48th week of 2010 patent applcation highlights part 54 |
Patent application number | Title | Published |
20100305101 | Leptin genotype and -adrenergic agonists - A method of identifying livestock animal subgroups of the same species, from a group of livestock animals of the same species wherein the subgroup has similar genetic predispositions for response to Zilpaterol Hydrochloride (ZH) treatment with respect to marbling, HCW gain, REA size gain, DDMI, % EBF, and YG's. The genetic potential of each animal to respond to ZH treatment is established by determining the LeptinArg25Cys genotype and segregating individual animals into subgroups based upon the LeptinArg25Cys genotype. | 2010-12-02 |
20100305102 | HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES - The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, | 2010-12-02 |
20100305103 | GENES DIFFERENTIALLY EXPRESSED IN BIPOLAR DISORDER AND/OR SCHIZOPHRENIA - This invention provides molecular markers that are prognostic and/or diagnostic for a psychiatric disorder. In particular, genes are identified whose expression is altered in schizophrenia and/or bipolar disorder thereby providing prognostic and diagnostic markers for the disorder. In addition genes are identified whose dysregulation provides markers that allow diagnostic distinction between schizophrenia and bipolar disorder. | 2010-12-02 |
20100305104 | Oxadiazole Diaryl Compounds - The invention relates to compounds of formula (I): | 2010-12-02 |
20100305105 | PHENYLSULFOXYOXAZOLE COMPOUND INHIBITORS OF UREA TRANSPORTERS - Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein. | 2010-12-02 |
20100305106 | INHIBITORS OF FATTY ACID UPTAKE AND METHODS OF USE - The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2. | 2010-12-02 |
20100305107 | QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS - Disclosed are quinoline compounds having affinity for the 5-HT | 2010-12-02 |
20100305108 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention 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. | 2010-12-02 |
20100305109 | POTASSIUM CHANNEL MODULATORS - Disclosed herein are KCNQ potassium channels modulators of formula (I) | 2010-12-02 |
20100305110 | CONDENSED IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS - The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R | 2010-12-02 |
20100305111 | SUBSTITUTED PIPERIDINES - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases. | 2010-12-02 |
20100305112 | PYRIMIDINE INHIBITORS OF KINASE ACTIVITY - Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, | 2010-12-02 |
20100305113 | Substituted Imidazopyridazines as Lipid Kinase Inhibitors - The invention relates to novel compounds of the formula I, | 2010-12-02 |
20100305114 | Heterocyclic Aromatic Compounds Useful As Growth Hormone Secretagogues - Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I | 2010-12-02 |
20100305115 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - The present invention relates to compounds of formula (I) wherein c, X, Y, R | 2010-12-02 |
20100305116 | Compounds Comprising a Cyclobutoxy Group - The present invention relates to compounds comprising a cyclobutoxy group, processes for preparing them, phar-maceutical compositions comprising said compounds and their use as pharmaceuticals. | 2010-12-02 |
20100305117 | SUBSTITUTED PTERIDINES USEFUL FOR THE TREATMENT AND PREVENTION OF VIRAL INFECTIONS - The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections. | 2010-12-02 |
20100305118 | PYRIMIDINE INHIBITORS OF KINASE ACTIVITY - Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, | 2010-12-02 |
20100305119 | Method for the treatment of anthrax infections - A method of treating an anthrax infection wherein a compound of formula I | 2010-12-02 |
20100305120 | COMPOUNDS FOR TREATING MUSCULAR DYSTROPHY - Compounds of formula (I): wherein X, L | 2010-12-02 |
20100305121 | NOVEL ANTAGONISTS OF THE HUMAN FATTY ACID SYNTHASE THIOESTERASE - The present invention provides for compounds of formula (I)-(XIII), as well as pharmaceutically acceptable salts thereof, metabolites thereof, pro-drugs thereof, and pharmaceutical kits that include such compounds. The present invention also provides for the compounds of formula (I)-(XIII) for use in medical therapy or diagnosis. The present invention also provides for the use of the compounds of formula (I)-(XIII) in treating cancer in mammals (e.g., humans), as well inhibiting tumor cell growth in such mammals. The present invention also provides for methods of inhibiting FAS. The methods include contacting FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of inhibiting the TE domain of the FAS. The methods include contacting the thioesterase TE domain of the FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of treating cancer in mammals, as well as methods of inhibiting tumor cell growth in such mammals. The methods include administering a compound of formula (I)-(XIII) to a mammal in need of such treatment. | 2010-12-02 |
