04th week of 2012 patent applcation highlights part 48 |
Patent application number | Title | Published |
20120022049 | NICOTINIC RECEPTOR AGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided. | 2012-01-26 |
20120022050 | HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF - Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein. | 2012-01-26 |
20120022051 | RAPID ONSET LIQUID MIDAZOLAM COMPOSITION FOR BUCCAL ADMINISTRATION - This application discloses liquid compositions for administration to a patient comprising midazolam and a pharmaceutically acceptable carrier, wherein the pH of the composition is about 6 or higher, the composition comprises less than about 200 mg/ml cyclodextrin, and at least about 50% of the midazolam is present in solution. Uses of these compositions are also disclosed. | 2012-01-26 |
20120022052 | SMALL MOLECULE INHIBITORS OF KYNURENINE-3-MONOOXYGENASE - The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof. | 2012-01-26 |
20120022053 | Oxadiazine Derivatives - Compounds of the formula | 2012-01-26 |
20120022054 | NOVEL SUBSTITUTED ARYL DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS ANTI-HIV AGENTS - The present invention concerns novel substituted aryl derivatives, their process of preparation and their use for inhibiting virus replication and for treating viral diseases or disorders such as HIV and/or HCV infection. | 2012-01-26 |
20120022055 | PEST CONTROLLING COMPOSITION - The present invention provides a pest controlling composition comprising, as active ingredients, an amide compound of the formula (I) and a neonicotinoid compound; and so on. | 2012-01-26 |
20120022056 | FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS - Compounds of formula (I) wherein R | 2012-01-26 |
20120022057 | BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I). | 2012-01-26 |
20120022058 | 4,5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES - Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans. | 2012-01-26 |
20120022059 | SUBSTITUTED FURANCARBOXAMIDES, AND USE THEREOF - The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals. | 2012-01-26 |
20120022060 | Tricyclic Azaindoles - Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation. | 2012-01-26 |
20120022061 | BENZO [C] PHENANTHRIDINES AS ANTIMICROBIAL AGENTS - The present invention provides compounds of formula I: formula (I) wherein X | 2012-01-26 |
20120022062 | Flavanoid Compounds and Process for Preparation Thereof - The present invention relates to flavanoid compounds of general formula (X | 2012-01-26 |
20120022063 | Oligomer-Cannabinoid Conjugates - The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds. | 2012-01-26 |
20120022064 | DIHYDROQUINOLINONE DERIVATIVES - The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. | 2012-01-26 |
20120022065 | C-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 2012-01-26 |
20120022066 | Insecticidal Triazines and Pyrimidines - The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds. | 2012-01-26 |
20120022067 | THIAZOLE AND OXAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2012-01-26 |
20120022068 | NOVEL HETEROCYCLIC NF-kB INHIBITORS - The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, | 2012-01-26 |
20120022069 | ACRYLAMIDE COMPOUNDS AND THE USE THEREOF - The invention relates to acrylamide compounds of Formula I mentioned below. | 2012-01-26 |
20120022070 | Heat Shock Protein 90 Inhibitors, Methods Of Preparing Same, And Methods For Their Use - Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided. | 2012-01-26 |
20120022072 | PTERIN ANALOGS - Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies. | 2012-01-26 |
20120022073 | COMPOUND FOR THE TREATMENT OF ENTEROVIRUSES - The present invention relates to the treatment, alleviation, prevention or reduction in the incidence of symptoms, diseases or conditions resulting from or associated with enteroviruses, more particularly the enteroviral infections they cause. | 2012-01-26 |
20120022074 | ORGANIC COMPOUNDS - The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders. | 2012-01-26 |
20120022075 | NOVEL PHENYLPYRROLE DERIVATIVE - The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: | 2012-01-26 |
20120022076 | DERIVATIVES OF N-(ARYLAMINO)SULFONAMIDES AS INHIBITORS OF MEK - This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases. | 2012-01-26 |
