公开(公告)号：US11478478B2

公开(公告)日：2022-10-25

申请号：US16735956

申请日：2020-01-07

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED

发明人： Dominique Amans ,  Stephen John Atkinson ,  Lee Andrew Harrison ,  David Jonathan Hirst ,  Robert Peter Law ,  Matthew Lindon ,  Alexander Preston ,  Jonathan Thomas Seal ,  Christopher Roland Wellaway

IPC分类号： A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D215/227 ,  C07D215/46 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D498/04 ,  A61P29/00 ,  A61P37/00 ,  A61P31/12 ,  A61P35/00 ,  C07D215/44 ,  A61K31/4375 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/5386 ,  C07D498/08

摘要： The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US11229623B2

公开(公告)日：2022-01-25

申请号：US16796989

申请日：2020-02-21

申请人： GlaxoSmithKline Intellectual Property (No.2) Limited

发明人： Edward J. Brnardic ,  Carl A. Brooks ,  Brian Griffin Lawhorn ,  Guosen Ye ,  Linda S. Barton ,  Brian W. Budzik ,  Jay M. Matthews ,  John Jeffrey McAtee ,  Jaclyn R. Patterson ,  Joseph E. Pero ,  Robert Sanchez ,  Matthew Robert Sender ,  Lamont Roscoe Terrell ,  David J. Behm ,  James V. Thomas

IPC分类号： A61K31/40 ,  A61K31/695 ,  A61K31/424 ,  A61K31/4155 ,  A61K31/4025 ,  A61K31/4439 ,  A61K31/429 ,  A61K31/4245 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5386 ,  A61K31/427 ,  A61K31/407 ,  A61K45/06 ,  C07D207/48 ,  C07D513/04 ,  C07D401/12 ,  C07D409/12 ,  C07D498/10 ,  C07D403/12 ,  C07D413/12 ,  A61P7/10 ,  A61P29/00 ,  A61P19/00 ,  A61P15/00 ,  A61P1/16 ,  A61P1/10 ,  A61P31/04 ,  A61P17/00 ,  A61P17/04 ,  A61P37/06 ,  A61P27/02 ,  A61P27/06 ,  A61P1/00 ,  A61P43/00 ,  A61P37/04 ,  A61P13/12 ,  A61P13/10 ,  A61P25/06 ,  A61P25/28 ,  A61P11/06 ,  A61P11/14 ,  A61P11/02 ,  A61P1/04 ,  A61P1/18 ,  A61P3/04 ,  A61P3/00 ,  A61P9/00 ,  A61P3/10 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C07D417/12 ,  C07D491/107 ,  C07F7/08

摘要： The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

公开(公告)号：US11214582B2

公开(公告)日：2022-01-04

申请号：US17018301

申请日：2020-09-11

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED ,  ANACOR PHARMACEUTICALS, INC.

发明人： Carlos Alemparte-Gallardo ,  Michael Richard Kevin (Dickon) Alley ,  David Barros-Aguirre ,  Ilaria Giordano ,  Vincent Hernandez ,  Xianfeng Li ,  Jacob J. Plattner

IPC分类号： C07F5/02 ,  A61K31/69 ,  A61K45/06

摘要： Substituted benzoxaboroles whose structure comprises Formula (III), wherein R3 is selected from —CH3, —CII2CII3, —CII2═CII2, —CII2CII2CII3, —CH(CH3)2, —CH2CH2═CH2, and cyclopropyl, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, and —CH(CH3)2; compositions containing such compounds, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

公开(公告)号：US20210340246A1

公开(公告)日：2021-11-04

申请号：US17373223

申请日：2021-07-12

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED

发明人： Myrna A. MONCK ,  Narendra B. BAM ,  Jennifer DALLY ,  Michelle SPATARA

IPC分类号： C07K16/24

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

公开(公告)号：US20210053999A1

公开(公告)日：2021-02-25

申请号：US17089058

申请日：2020-11-04

申请人： GlaxoSmithKline Intellectual Property (No.2) Limited ,  Anacor Pharmaceuticals, Inc.

发明人： Michael Richard Kevin Alley ,  Vincent S. Hernandez ,  Jacob J. Plattner ,  Xianfeng Li ,  David Barros-Aguirre ,  Ilaria Giordano

IPC分类号： C07F5/04 ,  A61K31/69 ,  C07F5/02 ,  A61K45/06

摘要： Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

公开(公告)号：US10849897B2

公开(公告)日：2020-12-01

申请号：US16489876

申请日：2018-02-27

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED

发明人： Stephen John Atkinson ,  Emmanuel Hubert Demont ,  Lee Andrew Harrison ,  Etienne Levernier ,  Alexander G. Preston ,  Jonathan Thomas Seal ,  Ian David Wall ,  Robert J. Watson ,  James Michael Woolven

IPC分类号： A61K31/506 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/501 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention is directed to pyridyl derivatives which are bromodomain inhibitors, pharmaceutical compositions comprising the compounds and the use of the compounds or the compositions in the treatment of various diseases or conditions.

公开(公告)号：US10537638B2

公开(公告)日：2020-01-21

申请号：US14775900

申请日：2014-03-13

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED

发明人： George Crotts ,  Sorina Morar-Mitrica

IPC分类号： A61K39/395 ,  C07K16/28 ,  A61K47/18 ,  A61K47/26 ,  A61K9/00

摘要： The present invention is directed formulations for low concentrations of therapeutic proteins and methods of making the same. In one aspect the present invention is directed to a formulation for a therapeutic protein comprising: a) the therapeutic protein; and b) a surfactant; wherein the molar ratio of surfactant to therapeutic protein is at least 100. In another aspect the present invention is directed to a formulation for a therapeutic protein comprising: a) the therapeutic protein; and b) an antioxidant, wherein the molar ratio of antioxidant to therapeutic protein is at least 750.

公开(公告)号：US20180207145A1

公开(公告)日：2018-07-26

申请号：US15924952

申请日：2018-03-19

申请人： GlaxoSmithKline Intellectual Property (No. 2) Limited

发明人： Michael WASHBURN

IPC分类号： A61K31/4462 ,  A61K31/5513 ,  A61K9/08 ,  A61K47/40 ,  A61K9/00 ,  A61K39/42 ,  C07K16/10 ,  A61K31/4196 ,  A61K31/4184 ,  A61K31/519 ,  A61K31/7068 ,  A61K31/433 ,  A61K31/41 ,  A61K31/422 ,  A61K31/437 ,  A61K31/55 ,  A61K31/4545 ,  A61K31/5377 ,  C12N15/113 ,  A61K31/7056 ,  A61K31/215 ,  A61K31/351

CPC分类号： A61K31/4462 ,  A61K9/0019 ,  A61K9/0073 ,  A61K9/08 ,  A61K31/215 ,  A61K31/351 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/7012 ,  A61K31/7056 ,  A61K31/7068 ,  A61K39/42 ,  A61K47/40 ,  C07K16/1027 ,  C07K2317/24 ,  C12N15/1131 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2320/31 ,  A61K2300/00

摘要： Provided are compounds and pharmaceutically acceptable salts thereof, and combinations of compounds, their pharmaceutical compositions, their methods of preparation, and methods for their use in treating or preventing infectious disease.

公开(公告)号：US20180037595A1

公开(公告)日：2018-02-08

申请号：US15550658

申请日：2016-02-12

申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED ,  ANACOR PHARMACEUTICALS, INC.

发明人： M.R.K. (dickon) ALLEY ,  David BARROS-AGUIRRE ,  Ilaria GIORDANO ,  Vincent HERNANDEZ ,  Xianfeng LI ,  Jacob J. PLATTNER

IPC分类号： C07F5/02 ,  A61K31/69 ,  A61K45/06

CPC分类号： C07F5/025 ,  A61K31/69 ,  A61K45/06 ,  C07B2200/13

摘要： Compounds whose structure comprises Formula II, or a compound whose structure comprises Formula III wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2, compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

公开(公告)号：US09809540B2

公开(公告)日：2017-11-07

申请号：US15034583

申请日：2014-11-11

申请人： GlaxoSmithKline Intellectual Property (No.2) Limited

发明人： Francis Dominic Sanderson ,  Sarah Mary Vallance

IPC分类号： C07D211/54 ,  A61K31/4462

CPC分类号： C07D211/54 ,  A61K31/4462

摘要： A compound which is the hydrobromide salt of N-{4-chloro-2-hydroxy-3-[(3S)-3-piperidinylsulfonyl]phenyl}-N′-(3-fluoro-2-methylphenyl)urea, 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.