20100305122 | APOPTOSIS INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 2010-12-02 |
20100305123 | CLASS OF HISTONE DEACETYLASE INHIBITORS - This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH | 2010-12-02 |
20100305124 | Acylated Aminopyridine and Aminopyridazine Insecticides - The present invention relates to aminopyridine and aminopyridazine derivatives of the general formula (I) | 2010-12-02 |
20100305125 | SALT OF ABT-263 AND SOLID-STATE FORMS THEREOF - ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 2010-12-02 |
20100305126 | Pyrimidine Inhibitors of Kinase Activity - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, | 2010-12-02 |
20100305127 | NOVEL COMPOUNDS - Compounds of formula (I) | 2010-12-02 |
20100305128 | Pyrimidinyl-Thiophene Kinase Modulators - The present invention provides novel pyrimidinyl-thiophene kinase modulators and methods of using the novel pyrimidinyl-thiophene kinase modulators to treat diseases mediated by kinase activity. | 2010-12-02 |
20100305129 | COMPOSITIONS AND METHODS FOR INHIBITING GROWTH AND METASTASIS OF MELANOMA - There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof. | 2010-12-02 |
20100305130 | NASAL SPRAY DEVICE AND METHOD OF USE THEREOF - A single-use sprayer for nasal anesthesia is disclosed. The single-use sprayer includes a single dose of anesthetic and a delivery system adapted to dispense the single dose of anesthetic into a nostril. The single-use sprayer prevents patient-to-patient contamination, is easy to use and allows for self-administration, and has a simple, disposable configuration so as to lower the production cost. | 2010-12-02 |
20100305131 | Substituted Aminopropionic Derivatives as Neprilysin inhibitors - The present invention provides a compound of formula I′; | 2010-12-02 |
20100305132 | GLUTARALDEHYDE BASED BIOCIDAL COMPOSITIONS AND METHODS OF USE - Provided are biocidal compositions comprising glutaraldehyde and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems. | 2010-12-02 |
20100305133 | Prolyl Hydroxylase Inhibitors - The invention described herein relates to certain quinoxaline-5-carboxamide derivatives of formula (I) | 2010-12-02 |
20100305134 | SPECIFIC INHIBITORS OF PTERIDINE REDUCTASE WITH ANTIPARASITIC ACTION - The processes for the preparation of alkyl derivatives of N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-piperidin-2-carboxylic acid and N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-piperidin-4-carboxylic acid and of N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-pyrrolidin-2-carboxylic acid and N-[4-(2,4-diaminopteridin-6-ylmethylamino)benzoyl]-N-pyrrolidin-4-carboxylic acid. Their specific properties of inhibition versus Pteridine reductase of parasitic species. The processes for the preparation of alkyl derivatives of 1[4-(quinoxalin-2-ylamino)benzoyl]piperidin-mono and di-carboxylic acid and alkyl derivatives of 1-[4-(quinoxalin-2-ylamino)benzoyl]pyrrolidin-mono and di-carboxylic acid. The specific properties of inhibition versus Pteridine reductase of parasitic species. The processes for the preparation of alkyl derivatives of 4-(6,7-dimethoxy-quinoxalin-2-ylmethoxy)benzoic acid and alkyl derivatives of 2-(phenylsulfanil)-quinoxalin-5,7-diamine and their specific properties of inhibition versus Pteridine reductase of bacterial species. The pharmaceutical composition and their use in the treatment and prevention of parasitic infections caused by | 2010-12-02 |
20100305135 | AHCY HYDROLASE INHIBITORS FOR TREATMENT OF HYPER HOMOCYSTEINEMIA - The present invention is directed to AHCY inhibitors of formula (I) which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels. | 2010-12-02 |
20100305136 | QUINOLONE ANALOGS DERIVATIZED WITH SULFONIC ACID, SULFONATE OR SULFONAMIDE - The present invention provides quinolone analogs derivatized with a sulfonic acid, sulfonate or sulfonamide group, which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing quinolone analogs quinolone analogs derivatized with a sulfonic acid, sulfonate or sulfonamide group, and methods of using the same. | 2010-12-02 |
