Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.
Abstract: The invention relates to anhydrous crystalline orvepitant maleate (Form 1), pharmaceutical formulations comprising the same, its use in therapy and processes for preparing the same, wherein orvepitant is as shown in formula (I).
Type:
Grant
Filed:
April 9, 2009
Date of Patent:
November 13, 2012
Assignee:
Glaxo Group Limited
Inventors:
Stefania Beato, Franco Sartor, Ian Philip Steeples
Abstract: The present invention relates to a new and useful process for preparing N,N-substituted carbamoyl halides from secondary amines, carbon dioxide, trialkylsilyl chloride and a halogenating agent.
Abstract: A method of treatment of anxiety disorders which comprises administering to a host in need thereof an effective amount of a compound of formula (I):
Abstract: The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
Type:
Grant
Filed:
May 28, 2008
Date of Patent:
January 10, 2012
Assignee:
GlaxoSmithKline LLC
Inventors:
Kevin Kuntz, David Edward Uehling, Alex Gregory Waterson, Kyle Allen Emmitte, Kirk Stevens, John Brad Shotwell, Stephon Cornell Smith, Kristen E. Nailor, James M. Salovich, Brian John Wilson, Mui Cheung, Robert Anthony Mook, Erich W. Baum, Ganesh Moorthy
Abstract: The invention relates to 4-methylbenzenesulfonate salt of the compound of formula (I) in a crystalline form or a solvate thereof, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.
Type:
Grant
Filed:
August 4, 2009
Date of Patent:
January 10, 2012
Assignee:
GlaxoSmithKline LLC
Inventors:
Clare Louise Anderton, Ronnie Maxwell Lawrence, David Clapham
Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
Abstract: Novel pyrrolopyrimidines as shown in formula (I): and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
Type:
Grant
Filed:
August 6, 2008
Date of Patent:
July 19, 2011
Assignee:
GlaxoSmithKline LLC
Inventors:
Stanley Dawes Chamberlain, Felix Deanda, Jr., Roseanne Gerding, Masaichi Hasegawa, Kevin Kuntz, Huangshu Lei, Yasushi Miyazaki, Naohiko Nishigaki, Samarjit Patnaik, Aniko Redman, John Brad Shotwell, Kirk Stevens, Joseph Wilson, Bin Yang
Abstract: The present invention relates to novel indazole derivatives having pharmacological activity, processes for their preparation, compositions containing them and uses of these compounds in the treatment of estrogen receptor beta mediated diseases.
Type:
Grant
Filed:
March 5, 2008
Date of Patent:
June 14, 2011
Assignee:
Glaxo Group Limited
Inventors:
Christopher Norbert Johnson, David G Jones, Xi Liang, David Timothy MacPherson, Aaron B Miller, Antoinette Naylor, Steven James Stanway, Andrew Kenneth Takle, Giancarlo Trani
Abstract: The present invention relates to novel indole derivatives having pharmacological activity, processes for their preparation, compositions containing them and the use of these compounds in the treatment of estrogen receptor beta mediated diseases.
Type:
Grant
Filed:
February 17, 2009
Date of Patent:
June 7, 2011
Assignee:
Glaxo Group Limited
Inventors:
Christopher Norbert Johnson, David G. Jones, Xi Liang, David Timothy MacPherson, Aaron B Miller, Steven James Stanway, Andrew Kenneth Takle, Giancarlo Trani, Antoinette Wilson
Abstract: A pyridine derivative novel compounds of formula (I) or a pharmaceutically acceptable salt thereof where all variables are defined herein. The compounds are useful in the treatment of psychotic disorders.
Abstract: The truncated ErbB2 receptor (p95ErbB2) is shown to differ from the full-length ErbB2 receptor in its association with other ErbB receptors. The truncated receptor preferentially associated with ErbB3, whereas full length ErbB2 heterodimerizes with either EGFR or ErbB3. Consistent with p95ErbB2 heterodimerization with ErbB3, it is shown that heregulin (an ErbB3 ligand) stimulates p95ErbB2 phosphorylation in breast cancer cell lines. Described herein are methods of identifying patients suitable for treatment with a p95ErbB2 inhibitor, and methods of treating such patients.
Abstract: The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
Type:
Grant
Filed:
December 6, 2005
Date of Patent:
October 12, 2010
Assignee:
GlaxoSmithKline LLC
Inventors:
David Edward Uehling, Kirk Lawrence Stevens, Scott Howard Dickerson, Alex Gregory Waterson, Philip Anthony Harris, Douglas McCord Sammond, Robert Dale Hubbard, Holly Kathleen Emerson, Joseph W. Wilson
Abstract: The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
Type:
Grant
Filed:
December 4, 2006
Date of Patent:
October 5, 2010
Assignee:
GlaxoSmithKline LLC
Inventors:
David Edward Uehling, Robert Dale Hubbard, Alex Gregory Waterson, Kimberly Petrov, Neil Bifulco, Jr., Joseph Wendell Wilson, Jennifer Gabriel Badiang, Mul Cheung, Mariko Yamabe
Abstract: The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.
Type:
Grant
Filed:
June 8, 2009
Date of Patent:
September 21, 2010
Assignee:
GlaxoSmithKline LLC
Inventors:
Jing Fang, Dennis Heyer, Aaron Bayne Miller, Frank Navas, III, Terrence Lee Smalley, Jr., William J. Zuercher, Subba Reddy Katamreddy
Abstract: The use of various biomarkers to assess a subject's suitability for treatment with a EGFR/ErbB2 kinase inhibitor for a solid tumor are described. The biomarkers include TGFalpha, pS6, IGF-1R and levels of apoptosis occurring in tumor tissue.
Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.
Type:
Grant
Filed:
May 24, 2006
Date of Patent:
May 25, 2010
Assignee:
GlaxoSmithKline LLC
Inventors:
Jing Fang, Dennis Heyer, Subba Reddy Katamreddy, Kenneth William Batchelor, Richard Dana Caldwell
Abstract: There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein all variables are defined herein. Also provided are pharmaceutical compositions containing the same and methods for their use in therapy.
Abstract: The present invention relates to piperidine derivatives of formula (I) specifically 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof, useful in the treatment of conditions mediated by tachykinins.
Type:
Grant
Filed:
December 11, 2006
Date of Patent:
January 26, 2010
Assignee:
Glaxo Group Limited
Inventors:
Giuseppe Alvaro, Romano Di Fabio, Maria Elvira Tranquillini, Simone Spada
Abstract: The present invention relates to cycloalkylidene compounds with a variety of therapeutic uses, more particularly novel naphthalene compounds that are particularly useful for selective estrogen receptor modulation.
Type:
Grant
Filed:
June 21, 2005
Date of Patent:
January 19, 2010
Assignee:
Glaxo Smith Kline LLC
Inventors:
Dennis Heyer, Jing Fang, Frank Navas, III, Subba Reddy Katamreddy, Jennifer Poole Peckham, Philip Stewart Turnbull, Aaron Bayne Miller, Adwoa Akwabi-Ameyaw