Abstract: This invention relates to novel compounds of formula (I): and derivatives thereof useful 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?.
Type:
Grant
Filed:
May 20, 2010
Date of Patent:
April 2, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Hong Lin, Juan I. Luengo, Ralph A. Rivero, Mark James Schulz, Ren Xie, Jin Zeng
Abstract: The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
Type:
Grant
Filed:
March 18, 2011
Date of Patent:
April 2, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Barry Morgan, Stephen Hale, Christopher C. Arico-Muendel, Matthew Clark, Richard Wagner, David I. Israel, Malcolm L. Gefter, Dennis Benjamin, Nils Jakob Vest Hansen, Malcolm J. Kavarana, Steffan Phillip Creaser, George J. Franklin, Paolo A. Centrella, Raksha A. Acharya
Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating 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 by the administration of quinoline derivatives.
Type:
Grant
Filed:
May 16, 2008
Date of Patent:
March 26, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
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.
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:
Grant
Filed:
September 2, 2009
Date of Patent:
March 12, 2013
Assignee:
Glaxosmithkline LLC
Inventors:
Ivan Leo Pinto, Shahzad Sharooq Rahman, Neville Hubert Nicholson
Abstract: Deuterated forms of N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide and pharmaceutical compositions containing the same.
Type:
Grant
Filed:
July 26, 2012
Date of Patent:
March 5, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Jerry Leroy Adams, Dashyant Dhanak, Dirk A. Heerding, Calvin O. Manning
Abstract: Pyrrolopyrimidones compounds of the formula (I), salts thereof, and pharmaceutical compositions containing them are disclosed herein, as well as methods for their use in medicine, for instance as activators of AMPK.
Type:
Application
Filed:
May 3, 2011
Publication date:
February 28, 2013
Applicant:
GlaxoSmithKline LLC
Inventors:
Olivier Mirguet, Anne Marie Jeanne Bouillot
Abstract: Generally the method involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient.
Type:
Grant
Filed:
August 3, 2011
Date of Patent:
February 26, 2013
Assignee:
Glaxosmithkline, LLC
Inventors:
Richard L. Kirsh, Steven D. Finkelmeier, Robert Glinecke, Luigi Martini
Abstract: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. 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 PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Type:
Grant
Filed:
August 12, 2009
Date of Patent:
February 26, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Francis Louis Atkinson, Jeffrey Michael Axten, Maria Cichy-Knight, Michael Lee Moore, Vipulkumar Kantibhai Patel, Xinrong Tian, Christopher Roland Wellaway, Allison K. Dunn
Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). 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 IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Abstract: The present invention is a process comprising contacting a compound of formula 6: or a pharmaceutically acceptable salt thereof; with a deprotecting reagent to form a compound of formula A: or a pharmaceutically acceptable salt thereof; where R is H or OR1; R1 and each R1? are protecting groups; R1? is H or OH, and n is 0, 1, 2, 3, 4, or 5.
Type:
Application
Filed:
April 6, 2011
Publication date:
February 7, 2013
Applicant:
GLAXOSMITHKLINE LLC
Inventors:
Jose J. Conde, John Anthony Kowalski, Matthew Allen Zajac
Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
Type:
Application
Filed:
July 12, 2012
Publication date:
January 17, 2013
Applicant:
GLAXOSMITHKLINE LLC
Inventors:
Martha Alicia De La Rosa, Brian Alvin Johns, Emile Johann Velthuisen, Jason Weatherhead, Vicente Samano
Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). 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 IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Type:
Grant
Filed:
October 14, 2011
Date of Patent:
January 15, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Jianghe Deng, Jeffrey K. Kerns, Qi Jin, Guoliang Lin, Xichen Lin, Michael Lindenmuth, Christopher Neipp, Hong Nie, Sonia M Thomas, Katherine L. Widdowson
Abstract: Invented are novel pyrazole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
Abstract: The present invention relates to methods and pharmaceutical compositions relating to administering hypoglycemic agents and/or GLP-1 agonists wherein the mean maximum plasma concentration (Cmax) and/or Area Under the Curve (AUC) values of the hypoglycemic agent are increased and/or sustained.
Type:
Grant
Filed:
September 12, 2007
Date of Patent:
December 25, 2012
Assignee:
Glaxosmithkline LLC
Inventors:
Mark A. Bush, Jessica E. Matthews, Susan E. Walker