20120022077 | NOVEL CYANOPYRIMIDINE DERIVATIVE - The present invention relates to a novel cyanopyrimidine compound and a pharmaceutical composition which have a safe and potent adenosine A2a receptor agonistic activity. | 2012-01-26 |
20120022078 | ARYL INDOLE DERIVATIVES - A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R | 2012-01-26 |
20120022079 | Method For Producing Preparations Of Substances Poorly Soluble In Water - The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of
| 2012-01-26 |
20120022080 | Plasminogen Activator Inhibitor-1 Inhibitor - The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. | 2012-01-26 |
20120022081 | METHOD OF USING DIKETOPIPERAZINES AND COMPOSITION CONTAINING THEM - The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: | 2012-01-26 |
20120022082 | PYRAZINE DERIVATIVES - The invention concerns pyrazine derivatives of the Formula I | 2012-01-26 |
20120022083 | SMALL MOLECULE MODULATORS OF CELL ADHESION - Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: | 2012-01-26 |
20120022084 | Substituted 5-fluoro-1H-pyrazolopyridines and their use - The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2012-01-26 |
20120022085 | PROCESS FOR OBTAINING EXTRACTS CONTAINING METHYLXANTHINE DERIVATIVES FROM CAKES OF PLANTS OF THE GENUS THEOBROMA, AS WELL AS COMPOSITION AND USE OF SAID EXTRACT - The present invention refers to a process for obtaining standardized extracts of methylxanthine derivatives from cakes of plants of the genus | 2012-01-26 |
20120022086 | CATECHOLAMINE DERIVATIVES FOR OBESITY AND NEUROLOGICAL DISORDERS - Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds. | 2012-01-26 |
20120022087 | AMORPHOUS AMBRISENTAN - The invention relates to amorphous ambrisentan, preferably together with a surface stabiliser in the form of a stable intermediate. The invention further relates to methods of producing stable amorphous ambrisentan and pharmaceutical formulations containing stable amorphous ambrisentan. | 2012-01-26 |
20120022088 | PHARMACEUTICAL COMBINATION OF 5-FLUOROURACIL AND DERIVATE OF 1,4-DIHYDROPYRIDINE AND ITS USE IN THE TREATMENT OF CANCER - New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I | 2012-01-26 |
20120022089 | Solid Pharmaceutical Dosage Form - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 2012-01-26 |
20120022090 | NOVEL SUBSTITUTED BENZOXAZOLE, BENZIMIDAZOLE, OXAZOLOPYRIDINE AND IMIDAZOPYRIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) | 2012-01-26 |
20120022091 | KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin. | 2012-01-26 |
20120022092 | PROTEIN KINASE C INHIBITORS AND USES THEREOF - This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes. | 2012-01-26 |
20120022093 | CRYSTALLINE FORMS OF OXYMORPHONE HYDROCHLORIDE - The present invention is directed to crystalline forms of oxymorphone hydrochloride. | 2012-01-26 |
20120022094 | PHARMACEUTICAL FORMULATIONS - New and improved antihistaminic syrups are disclosed. | 2012-01-26 |
20120022095 | TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area. | 2012-01-26 |
20120022096 | PRO-NEUROGENIC COMPOUNDS - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 2012-01-26 |
20120022097 | Compositions and Methods for Treating Cancer - The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound. | 2012-01-26 |
20120022098 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 2012-01-26 |
20120022099 | NOVEL POLYMORPHIC FORMS OF AN AZABICYCLO-TRIFLUOROMETHYL BENZAMIDE DERIVATIVE - The present disclosure is directed to solid forms of the compound of formula (I): | 2012-01-26 |
20120022100 | ORGANIC COMPOUNDS - Disclosed are δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I) | 2012-01-26 |
20120022101 | SALT AND SOLVATES OF A TETRAHYDROISOQUINOLINE DERIVATIVE - (S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described. | 2012-01-26 |
20120022102 | METHOD FOR PREPARATION OF PITAVASTATIN AND ITS PHARMACEUTICAL ACCEPTABLE SALTS THEREOF - The present invention discloses a compound, which is alkali or alkaline earth metal salts of pitavastatin, wherein the alkali or earth metal comprise one or more of magnesium, zinc, potassium, strontium and barium. | 2012-01-26 |
20120022103 | ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF - The present application is directed to compounds that are TRPV1 antagonists and have formula (I) | 2012-01-26 |
