manipulation to reduce the incidence of and treat endovascular disease and its sequelae, to reduce the incidence of and treat arrhythmias and to reduce the incidence of malignancy - Manipulation of total body platelet activity via pharmacologic, mechanical, electrical or electronic means, or any combination thereof, or any other means, alone or in conjunction with manipulation of the activity of the coagulation cascade, for the purpose of reducing the incidence and severity of vascular disease in at risk populations, for the stabilization and reversal of said disease in patients already known to suffer from such disease, as well as for the purpose of reducing the incidence and severity of sequelae related to such disease, whether preclinical, subclinical or overtly manifested, or whether it is presently understood to be related to said vascular disease or not. | 2010-08-05 |
20100197708 | INDOLE COMPOUNDS - Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole. | 2010-08-05 |
20100197709 | NON-SEDATING BARBITURATE COMPOUNDS AS NEUROPROTECTIVE AGENTS - Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs. Preferred doses for a neuroprotective effect exceed the dosage of a corresponding sedative barbiturate without sedative side-effects such as anesthesia and death. | 2010-08-05 |
20100197710 | Methods Of Activating IRS-1 And AKT - The present invention provides methods of activating IRS-1 and/or AKT and methods of treating or preventing IRS-1- and/or AKT-related disease, condition, or disorder. | 2010-08-05 |
20100197711 | BENZOTHIAZOLE COMPOUNDS - The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival. | 2010-08-05 |
20100197712 | USE OF DOPAMINE STABILIZERS - At least one embodiment of the present invention relates to the use of a dopamine stabilizing substance in an oral, subcutaneous or intramuscular daily dose of 1-20 mg or in an intravenous daily dose of 0.1-2 mg in treatment of a neurological or psychiatric disorder characterized by a hypofunction of the dopamine system. At least one embodiment of the invention also relates to the use of a dopamine stabilizing substance in an oral, subcutaneous or intramuscular daily dose of 25-50 mg in treatment of a disorder caused by instability of neural circuits. | 2010-08-05 |
20100197713 | BUTONE DERIVATIVES USEFUL AS COOLING AGENTS - Cooling compounds of formula (I) wherein R | 2010-08-05 |
20100197714 | SPIRO-PYRANO-PYRAZOLE DERIVATIVES - The present invention relates to compounds of formula (I) below having pharmacological activity towards the sigma (σ) receptor, and more particularly to spiro-pyrano-pyrazole compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis. | 2010-08-05 |
20100197715 | PIPERIDINE DERIVATIVES - The present invention relates to a compound of formula I | 2010-08-05 |
20100197716 | N-LINKED HETEROCYCLIC ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS - The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): | 2010-08-05 |
20100197718 | TREATMENT OF PEDIATRIC TUMORS - A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma. | 2010-08-05 |
20100197719 | MEDICAMENT COMPOSITIONS CONTAINING ANTICHOLINERGICALLY-EFFECTIVE COMPOUNDS AND BETAMIMETICS - A pharmaceutical composition comprising:
| 2010-08-05 |
20100197720 | HETEROARYL-SUBSTITUTED DIAZATRICYCLOALKANES AND METHODS OF USE THEREOF - The present invention relates to amide and urea derivatives of heteroaryl-substituted diazatricycloalkanes, pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the methods of treatment involve modulating the activity of the α7 nAChR subtype by administering one or more of the compounds to treat or prevent disorders mediated by the α7 nAChR subtype. The diazatricycloalkanes typically consist of a 1-azabicyclooctane fused to pyrrolidine ring. The substituent heteroaryl groups are 5- or 6-membered ring heteroaromatics, such as 3-pyridinyl and 5-pyrimidinyl moieties, which are attached directly to the diazatricycloalkane. The secondary nitrogen of the pyrrolidine moiety is substituted with an arylcarbonyl (amide type derivative) or an arylaminocarbonyl (N-arylcarbamoyl) (urea type derivative) group. The compounds are beneficial in therapeutic applications requiring a selective interaction at certain nAChR subtypes. That is, the compounds modulate the activity of certain nAChR subtypes, particularly the α7 nAChR subtype, and do not have appreciable activity toward muscarinic receptors. Radiolabeled versions of the compounds can be used in diagnostic methods. | 2010-08-05 |
20100197721 | PYRROLO [3, 4-h] ISOQUINOLINE COMPOUNDS AND METHODS FOR MODULATING GATED ION CHANNELS - The present invention relates to compositions and methods to modulate the activity of gated ion channels. | 2010-08-05 |
20100197722 | Treatment for basal cell carcinoma - The present invention provides a method of treating basal cell carcinoma in a subject. Generally, the method includes administering to the subject an amount of IRM compound effective for treating basal cell carcinoma in a treatment cycle that includes at least two consecutive days in which the IRM compound is administered and at least one day in which the IRM compound is not administered. | 2010-08-05 |
20100197723 | BICYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME - Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same. | 2010-08-05 |
20100197724 | 6.5 -PYRROLOPIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS - The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety. | 2010-08-05 |
20100197725 | 1-OXO-ISOINDOLINE-4-CARBOXAMIDE AND 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLINE-5-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof. | 2010-08-05 |
20100197726 | INHIBITOR OF THE DIFFERENTIATION OF T CELLS INTO TH1 CELLS - The present invention is to provide an inhibitor that inhibits differentiation of T cells into Th1 cells. | 2010-08-05 |
20100197727 | Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) | 2010-08-05 |
20100197728 | CRYSTALLINE FORM OF A QUINOLINONE-CARBOXAMIDE COMPOUND - The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT | 2010-08-05 |
20100197729 | THERAPEUTIC ((PHENYL)IMIDAZOLYL)METHYLQUINOLINYL COMPOUNDS - Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed. | 2010-08-05 |
20100197730 | METHODS FOR TREATING ANXIETY - Disclosed are methods of treating anxiety by administering to a patient in need of such treatment a compound having the following formula (I). | 2010-08-05 |
20100197731 | KIND OF PIPERPHENTONAMINE HYDROCHLORIDE LYOPHILIZED POWDER FOR INJECTION AND PREPARATION AND USE THEREOF - A kind of piperphentonamine hydrochloride lyophilized powder for injection and a preparation method thereof. The injection is prepared by one portion of piperphentonamine hydrochloride, 2.5-30 parts of excipient and 400-600 parts of water for injection with pH 1.5-5.5 via freeze-drying. The excipient is mannitol, dextran, lactose, saccharose, polyethylene glycol, poloxamer, glycine, etc.; It is preferred that the injection comprises one part of piperphentonamine hydrochloride, 10 parts of mannitol and 500 parts of water for injection with pH 2.0-3.0. The product is prepared by adding said piperphentonamine hydrochloride and excipient into water for injection, heating at 40° C.-90° C., ultrasonic dissolving, degerming, individually packing, pre-freezing and multistage drying, and packaging. Individually packing into a tubular glass bottle with brown color is preferred. The appearance, color & luster and solubility of the injection are excellent, the stability is good and with long storage period. The invention also provides the uses of the injection in the preparation of a medicament for treatment of heart failure and/or cardioprotection. | 2010-08-05 |
20100197732 | Repaglinide Substantially Free of Dimer Impurity - The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D | 2010-08-05 |
20100197733 | PYRROLIDINES AND PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to compounds of formula (I) wherein Y, A, N and R | 2010-08-05 |
20100197734 | PLEUROMUTILIN DERIVATIVES AND THEIR USE AS ANTIMICROBIALS - A compound of formula (I) or of formula (II) wherein X is oxygen or sulfur, and Y is a residue of pipecolic acid or a residue of an amino acid, preferably a naturally occurring amino acid. | 2010-08-05 |
20100197735 | NOVEL PHENYLUREA INHIBITORS OF THE ENZYME SOAT-1 AND PHARMACEUTICAL/COSMETIC COMPOSITIONS COMPRISED THEREOF - Novel phenylurea compounds of formula (I): | 2010-08-05 |
