Patents Assigned to Glaxosmithkline Intellectual Property Development
  • Patent number: 9879021
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: January 30, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Mui Cheung, Michael P. Demartino, Hilary Schenck Eidam, Huiping Amy Guan, Donghui Qin, Chengde Wu, Zhen Gong, Haiying Yang, Haiyu Yu, Zhiliu Zhang
  • Publication number: 20170349577
    Abstract: Compound of formula (I) wherein: R1 is heteroaryl either unsubstituted or substituted by methyl, ethyl, halo or ?O; and R2 is H, methyl or ethyl; and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
    Type: Application
    Filed: December 17, 2015
    Publication date: December 7, 2017
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Anne Marie Jeanne BOUILLOT, Alexis DENIS, Ann Louise WALKER, John LIDDLE
  • Publication number: 20170340617
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: September 9, 2015
    Publication date: November 30, 2017
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Michael P. DEMARTINO, Huiping Amy GUAN
  • Patent number: 9815841
    Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: November 14, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Xiao Ding, Qian Liu, Kai Long, Yingxia Sang, Luigi Piero Stasi, Zehong Wan, Qiongfeng Xu, Colin Michael Edge
  • Patent number: 9809558
    Abstract: Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.
    Type: Grant
    Filed: October 1, 2014
    Date of Patent: November 7, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Peter Kumpalume, Oliver Schon, Christine Patricia Donahue, Ghotas Evindar, David I. Israel, David Paolella, Letian Kuai, Ninad V. Prabhu
  • Patent number: 9783546
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: October 10, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang
  • Publication number: 20170283404
    Abstract: Disclosed are novel crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.
    Type: Application
    Filed: September 4, 2015
    Publication date: October 5, 2017
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Mui CHEUNG, William M. CLARK, Hilary Schenck EIDAM, Kimberly Anne LAMEY, James V. THOMAS
  • Patent number: 9771424
    Abstract: The present invention relates to an ICOS binding protein, or antigen binding portion thereof that is an agonist 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: January 26, 2016
    Date of Patent: September 26, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Yao-Bin Liu, Patrick Mayes, Radha Shah Parmar
  • Patent number: 9763965
    Abstract: The present invention relates to aggregate particles comprising nanoparticulate drug particles. In particular, the present invention is directed to aggregate particles comprising nanoparticulate drug particles of umeclidinium bromide and optionally vilanterol trifenatate and/or fluticasone furoate. Aggregate particles of the present invention may further comprise nanoparticulate excipient particles and one or more binders. The invention also relates to powder compositions suitable for inhalation that comprise said aggregate particles, processes of producing said aggregate particles, and use of said powder compositions in the treatment of respiratory diseases, such as asthma and COPD.
    Type: Grant
    Filed: April 11, 2013
    Date of Patent: September 19, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Michiel Mary Van Oort, John N. Hong
  • Patent number: 9737505
    Abstract: The compound (2R,2?R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate) possesses physicochemical properties suitable for pharmaceutical development and is capable of generating (R)-1-[6-[(R)-2-carboxy-pyrrolidin-1-yl]-6-oxo-hexanoyl]pyrrolidine-2-carboxylic acid (CPHPC) in quantities capable of depleting serum amyloid P component (SAP) efficiently following oral administration, making it useful in the treatment of amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: August 22, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
  • Patent number: 9738718
    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: December 21, 2016
    Date of Patent: August 22, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Yao-Bin Liu, Patrick Mayes, Radha Shah Parmar
  • Publication number: 20170224685
    Abstract: Described herein are methods of treating cancer using one or more PRMT5 inhibitors, for example using one or more compounds of Formulae (1-5) or (A-F), pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions thereof. Described herein are methods of treating cancer using one or more PRMT5 inhibitors, for example using one or more compounds of Formulae (1-5) or (A-F), pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions thereof.
    Type: Application
    Filed: August 4, 2015
    Publication date: August 10, 2017
    Applicants: Epizyme, Inc., Glaxosmithkline Intellectual Property Development Limited
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael Munchhof, Lei Jin, Elayne Penebre, Olena I. Barbash
  • Patent number: 9725407
    Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is an ester group; R2 is the side chain of a natural or non-natural alpha-amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: August 8, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
  • Patent number: 9718848
    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: December 5, 2016
    Date of Patent: August 1, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Jerry Adams, Kevin J. Duffy, Yiqian Lian
  • Patent number: 9708330
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: July 18, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Zehong Wan, Yingxia Sang, Qing Zhang
  • Publication number: 20170197978
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: May 26, 2015
    Publication date: July 13, 2017
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Jing DENG, Hui LEI, Xin MA, Xichen LIN
  • Patent number: 9701668
    Abstract: The present invention relates to the compound (2R,2?R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate) of formula (I), 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: April 27, 2015
    Date of Patent: July 11, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
  • Patent number: 9695161
    Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: July 4, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventor: Gren Wang
  • Publication number: 20170166894
    Abstract: Aptamers for topical delivery and methods for topical use of aptamers are described. Aptamers that bind to interleukin (IL)-23 (IL-23 aptamers) and methods of using such aptamers are also described.
    Type: Application
    Filed: March 17, 2015
    Publication date: June 15, 2017
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Kellie Marie DEMOCK, Christine Patricia DONAHUE, Robert L. HALE, Jon LENN, Jennifer NELSON, P. Shannon PENDERGRAST
  • Patent number: 9650364
    Abstract: Disclosed are compounds that are inhibitors of RIP2 kinase and methods of making and using the same.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: May 16, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limted
    Inventors: Linda N. Casillas, Adam Kenneth Charnley, Xiaoyang Dong, Pamela A. Haile, Michael P. Demartino, John F. Mehlmann