20100305137 | PIPERAZINE DERIVATIVES AND METHODS OF USE - The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility. | 2010-12-02 |
20100305138 | PYRIDYL DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): | 2010-12-02 |
20100305139 | METHOD OF TREATING ABNORMAL LIPID METABOLISM - The present invention provides a pharmaceutical agent for the treatment and/or prophylaxis of abnormal blood glucose and lipid metabolism associated with eating, for which a sufficient treatment method or a therapeutic drug has not been found. | 2010-12-02 |
20100305140 | BENZIMIDAZOLE DERIVATIVES WHICH ARE TO BE USED AS ANTAGONIST FOR THE CB1-RECEPTOR - Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R | 2010-12-02 |
20100305141 | TETRAHYDROINDOLONE DERIVATIVES FOR TREATMENT OF NEUROLOGICAL CONDITIONS - Compositions comprising tetrahydroindolone derivatives in which the tetrahydroindolone moiety is covalently linked to a substituted arylpiperazine moiety and methods for treating neurological and psychiatric conditions using such compositions are disclosed. | 2010-12-02 |
20100305142 | 3-AMINOIMIDAZO 1,2-A PYRIDINE DERIVATIVES HAVING AN SGLT1- AND SGLT2-INHIBITING ACTION FOR THE TREATMENT OF TYPE 1 AND TYPE 2 DIABETES - Novel compounds of the formula (I), in which W, T, R | 2010-12-02 |
20100305143 | PYRROLOPYRIMIDINE COMPOUNDS - Compounds of formula (I) are A | 2010-12-02 |
20100305144 | PREVENTION OF RECURRENCE OF URETHRAL STRICTURE AFTER A CONVENTIONAL TREATMENT - Prevention of recurrence of urethral stricture after a conventional treatment. Composition applicable to the prevention of recurrence of urethral stricture after a conventional treatment, including a pharmaceutically effective amount of halofuginone. Urethral stricture, a common disease, appears secondary to urethritis, urethral infection, urethral inflammation, urethral instrumentation, urethral catheterization, urethral trauma, urethral surgery and all types of urethral lesions. Conventional treatments by internal urethrotomy, urethral dilation or surgical urethroplasty are available and can cure urethral stricture, but with a relatively high rate of recurrence of the stricture. Halofuginone can prevent the recurrence of urethral stricture after a conventional treatment via internal urethrotomy, urethral dilation or surgical urethroplasty. | 2010-12-02 |
20100305145 | Substituted Aminobutyric Derivatives as Neprilysin Inhibitors - The present invention provides a compound of formula I′; | 2010-12-02 |
20100305146 | Method for the Production of 1,3-Dioxolane-2-Ones and Carboxylic Acid Esters by Means of Transacylation in Basic Reaction Conditions - The invention relates to a method for producing 1,3-dioxolane-2-ones of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1 to R5 have the meanings indicated in the claims and the description. The invention further relates to a method for producing 2-hydroxy carboxylic acid esters of general formula (5) with or without isolation of the intermediate in the form of a derivative of the 1,3-dioxolane-2-one of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1, R2, and R6 have the meanings indicated in the claims and the description. The method according to the invention allows the reaction to take place in very gentle basic conditions, causing fewer secondary reactions and providing a greater yield than reactions in highly polar aprotic solvents. Acid-sensitive and/or temperature-sensitive compounds can be synthesized. | 2010-12-02 |
20100305147 | CHEMICALLY MODIFIED SMALL MOLECULES - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer. | 2010-12-02 |
20100305148 | DI-ESTER PRODRUGS OF CAMPTOTHECIN, PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTICAL APPLICATIONS - The present invention is related to 10,20-di-O ester derivatives of camptothecin and pharmaceutical formulations thereof. The compounds and pharmaceutical formulations of the present invention possess increased biological life span and bioavailability and reduced toxicity, while maintaining anti-cancer activity. | 2010-12-02 |
20100305149 | Polyal Drug Conjugates Comprising Variable Rate-Releasing Linkers - Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described. | 2010-12-02 |
20100305150 | TUBEROUS SCLEROSIS TREATMENT - Rapamycin derivatives for use in the treatment of neurocutaneous disorders. | 2010-12-02 |
20100305151 | O-Methylated Rapamycin Derivatives For Alleviation And Inhibition Of Lymphoproliferative Disorders - The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal. | 2010-12-02 |