20100197736 | CETP ACTIVITY INHIBITORS - The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): | 2010-08-05 |
20100197737 | ACTIVE AGENT COMBINATIONS HAVING INSECTICIDAL AND ACARICIDAL PROPERTIES - The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) | 2010-08-05 |
20100197738 | FLY CONTROL METHOD - This invention relates to a method of controlling or preventing infestations of flies on an animal by applying to the animal a composition comprising an parasiticidally effective amount of a compound of Formula 1, (3-bromo-N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide), or an N-oxide, or a salt thereof, | 2010-08-05 |
20100197739 | Stable Suspension Concentrate Formulation for Water-Soluble Compounds - The present invention is directed to an insecticidal water based suspension concentrate formulation comprising a water-soluble insecticide selected from the group consisting of N-cyanomethyl-4-(trifluoromethyl)nicotinamide and (EZ)-1-(6-chloro-3-pyridylmethyl)-N-nitroimidazolidin-2-ylidineamine and at least one water-soluble salt selected from the group consisting of magnesium sulfate (hydrated and anhydrous forms) and sodium sulfate, wherein the water-soluble insecticide is present in an insecticidally effective amount and methods of use. | 2010-08-05 |
20100197740 | Method of Screening Compounds Having Anti-Amyloid Properties - The invention relates to a method of screening compounds having anti-amyloid properties. The method of screening compounds that are capable of dissociating or preventing high-affinity complexes between β-amyloid peptides and nicotinic acetylcholine receptors of human cortical tissues makes it possible to rapidly identify compounds intended for the curative and/or preventive treatment of neurodegenerative diseases, especially Alzheimer's disease. | 2010-08-05 |
20100197741 | Ternary Fungicidal Compositions Comprising Boscalid and Chlorothalonil - Ternary fungicidal compositions comprising as active components | 2010-08-05 |
20100197742 | NEW FORMULATIONS AND USE THEREOF - A pharmaceutical formulation comprising one or more active pharmaceutical ingredients (APIs) suitable for intraoral uptake, that comprises cocoa powder, a process for manufacturing the formulation and use of the formulation for medical treatment. | 2010-08-05 |
20100197743 | Use of sulphur-containing heteroaromatic acid analogues - The present invention relates to the use of compounds according to formula (I) | 2010-08-05 |
20100197744 | Organic Compounds - Novel compounds that are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of the present invention may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system. | 2010-08-05 |
20100197745 | GAMMA-GLUTAMYL TRANSPEPTIDASE INHIBITORS AND METHODS OF USE - The present invention enhances the effects of antitumor agents and increases the sensitivity of therapy-resistant tumor cells to antitumor agents such as chemotherapeutic agents and radiation. The present invention is thus directed to compositions and methods for inhibiting and killing neoplastic cancer cells, for example for the treatment, inhibition or prevention of tumors or malignant growths or other neoplasias in mammals. The GGT inhibitor compounds used in the methods of the present invention comprise a class of benzylthiadiazol benzenesulfoniamides represented by the general structure Formula (I) ( | 2010-08-05 |
20100197746 | SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO AND ANALOGUES THEREOF - The present invention provides compounds of formula (I): | 2010-08-05 |
20100197747 | Synergistic Insecticidal Mixtures - The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests. | 2010-08-05 |
20100197748 | ANTI-MICROBIAL COMPOSITION - The present invention provides an anti-microbial composition comprising (i) an antimicrobial agent with surfactant properties; (ii) a siloxane selected from those having the formulae (H | 2010-08-05 |
20100197749 | CHEMICAL COMPOUNDS - The invention relates to chemical compounds of formula (I) and (II): | 2010-08-05 |
20100197750 | Preservation Of Ergothioneine - Compositions comprising ergothioneine and a trimethylamine absorber are provided. Also provided are methods for preventing, reducing or minimizing the fishy, amine odor, due to trimethylamine, that is associated with the processing and/or storage of a preparation containing ergothioneine, by combining with the ergothioneine, during processing or prior to storage, a trimethylamine absorber in an amount sufficient to prevent the detection of any trimethylamine odor by the human nose. A method is further provided for ameliorating the methylamine odor associated with an aqueous ergothioneine-containing preparation after it has developed a fishy trimethylamine odor. | 2010-08-05 |
20100197751 | COMPOSITIONS OF PEGYLATED SOLUBLE TUMOR NECROSIS FACTOR RECEPTORS AND METHODS OF PREPARING - The present invention provides for improved compositions comprising a PEGsTNF-R1 which, in addition to having useful higher concentrations, demonstrate decreased viscosity (<400 cP) and improved stability. | 2010-08-05 |
20100197752 | UROCANIC ACID DERIVATIVES USEFUL FOR THE TREATMENT OF IMMUNE-RELATED AND INFLAMMATORY DISEASES - The invention relates to derivatives of urocanic acid that have improved efficacy and/or tissue penetration properties. The invention further provides use of these derivatives in a medicament for modulating an immune-related disease in an individual. Imidazole derivative, or a salt thereof, selected from O I1 W—C—R1 H— (formula 1); o I1 W—C—R1 and HN N r<1 NH (formula 2); O O Ov ̂ W—C—R1 and HN N (formula 3); | 2010-08-05 |
20100197753 | Benzamides Useful as S1P Receptor Modulators - The invention relates to novel aromatic compounds of the formula | 2010-08-05 |
20100197754 | CRYSTALLINE N--5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride - An improved AKT inhibiting compound, crystalline N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride. | 2010-08-05 |
20100197755 | HYDRAZONE MODULATORS OF CANNABINOID RECEPTORS - Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein. | 2010-08-05 |
20100197756 | Indole-3-Sulphur Derivatives - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. (I) | 2010-08-05 |
20100197757 | OXINDOLES AS KINASE INHIBITORS - The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition. | 2010-08-05 |
20100197758 | ISCHEMIA/REPERFUSION PROTECTION COMPOSITIONS AND METHODS OF USING - The invention provides for ischemia/reperfusion protection compositions having one or more ketone bodies and melatonin. The invention also provides for methods of using such compositions to reduce or prevent ischemia/reperfusion injury due to blood loss, stroke or cardiopulmonary arrest or surgery. | 2010-08-05 |
20100197759 | Administration of dithiolane compounds for photoprotecting the skin - Dithiolane compounds having the structural formula (I): | 2010-08-05 |
20100197760 | DISUBSTITUTED PHENYLPYRROLIDINES AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION - The present invention provides compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-(disubstituted aryl)-pyrrolidines for the treatment of central nervous system disorders. | 2010-08-05 |
20100197761 | Fused cyclic compounds - The present invention provides a compound represented by the formula (I): | 2010-08-05 |
20100197762 | ANTISENSE COMPOUNDS - Provided herein are gapmer oligomeric compounds for reduction of target RNA in vivo comprising different nucleotide modifications within one or both wing regions. Also provided are methods of using such oligomeric compounds, including use in animals. In certain embodiments, such compound have desirable potency and toxicity characteristics. | 2010-08-05 |
20100197763 | RNA Interference Mediated Inhibition of Cyclic Nucleotide Type 4 Phosphodiesterase (PDE4B) Gene Expression Using Short Interfering Nucleic Acid (siNA) - The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-7, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-I, MMP-2, MMP-3, MMP-9 and MMP-12. Specifically, the invention relates to double stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA), and multifunctional siNA molecules capable of mediating RNA interference (RNAi) against cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression, including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. The present invention also relates to small nucleic acid molecules, such as siNA, siRNA, antisense and others that can inhibit the function of endogenous RNA molecules or RNAi pathway components (RNAi inhibitors), such as endogenous micro-RNA (miRNA) (e.g, miRNA inhibitors) or endogenous short interfering RNA (siRNA), (e.g., siRNA inhibitors) or that can inhibit the function of RISC (e.g., RISC inhibitors), to modulate PDE4B gene expression by interfering with the regulatory function of such endogenous RNAs or proteins associated with such endogenous RNAs (e.g., RISC) including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. Such small nucleic acid molecules are useful, for example, in providing compositions to prevent, inhibit, or reduce inflammatory, respiratory, and autoimmune diseases, traits, and conditions, and/or other disease states associated with PDE4B gene expression or activity in a subject or organism. | 2010-08-05 |
20100197764 | ANTISENSE MODULATION OF ACYL COA CHOLESTEROL ACYLTRANSFERASE-2 EXPRESSION - Antisense compounds, compositions and methods are provided for modulating the expression of acyl CoA cholesterol acyltransferase-2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding acyl CoA cholesterol acyltransferase-2. Methods of using these compounds for modulation of acyl CoA cholesterol acyltransferase-2 expression and for treatment of diseases associated with expression of acyl CoA cholesterol acyltransferase-2 are provided. | 2010-08-05 |
20100197765 | METHOD FOR PROMOTING THE EXPRESSION OF P53, AND P53 EXPRESSION PROMOTER FOR USE IN THE METHOD - A method for promoting expression of p53 mRNA and an expression promoting agent for use in the method are provided. The expression of the p53 gene can be promoted by inhibiting the binding between RNA transcribed from exon 1 of the vegf-A gene and mRNA transcribed from the p53 gene. The inhibition of the binding can be achieved by, for example, degrading the RNA transcribed from the exon 1 of the vegf-A gene, inhibiting transcription of RNA from the exon 1 of the vegf-A gene, or binding a nucleic acid that is different from the mRNA transcribed from the p53 gene to the RNA transcribed from the exon 1 of the vegf-A gene. | 2010-08-05 |
20100197766 | Antisense Oligonucleotides Directed to Ribonucleotide Reductase R2 and Uses Thereof in the Treatment of Cancer - The present invention provides antisense oligonucleotides directed to a mammalian ribonucleotide reductase R2 gene and combinations of the antisense oligonucleotides with one or more chemotherapeutic agents for use in the treatment of cancer. | 2010-08-05 |
20100197767 | NUCLEIC ACID CONSTRUCT SYSTEMS CAPABLE OF DAIGNOSING OR TREATING A CELL STATE - Nucleic acid construct systems are disclosed capable of diagnosing and treating a cell state (e.g. disease state). Methods of diagnosing and treating disease states using the nucleic acid constructs described herein are also disclosed. In addition, methods of screening for agents capable of reversing a disease phenotype using the nucleic acid constructs of the present invention are disclosed. | 2010-08-05 |
20100197768 | METHODS AND COMPOSITIONS RELATED TO THE STRUCTURE AND FUNCTION OF APOBEC3G - Disclosed are methods and compositions related to the structure and function of APOBEC3G. | 2010-08-05 |
20100197769 | PLASMID CONTAINING A SEQUENCE ENCODING A DISINTEGRIN DOMAIN OF METARGIDIN (RDD) - The invention relates to a pORT plasmid containing a sequence encoding all or part of a disintegrin domain of metargidin (RDD) or a derivative thereof under the control of strong cytomegalovirus promoter, in particular a plasmid having the sequence shown in SEQ ID NO:2. | 2010-08-05 |
20100197770 | Methods for Determining Heptocellular Carcinoma Subtype and Detecting Hepatic Cancer Stem Cells - The invention provides a method of determining an HCC subtype in a subject comprising a) obtaining a sample from the subject, b) assaying the sample to detect the expression of 1 or more biomarkers, and c) correlating the expression of the biomarkers with an HCC subtype in a subject. The invention further provides methods of detecting HCC stem cells in a sample. Additionally, the invention provides methods and compositions for treating subjects with HCC that take advantage of the biomarkers associated with HCC stem cells. | 2010-08-05 |