20120022104 | PECTIN-CONTAINING JELLY FORMULATION - There is disclosed a technique for imparting an appropriate rupture strength and high drug-release properties to a jelly formulation comprising pectin. The jelly formulation of the present invention comprises a drug, pectin, and divalent metal ion, and further comprises a component selected from sucrose, maltitol and C3-C4 alditols, and a component selected from C5-C6 alditols in combination. | 2012-01-26 |
20120022105 | GREASE-LIKE GEL FOR REPELLING RODENTS - Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin. | 2012-01-26 |
20120022106 | POLYMORPHIC FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE - Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed. | 2012-01-26 |
20120022107 | 2-(PIPERIDIN-1-YL)-4-AZOLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 2012-01-26 |
20120022108 | ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, R | 2012-01-26 |
20120022109 | OXADIAZOLE DERIVATIVES - The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis. | 2012-01-26 |
20120022110 | PHARMACEUTICAL DEPOT FOR 5-FLUORO-2-[[(1S)-1-(5-FLUORO-2-PYRIDYL)ETHYL]AMINO]-6-[(5-ISOPROPOXY-1H-- PYRAZOL-3-YL)AMINO]PYRIDINE-3-CARBONITRILE - A pharmaceutical depot comprising (i) 5-fluoro-2-[[(1S)-1-(5-fluoro-2-pyridyl)ethyl]amino]-6-[(5-isopropoxy-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrile, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation. | 2012-01-26 |
20120022111 | SPOT-ON PESTICIDE COMPOSITION - A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area. | 2012-01-26 |
20120022112 | USE OF ANTHRANILAMIDE DERIVATIVES FOR CONTROLLING INSECTS AND SPIDER MITES BY DRENCHING, SOIL MIXING, FURROW TREATMENT, DRIP APPLICATION, SOIL, STEM OR FLOWER INJECTION, IN HYDROPONIC SYSTEMS, BY PLANTING HOLE TREATMENT OR DIP APPLICATION, FLOATING OR SEEDBOX APPLICATION OR BY TREATING SEED, AND ALSO FOR ENHANCING THE STRESS TOLERANCE OF PLANTS TO ABIOTIC STRESS - The present invention relates to the use of anthranilamide derivatives of the general formula (I) | 2012-01-26 |
20120022113 | METHODS FOR SUPPRESSING TIPDC TRAFFICKING OR ACCUMULATION AND PREVENTING HYPERCYTOKINEMIA - The present invention features methods for preventing or ameliorating hypercytokinemia or preventing lethality-associated with infection by highly pathogenic strains of influenza virus by suppressing TNF-α/Inducible nitric oxide synthase-Producing dendritic cell trafficking or accumulation. In particular embodiments, the expression MyD88, CCR2, MCP-I or MCP-3 is targeted. | 2012-01-26 |
20120022114 | Low-dose, non-irritating nicotine nasal composition to reduce the desire to smoke - A composition for administration to the nasal mucosa of a subject comprises a solution of nicotine or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable solvent. The composition has a nicotine concentration less than 0.08 mg/ml. The composition used alone assists in reduction of the desire of a subject to smoke tobacco. It also reduces the nasal symptoms associated with administration of higher concentrations of nicotine to the nasal mucosa. | 2012-01-26 |
20120022115 | HYDROXYPYRIDONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC USE FOR TREATING PROLIFERATIVE DISEASES - Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease. | 2012-01-26 |
20120022116 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF PATHOLOGICAL CONDITION(S) RELATED TO GPR35 AND/OR GPR35-HERG COMPLEX - Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject. The compounds having a formula (I), (II) or (III): | 2012-01-26 |
20120022117 | Salts or Co-Crystals of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol - A salt or cocrystal of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol (component a) and at least one acid component (b1) or at least one acid component (b2), wherein the salt or cocrystal of component (a) and component (b2) is present in crystalline and/or amorphous form, a pharmaceutical composition comprising said salt or cocrystal, and a method of treating pain in a subject in need thereof by administering an effective amount of said salt or cocrystal. | 2012-01-26 |
20120022118 | COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention relates to compounds of structural formula (I): | 2012-01-26 |
20120022119 | HETEROCYCLIC ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are heteroaryl compounds that are antagonists of PGD | 2012-01-26 |
