Abstract: Provided are compounds of formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.
Type:
Grant
Filed:
June 30, 2016
Date of Patent:
March 26, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Wieslaw Mieczyslaw Kazmierski, Martha Alicia De La Rosa, Vicente Samano
Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
Type:
Grant
Filed:
November 14, 2017
Date of Patent:
March 5, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Pamela A. Haile, Robert W. Marquis, Jr., John F. Mehlmann, Joseph J. Romano, Robert R. Singhaus, Jr., Gren Z. Wang
Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
Type:
Grant
Filed:
January 3, 2018
Date of Patent:
January 29, 2019
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: The present invention provides methods of treating cancer in a human in need thereof comprising administering to the human: a therapeutically effective amount of a monoclonal antibody that binds to human OX40 comprising: (a) a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:1; (b) a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:2; (c) a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:3; (d) a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:7; (e) a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:8; and (f) a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:9; and a therapeutically effective amount of a monoclonal antibody that binds to human PD-1 comprising: (a) a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:54; (b) a heavy chain variable region CDR2 comprising the amino acid
Abstract: The present invention relates to LpxC antibacterial compounds of Formula (IA): corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.
Type:
Application
Filed:
December 8, 2016
Publication date:
December 20, 2018
Applicant:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Qi JIN, Denise Teotico POHLHAUS, Jared T. SPLETSTOSER
Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.
Type:
Grant
Filed:
September 22, 2015
Date of Patent:
December 4, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Niall Andrew Anderson, Ian Baxter Campbell, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou
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 Alzheimer's disease.
Type:
Grant
Filed:
July 21, 2015
Date of Patent:
November 13, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Zehong Wan, Xiaomin Zhang, Jian Wang, Matthew Robert Sender, Eric Steven Manas, Raphael Anthony Rivero, Joseph E Pero, Christopher Ernst Neipp, Vipulkumar Kantibhai Patel
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:
January 23, 2018
Date of Patent:
October 30, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
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:
May 27, 2015
Date of Patent:
October 23, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
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:
October 2, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Xiao Ding, Luigi Piero Stasi, Zehong Wan, Colin Michael Edge
Abstract: A process for the microbial synthesis of migalastat, specifically a process for the production of migalastat comprising culturing a microorganism under conditions such that at least one imino sugar is produced and detecting and/or isolating an imino sugar produced by said microorganism, and the microorganisms used in this process. The invention also comprises migalastat produced according to the above method and pharmaceutical compositions and uses thereof.
Type:
Grant
Filed:
February 17, 2015
Date of Patent:
September 18, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Emilio Alvarez-Ruiz, Andrew John Collis, Alison Sarah Dann, Andrew Peter Fosberry, Sarah Jane Ready, Maria Jesus Vazquez Muniz
Abstract: A compound of Formula (I), or a salt thereof, compositions comprising the compound, processes for its preparation and its use in therapy, for example in the treatment of parasitic diseases such as Chagas disease, Human African Trypanosomiasis (HAT) and leishmaniasis, particularly visceral leishmaniasis (VL).
Type:
Grant
Filed:
May 26, 2016
Date of Patent:
September 4, 2018
Assignees:
GlaxoSmithKline Intellectual Property Development Limited, The University of Dundee
Inventors:
Stephen Brand, Elisabet Viayna Gaza, Ian Gilbert, Eun Jung Ko, Maria Marco Martin, Timothy James Miles, Lars Henrik Sandberg, Michael George Thomas
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt 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 and conditions 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:
January 27, 2016
Date of Patent:
August 14, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Keith Biggadike, Aurelie Cecile Champigny, Diane Mary Coe, Deborah Needham, Daniel Terence Tape
Abstract: Disclosed herein are combinations of an OX40 modulator and a CTLA-4 modulator, pharmaceutical compositions thereof, uses thereof, and methods of treatment comprising administering said combination, including uses in cancer.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 9, 2018
Applicant:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Abstract: Disclosed herein are combinations of an OX40 modulator and a PD-1 modulator, pharmaceutical compositions thereof, uses thereof, and methods of treatment comprising administering said combination, including uses in cancer.
Type:
Application
Filed:
August 3, 2016
Publication date:
August 9, 2018
Applicant:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Abstract: A compound of formula (I) or a salt thereof wherein R1 represents a hydrogen atom, a methyl group or a ethyl group R2 represents a hydrogen atom or a fluorine atom R3 represents a hydrogen atom, a methyl group or an ethyl group.
Type:
Grant
Filed:
March 26, 2014
Date of Patent:
July 17, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Niall Andrew Anderson, Brendan John Fallon, John Martin Pritchard
Abstract: A compound according to formula (I) wherein R1 is hydrogen, cyclopropyl, or pyrazolyl, wherein said pyrazolyl is optionally substituted by one or two methyl groups; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 22, 2015
Date of Patent:
June 26, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou, Stephen Swanson
Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, and Z are as defined herein, and methods of making and using the same.
Type:
Grant
Filed:
February 14, 2017
Date of Patent:
June 12, 2018
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Michael Jonathan Bury, Linda N. Casillas, Adam K. Charnley, Michael P. Demartino, Xiaoyang Dong, Patrick M. Eidam, Pamela A. Haile, Robert W. Marquis, Jr., Joshi M. Ramanjulu, Joseph J. Romano, Ami Lakdawala Shah, Robert R. Singhaus, Jr., Gren Wang