Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.
Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
Type:
Grant
Filed:
February 1, 2008
Date of Patent:
May 10, 2011
Assignee:
Novartis AG
Inventors:
Shifeng Pan, Wenqi Gao, Nathanael S Gray, Yuan Mi, Yi Fan
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Type:
Grant
Filed:
October 20, 2010
Date of Patent:
May 10, 2011
Assignee:
Hoffmann-La Roche Inc.
Inventors:
David Robert Bolin, Matthew Michael Hamilton
Abstract: A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.
Type:
Grant
Filed:
October 12, 2005
Date of Patent:
May 10, 2011
Assignee:
Pfizer, Inc.
Inventors:
Antone John deBettencourt, III, Evgenyi Yur'evich Shalaev
Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
Type:
Grant
Filed:
October 19, 2010
Date of Patent:
April 19, 2011
Assignee:
Serenex, Inc.
Inventors:
Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl, optionally substituted arylcarbonyl, lower alkoxycarbonyl or the like; R4 is lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
Abstract: Sulfonyl derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.
Type:
Grant
Filed:
August 3, 2005
Date of Patent:
March 29, 2011
Assignee:
Merck Sharp & Dohme
Inventors:
Sherman T. Waddell, James M. Balkovec, Gina M. Santorelli, Aaron H. Leeman, Milana Maletic, Xin Gu
Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.
Abstract: Novel compounds of the formula (I), in which D, E, G, W, X, Y, T, R1 and R2 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
Type:
Grant
Filed:
March 8, 2004
Date of Patent:
March 15, 2011
Assignee:
Merck Patent GmbH
Inventors:
Christos Tsaklakidis, Dieter Dorsch, Werner Mederski, Bertram Cezanne, Johannes Gleitz
Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
Type:
Grant
Filed:
December 19, 2007
Date of Patent:
March 15, 2011
Assignee:
Serenex, Inc.
Inventors:
Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
Abstract: The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).
Type:
Grant
Filed:
October 22, 2007
Date of Patent:
March 8, 2011
Assignee:
AstraZeneca AB
Inventors:
Leonie Campbell, Kurt Gordon Pike, Abid Suleman, Michael James Waring
Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
Type:
Grant
Filed:
June 25, 2007
Date of Patent:
March 8, 2011
Assignee:
SmithKline Beecham (Cork) Limited
Inventors:
Christopher S. Brook, Wei Chen, Philip C. Dell'Orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
Type:
Grant
Filed:
July 14, 2006
Date of Patent:
March 1, 2011
Assignee:
Laboratorios Del Dr. Esteve, S.A.
Inventors:
Antoni Torrens, Jordi Quintana, Helmut Buschmann, Albert Dordal, Josep Mas
Abstract: The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.
Abstract: The present invention relates to novel processes for preparing DPP-IV inhibitors having the structure of formula I, and pharmaceutically acceptable salt thereof, which are useful for treatment of Type 2 diabetes.
Type:
Grant
Filed:
June 27, 2007
Date of Patent:
February 22, 2011
Assignee:
Glenmark Pharmaceuticals, S.A.
Inventors:
Abraham Thomas, V. S. Prasada Rao Lingam, Ashok Bhausaheb Kadam, Suresh M. Kadam, Shantaram Kashinath Phatangare, Deepak Vitthal Ukride
Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
February 15, 2011
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Haiqing Yuan, John E. Donello
Abstract: Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NR1 or C(R4)(R4a); K is selected from NR2 or C(R5)(R5a); L is selected from NR3 or C(R6)(R6a); and A, X, Y, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R8, R10, R11, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
Type:
Grant
Filed:
June 13, 2006
Date of Patent:
February 15, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jingwu Duan, Zhonghui Lu, David S. Weinstein, Bin Jiang
Abstract: It is an object to provide a noble anthracene derivative, a light emitting element with a high luminous efficiency, and further a light emitting element with a long lifetime. It is another object to provide a light emitting device and electronic device with a long lifetime by using the light emitting element. An anthracene derivative represented by General Formula (1) is provided. Since the anthracene derivative represented by General Formula (1) has a high luminous efficiency, when the anthracene derivative is used for a light emitting element, the light emitting element can have a high luminous efficiency. Further, when the anthracene derivative represented by General Formula (1) is used for a light emitting element, the light emitting element can have a long lifetime.
Type:
Grant
Filed:
September 24, 2007
Date of Patent:
February 1, 2011
Assignee:
Semiconductor Energy laboratory Co., Ltd.
Abstract: An optically active 3-aminopyrrolidine (3AP) salt has a high optical purity which is useful as an intermediate in an industrial production method of an optically active 3AP, an efficient method for producing it, and an efficient industrial method for optical resolution of 3AP. Optical resolution of 3AP is efficiently carried out by reacting racemic 3AP with optically active 2-methoxyphenylacetic acid in the presence of a mineral acid such as hydrochloric acid in an aqueous solvent, followed by separation of the resulting diastereomer salt constituted by 1 mole of optically active 3AP and 2 moles of optically active 2-methoxyphenylacetic acid.
Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.
Type:
Grant
Filed:
June 25, 2004
Date of Patent:
January 4, 2011
Assignee:
Novartis AG
Inventors:
Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang