公开(公告)号：US20190194145A1

公开(公告)日：2019-06-27

申请号：US16286920

申请日：2019-02-27

Applicant: GlaxoSmithKline Intellectual Property Development Limit

Inventor： Adam K. CHARNLEY ,  Xiaoyang DONG

IPC: C07D239/94 ,  C07D471/04 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14

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.

公开(公告)号：US10328052B2

公开(公告)日：2019-06-25

申请号：US15771442

申请日：2016-10-25

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Alexis Denis ,  Olivier Mirguet ,  Jérôme Toum

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

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.

公开(公告)号：US20190152946A1

公开(公告)日：2019-05-23

申请号：US16308542

申请日：2017-06-08

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： John David HARLING ,  Christopher TINWORTH

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

Abstract: 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

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

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

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

Abstract: 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

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Ann Marie Diederich ,  Robert Herrmann

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

Abstract: 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

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

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

IPC: 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 classification number: 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

Abstract: 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

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： John F. Mehlmann ,  Joseph J. Romano

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

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.

公开(公告)号：US20190023791A1

公开(公告)日：2019-01-24

申请号：US15749141

申请日：2016-08-03

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

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

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

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 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.

公开(公告)号：US20190010135A1

公开(公告)日：2019-01-10

申请号：US16129867

申请日：2018-09-13

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Weichun Chen ,  Ebere F. Igboko ,  Xichen Lin ,  Hongfu Lu ,  Feng Ren ,  Paul Bryan Wren ,  Zhongmiao Xu ,  Ting Yang ,  Lindong Zhu

IPC: C07D307/18 ,  C07D241/04 ,  C07D309/08 ,  C07C317/50 ,  C07C317/42 ,  C07C311/47 ,  C07D305/06 ,  C07D213/34 ,  C07D295/135 ,  C07D211/54 ,  C07D207/10 ,  C07D487/04 ,  C07D471/04 ,  C07D239/26 ,  C07D233/64

CPC classification number: C07D307/18 ,  C07C311/47 ,  C07C317/42 ,  C07C317/50 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D207/10 ,  C07D211/54 ,  C07D213/34 ,  C07D233/64 ,  C07D239/26 ,  C07D241/04 ,  C07D295/135 ,  C07D305/06 ,  C07D309/08 ,  C07D471/04 ,  C07D487/04

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.

公开(公告)号：US20180340023A1

公开(公告)日：2018-11-29

申请号：US15987942

申请日：2018-05-24

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Steven Grant ,  Martin Orecchia ,  Chika Akinseye ,  Laura Hook ,  Alan Lewis ,  Tejinder Bhinder

IPC: C07K16/24

Abstract: The present disclosure relates to compositions, for treating interleukin 5 (IL-5) mediated diseases, and related methods.