20120022120 | ANTIMYCOTIC PHARMACEUTICAL COMPOSITION - In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25° C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture. | 2012-01-26 |
20120022121 | INDOLES, DERIVATIVES AND ANALOGS THEREOF AND USES THEREFOR - Indole derivatives and analogous compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer. | 2012-01-26 |
20120022122 | TREATMENT AND PREVENTION OF DELETERIOUS EFFECTS ASSOCIATED WITH ALCOHOL CONSUMPTION - The present invention provides to methods and compositions that treat or prevent deleterious effects associated with alcohol consumption including alcohol-induced flush reaction and hangover. The methods and compositions include famotidine and optionally succinic acid. The present invention further demonstrates compositions that include famotidine are effective at treating symptoms associated with a flush reaction in subjects that are not significantly responsive to treatments with the H1 antagonist loratidine or the H2 antagonist cimetidine. | 2012-01-26 |
20120022123 | SUBSTITUTED (THIOPHENYL-CARBONYL)IMIDAZOLIDINONES, AND USE THEREOF - The present invention relates to novel substituted (thiophenyl-carbonyl)imidazolidinones, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals. | 2012-01-26 |
20120022124 | POLYMORPHS OF ELTROMBOPAG AND ELTROMBOPAG SALTS AND PROCESSES FOR PREPARATION THEREOF - New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia. | 2012-01-26 |
20120022125 | PYRROLIDINE TRIPLE REUPTAKE INHIBITORS - In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter. | 2012-01-26 |
20120022126 | Method Of Treating Diabetes Mellitus - The invention provides methods of treating a diabetic subject comprising administering a glucosylceramide synthase inhibitor to the subject. | 2012-01-26 |
20120022127 | PROCESS FOR PREPARING PYRROLIDINIUM SALTS - A two step process for preparing a compound of formula I | 2012-01-26 |
20120022128 | PKIB and NAALADL2 for Target Genes of Prostate Cancer Therapy and Diagnosis - The invention features methods for detecting prostate cancer, especially hormone-refractory prostate cancer (HRPC) or castration-resistant prostate cancer (CRPC), by detecting over-expression of PKIB or NAALADL2 compared the normal organs. Also disclosed are methods of identifying compounds for treating and preventing prostate cancer including HRPC, based on the over-expression of PKIB or NAALADL2 in the prostate cancer, the cell proliferation function of PKIB or NAALADL2, the intracellular localization of PKIB or NAALADL2 or the interaction between PKIB and PKA-C. Also, provided are a method for treating prostate cancer by administering a double-stranded molecule against the PKIB or NAALADL2 gene. The invention also provides products, including the double-stranded molecules and vectors encoding them, as well as compositions comprising the molecules or vectors, useful in the provided methods. | 2012-01-26 |
20120022129 | Targeting of Histone Deacetylase 2, Protein Kinase CK2, and Nuclear Factor NRF2 For Treatment of Inflammatory Diseases - Methods for the treatment or prevention of diseases which are caused by the degradation of histone deacetylase 2 (HDAC2) in cells are described. The diseases which may be treated by the methods of the invention include chronic obstructive pulmonary disease (COPD) and asthma. The invention provides methods for treating or preventing of diseases caused by the degradation of HDAC2 by providing to the subject in need of treatment or prevention a molecular compound capable of preventing the degradation of HDAC2. Such molecular compounds include protein kinase CK2 inhibitors, ubiquitination inhibitors, ubiquitin-proteosome inhibitors, nuclear factor (erythroid-derived 2)-like 2 (Nrf2) activators and MAPK phosphatase 1 activators. Methods are also provided for the treatment and prevention of diseases caused by the degredation of HDAC2 by interfering with the expression of protein kinase CK2 or by increasing expression of Nrf2. | 2012-01-26 |
20120022130 | METHOD OF REGULATING NFATc2 ACTIVITY IN LYMPHOCYTES - A method of decreasing NFATc2 activity in a lymphocyte includes administering to the lymphocyte an amount of an NFATc2 mRNA antagonist that binds to a binding site on the 3′UTR of NFATc2 mRNA effective to decrease the activity of NFATc2 mRNA in the lymphocyte. | 2012-01-26 |
