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01st week of 2013 patent applcation highlights part 58
Patent application numberTitlePublished
20130005708HISTAMINE ANTAGONIST TREATMENT OF INFLAMMATORY SKIN DISORDERS - Presented herein inter alia are compositions, methods, and kits for treating an inflammatory skin disorder using a histamine antagonist. In certain embodiments, the compositions, methods, and kits are for treating urticaria and its symptoms. In certain embodiments, the composition, methods, and kits include a topical pharmaceutical preparation with an effective amount of alcaftadine as an active agent.2013-01-03
20130005709SULFONE COMPOUNDS AS 5-HT6 RECEPTOR LIGANDS - The present invention relates to novel sulfone compounds as 5-HT2013-01-03
20130005710AMINOPYRIDINE DERIVATIVE - The present invention provides a novel aminopyridine derivative that is excellent in pharmaceutical effects such as a neuroprotective effect, a neurogenesis or nerve regeneration promoting effect, and a cognitive function improving effect and, preferably, is low toxic and delivered at a high rate to the central nervous system. Specifically, the present invention provides a compound represented by the formula (I), wherein ring A represents a monocyclic aromatic hydrocarbon ring or the like; ring B may further have a substituent(s); ring D represents a monocyclic aromatic hydrocarbon ring or the like; L represents a bond, or a methylene group or the like; X represents —NRa- or the like, wherein Ra represents a hydrogen atom or the like; n represents 1 or 2; and R2013-01-03
20130005711FASUDIL IN COMBINATION THERAPIES FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT2013-01-03
20130005712COMPOSITION FOR NOXIOUS ORGANISMS-CONTROLLING AGENT AND METHOD FOR USING THE SAME - The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivatives represented by general formula (I) being useful as an insecticide or acaricide and one or more compounds selected from the compounds having insecticidal, acaricidal or nematocidal activity:2013-01-03
20130005713Process for Preparing Diaminophenothiazinium Compounds - Process for preparing compounds of the diaminophenothiazinium type including a step for purification of derivatives (II). The products resulting from this process have a high degree of purity. Use of these compounds for the preparation of medicaments.2013-01-03
20130005714Water-Soluble Meloxicam Granules - Water soluble meloxicam granules comprising: 2013-01-03
20130005715ANIMAL REPELLENT - The present invention provides an animal repellent comprising, as an active ingredient, a compound having an odor innately inducing fear in animals, which is free from acclimation of animals to the aforementioned odor. The present invention relates to animal repellent comprising, as an active ingredient, at least one kind selected from a heterocyclic compound represented by the formula (I):2013-01-03
20130005716DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS - Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.2013-01-03
201300057173-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS HAVING ANALGESIC AND/OR IMMUNO STIMULANT ACTIVITY - Compounds of Formulas 1 and 22013-01-03
20130005718COMPOSITIONS AND METHODS OF TREATING CHRONIC PAIN BY ADMINISTERING PROPOFOL DERIVATIVES - Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.2013-01-03
20130005719METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.2013-01-03
20130005720PHARMACEUTICAL COMPOSITION FOR TREATING CANCER AND APPLICATIONS THEREOF - This invention relates to a pharmaceutical composition for treating cancer, comprising an effective amount of a compound represented by formula (I):2013-01-03
20130005721INDOLIZINE INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.2013-01-03
20130005722Pharmaceutical Composition of Mycophenolate Mofetil and Process for Preparing Thereof - The present invention is a pharmaceutical composition comprising mycophenolate mofetil in an amount of about 75 to about 200 mg/ml and a suspending agent(s) in an amount of less than 1 mg/ml, as a dry formulation suitable, when constituted with water, for forming a suspension for oral administration, where mg/ml represents concentration after constitution with water.2013-01-03
20130005723TRIAZINE COMPOUNDS AS PI3 KINASE AND MTOR INHIBITORS - Compounds of formula I2013-01-03
20130005724PYRIDINO-PYRIDINONE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I):2013-01-03
20130005725CHEMICAL COMPOUNDS - There is provided pyrimidinyl compounds of Formula (I),2013-01-03
20130005726COMPOSITIONS AND METHODS FOR TREATING INFLAMMATORY DISORDERS - A method for treating in a subject with an inflammatory disorder and/or immunological disorder associated with NOD2 activation includes administering to the subject a therapeutically effective amount of at least one tyro sine kinase inhibitor that substantially inhibits nucleotide-binding oligomerization domain containing 2 (NOD2):receptor-interacting protein 2 (RIP2) signaling in a NOD2-bearing cell and is not cytotoxic to the cell.2013-01-03
20130005727QUINAZOLINE DERIVATIVES - The invention concerns quinazoline derivatives of Formula I2013-01-03
20130005728SUBSTITUTED PYRIMIDINES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS - The present invention is directed to a substituted pyrimidine compound of formula (I)2013-01-03
20130005729METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.2013-01-03
20130005730NOVEL 1,3-OXAZOLIDINE COMPOUNDS AND THEIR USE AS RENIN INHIBITORS - The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.2013-01-03
20130005731CRYSTALLINE FORMS OF NEUROTROPHIN MIMETIC COMPOUNDS AND THEIR SALTS - The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.2013-01-03
20130005732NEW MEDICAL USE OF TRIAZINE DERIVATIVES - Compounds of formula (I):2013-01-03
20130005733COMBINATION ANTI-CANCER THERAPY - Methods and compositions for treating cancer comprising administering to a patient inhibitors of mT0RC1/C2, IGF-1 R, and IR. In some aspects, a combination of an mT0RC1/C2 inhibitor and an IGF-1 R/IR inhibitor is employed. Other aspects are described herein.2013-01-03
20130005734THERAPEUTIC COMPOSITIONS - The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.2013-01-03
20130005735ORGANIC COMPOUNDS - The present invention relates to compounds of formula (I)2013-01-03
20130005736ANTIVIRAL AGENTS - This invention relates to compounds of formula I2013-01-03
20130005737COMPOSITIONS, METHODS AND KITS FOR TREATING LEUKEMIA - Compositions, kits and methods for treating leukemia in a subject (e.g., human) include a first anti-cancer drug consisting of: Δ2013-01-03
20130005738Monocyclic Heteroaryl Compounds - This invention relates to compounds of the general formula:2013-01-03
20130005739PHARMACEUTICAL PREPARATIONS COMPRISING A COS RELEASING COMPOUND - The present invention relates to pharmaceutical compositions comprising a COS releasing compound according to formula (I) and to methods of preparing such compositions. Said pharmaceutical compositions may preferably be used for the treatment and/or the prevention of cardiovascular diseases.2013-01-03
20130005740PROCESS FOR PREPARATION OF OVER-THE-COUNTER GELATIN OR PECTIN-BASED DRUG DELIVERY - Disclosed herein is a process producing a therapeutic comestible gummie product, the process comprises providing a sugar and/or sugar alcohol, water and heating to at least 80° C. to produce a first mixture. A gelling agent and water is also provided and heat to at least 80° C. to produce a second mixture. Combining the first and second mixtures to produce a slurry. The slurry is heated to at least 112° C. to produce a gummie base. The gummie base is cooled to an optimal temperature of below 90° C. for the addition of an active drug and the active drug is substantially uniformly mixed with the gummie base. In some embodiments the active is drug is mixed with an ingestible oil and added to the cooling slurry. The gummie base and active drug mixture is then poured into molding trays and allowed to cure. Also disclosed herein by way the process of the present disclosure is therapeutic comestible gummie product. Furthermore, the present disclosure comprises a therapeutic comestible gummie product comprising ibuprofen and/or other active drug(s).2013-01-03
20130005741SUBSTITUTED PYRIMIDINE AS A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST - The present invention is directed to a 2,6-substituted-4-monosubstitutedamino-pyrimidine compound of formula (I):2013-01-03
20130005742Substituted Diphenylpyrazine Derivatives - This invention relates to novel substituted diphenylpyrazines and 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 PGI2013-01-03
20130005743New positive allosteric modulators of nicotinic acetylcholine receptor - The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.2013-01-03
20130005744INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS - The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.2013-01-03
20130005745INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.2013-01-03
20130005746INHIBITORS OF BRUTONS TYROSINE KINASE FOR THE TREATMENT OF SOLID TUMORS - Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.2013-01-03
20130005747METHOD FOR SELECTING A CANCER THERAPY - The present invention provides a method for determining whether or not a cancer subject is suitable for treatment with a purine-based roscovitine-like inhibitor, which method comprises the step of determining the ras status of the cancer, wherein a determination that the subject has mutant ras status is indicative that the subject is suitable for treatment with a purine-based roscovitine-like inhibitor.2013-01-03
20130005748COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.2013-01-03
20130005749NOVEL FORMULATION AND TREATMENT METHODS - The invention relates to extended release compositions and formulations comprising 6-thioguanine (6-TG), and methods for treating diseases or conditions responsive to 6-TG.2013-01-03
20130005750HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I)2013-01-03
20130005751HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I)2013-01-03
20130005752METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.2013-01-03
20130005753HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I)2013-01-03
20130005754SOLID FORMS OF (S)-ETHYL 2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)PHEN- YL)-2,2,2-TRIFLUOROETHOXY)-PYRIMIDIN-4-YL)PHENYL)PROPANOATE AND METHODS OF THEIR USE - Solid forms of (S)-ethyl 2-amino-3 -(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.2013-01-03
20130005756METHOD FOR TREATING PULMONARY DISEASES USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema. Particularly, this invention is directed to methods of treating pulmonary diseases such as asthma; chronic obstructive pulmonary disease; respiratory tract illness caused by respiratory syncytial virus; pulmonary arterial hypertension; acute respiratory distress syndrome and ventilator induced lung injury; cystic fibrosis; bronchiectasis; alpha-1-antitrypsin deficiency; rhinitis; rhinosinusitis; primary ciliary dyskinesia; pneumonia; bronchiolitis caused by agents other than respiratory syncytial virus; and interstitial lung disease including lymphangioleiomyomatosis; idiopathic pulmonary fibrosis; obliterative bronchiolitis or bronchiolitis obliterans organizing pneumonia due to lung transplantation or HSCT; nonspecific interstitial pneumonia; cryptogenic organizing pneumonia; acute interstitial pneumonia; respiratory bronchiolitis-associated interstitial lung disease; or pulmonary sarcoidosis. The method comprises administering to a subject an effective amount of a rho kinase inhibitor compound to treat the disease.2013-01-03
20130005757PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND A CARDIOVASCULAR AGENT AND METHODS OF USING THE SAME - The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.2013-01-03
20130005758MANUFACTURE, METHOD AND USE OF DRUG-ELUTING MEDICAL DEVICES FOR PERMANENTLY KEEPING BLOOD VESSELS OPEN - The invention relates to stents and catheter balloons having optimized coatings for eluting rapamycin as well as methods for manufacturing these coatings.2013-01-03
20130005759SMALL MOLECULE MODIFIERS OF MICRORNA MIR-122 - MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.2013-01-03
20130005760HETEROCYCLIC COMPOUND HAVING AZOLE GROUP - A heterocyclic compound of formula (I) or a salt thereof:2013-01-03
20130005761PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS - The present invention relates to a composition comprising the compound of formula (1),2013-01-03
20130005762COMBINATION OF DROLOXIFENE AND CLOPIDOGREL - The invention relates to the composition and use of a medicament comprising a fixed dose combination of droloxifene and clopidogrel.2013-01-03
20130005763SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of a drug in the lower gastrointestinal tract, and thereby provide a sustained-release solid preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release solid preparation containing (A) a pharmacologically active drug, (B) carboxyvinyl polymer, (C) povidone, and (D) carmellose sodium, xanthan gum, or sodium carboxymethyl starch.2013-01-03
20130005764QUININE DOSAGE FORMS AND METHODS OF USE THEREOF - Disclosed herein are quinine formulations and methods of using quinine formulations. Specifically disclosed are methods of using quinine and informing a user of information, including potential adverse effects, the effect of food on quinine's pharmacokinetics, effect of dosing various strengths of quinine, effect of maximum plasma concentrations of quinine in a patient as it relates to adverse events, effects of deviating from the prescribed dosage, etc.2013-01-03