20100197771 | INFLUENZA VIRUS VACCINE COMPOSITION AND METHODS OF USE - The present invention is directed to enhancing the immune response of a human in need of protection against IV infection by administering in vivo, into a tissue of the human, at least one polynucleotide comprising one or more regions of nucleic acid encoding an IV protein or a fragment, a variant, or a derivative thereof. The present invention is further directed to enhancing the immune response of a human in need of protection against IV infection by administering, in vivo, into a tissue of the human, at least one IV protein or a fragment, a variant, or derivative thereof. The IV protein can be, for example, in purified form or can be an inactivated IV, such as those present in inactivated IV vaccines. The polynucleotide is incorporated into the cells of the human in vivo, and an immunologically effective amount of an immunogenic epitope of an IV, or a fragment, variant, or derivative thereof is produced in vivo. The IV protein (in purified form or in the form of an inactivated IV vaccine) is also administered in an immunologically effective amount. | 2010-08-05 |
20100197772 | Tissue-Specific MicroRNAs and Compositions and Uses Thereof - The invention provides for isolated nucleic acid sequences of newly discovered micro RNAs that have been identified to exist in normal Human B cells and/or in tumor-related Human B cells, using an integrated bioinformatics method and pipeline described herein. | 2010-08-05 |
20100197773 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF PTP1B GENES - This invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a PTP1B gene. The invention also relates to a pharmaceutical composition comprising the dsRNA or nucleic acid molecules or vectors encoding the same together with a pharmaceutically acceptable carrier; methods for treating diseases caused by the expression of a PTP1B gene using said pharmaceutical composition; and methods for inhibiting the expression of PTP1B in a cell. | 2010-08-05 |
20100197774 | MicroRNA EXPRESSION ABNORMALITIES IN PANCREATIC ENDOCRINE AND ACINAR TUMORS - The present invention provides novel methods and compositions for the diagnosis, prognosis and treatment of pancreatic cancer. The invention also provides methods of identifying anti-pancreatic cancer agent. | 2010-08-05 |
20100197775 | METHODS AND COMPOSITIONS FOR TREATING & DIAGNOSING MOOD DISORDERS, SCHIZOPHRENIA, AND NEURO-PSYCHIATRIC DISORDERS - This invention provides: methods of determining a predisposition or susceptibility of a subject to a mood disorder, a schizophrenia, or a neuro-psychiatric disease or disorder, comprising detecting a presence of a polymorphism in a vesicular monoamine transporter 1 (VMAT1) gene or a haplotype comprising the polymorphism, and methods of treating a mood disorder, a schizophrenia, or a neuro-psychiatric disease or disorder in a subject, comprising contacting the subject with a composition that encodes a VMAT protein or modulates an expression or activity of same. | 2010-08-05 |
20100197776 | DIRECT DISSOLUTION OF DOCETAXEL IN A SOLVENT IN POLYSORBATE 80 - The disclosure relates to the solubilization of docetaxel in an organic solvent, to the mixture thereof with polysorbate 80, and to the evaporation of the solvent. | 2010-08-05 |
20100197777 | Synergistic combination of analgesic compounds - The present invention relates to a pharmaceutical composition comprising as active substances:
| 2010-08-05 |
20100197778 | PROANTHOCYANIDINS FOR THE TREATMENT OF AMYLOID AND ALPHA-SYNUCLEIN DISEASES - A method of treating an amyloid disease, or a disease characterized by IAPP amyloid fibrils or islet amyloid deposits, in a mammalian subject. The method includes administering to the mammal a therapeutically effective amount of a various disclosed procyanidins or proanthocyanidins characterized by disclosed general formulae. A pharmaceutical composition and use of the composition comprising a therapeutically effective amount of a procyanidin and a pharmaceutically acceptable excipient. The therapeutic amount of the proanthocyanidin is selected for efficacy in treating IAPP amyloid fibrils or islet amyloid deposits in a mammalian subject. | 2010-08-05 |