20100305152 | METHOD OF INHIBITING THE GROWTH OF HELICOBACTER PYLORI - The shikimate pathway links metabolism of carbohydrates to biosynthesis of aromatic compounds, which is an attractive target for the rational drug and herbicide design because it is essential in algae, higher plants, bacteria, and fungi, but absent from mammals. Thus, the present invention provides a method of inhibiting the growth of bacteria or fungi, especially | 2010-12-02 |
20100305153 | AMINOISOQUINOLINE THROMBIN INHIBITOR WITH IMPROVED BIOAVAILABILITY - The invention relates to the compound N-(2-oxo-2-propoxyethyl)-β-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases. | 2010-12-02 |
20100305154 | Prolyl Hydroxylase Inhibitors - The invention described herein relates to certain quinoline-8-carboxamide derivatives of formula (I) | 2010-12-02 |
20100305155 | SUBSTITUTED PYRAZOLE INHIBITORS OF C-MET PROTEIN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 2010-12-02 |
20100305156 | INHIBITORS OF C-MET PROTEIN KINASE - The present invention relates to compounds of formula I, which is useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising compounds of formula I and methods of using the compositions in the treatment of proliferative disorders. | 2010-12-02 |
20100305157 | DERIVATIVES OF DICARBOXYLIC AMINO ACIDS AND THEIR APPLICATION IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - Products of a general formula (I) and their use in the manufacture of medicines useful for the treatment of neurodegenerative diseases such as Alzheimer's disease or, in general, any disease or pathology produced by alterations of biological functions that can be treated or therapeutically modified by these products. | 2010-12-02 |
20100305159 | CRYSTALLINE FORM OF PIPERIDINE COMPOUND - The present invention is to provide a crystalline form of (2R,4S)-1-{N-(3,5-bistrifluoromethylbenzyl)-N-methyl}aminocarbonyl-2-(4-fluoro-2-methylphenyl)-4-(2-hydroxyethylaminocarbonyloxy)piperidine or a solvate thereof. | 2010-12-02 |
20100305160 | ANESTHETIC METHODS AND COMPOSITIONS - The present invention relates to compositions and methods use in pain reduction, including but not limited to, peripheral nerve blocks. In particular, the present invention relates to compositions and methods for the administration of perineural dexmedetomidine and ropivacaine in combination for increased antinociception in peripheral nerve blocks. In addition, this invention relates to any use of dexmedetomidine alone or in combination with other agents for the purpose of decreasing inflammation around peripheral nerves, thereby decreasing the potential for peripheral nerve injury. Further, the invention relates to the use of dexmedetomidine to reduce inflammation in the muscle to lessen or prevent muscle damage. | 2010-12-02 |
20100305161 | COMBINATIONS OF FUNGICIDAL AZOLES AND PYRION COMPOUNDS - The present invention relates to combinations of a fungicidal triazole, or a salt thereof, and a pyrion compound, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of a fungicidal triazole, or a salt thereof, selected from the group consisting of azaconazole, bromuconazole, cyproconazole, difenoconazole, epoxiconazole, fenbuconazole, fluquinconazole, flusilazole, hexaconazole, ipconazole, metconazole, penconazole, propiconazole, prothioconazole, simeconazole, tebuconazole, tetraconazole, and triticonazole, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox and pyrion disulfide in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, viruses, and the like. | 2010-12-02 |
20100305162 | Methods for the Synthesis of Pyridoxamine - The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): | 2010-12-02 |
20100305163 | PHARMACEUTICAL FORMULATIONS COMPRISING NSAID AND PROTON PUMP INHIBITOR DRUGS - Aspects of the invention relate to pharmaceutical formulations comprising an NSAID and acid reducer drug for therapeutic purposes, and methods of preparing the same. Further aspects of the invention relate to fixed dose pharmaceutical formulations comprising naproxen, or pharmaceutically acceptable salts thereof, and esomeprazole, or pharmaceutically acceptable salts thereof. | 2010-12-02 |
20100305164 | 5-(4-METHANESULFONYL-PHENYL)-THIAZOLE DERIVATIVES FOR THE TREATMENT OF ACUTE AND CHRONIC INFLAMMATORY DISEASES - A compound of formula (I): | 2010-12-02 |
20100305165 | THIOCOLCHICINE DERIVATIVES, METHOD OF MAKING AND METHODS OF USE THEREOF - Disclosed herein are thiocolchicine derivatives suitable for use as muscle relaxants, methods of making the derivatives, and compositions comprising the derivatives. | 2010-12-02 |
20100305166 | NOVEL COMPOUNDS - A compound of formula (I) or salts thereof, | 2010-12-02 |
20100305167 | Administration of an Inhibitor of HDAC - Methods of treating patients with SNDX-275 are provided. | 2010-12-02 |
20100305168 | PERSONAL-CARE COMPOSITION COMPRISING A CATIONIC ACTIVE - In one embodiment, a personal-care composition in the form of an oil-in-water emulsion comprises an anionic pairing agent, a cationic active, and an anionic thickener. In another embodiment, the anionic pairing agent is pre-formed from the neutralization of an acid with a base. In another embodiment, the anionic pairing agent is formed in situ from the neutralization of an acid with a base. In one embodiment, the molar ratio of the base to the acid is at least about 0.70. In another embodiment, the equivalent ratio of the anionic pairing agent to the cationic active is at least about 0.70. The personal-care composition allows for previously unattainable levels of the cationic active to locate within the oil phase of the emulsion. | 2010-12-02 |
20100305169 | PERSONAL-CARE COMPOSITION COMPRISING A CATIONIC ACTIVE - A personal-care composition in the form of an oil-in-water emulsion comprises a water phase, an oil phase, an anionic pairing agent, a cationic active, and an anionic thickener. In one embodiment, the anionic pairing agent is pre-formed from the neutralization of an acid with a base. In another embodiment, the anionic pairing agent is formed in situ from the neutralization of an acid with a base. At least 25% by weight of the cationic active is present in the oil phase. In certain embodiments, a method for regulating keratinous tissue condition and a method for improving deliverability of a cationic active in the presence of an anionic thickener comprise the steps of: providing the aforementioned personal-care composition, and applying the composition to keratinous tissue in need of treatment. The personal-care composition allows for previously unattainable levels of the cationic active to locate within the oil phase of the emulsion. | 2010-12-02 |
20100305170 | Agents for Combating Plant Pests - The present invention relates to compositions for controlling plant pests, which contain the compound of the formula (I) | 2010-12-02 |
20100305171 | Methods for Concomitant Administration of Colchicine and a Second Active Agent - Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided. | 2010-12-02 |
20100305172 | Methods for Concomitant Administration of Colchicine and a Second Active Agent - Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided. | 2010-12-02 |
20100305173 | HYDROXYETHYLAMINO SULFONAMIDE DERIVATIVES - This invention relates to novel hydroxyethylamino sulfonamides, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor. | 2010-12-02 |
20100305174 | Novel Heterocyclic Derivatives - The present invention relates to novel heterocyclic derivatives of formula (I) and their pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, their pharmaceutical compositions, and their prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (1). | 2010-12-02 |
20100305175 | PHARMACEUTICAL LATRUNCULIN FORMULATIONS - The present invention relates to an aqueous pharmaceutical formulation comprising at least one latrunculin and the formulation does not contain a substantial amount of dimethyl sulfoxide. In one embodiment, the present invention is directed to an aqueous pharmaceutical formulation comprising at least one latrunculin in an amount of 0.001-2% w/v, a non-ionic surfactant in an amount of 0.01-2% w/v, and a tonicity agent to maintain a tonicity between 200-400 mOsm/kG, at a pH between 4 to 8, wherein the latrunculin, the surfactant, and the tonicity agent are compatible in the formulation, and the formulation does not contain a substantial amount of dimethyl sulfoxide. The formulation is stable for at least six month at refrigerated temperature. The present invention further provides a method of reducing intraocular pressure, a method of treating glaucoma, a method of inhibiting wound healing after trabeculectomy, and a method of inhibiting angiogenesis. | 2010-12-02 |
20100305176 | (S,R.)-3-PHENYL-4,5 DIHYDRO-5-ISOXAZOLE ACETIC ACID-NITRIC OXIDE AND USE THEREOF AS ANTI-CANCER AND ANTIVIRAL AGENT - The present invention relates to an isoxazole derivative, the compound of formula (I) | 2010-12-02 |
