Abstract: The present invention relates to biaryl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
Type:
Grant
Filed:
October 6, 2016
Date of Patent:
July 30, 2019
Assignees:
GlaxoSmithKline Intellectual Property Development Limited, Astex Therapeutics Limited
Inventors:
James Callahan, Jeffrey K. Kerns, Peng Li, Tindy Li, Brent W. McCleland, Hong Nie, Joseph E. Pero, Thomas Glanmor Davies, Maria Grazia Carr, Charlotte Mary Griffiths-Jones, Thomas Daniel Heightman, David Norton, Marinus Leendert Verdonk, Alison Jo-Anne Woolford, Hendrika Maria Gerarda Willems
Abstract: A compound of Formula (I) wherein Y1, Y2, X1, X2, R1, R2, R3, R4, R5, R6, R8, and R9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.
Type:
Grant
Filed:
May 15, 2018
Date of Patent:
July 30, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.
Type:
Grant
Filed:
August 15, 2016
Date of Patent:
July 30, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Haifeng Cui, Alan Hennessy, Qi Jin, Timothy James Miles, Stephen Frederick Moss, Neil David Pearson
Abstract: The present invention relates to an ICOS binding protein or antigen binding portion thereof that is an agonist to human ICOS and does not induce complement, ADCC, or CDC when placed in contact with a T cell in vivo and methods of treating cancer, infectious disease and/or sepsis with said ICOS binding protein or antigen binding portion thereof. Further the ICOS binding proteins or antigen binding portions thereof of the present invention are capable of activating a T cell when placed in contact with said T cell; stimulating T cell proliferation when placed in contact with said T cell and/or inducing cytokine production when placed in contact with said T cell. The present invention relates to ICOS binding proteins or antigen binding portions thereof comprising one or more of: SEQ ID NO:1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:4; SEQ ID NO:5; and/or SEQ ID NO:6.
Type:
Grant
Filed:
August 25, 2016
Date of Patent:
July 16, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Yao-Bin Liu, Patrick Mayes, Radha Shah Parmar
Abstract: The present invention relates to arylcyclohexyl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
Type:
Grant
Filed:
October 6, 2016
Date of Patent:
July 16, 2019
Assignees:
GlaxoSmithKline Intellectual Property Development Limited, Astex Therapeutics Limited
Inventors:
James Callahan, Jeffrey K. Kerns, Tindy Li, Brent W. McCleland, Hong Nie, Joseph E. Pero, Thomas Glanmor Davies, Charlotte Mary Griffiths-Jones, Thomas Daniel Heightman, Steven Howard, David Norton, Marinus Leendert Verdonk, Alison Jo-Anne Woolford
Abstract: An oral care compositon is described for use in the treatment or alleviation of the symptoms of dry mouth comprising polyvinyl pyrrolidone (PVP) or a derivative thereof, an anionic mucoadhesive polymer and an orally acceptable carrier or excipient.
Abstract: This application discloses antigen binding proteins that bind Lymphocyte Activation Gene 3 (LAG-3), and more particularly to antigen binding proteins that cause depletion of LAG-3+ activated T cells.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
July 9, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Paul Andrew Hamblin, Alan Peter Lewis, Thomas Matthew Webb
Abstract: A compound of formula (I): being 4-(3-Fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl) ethyl) pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy) phenyl) butanoic acid, or a salt thereof.
Type:
Grant
Filed:
March 15, 2018
Date of Patent:
July 9, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, John Martin Pritchard, Joanna Mary Redmond
Abstract: The invention relates to an immunization regimen whereby an infant is protected against respiratory syncytial virus (RSV) through administration of a first anti-RSV immune response inducing composition to his or her mother during pregnancy, followed by administration of a second anti-RSV immune response inducing composition to the infant after birth.
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 29, 2018
Date of Patent:
July 2, 2019
Assignee:
GlaxoSmithKline LLC
Inventors:
Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
Abstract: The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
Type:
Grant
Filed:
September 13, 2018
Date of Patent:
July 2, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
Type:
Grant
Filed:
April 20, 2016
Date of Patent:
July 2, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
John David Harling, Ian Edward David Smith
Abstract: The present invention relates to the compound ((2R,2?R)-bis(((tetrahydro-2H-pyran-4-carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
Type:
Grant
Filed:
October 25, 2016
Date of Patent:
June 25, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: Meningococcal protein NMB 1870 has been described in the prior art. The inventors have found that NMB 1870 is an effective antigen for eliciting anti-meningococcal antibody responses, and that it is expressed across all meningococcal serogroups. Forty-two different NMB 1870 sequences have been identified, and these group into three variants. Serum raised against a given variant is bactericidal within the same variant group, but is not active against strains which express one of the other two variants i.e. there is intra-variant cross-protection, but not inter-variant cross-protection. For maximum cross-strain efficacy, therefore, the invention uses mixture comprising different variants of NMB 1870.
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:
January 9, 2018
Date of Patent:
June 11, 2019
Assignee:
GlaxoSmithKline LLC
Inventors:
Rosanna Tedesco, Junya Qu, Robert Sanchez, Ralph A. Rivero
Abstract: Provided herein are crystalline beta-D-nicotinamide riboside chloride compositions and methods of preparation and use thereof. Also provided are related pharmaceutical compositions and methods of use thereof. The crystalline beta-D-nicotinamide riboside chloride compositions may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, or for increasing insulin sensitivity in a subject.
Abstract: The present Invention relates to pharmaceutical compositions useful in the treatment or prevention or cure of viral infections, such as HCV infections, and diseases associated with such infections.
Abstract: Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.
Type:
Grant
Filed:
October 24, 2017
Date of Patent:
June 4, 2019
Assignees:
GlaxoSmithKline Intellectual Property (No. 2) Limited, Anacor Pharmaceuticals, Inc.
Inventors:
Michael Richard Kevin Alley, Vincent Hernandez, Jacob J. Plattner, Xianfeng Li, David Barros-Aguirre, Ilaria Giordano
Abstract: The present invention encompasses a novel S. aureus bioconjugate vaccine. More generally, the invention is directed to Gram-positive and other bioconjugate vaccines containing a protein carrier, at least one polysaccharide such as a capsular Gram-positive polysaccharide, and, optionally, an adjuvant or pharmaceutically acceptable carrier. The instant invention also includes methods of producing Gram-positive and other bioconjugate vaccines. An N-glycosylated protein is also provided that contains one or more polysaccharides such as Gram-positive polysaccharides. The invention is additionally directed to engineered prokaryotic organisms comprising nucleotide sequences encoding a glycosyltransferase of a first prokaryotic organism and a glycosyltransferase of a second prokaryotic organism. The invention further includes plasmids and prokaryotic cells transformed with plasmids encoding polysaccharides and enzymes which produce an N-glycosylated protein and/or bioconjugate vaccine.
Type:
Grant
Filed:
January 25, 2017
Date of Patent:
June 4, 2019
Assignee:
GlaxoSmithKline Biologicals SA
Inventors:
Michael Wacker, Michael Kowarik, Michael Wetter