Abstract: The invention relates to antibodies which treat diseases in which human IL-8, Gro-alpha, Gro-beta, Gro-gamma, GCP-2, and/or ENA-78 are implicated.
Type:
Grant
Filed:
May 1, 2013
Date of Patent:
March 28, 2017
Assignee:
GlaxoSmithKline LLC
Inventors:
Alexander Harrison Taylor, John Richard White, Yu Xu
Abstract: A continuous dosage form coating apparatus uses vibrational impulses to maintain a dosage forms in a fluid state to expose them to a coating material atomized by spraying.
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: Provided herein are novel sirtuin-modulating compounds 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:
October 29, 2010
Date of Patent:
January 31, 2017
Assignee:
GLAXOSMITHKLINE LLC
Inventors:
Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
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: 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 1 to 4; 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 is based on the finding that enrichment of D3-creatinine in a urine sample following oral administration of a single defined dose of D3-creatine can be used to calculate total-body creatine pool size and total body skeletal muscle mass in a subject. The invention further encompasses methods for detecting creatinine and D3-creatinine in a single sample. The methods of the invention find use, inter alia, in diagnosing disorders related to skeletal muscle mass, and in screening potential therapeutic agents to determine their effects on muscle mass.
Type:
Application
Filed:
April 13, 2016
Publication date:
August 4, 2016
Applicants:
GLAXOSMITHKLINE LLC, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
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: A process for the identification of compounds with a molecular weight in the range 100 to 750 which inhibit the binding of the first and/or second bromodomains of human BRD-2 to 4 to acetylated lysine residues of their physiological partner proteins which comprises selecting those compounds which are able to: a) form a hydrogen bonding interaction in which the compound accepts a hydrogen bond from the sidechain NH2 group of the asparagine residue found at: BRD-2 BRD-2 BRD-3 BRD-4 BRD-4 BD1 BD2 BD1 BRD-3 BD2 BD1 BD2 ASN156 ASN429 ASN116 ASN391 ASN140 ASN433 or b) accept a water-mediated hydrogen bond in which the compound accepts a hydrogen bond from a water that is itself hydrogen-bonded to the sidechain hydroxyl of the tyrosine residue found at BRD-2 BRD-3 BRD-4 BD1 BRD-2 BD2 BD1 BRD-3 BD2 BD1 BRD-4 BD2 TYR113 TYR386 TYR73 TYR348 TYR97 TYR390 and c) which are also able to form a Van der Waals interaction with a lipophilic
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