Abstract: This invention relates to methods for the preparation of a compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1).
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:
December 19, 2017
Date of Patent:
November 6, 2018
Assignee:
GlaxoSmithKline LLC
Inventors:
Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
Abstract: Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.
Type:
Grant
Filed:
July 19, 2012
Date of Patent:
October 30, 2018
Assignee:
GlaxoSmithKline LLC
Inventors:
Claire Louise Ambery, Christopher David Edwards
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 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:
June 20, 2016
Date of Patent:
July 31, 2018
Assignee:
GlaxoSmithKline, LLC
Inventors:
Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
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: This invention relates to novel substituted benzamide 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 15, 2016
Date of Patent:
May 1, 2018
Assignee:
GLAXOSMITHKLINE LLC
Inventors:
Joelle Lorraine Burgess, Steven David Knight
Abstract: Provided herein are novel substituted bicyclic aza-heterocycle 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 19, 2012
Date of Patent:
May 1, 2018
Assignee:
GLAXOSMITHKLINE LLC
Inventors:
Rebecca L. Casaubon, Radha Narayan, Christopher Oalmann, Chi B. Vu
Abstract: The present invention relates to genetically modified host cells, in particular yeast cells, comprising at least one isolated polynucleotide encoding a Killer Expression protease (Kex2p) or a fragment and/or variant thereof which has at least one Kex2p functional activity and at least one isolated polynucleotide encoding a Protein Disulfide-Isomerase (Pdi1) or a fragment and/or variant thereof which has at least one Pdi functional activity.
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: Aspects of the present invention relate to methods of making an external nasal dilator amenable to continuous and automated manufacture. For example, in one embodiment of the method, a roll of a three-layered material is used as the starting material, the three layers consisting substantially and respectively of (1) a resilient sheet, (2) an adhesive-protecting sheet, and (3) an adhesive layer between the resilient sheet and the adhesive-protecting sheet. A series of dies are used to cut the three-layered material into the appropriate shape and (when necessary) to impress grooves in the resilient sheet.
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:
April 21, 2016
Date of Patent:
January 30, 2018
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 important intermediates in the preparation of a compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1).
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:
September 3, 2015
Date of Patent:
January 23, 2018
Assignee:
GLAXOSMITHKLINE LLC
Inventors:
Junya Qu, Ralph A. Rivero, Robert Sanchez, Rosanna Tedesco