20100305177 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR DIABETIC MACULOPATHY - A prophylactic or therapeutic agent for diabeticmaculopathy, which can be administered for a long time and exhibits efficacy in a mechanism different from that of existing medicines. The invention relates to a prophylactic or therapeutic agent for diabetic maculopathy, comprising, as an active ingredient, a compound represented by the general formula: | 2010-12-02 |
20100305178 | Pharmaceutical Composition - A topical composition comprises at least 5-wt % metronidazole or a pharmacologically acceptable derivative thereof in a non-aqueous vehicle. The composition may be used in the treatment of conditions of the colon, rectum, anorectum and perianal region, in particular inflammatory bowel disease and perianal Crohn's disease. The composition also relieves pain and inflammation and promotes healing of the colon, rectum, and anorectum and perianal region following surgical operations. One advantage of the composition is that topical administration of metronidazole results in a primarily local effect and thus side effects observed from systemic administration are avoided. | 2010-12-02 |
20100305179 | ORAL SUSTAINED-RELEASE TABLET - (Object) An oral sustained-release tablet is provided, which does not cause initial rapid increases in the bloodlevels of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) and can maintain constant the blood levels. | 2010-12-02 |
20100305180 | INHIBITORS OF UBIQUITIN E1 - The present invention features pyrazolidinyl compounds, pharmaceutical compositions of substituted pyrazolidinyl compounds and methods of treating a patient suffering from cancer or viral infection, the method comprising administering to a patient one or more pyrazolidinyl compounds of the invention. | 2010-12-02 |
20100305181 | METHODS FOR TREATING A VARIETY OF DISEASES AND CONDITIONS, AND COMPOUNDS USEFUL THEREFOR - In accordance with the present invention, there are provided novel compounds that have a variety of properties, i.e., antioxidant, anti-inflammatory, antiviral, antibacterial, and antifungal properties. Invention compounds, therefore, have the ability to impart a variety of beneficial physiological effects, e.g., to protect neurons and/or to promote neuroregeneration and/or to promote memory formation and/or to act as protein phosphatase or kinase inhibitors and/or to act as lipoxygenase inhibitors. Such compounds are useful for treatment of a variety of indications, including neurodegenerative diseases and conditions, diabetes, ischemia associated with heart disease, and memory deficit. In another aspect of the present invention, there are also provided formulations containing one or more of the above-described compounds, optionally further containing additional neurologically active compound(s) and/or adjuvants to facilitate delivery thereof across the blood/brain barrier. In still another aspect of the present invention, there are further provided methods for treating a wide variety of neurological indications, e.g., acute neural injuries, chronic injuries, promoting memory formation, and the like. | 2010-12-02 |
20100305182 | COMPOUNDS AND METHODS FOR MODULATING COMMUNICATION AND VIRULENCE IN QUORUM SENSING BACTERIA - The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds. | 2010-12-02 |
20100305183 | METHOD AND COMPOSITION FOR REDUCING REPERFUSION INJURY - The present invention relates to a method of preventing and/or reducing reperfusion injury to a tissue, organ, or organ system in a subject. The method includes administering to the subject an effective amount of a substance P receptor antagonist. | 2010-12-02 |
20100305184 | INHIBITORS OF THE ATB(0,+) TRANSPORTER AND USES THEREOF - The present invention includes inhibitors of the amino acid transporter ATB | 2010-12-02 |
20100305185 | DIAGNOSTIC METHOD - It has been demonstrated that the level of HBP increases in individuals that subsequently develop severe sepsis. Accordingly, the level of HBP, HBP/WBC ratio or HBP/NC ratio in an individual can be used to determine whether or not an individual is at risk of developing severe sepsis. | 2010-12-02 |
20100305186 | METHODS FOR MEDIATING GENE SUPPRESSION - The present invention is concerned with methods for enhancing gene suppression in cells and in particular it is concerned with improved methods for enhancing RNAi-mediated gene silencing by manipulation of factors associated with RNAi. The present invention is also concerned with methods for identifying factors which down-regulate as well as those which up-regulate RNAi. It is also concerned with genetic constructs useful for enhancing or modulating gene silencing and cells harbouring such constructs. | 2010-12-02 |
