Abstract: Compounds of formula (I) and salts thereof are provided: wherein R4, R5, R6, Q, A, and Y are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
January 1, 2013
Assignee:
Glaxo Group Limited
Inventors:
David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Paul Adrian Wyman
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Type:
Grant
Filed:
April 29, 2009
Date of Patent:
December 11, 2012
Assignee:
Glaxo Group Limited
Inventors:
Thomas Daniel Heightman, John Skidmore, Hailong Wang, Colin David Eldred, Jag Paul Heer
Abstract: The present invention provides compounds of formula (I) or salts thereof: having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated by S1P1 receptors.
Type:
Grant
Filed:
April 17, 2008
Date of Patent:
December 4, 2012
Assignee:
Glaxo Group Limited
Inventors:
Mahmood Ahmed, Gerard Martin Paul Giblin, James Myatt, David Norton, Dean Andrew Rivers
Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
October 30, 2012
Assignee:
Glaxo Group Limited
Inventors:
David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
Abstract: Compounds of formula (I) and salts are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 16, 2012
Assignee:
Glaxo Group Limited
Inventors:
Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
Abstract: Compounds of formula (I) and salts are provided: wherein R5 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R6 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 16, 2012
Assignee:
Glaxo Group Limited
Inventors:
Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
Abstract: Compounds of formula (I) and salts are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6alkoxy, and C1-6alkoxy substituted with one or more fluorine atoms; and R6 is selected from halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6alkoxy and C1-6alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C1-6alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 9, 2012
Assignee:
Glaxo Group Limited
Inventors:
Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
October 2, 2012
Assignee:
Glaxo Group Limited
Inventors:
David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Type:
Grant
Filed:
December 19, 2008
Date of Patent:
July 17, 2012
Assignee:
Glaxo Group Limited
Inventors:
Emmanuel Hubert Demont, Jag Paul Heer, John Skidmore, Ian David Wall, Jason Witherington, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Type:
Grant
Filed:
June 18, 2009
Date of Patent:
July 10, 2012
Assignee:
Glaxo Group Limited
Inventors:
Jose Luis Castro Pineiro, Xichen Lin, Qian Liu, Kevin Meng, Feng Ren, David R Vesey, Baowei Zhao
Abstract: The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to (Cis)-N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt thereof, and N-{[4-cyano-2-(trifluoromethyl)phenyl]methyl}-3-{[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino}cyclohexanecarboxamide; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 9, 2010
Date of Patent:
July 3, 2012
Assignee:
GlaxoSmithKline LLC.
Inventors:
Yun Ding, Reema K. Thalji, Joseph P. Marino, Jr.
Abstract: The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R4, R5, R6, A, B, Y, Z, n, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Type:
Grant
Filed:
October 10, 2008
Date of Patent:
May 8, 2012
Assignee:
GlaxoSmithKline, LLC
Inventors:
Yun Ding, Reema K. Thalji, Joseph P. Marino, Jr.
Abstract: The invention relates to compounds of formula (I) wherein one of R5 and R6 is hydrogen or R2 and the other is (a) pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the S1P1 receptor.
Type:
Grant
Filed:
December 19, 2007
Date of Patent:
January 24, 2012
Assignee:
Glaxo Group Limited
Inventors:
Mahmood Ahmed, James Myatt, David Norton, Dean Andrew Rivers
Abstract: The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R5a, R6a A, B, Y, x, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Type:
Grant
Filed:
October 10, 2008
Date of Patent:
August 30, 2011
Assignee:
Glaxosmithkline, LLC
Inventors:
Yun Ding, Reema K. Thalji, Joseph P. Marino, Jr.
Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or S1P receptors.
Type:
Grant
Filed:
August 1, 2007
Date of Patent:
July 20, 2010
Assignee:
Praecis Pharmaceuticals
Inventors:
Ghotas Evindar, Hongfeng Deng, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang
Abstract: The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
Type:
Grant
Filed:
July 20, 2007
Date of Patent:
July 6, 2010
Assignee:
GlaxoSmithKline LLC
Inventors:
Krista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
Type:
Grant
Filed:
April 25, 2006
Date of Patent:
July 21, 2009
Assignee:
SmithKline Beecham Corporation
Inventors:
Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita