Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Type:
Grant
Filed:
September 4, 2014
Date of Patent:
January 5, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
Type:
Grant
Filed:
October 15, 2013
Date of Patent:
December 29, 2015
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
Abstract: The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system (CNS) bioavailability and their associated methods of preparation including their use for treatment of exposure to AChE inhibitors such as an organophosphate (OP) insecticides and nerve agents.
Type:
Grant
Filed:
May 22, 2014
Date of Patent:
October 20, 2015
Assignee:
SOUTHWEST RESEARCH INSTITUTE
Inventors:
William E. Bauta, William R. Cantrell, Jr., Michael W. Tidwell
Abstract: The invention relates to compositions and methods for treating various diseases or medical conditions by administering a methylxanthine compound. Specifically, the invention relates to compositions and methods for treating cytochrome oxidase (CcOX) mediated diseases or medical conditions by administering compositions comprising a methyl xanthine compound.
Type:
Grant
Filed:
June 29, 2009
Date of Patent:
October 13, 2015
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
Clifford S. Deutschman, Richard J. Levy
Abstract: The present invention relates to an improved process for the preparation of Roflumilast. The present invention also relates to crystalline Form-I of Roflumilast.
Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
Abstract: The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.
Type:
Grant
Filed:
February 12, 2013
Date of Patent:
September 22, 2015
Assignee:
Wyeth LLC
Inventors:
Quinhong Lu, Mannching Sherry Ku, Warren Chew, Gloria Cheal, Anthony F. Hadfield, Mahmoud Mirmehrabi
Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
Type:
Grant
Filed:
May 8, 2014
Date of Patent:
September 22, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
Abstract: The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.
Type:
Grant
Filed:
April 13, 2012
Date of Patent:
September 15, 2015
Assignee:
INNOV88 LLC
Inventors:
Anderson Gaweco, John Walker, Joseph B. Monahan, Jerry W. Cubbage, Jeffery Carroll
Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
Type:
Grant
Filed:
April 26, 2013
Date of Patent:
September 15, 2015
Assignee:
Janssen Pharmaceutica NV
Inventors:
Jerome Emile Georges Guillemont, Magali Madeleine Simone Motte, David Francis Alain Lancois, Wendy Mia Albert Balemans
Abstract: An objective of the present invention is to provide a process for producing 4-carbonyl oxyquinoline derivatives useful as agricultural and horticultural pesticides and fungicides. The objective can be attained by a process for producing 4-carbonyl oxyquinoline derivatives represented by general formula (1), the process including reacting a quinolone derivative with a halogenated compound or an acid anhydride in the presence of a phase transfer catalyst and a base.
Abstract: The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
September 8, 2015
Assignee:
Intrexon Corporation
Inventors:
Sheela K. Chellappan, Robert E. Hormann, Inna Shulman
Abstract: The present invention is concerned with a process for preparing 5-(2{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to novel cysteinyl leukotriene (specifically LTD4) antagonists, mainly to quinolin, quinoxaline or benz[c]thiazole derivatives represented by the general formula (I), or the pharmaceutically acceptable salt thereof, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to cysteinyl leukotriene, in mammals, more specially in humans.
Type:
Grant
Filed:
July 26, 2012
Date of Patent:
August 11, 2015
Assignee:
Sun Pharma Advanced Research Company Ltd.
Inventors:
Rajendrasinh Rathod, Tushar Bhatt, Kiritkumar Joshi, Binaka Dole, Kadiyala V. S. N. Murty, Rajamannar Thennati
Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
Type:
Grant
Filed:
March 11, 2014
Date of Patent:
August 11, 2015
Assignee:
Dart NeuroScience (Cayman) Ltd.
Inventors:
Jillian Basinger, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi-Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
Abstract: The invention relates to a process for the preparation of a compound of formula (I) wherein R1 is C1C6 alkyl or benzyl by reacting a compound of formula (II) wherein R1 is as defined for formula (I) with 2-quinoline carboxaldehyde. The process is suitable for use on an industrial scale.
Type:
Grant
Filed:
December 14, 2012
Date of Patent:
August 11, 2015
Assignee:
Atopix Therapeutics Limited
Inventors:
Jacques Tonnel, Tony Pintus, Alain Burgos