20130005765Methods and Compositions for Controlling Ectoparasites - A method for inhibiting hatching of an ectoparasite egg, the method comprising exposing the ectoparasite egg to at least one metal chelating agent and/or metalloprotease inhibitor, wherein the metal chelating agent is a compound comprising at least two heteroatoms able to simultaneously coordinate with a metal ion, at least one of the two heteroatoms being selected from nitrogen, sulfur, oxygen and phosphorus, wherein the compound comprises at least one carbocyclic ring substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom, or the compound comprises at least one heterocyclic ring containing at least one heteroatom, wherein said heterocyclic ring is optionally substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom is provided. Methods of treating ectoparasite infestations and compositions for use in such methods are also provided.2013-01-03
201300057665-[(3,3,3-TRIFLUORO-2-HYDROXY-1-ARYLPROPYL)AMINO]-1H-QUINOLIN-2-ONES, A PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS - The present invention relates to compounds of formula I,2013-01-03
20130005767THERAPEUTIC COMPOUNDS - Disclosed herein are compounds of the formula2013-01-03
20130005768COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.2013-01-03
20130005769INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds:2013-01-03
20130005770ORGANIC COMPOUNDS - The present invention relates to a compound of the formula I2013-01-03
20130005771OXADIAZOLE COMPOUNDS, THEIR PREPARATION AND USE - The present invention relates to oxadiazole compounds in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable prodrugs and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the oxadiazole compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the treatment of cancer, particularly chronic myeloid leukemia (CML). The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.2013-01-03
20130005772METHODS FOR DELIVERING A DRUG TO A HOSPITAL PATIENT FOR SHORT-TERM USE WHILE MINIMIZING LONG-TERM USE OF THE DRUG - Novel methods for delivering a drug to hospital patients for short-term in-hospital use while minimizing long-term use of the drug. Embodiments are provided in which hospitals are identified which may be eligible to treat patients, for example, perform certain types of surgery, and which have measures in place to limit use of the drug to short-term use. The identified hospitals are preferably registered in a storage medium, including computer readable storage media, and may be authorized to receive the shipments of the drug. The received drug may then be dispensed to the patient.2013-01-03
20130005773FLUORO-SUBSTITUTED 2-ARYL-3,5-DICYANO-4-INDAZOLYL-6-METHYL-1,4-DIHYDROPYRIDINES AND USES THEREOF - The present invention relates to novel, fluoro-substituted 2-aryl-3,5-dicyano-4-(1H-indazol-5-yl)-6-methyl-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly Cancer and other proliferative disorders.2013-01-03
20130005774TOPICAL FOAM COMPOSITION - The present invention relates to a novel oil in water emulsion aerosol foam composition containing an active agent for the treatment of various chronic and acute skin conditions, particularly acne and psoriasis; and processes for preparing the emulsion aerosol foam compositions. In particular, the present invention relates to oil in water emulsion aerosol foam compositions containing a retinoid in the oil phase.2013-01-03
20130005775METHODS OF TREATING ULCERATIVE COLITIS - Methods of treating and managing ulcerative colitis, using imidazole-based compounds that inhibit S1P lyase, are disclosed.2013-01-03
20130005776METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.2013-01-03
20130005777SORAFENIB ETHYLSULFONATE SALT, PROCESS FOR PREPARATION AND USE - The present invention provides sorafenib ethane sulphonate, process for its preparation, pharmaceutical composition comprising sorafenib ethane sulphonate and its use for the treatment of cancer. Formula (III).2013-01-03
20130005778URETHANES, UREAS, AMIDINES AND RELATED INHIBITORS OF FACTOR XA - The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.2013-01-03
20130005779METHODS FOR TREATING HYPERLIPIDEMIA WITH INTERMEDIATE RELEASE NICOTINIC ACID COMPOSITIONS HAVING UNIQUE BIOPHARMACEUTICAL CHARACTERISTICS - Methods for treating hyperlipidemia with intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, without causing drug-induced hepatotoxicity to a level which would require discontinuation of the therapy, are disclosed. According to the methods of the present invention, the intermediate nicotinic acid formulations are administered as a single dose once-a-day during the evening or at night. While the methods of the present invention contemplate administering the intermediate release nicotinic acid formulations at any time during a 24 hour period, it is preferable to administer them as a single dose during the evening or at night between about 6:00 pm. and 12:00 a.m., preferably between about 8:00 p.m. and 12:00 a.m., and most preferably between about 8:00 p.m. and 10:00 p.m.2013-01-03
