Abstract: Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.
Type:
Grant
Filed:
November 3, 2010
Date of Patent:
November 12, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Emmanuel Hubert Demont, Romain Luc Marie Gosmini
Abstract: Disclosed are novel pharmaceutical compositions containing N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.
Type:
Grant
Filed:
December 20, 2011
Date of Patent:
November 12, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Douglas J. DeMarini, Francisco Henriquez, Ngocdiep T. Le, Lihong Wang
Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
Type:
Grant
Filed:
August 7, 2009
Date of Patent:
November 5, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Sebastien Andre Campos, Diane Mary Coe, Naimisha Trivedi
Abstract: The present invention relates to compounds of formula (I): wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.
Type:
Grant
Filed:
February 8, 2011
Date of Patent:
November 5, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Helene Bazin-Lee, Diane Mary Coe, David A. Johnson, Charlotte Jane Mitchell
Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
Type:
Grant
Filed:
February 26, 2010
Date of Patent:
November 5, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Nicola Mary Aston, Paul Bamborough, Ann Louise Walker
Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the ā(CH2)nā moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
Type:
Grant
Filed:
August 7, 2009
Date of Patent:
October 22, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Helene Bazin-Lee, Diane Mary Coe, Linos Lazarides, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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.
Type:
Grant
Filed:
November 2, 2012
Date of Patent:
October 15, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
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:
March 13, 2013
Date of Patent:
September 24, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Junya Qu, Ralph A. Rivero, Robert Sanchez, Rosanna Tedesco
Abstract: The present invention provides methods of inhibiting human myeloid leukemia cell growth and proliferation by administering a thrombopoietin receptor agonist (TpoRA), a derivative, or variant thereof, to an individual with AML.
Type:
Grant
Filed:
October 8, 2008
Date of Patent:
September 10, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Alan Gewirtz, Anna Kalota, Connie L. Erickson-Miller
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:
Application
Filed:
February 22, 2013
Publication date:
September 5, 2013
Applicant:
GlaxoSmithKline LLC
Inventors:
Mark A. SEEFELD, Meagan B. Rouse, Dirk A. Heerding, Dennis S. Yamashita, Kenneth C. McMulty
Abstract: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L? are suitable leaving groups, with a compound of formula (III) UNH2??(III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L?.
Type:
Grant
Filed:
January 22, 2010
Date of Patent:
August 20, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
Abstract: The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form.
Abstract: The invention is directed to novel indazole carboxamide derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 and Z 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.
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