Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.
Abstract: Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
Type:
Grant
Filed:
November 15, 2012
Date of Patent:
July 23, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Christopher Oalmann, Jeremy S Disch, Pui Yee Ng, Robert B Perni
Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
Type:
Grant
Filed:
November 15, 2012
Date of Patent:
July 23, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Pingyun Chen, Ricky Couch, Maosheng Duan, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Beth Adams Norton, Matthew Tallant
Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
Abstract: The present invention relates to substituted triazole compounds of the formula (I): and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.
Type:
Grant
Filed:
November 7, 2008
Date of Patent:
July 16, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Anne Marie Jeanne Bouillot, Alain Laroze, Lionel Trottet
Abstract: A novel combination comprising the VEGFR inhibitor 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, with a B-Raf inhibitor, particularly N-(3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl)-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of VEGFR and/or B-Raf is beneficial.
Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.
Type:
Grant
Filed:
May 6, 2010
Date of Patent:
July 2, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Connie L. Erickson-Miller, Michael Arning
Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
Abstract: This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazole boronic acid compounds for treating cancer.
Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
Type:
Application
Filed:
February 6, 2013
Publication date:
June 13, 2013
Applicant:
GlaxoSmithKline LLC
Inventors:
Ivan Leo PINTO, Shahzad Sharooq Rahman, Neville Hubert Nicholson
Abstract: This invention provides, among other things, polymorphs of the hydrochloride salt of (S)-3-aminomethyl-7-(3-hydroxy-propoxy)-3H-benzo[c][1,2]oxaborol-1-ol.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
June 11, 2013
Assignees:
GlaxoSmithKline LLC, Anacor Pharmaceuticals, Inc.
Inventors:
Conrad Wheeler, Dan Todd, Pingyun Chen, Beth A. Norton
Abstract: A pharmaceutical composition such as a swallow tablet or capsule formulation is described comprising paracetamol, calcium carbonate, at least one binding agent and at least one disintegrating agent in the form of a granulate, optionally combined with one or more pharmaceutically acceptable extragranular components.
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.
Type:
Application
Filed:
January 31, 2013
Publication date:
June 6, 2013
Applicant:
GlaxoSmithKline LLC
Inventors:
George Adjabeng, Jerry Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
Abstract: Invented is a method of treating degenerative diseases/injuries, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.
Abstract: The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
Type:
Grant
Filed:
July 24, 2009
Date of Patent:
May 28, 2013
Assignee:
GlaxoSmithKline, LLC
Inventors:
Michael Jonathan Bury, Mui Cheung, Hilary Schenck Eidam, Ryan Michael Fox, Krista Goodman, Eric Steven Manas
Abstract: A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolineamines.
Type:
Grant
Filed:
November 11, 2011
Date of Patent:
May 21, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Karen Elizabeth Lackey, Robert J. Mullin, Neil Spector, Edgar Raymond Wood, III, Wenle Xia
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.
Type:
Grant
Filed:
October 3, 2011
Date of Patent:
May 7, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Junya Qu, Ralph Rivero, Robert Sanchez, Rosanna Tedesco
Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
Type:
Grant
Filed:
February 7, 2008
Date of Patent:
April 2, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding