Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Type:
Grant
Filed:
May 15, 2013
Date of Patent:
February 7, 2017
Assignee:
GlaxoSmithKline LLC
Inventors:
Joelle Lorraine Burgess, Steven David Knight
Abstract: Compounds of formula (I) and salts thereof: wherein R1 is n-C1-6alkyl or C1-2alkoxyC1-2alkyl-, R2 is halo, OH or C1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, 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, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
Abstract: The present invention relates to Compounds of formula (I) and salts thereof: wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 0 to 3; 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, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
Abstract: Compounds of formula (I) and salts thereof: wherein R1 is n-C4-6alkyl or C1-2alkoxyC1-2alkyl-; R2 is hydrogen or methyl; each R3 is hydroxy, halo or n-C1-3alkyl; m is an integer having a value of 2 to 4; n is an integer having a value of 0 to 3; and p is an integer having a value of 0 to 2, 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, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.
Type:
Grant
Filed:
October 20, 2015
Date of Patent:
September 20, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Jerry Leroy Adams, Thomas H. Faitg, Neil W. Johnson, Hong Lin, Xin Peng
Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
Type:
Grant
Filed:
July 9, 2015
Date of Patent:
August 2, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
James Brackley, III, Joelle Lorraine Burgess, Seth Wilson Grant, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Type:
Grant
Filed:
December 12, 2013
Date of Patent:
July 5, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Carla A. Donatelli
Abstract: Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2?- and 3?-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.
Type:
Grant
Filed:
June 6, 2012
Date of Patent:
June 28, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Karsten Koppetsch, Bruce G. Szczepankiewicz, Robert B Perni
Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; 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:
October 13, 2011
Date of Patent:
May 24, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
Type:
Grant
Filed:
November 4, 2013
Date of Patent:
May 17, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Ghergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.
Type:
Grant
Filed:
December 14, 2012
Date of Patent:
May 17, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Nianhe Han, Brian Alvin Johns, Jun Tang
Abstract: Aspects of the present invention are directed to a metered dose container that is transit proof. A container of the present invention may comprise a body having a vertical axis; a cap movable along the vertical axis of the body; a removable ring coupled to and between the moveable cap and the body, and a barrier, inside the body and coupled to the moveable cap. The barrier may define a loading chamber and separate the body into a storage chamber and a dispensing chamber. The barrier is adapted to be movable along the vertical axis of the body to form a transit position and a dispensing position.
Type:
Grant
Filed:
August 8, 2013
Date of Patent:
March 1, 2016
Assignee:
GlaxoSmithKline, LLC
Inventors:
Ramesh Ramachandran, Amit Sabharwal, Sukhdev Singh Saini
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:
Grant
Filed:
April 6, 2011
Date of Patent:
January 26, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Jose J. Conde, John Anthony Kowalski, Matthew Allen Zajac
Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; 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:
May 16, 2014
Date of Patent:
January 12, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
Abstract: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, exce