20130005780CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS OF TAPENTADOL - The present invention provides atazanavir sulfate substantially free of diastereomeric impurities. The present invention also provides atazanavir sulfate having D-tertiary leucine analogues less than 0.1%. The present invention further relates to an improved process for preparing atazanavir sulfate, substantially free of its diastereoisomeric impurities, which comprises of reacting diamino compound (IV) with N-methoxycarbonyl-(L)-tertiary-leucine (V) having D-isomer less than 0.1% to obtain atazanavir base; conversion of atazanavir base to atazanavir sulfate by reacting with sulfuric acid and crystallization of atazanavir sulfate from suitable organic solvent(s).2013-01-03
20130005781PRODRUGS OF DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS - Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.2013-01-03
20130005782METHOD FOR INTEGRIN LIGAND DISCOVERY - This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery base upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.2013-01-03
20130005783Prevention And Treatment Of Diseases Caused By Elevated Levels Of Deoxy-Sphingolipids - Substances and methods of use of substances capable of inhibiting serine-palmitoyltransferase (SPT) and/or capable of competing with L-alanine and glycine, including in the reaction catalysed by SPT, including L-serine and D-serine and other compounds, to suppress cytotoxic sphingolipid metabolites, in particular deoxy-sphingolipids. The substances and methods can be used to prevent and treat disease caused by or associated with elevated levels of deoxy-sphingolipids, namely, diabetes (type 1 and type 2 diabetes), particularly diabetic neuropathy, neurodegenerative diseases such as hereditary and sensory neuropathy type I (HSAN1), amyotrophic lateral sclerosis (ALS), Alzheimer disease, other neurological disorders (e.g. depressive disorders, schizophrenia), medication-induced neuriopathies (e.g. induced by treatment with cytostatics like paclitaxel, cis-platin compounds etc.) and other metabolic disorders such as glycogen storage disease type 1a and asthma.2013-01-03
20130005784CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES - The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.2013-01-03
20130005785METHODS OF TREATING BACTERIAL VAGINOSIS WITH AQUEOUS-BASED METRONIDAZOLE GEL FORMULATIONS - The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.2013-01-03
20130005786THERAPEUTIC INVENTION - The invention provides a method of treating acute demyelinating optic neuritis in a patient suffering therefrom, which method comprises administering a compound to the patient, wherein the compound is phenytoin or an analog or prodrug thereof. The compound acts as a neuroprotectant by partial blocking of voltage-gated sodium channels in axonal other cell membranes thereby reducing the entry of sodium into the respective cell in vivo. The treatment is particularly concerned with preserving vision after onset of the acute demyelinating optic neuritis.2013-01-03
20130005787HIGH DOSAGE MUCOADHESIVE METRONIDAZOLE AQUEOUS-BASED GEL FORMULATIONS AND THEIR USE TO TREAT BACTERIAL VAGINOSIS - The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.2013-01-03
20130005788ANTI-FRANCISELLA AGENTS - A series of celecoxib derivatives defined by Formula I:2013-01-03
20130005789Nicotinic Acetylcholine Receptor Sub-Type Selective Amides of Diazabicycloalkanes - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).2013-01-03
20130005790INORGANIC SALT COMPLEXES OF VILDAGLIPTIN - The present invention relates to the use of novel vildagliptin complexes for the manufacture of high purity vildagliptin of Formula I and/or pharmaceutical acceptable salts thereof. Further objects of the present invention are pharmaceutically acceptable complexes of vildagliptin and/or amorphous and crystalline forms, anhydrous forms, amorphous and crystalline hydrates, amorphous and crystalline solvates of the complexes and a process for the preparation thereof. Another object of the present invention is the high purity vildagliptin and pharmaceutically acceptable salts thereof prepared form the vildagliptin complexes of the present invention, a process for the preparation thereof and pharmaceutical compositions containing vildagliptin base, pharmaceutically acceptable salts and/or complexes and use thereof for the treatment of type 2 diabetes (NIDDM). The present invention provides pharmaceutically advantageous high purity vildagliptin complexes.2013-01-03
20130005791RNAi MODULATION OF RSV AND THERAPEUTIC USES THEREOF - The present invention is based on the in vivo demonstration that RSV can be inhibited through intranasal administration of iRNA agents as well as by parenteral administration of such agents. Further, it is shown that effective viral reduction can be achieved with more than one virus being treated concurrently. Based on these findings, the present invention provides general and specific compositions and methods that are useful in reducing RSV mRNA levels, RSV protein levels and viral titers in a subject, e.g., a mammal, such as a human. These findings can be applied to other respiratory viruses.2013-01-03
20130005792BIOMARKERS TO IDENTIFY HIV-SPECIFIC T-CELL SUBSETS - The invention relates to expression profiles of HIV-specific T-cells and their methods of use, including but not limited to treatment of HIV, increasing T-cell function and/or survival in HIV infected subjects, monitoring HIV disease progression and classifying HIV infected subjects as controllers or chronic progressors.2013-01-03
20130005793Compositions and Methods for Inhibiting Gene Expression of Hepatitis B Virus - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a Hepatitis B Virus 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 Hepatitis B Virus infection using said pharmaceutical composition; and methods for inhibiting the expression of a Hepatitis B Virus gene in a cell.2013-01-03
20130005794METHODS AND SEQUENCES TO SUPPRESS PRIMATE HUNTINGTON GENE EXPRESSION - Disclosed herein are sequences, molecules and methods used to suppress the expression of HD genes encoding for huntingtin protein in primates including 2013-01-03
20130005795Use of Light Sensitive Genes - The invention relates to the use of a light-gated ion channel for the manufacture of a medicament for the treatment of blindness and a method for expressing said cell specific fashion, e.g. in ON-bipolar cells, ON-ganglion cells, or AII amacrine cells.2013-01-03
20130005796METHOD FOR PROLIFERATING CARDIOMYOCYTES USING MICRO-RNA - Disclosed are: a method for proliferating cardiomyocytes, wherein a miRNA that promotes the proliferation of cardiomyocytes is used; a vector for the treatment of heart diseases; and a pharmaceutical composition or the like for the treatment of heart diseases. Specifically disclosed are: a method for proliferating cardiomyocytes, which uses a miRNA that has a cardiomyocyte proliferation promoting action; a vector for the treatment of heart diseases, which comprises the miRNA; and a pharmaceutical composition or the like for the treatment of heart diseases, which contains the vector. The miRNA is preferably one selected from the group consisting of miR-148a, miR-148b, miR-152 and miR-373 that are mature miRNAs, precursors of the aforementioned miRNAs, and mutants and analogues of the miRNAs and the precursors.2013-01-03
20130005797ENDOSOMOLYTIC POLY(AMIDOAMINE) DISULFIDE POLYMERS FOR THE DELIVERY OF OLIGONUCLEOTIDES - The present invention provides endosomolytic poly(amidoamine)disulfide polymers, polyconjugates, compositions and methods for the delivery of oligonucleotides for therapeutic purposes.2013-01-03
20130005798ANTIPROTOZOAL COMPOUND DERIVED FROM COELENTERATA - The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R2013-01-03
20130005799THE USE OF FENOTEROL AND FENOTEROL ANALOGUES IN THE TREATMENT OF GLIOBLASTOMAS AND ASTROCYTOMAS - This disclosure concerns the discovery of the use of fenoterol and (R,R)- and (R,S)-fenoterol analogues for the treatment of a tumor expressing a β2-adrenergic receptor, such as a primary brain tumor, including a glioblastoma or astrocytoma expressing a β2-adrenergic receptor. In one example, the method includes administering to a subject a therapeutically effective amount of fenoterol, a specific fenoterol analogue or a combination thereof to reduce one or more symptoms associated with the tumor, thereby treating the tumor in the subject.2013-01-03
20130005800COMPOSITION FOR TRANSDERMAL OR TRANSMUCOSAL ADMINISTRATION - The invention provides a composition for transdermal or transmucosal administration useful as an anti-Alzheimer's drug, an antiparkinson drug, an antidepressant, a psychoactive drug, or to treat drug dependence. The composition has an effective dose of a racemate or an optically acceptable substance of 1-(benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable salt thereof and a vehicle, which can be administered without an invasion of skin or mucous membrane. The composition enables its active ingredient to stably arrive in a sufficient effective amount through the skin and mucous membrane to the body or brain. The composition is free of disadvantages such as a reduction in an active component caused by a first pass effect in the liver, as well as pain, damage or infection.2013-01-03
20130005801PHENYLCARBAMATE COMPOUND AND MUSCLE RELAXANT CONTAINING THE SAME - A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.2013-01-03
20130005802TREATMENT OF WNT/FRIZZLED-RELATED DISEASES - Methods of treating Wnt/Frizzled-related diseases, comprising administering niclosamide compounds are provided. Methods of predicting whether a disease will respond to treatment with a niclosamide compound are also provided.2013-01-03
20130005803USE OF COMPOUNDS IN THE TREATMENT OR PREVENTION OF SKIN DISORDERS - The use of compounds in the treatment of skin disorders is described. In particular, the use of a compound of formula (I)2013-01-03
20130005804Novel Uses of Neuraminidase Inhibitors in Infectious Diseases - The present invention relates to methods of decreasing the infectivity, morbidity and rate of mortality, in treating diseases associated with a variety of pathogenic organisms, specifically diseases involving one or more pathogens that require neuraminidase as a virulence factor. In addition, the present invention uses biology based therapy to treat neuraminidase dependent infections or diseases dependent on sialic acid metabolism.2013-01-03
20130005805ESTERS FOR TREATMENT OF OCULAR INFLAMMATORY CONDITIONS - The present invention relates to ophthalmic compositions and methods for the treatment of dry eye and other inflammatory ocular conditions. In particular, the present invention relates to a composition comprising an esterified anti-inflammatory lipid mediator, which is an ester of an anti-inflammatory lipid mediator that is a reaction product of the anti-inflammatory lipid mediator and a monohydric alcohol or an amide wherein the majority of the anti-inflammatory lipid mediator is present in an ester form. In this way, the compositions are substantially free of an acid form of the anti-inflammatory lipid mediators. This composition can be topically delivered to the ocular surface via a preparation, solution, gel, ointment, and/or strip and/or a contact lens.2013-01-03
20130005806ANALYSIS OF TMLHE AND CARNITINE BIOSYNTHESIS FOR AUTISM DIAGNOSIS - Embodiments of the invention include determining whether an individual has autism spectrum disorder or is at risk for developing autism spectrum disorder or at risk for regression of or into autism spectrum disorder. Specific embodiments include the determination of indicative levels of carnitine or other metabolites in carnitine biosynthesis and may include assaying for mutations in TMLHE, including in exon 2, for example. In some cases one can assay for mutations in TMLHE in the absence of biochemical analysis of carnitine biosynthesis metabolites. An individual with deficiency in TMLHE and/or carnitine levels may be administered carnitine, acetylcarnitine, butyrobetaine, or a combination thereof, for example.2013-01-03
20130005807ANTIMICROBIAL COMPOSITION - The objective of the present invention is to provide an antimicrobial composition that can be safely used with a broad range of foods and beverages, cosmetics, drugs, and other similar products while showing growth inhibition activity against a wide variety of microorganisms. The present invention relates to the antimicrobial composition comprising at least one cooling agent selected from the group consisting of menthyl 3-hydroxybutanoate, 2-methyl-3-(menthoxy)propane-1,2-diol, 2-(menthoxy)ethanol, 3-menthoxypropan-1-ol, 2-(2-menthoxyethoxy)ethanol, and menthyl glyoxylate.2013-01-03
20130005808VASELINE-LIKE COMPOSITION AND COSMETIC - The present invention relates to a vaseline-like composition, comprising one type or two or more types of components selected from the following components (C), (D) and (E) at 5% by weight to 20% by weight, the following component (A) at 40% by weight to 90% by weight, and the following component (B) at 5% by weight to 50% by weight, and to a cosmetic containing the vaseline-like composition: component (A): one or more types of ester compounds selected from diisostearyl malate and diglyceryl triisostearate; component (B): a hydrocarbon wax having a melting point of 70° C. to 130° C.; component (C): a poly(12-hydroxystearic acid) having an average degree of polymerization of 3 to 20; component (D): a poly(12-hydroxystearic acid) derivative obtained by esterifying a poly(12-hydroxystearic acid) having an average degree of polymerization of 3 to 20 and a polyvalent alcohol having a valence of 5 or more; and, component (E): a dimer dilinoleic acid derivative.2013-01-03
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