公开(公告)号：US20190231887A1

公开(公告)日：2019-08-01

申请号：US16255947

申请日：2019-01-24

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Alan Hornsby DAVIDSON ,  Alan Hastings DRUMMOND ,  Lindsey Ann NEEDHAM

IPC分类号： A61K47/54 ,  C07D277/46 ,  C07D471/04 ,  C07C237/22 ,  C07D215/233 ,  C07D213/73

CPC分类号： A61K47/542 ,  A61K47/54 ,  C07C237/22 ,  C07C2601/08 ,  C07D213/73 ,  C07D215/233 ,  C07D277/46 ,  C07D471/04

摘要： Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

公开(公告)号：US10364254B2

公开(公告)日：2019-07-30

申请号：US15752639

申请日：2016-08-15

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Haifeng Cui ,  Alan Hennessy ,  Qi Jin ,  Timothy James Miles ,  Stephen Frederick Moss ,  Neil David Pearson

IPC分类号： A61P31/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： 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.

公开(公告)号：US10351627B2

公开(公告)日：2019-07-16

申请号：US15246662

申请日：2016-08-25

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Yao-Bin Liu ,  Patrick Mayes ,  Radha Shah Parmar

IPC分类号： C07K16/28 ,  A61K39/395 ,  A61K45/06 ,  C07K16/30 ,  A61K39/00

摘要： 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.

公开(公告)号：US10328052B2

公开(公告)日：2019-06-25

申请号：US15771442

申请日：2016-10-25

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Alexis Denis ,  Olivier Mirguet ,  Jérôme Toum

IPC分类号： C07D405/14 ,  A61K31/4025 ,  A61K39/395

摘要： 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.

公开(公告)号：US20190152946A1

公开(公告)日：2019-05-23

申请号：US16308542

申请日：2017-06-08

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： John David HARLING ,  Christopher TINWORTH

IPC分类号： C07D401/12 ,  A61P35/00 ,  C07K5/12 ,  A61K47/64 ,  A61K47/65

摘要： A method of treating disorders associated with aberrant kinase activity, wherein the kinase is. IRAK3, GAK, TEC, PTK2B(PYK2), AURKA, RPS6KA1(RSK3), MAPK9(JNK2), BTK, PTK2 or AKT2, said method comprising degrading said kinase.

公开(公告)号：US20190142949A1

公开(公告)日：2019-05-16

申请号：US16244186

申请日：2019-01-10

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： John Alexander BROWN ,  Katherine Louise Jones ,  Rabinder Kumar Prinjha ,  Jason Witherington

IPC分类号： A61K47/54 ,  A61K31/4709 ,  A61K31/4439 ,  C07D405/14 ,  C07D401/12 ,  C07D401/04

摘要： The present invention relates to covalent conjugates of BET inhibitors and alpha amino acid esters, processes for their preparation, compositions containing them, and to their use in the treatment of various disorders in particular inflammatory and autoimmune diseases, such as rheumatoid arthritis; and cancers.

公开(公告)号：US10287280B2

公开(公告)日：2019-05-14

申请号：US15548500

申请日：2016-02-12

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Ann Marie Diederich ,  Robert Herrmann

IPC分类号： C07D413/12 ,  A61K31/553 ,  C07C223/04 ,  C07D249/10 ,  C07D267/14

摘要： Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

公开(公告)号：US20190119223A1

公开(公告)日：2019-04-25

申请号：US16094910

申请日：2017-05-11

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： Brian Alvin JOHNS ,  Wieslaw Mieczyslaw KAZMIERSKI ,  Martha Alicia DE LA ROSA ,  Vicente SAMANO

IPC分类号： C07D257/04 ,  C07C323/63 ,  C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D405/12 ,  C07D417/12 ,  C07D285/08 ,  C07C323/42 ,  C07C323/45 ,  C07F9/6524 ,  C07D401/04 ,  C07D401/10 ,  C07D249/06 ,  C07D249/08 ,  C07D271/06

CPC分类号： C07D257/04 ,  C07C323/42 ,  C07C323/45 ,  C07C323/63 ,  C07D249/06 ,  C07D249/08 ,  C07D271/06 ,  C07D285/08 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07F9/6524

摘要： Provided are IDO inhibitor 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 diseases.

公开(公告)号：US10189820B2

公开(公告)日：2019-01-29

申请号：US15730664

申请日：2018-01-03

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

发明人： John F. Mehlmann ,  Joseph J. Romano

IPC分类号： A61K31/5355 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/22 ,  C07D493/10 ,  C07D498/18 ,  C07F9/6558

摘要： 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.

公开(公告)号：US20190023791A1

公开(公告)日：2019-01-24

申请号：US15749141

申请日：2016-08-03

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  MERCK SHARP & DOHME CORP.

发明人： Axel HOOS ,  David KAUFMAN ,  Elaine PINHEIRO ,  Herbert STRUEMPER ,  Niranjan YANAMANDRA

IPC分类号： C07K16/28 ,  A61P35/00 ,  A61K9/00

摘要： 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 sequence of SEQ ID NO:55; (c) a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:56; (d) a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:57; (e) a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:58; and (f) a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:59.