20120022131 | BREAST CANCER RELATED GENE RQCD1 - The present invention provides methods for detecting and diagnosing cancer, such methods involving the determination of the expression level of the RQCD1, GIGYF1 or GIGYF2 genes. These genes were discovered to discriminate cancer cells from normal cells. Furthermore, the present invention provides methods of screening for therapeutic agents useful in the treatment of cancer and methods for treating cancer. Moreover, the present invention provides siRNAs targeting the RQCD1, GIGYF1 and/or GIGYF2 genes, all of which are suggested to be useful in the treatment of cancer. | 2012-01-26 |
20120022132 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF MUTANT EGFR GENE - The invention relates to a double-stranded ribonucleic acid (dsRNA) targeting a mutant Epidermal Growth Factor Receptor (EGFR), and methods of using the dsRNA to inhibit expression of mutant EGFR. | 2012-01-26 |
20120022133 | ANTISENSE MODULATION OF CHOLESTERYL ESTER TRANSFER PROTEIN EXPRESSION - Antisense compounds, compositions and methods are provided for modulating the expression of cholesteryl ester transfer protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding cholesteryl ester transfer protein. Methods of using these compounds for modulation of cholesteryl ester transfer protein expression and for treatment of diseases associated with expression of cholesteryl ester transfer protein are provided. | 2012-01-26 |
20120022134 | METHODS AND MEANS FOR EFFICIENT SKIPPING OF EXON 45 IN DUCHENNE MUSCULAR DYSTROPHY PRE-mRNA - The invention relates to a method for inducing or promoting skipping of exon 45 of DMD pre-mRNA in a Duchenne Muscular Dystrophy patient, preferably in an isolated (muscle) cell, the method comprising providing said cell with a molecule that binds to a continuous stretch of at least 21 nucleotides within said exon. The invention further relates to such molecule used in said method. | 2012-01-26 |
20120022135 | PHD2 INHIBITION FOR BLOOD VESSEL NORMALIZATION, AND USES THEREOF - A key function of blood vessels, to supply oxygen, is impaired in tumors because of abnormalities in their endothelial lining. PHD proteins serve as oxygen sensors and may regulate oxygen delivery. Therefore the role of endothelial PHD2 in vessel shaping by implanting tumors in PHD2 | 2012-01-26 |
20120022136 | Cellular Genes Regulated by HIV-1 Infection and Methods of Use Thereof - This invention provides cellular gene products which have anti-apoptotic activity in HIV-1 infected cells and provides agents for the inhibition of the cellular gene products. | 2012-01-26 |
20120022137 | METHOD OF CONTROLLING INITIAL DRUG RELEASE OF siRNA FROM SUSTAINED-RELEASE IMPLANTS - The present invention provides an intraocular implant comprising siRNA combined with a excipient effective to retard the initial release of the siRNA from an implant, wherein said siRNA and excipient is associated with a biocompatible polymer (e.g., a polymeric matrix), configured to release said siRNA into the eye of a patient at therapeutic levels for a time sufficient to treat an ocular condition or disease. | 2012-01-26 |
20120022138 | MEANS FOR INHIBITING THE EXPRESSION OF ANG2 - The present invention is related to an siRNA comprising an antisense strand and a sense strand, wherein all or a portion of said antisense strand comprises an antisense duplex region, wherein all or a portion of said sense strand comprises a sense duplex region, wherein said antisense duplex region is at least partially complementary to said sense duplex region, wherein said siRNA comprises a duplex region consisting of said antisense duplex region and said sense duplex region, and wherein: a) said antisense strand comprises a nucleotide sequence of SEQ ID NO: 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 68, 74, 76, 78, 80, 82, 84, 86, 88, 90, 92, 94, 96, 98, 100, 102 or 104; or b) said antisense strand comprises an antisense duplex region, all or a portion of which, is complementary to a portion of SEQ ID NO: 1 or 70. | 2012-01-26 |
20120022139 | Short Interfering Ribonucleic Acid (siRNA) for Oral Administration - Short interfering ribonucleic acid (siRNA) for oral administration, said siRNA comprising two separate RNA strands that are complementary to each other over at least 15 nucleotides, wherein each strand is 49 nucleotides or less, and wherein at least one of which strands contains at least one chemical modification. | 2012-01-26 |
