Patents Assigned to Glaxosmithkline Intellectual Property Development
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Patent number: 9879021Abstract: 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 cType: GrantFiled: September 10, 2015Date of Patent: January 30, 2018Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Mui Cheung, Michael P. Demartino, Hilary Schenck Eidam, Huiping Amy Guan, Donghui Qin, Chengde Wu, Zhen Gong, Haiying Yang, Haiyu Yu, Zhiliu Zhang
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Publication number: 20170349577Abstract: 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: ApplicationFiled: December 17, 2015Publication date: December 7, 2017Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Anne Marie Jeanne BOUILLOT, Alexis DENIS, Ann Louise WALKER, John LIDDLE
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Publication number: 20170340617Abstract: 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 cType: ApplicationFiled: September 9, 2015Publication date: November 30, 2017Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Michael P. DEMARTINO, Huiping Amy GUAN
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Patent number: 9815841Abstract: 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: GrantFiled: January 28, 2015Date of Patent: November 14, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Xiao Ding, Qian Liu, Kai Long, Yingxia Sang, Luigi Piero Stasi, Zehong Wan, Qiongfeng Xu, Colin Michael Edge
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Patent number: 9809558Abstract: 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: GrantFiled: October 1, 2014Date of Patent: November 7, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Peter Kumpalume, Oliver Schon, Christine Patricia Donahue, Ghotas Evindar, David I. Israel, David Paolella, Letian Kuai, Ninad V. Prabhu
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Patent number: 9783546Abstract: 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: GrantFiled: July 21, 2015Date of Patent: October 10, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Zehong Wan, Xiaomin Zhang, Jian Wang
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Publication number: 20170283404Abstract: 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: ApplicationFiled: September 4, 2015Publication date: October 5, 2017Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Mui CHEUNG, William M. CLARK, Hilary Schenck EIDAM, Kimberly Anne LAMEY, James V. THOMAS
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Patent number: 9771424Abstract: 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: GrantFiled: January 26, 2016Date of Patent: September 26, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Yao-Bin Liu, Patrick Mayes, Radha Shah Parmar
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Patent number: 9763965Abstract: 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: GrantFiled: April 11, 2013Date of Patent: September 19, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Michiel Mary Van Oort, John N. Hong
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Patent number: 9737505Abstract: 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: GrantFiled: October 28, 2015Date of Patent: August 22, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
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Patent number: 9738718Abstract: 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: GrantFiled: December 21, 2016Date of Patent: August 22, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Yao-Bin Liu, Patrick Mayes, Radha Shah Parmar
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Publication number: 20170224685Abstract: 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: ApplicationFiled: August 4, 2015Publication date: August 10, 2017Applicants: Epizyme, Inc., Glaxosmithkline Intellectual Property Development LimitedInventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael Munchhof, Lei Jin, Elayne Penebre, Olena I. Barbash
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Patent number: 9725407Abstract: 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: GrantFiled: January 22, 2016Date of Patent: August 8, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
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Patent number: 9718848Abstract: 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: GrantFiled: December 5, 2016Date of Patent: August 1, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Jerry Adams, Kevin J. Duffy, Yiqian Lian
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Patent number: 9708330Abstract: 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: GrantFiled: January 23, 2014Date of Patent: July 18, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Zehong Wan, Yingxia Sang, Qing Zhang
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Publication number: 20170197978Abstract: 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: ApplicationFiled: May 26, 2015Publication date: July 13, 2017Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Jing DENG, Hui LEI, Xin MA, Xichen LIN
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Patent number: 9701668Abstract: 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: GrantFiled: April 27, 2015Date of Patent: July 11, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
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Patent number: 9695161Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.Type: GrantFiled: March 25, 2016Date of Patent: July 4, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventor: Gren Wang
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Publication number: 20170166894Abstract: 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: ApplicationFiled: March 17, 2015Publication date: June 15, 2017Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Kellie Marie DEMOCK, Christine Patricia DONAHUE, Robert L. HALE, Jon LENN, Jennifer NELSON, P. Shannon PENDERGRAST
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Patent number: 9650364Abstract: Disclosed are compounds that are inhibitors of RIP2 kinase and methods of making and using the same.Type: GrantFiled: February 19, 2014Date of Patent: May 16, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimtedInventors: Linda N. Casillas, Adam Kenneth Charnley, Xiaoyang Dong, Pamela A. Haile, Michael P. Demartino, John F. Mehlmann