20100305187 | METHODS AND COMPOUNDS FOR TREATING DISEASES CAUSED BY REACTIVE OXYGEN SPECIES - Provided is a method of treating a patient having an inflammatory disease by using a compound which inhibits the complex I-mediated ROS production, a medicament containing such compound and methods for screening for such compounds. | 2010-12-02 |
20100305188 | NUCLEIC ACID CAPABLE OF REGULATING THE PROLIFERATION OF CELL - Provided are an agent for suppressing or promoting cell proliferation, a diagnostic reagent or therapeutic drug for a disease resulting from a cell proliferation abnormality, an agent for inducing apoptosis, an agent for suppressing or promoting the expression of a target gene for a nucleic acid such as a microRNA, and a method of suppressing or promoting cell proliferation. | 2010-12-02 |
20100305189 | PHARMACEUTICAL COMPOSITION FOR PREVENTING, STABILISING AND/OR INHIBITING BLOOD AND LYMPH VASCULARIZATION - A pharmaceutical composition including as active agent, an antisens oligonucleotide having the sequence SEQ ID NO: 1 in a concentration from about 0.40 mg/ml to about 2 mg/ml and the use thereof for preventing, stabilizing and/or inhibiting blood and lymph vascularization. | 2010-12-02 |
20100305190 | NUCLEIC ACID COMPLEX AND NUCLEIC ACID DELIVERY COMPOSITION - The present invention provides a nucleic acid complex with low toxicity and high safety that can persistently maintain a nucleic acid, such as siRNA or the like, in a cell; and a nucleic acid delivery composition that can efficiently deliver the nucleic acid complex into a cell. A nucleic acid complex with low toxicity and high safety that can persistently maintain a nucleic acid in a cell can be obtained by forming a complex using a nucleic acid to be introduced into a cell, and a highly branched cyclic dextrin. Moreover, when a carrier comprising (A) a diacylphosphatidylcholine, (B) cholesterol and/or a derivative thereof, and (C) an aliphatic primary amine is used as a nucleic acid delivery carrier to introduce the nucleic acid complex into a cell, the safety, the efficiency of intracellular delivery, and the persistence of the nucleic acid in the cell can be further improved. | 2010-12-02 |
20100305191 | RNA INTERFERENCE MEDIATED INHIBITION OF ADENOSINE A1 RECEPTOR (ADORA1) GENE EXPRESSION USING SHORT INTERFERING RNA - The present invention concerns methods and reagents useful in modulating adenosine A1 receptor (ADORA1) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small interfering RNA (siRNA) molecules capable of mediating RNA interference (RNAi) against ADORA1 and related receptors. | 2010-12-02 |
20100305192 | COMPOSITIONS AND METHODS FOR SHORT INTERFERING NUCLEIC ACID INHIBITION OF NAV1.8 - The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Na | 2010-12-02 |
20100305193 | RNAI-MEDIATED INHIBITION OF GREMLIN FOR TREATMENT OF IOP-RELATED CONDITIONS - RNA interference is provided for inhibition of gremlin in intraocular pressure-related conditions, including ocular hypertension and glaucoma such as normal tension glaucoma and open angle glaucoma. | 2010-12-02 |
20100305194 | MODIFIED AND STABILIZED GDF PROPEPTIDES AND USES THEREOF - Modified and stabilized propeptides of Growth Differentiation Factor proteins, such as GDF-8 and Bone Morphogenetic Protein-11, are disclosed. Also disclosed are methods for making and using the modified propeptides to prevent or treat human or animal disorders in which an increase in muscle tissue would be therapeutically beneficial. Such disorders include muscle or neuromuscular disorders (such as amyotrophic lateral sclerosis, muscular dystrophy, muscle atrophy, congestive obstructive pulmonary disease, muscle wasting syndrome, sarcopenia, or cachexia), metabolic diseases or disorders (such as such as type 2 diabetes, noninsulin-dependent diabetes mellitus, hyperglycemia, or obesity), adipose tissue disorders (such as obesity), and bone degenerative diseases (such as osteoporosis). | 2010-12-02 |
20100305195 | MICRORNA MEDIATOR OF CARDIOMYOPATHY AND HEART FAILURE - Provided herein is a microRNA, specifically, β-myosin microRNA, compositions comprising β-myosin microRNA and methods of inhibiting or reducing expression of β-myosin microRNA. Also provided are genetically modified cells and animals comprising exogenous β-myosin microRNA. Provided herein are methods of screening for agents that modulate β-myosin microRNA expression. In addition, methods of identifying target genes that are regulated by β-myosin microRNA and methods of modulating such genes are described. Methods of diagnosing or determining whether a subject is at risk for a cardiovascular disorder are also described. | 2010-12-02 |
20100305196 | COMPOSITION FOR TREATING PROSTATE CANCER (PCa) - The present invention relates to an active (immunostimulatory) composition comprising at least one RNA, preferably an mRNA, encoding at least two (preferably different) antigens capable of eliciting an (adaptive) immune response in a mammal wherein the antigens are selected from the group consisting of PSA (Prostate-Specific Antigen), PSMA (Prostate-Specific Membrane Antigen), PSCA (Prostate Stem Cell Antigen), and STEAP (Six Transmembrane Epithelial Antigen of the Prostate). The invention furthermore relates to a vaccine comprising said active (immunostimulatory) composition, and to the use of said active (immunostimulatory) composition (for the preparation of a vaccine) and/or of the vaccine for eliciting an (adaptive) immune response for the treatment of prostate cancer (PCa), preferably of neoadjuvant and/or hormone-refractory prostate cancers, and diseases or disorders related thereto. Finally, the invention relates to kits, particularly to kits of parts, containing the active (immunostimulatory) composition and/or the vaccine. | 2010-12-02 |
20100305197 | Conditionally Active Ribozymes And Uses Thereof - This invention relates, at least in part, to conditionally active ribozymes and uses of such ribozymes. Some aspects of this invention relate to the engineering of conditionally active ribozymes. In some embodiments, the splicing activity of such ribozymes is modulated by at least one regulatory element. Some aspects of this invention relate to uses of conditionally active ribozymes. RNA detection technology, conditional RNA expression technology, cell tagging technology, therapeutic approaches, and synthetic biology are examples of areas in which conditionally active ribozymes according to some aspects of the invention can be employed. RNA folding models useful in the design of conditionally active ribozymes with altered splicing efficiency and/or substrate specificity are provided. Compositions and methods to manufacture medicaments containing conditionally active ribozymes are also described. | 2010-12-02 |
20100305198 | CATIONIC LIPIDS - This invention relates to cationic lipids. More particularly the invention relates to biodegradable cationic lipids having a plurality of cationic headgroups and one or more lipophilic tail groups. The lipids are of utility in various applications, and in particular in permitting transfection of molecules, and in particular DNA and RNA, into cells. As such the lipids have specific utility in the field of gene therapy as well as other applications such as delivery of small molecules into cells, detergents, and metal ion complexation for medical or industrial applications. | 2010-12-02 |
20100305199 | THERAPEUTIC REGIMEN FOR TREATING CANCER - The invention provides a method for treating cancer in a human comprising administering to the human a dose of a pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier and (ii) an adenoviral vector comprising a nucleic acid sequence encoding TNF-α operably linked to a promoter, wherein the dose comprises about 1×10 | 2010-12-02 |
20100305200 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 2010-12-02 |
20100305201 | Method of Treating a Tumor and Biodistribution of a Drug Delivered by Worm-Like Filomicelles - Provided are filomicelle nanocarrier systems for the controlled transport and bioselective delivery of encapsulatable, cytotoxic active agents contained therein, particularly anticancer agents. Further provided are methods for controlling destabilization of the filomicelle membrane and the resulting hydrolysis-triggered, controlled release of the active agent(s) encapsulated therein by controlling the blend ratio (mol %) of hydrolysable PEO-block copolymer of the hydrophilic component(s) and of the more hydrophobic PEO-block copolymer component(s), wherein bioselective release of the encapsulated cytotoxic agents is distributed intracellularly, and wherein lowered dosage of the drug was delivered to the non-tumor organs. Thus, the filomicelle system offers enhanced tumor-selective biodistribution of a drug, and a reduced toxicity of the encapsulated drug to other organs. | 2010-12-02 |