20120022140 | Method of treating a cancer with a survivin antisense oligonucleotide and paclitaxel - Provided is a method of treating cancer of the stomach, comprising administering to a patient a therapeutically effective combination of a Survivin antisense oligonucleotide and paclitaxel. | 2012-01-26 |
20120022141 | COMPOSITIONS AND METHODS FOR INHIBITING EXPRESSION OF A GENE FROM THE JC VIRUS - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a gene from the JC Virus (JC virus genome), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of a gene from the JC Virus. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by JC virus expression and the expression of a gene from the JC Virus using the pharmaceutical composition; and methods for inhibiting the expression of a gene from the JC Virus in a cell. | 2012-01-26 |
20120022142 | RNA Interference Mediated Inhibition of Signal Transducer and Activator of Transcription 1 (STAT1) 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 STAT1 gene expression and/or activity, and/or modulate a STAT1 gene expression pathway. 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) molecules that are capable of mediating or that mediate RNA interference (RNAi) against STAT1 gene expression. | 2012-01-26 |
20120022143 | RNA Interference Mediated Inhibition of the Thymic Stromal Lymphopoietin (TSLP) Gene Expression Using Short Interfering Nucliec 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 TSLP gene expression and/or activity, and/or modulate a TSLP gene expression pathway. 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) molecules that are capable of mediating or that mediate RNA interference (RNAi) against TSLP gene expression. | 2012-01-26 |
20120022144 | Antisense Oligonucleotides for Inducing Exon Skipping and Methods of Use Thereof - An antisense molecule capable of binding to a selected target site to induce exon skipping in the dystrophin gene, as set forth in SEQ ID NO: 1 to 202. | 2012-01-26 |
20120022145 | Antisense Oligonucleotides for Inducing Exon Skipping and Methods of Use Thereof - An antisense molecule capable of binding to a selected target site to induce exon skipping in the dystrophin gene, as set forth in SEQ ID NO: 1 to 202. | 2012-01-26 |
20120022146 | SIGNAL ACTIVATED MOLECULAR DELIVERY - Provided herein are signal activatable molecular constructs for enzyme-assisted delivery of molecules and related components, such as a sensor domain, compositions, methods and systems. | 2012-01-26 |
20120022147 | 2, 6 XYLIDINE DERIVATIVES FOR THE TREATMENT OF PAIN - The disclosure herein provides a composition compound of formula 1. The disclosure also provides a method of synthesizing the compound of formula 1. The compound of formula 1 or its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof may be formulated as pharmaceutical composition to be used for treatment of pain. The pharmaceutical composition of compound of formula 1 or the final compound may be formulated for non-invasive peroral, topical (example transdermal), enteral, transmucosal, targeted delivery, sustained release delivery, delayed release, pulsed release and parenteral methods. Such compositions may be used to treat chronic pain manifested with chronic diseases or its associated complications. The compound of formula 1 may also be offered as a kit. | 2012-01-26 |
20120022148 | Curcuminoids in Combination Docetaxel for the Treatment of Cancer and Tumour Metastasis - The present invention relates to a curcuminoid for enhancing the clinical efficacy of Docetaxel for the treatment of cancers and metastases. | 2012-01-26 |
20120022149 | PHARMACEUTICAL COMPOSITION WITH ENHANCED SOLUBILITY CHARACTERISTICS - There are disclosed pharmaceutical compositions, particularly ophthalmic compositions, that contain relatively high concentrations of solubility enhancing polymer (e.g., polyether polymer, polyvinyl polymer or a combination thereof) for providing enhanced solubility of one or more therapeutic agents. In a preferred embodiment, the composition is a multi-dose topical aqueous ophthalmic composition that contains relatively high concentrations of solubility enhancing polymer (e.g., polyether polymer, polyvinyl polymer or a combination thereof) for providing enhanced solubility of one or more therapeutic agents. | 2012-01-26 |