公开(公告)号：WO2017079205A1

公开(公告)日：2017-05-11

申请号：PCT/US2016/059999

申请日：2016-11-02

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： FATHEREE, Paul R. ,  JACOBSEN, John R. ,  BEAUSOLEIL, Anne-Marie ,  BRANDT, Gary E.L. ,  FLEURY, Melissa ,  JIANG, Lan ,  SMITH, Cameron ,  SULLIVAN, Steven D.E. ,  VAN ORDEN, Lori Jean ,  COLSON, Pierre-Jean ,  FASS, Gene Timothy ,  RAPTA, Miroslav ,  BENJAMIN, Noah ,  DABROS, Marta ,  THALLADI, Venkat R.

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P11/00

CPC分类号： C07D471/04

摘要： The invention provides compounds of formula (I): wherein X is (I) and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

摘要翻译： 本发明提供了可用作JAK激酶抑制剂的式（I）化合物：其中X是（I）且变量在说明书中定义，或其药学上可接受的盐。 本发明还提供包含此类化合物的药物组合物，使用此类化合物治疗呼吸系统疾病的方法，以及可用于制备此类化合物的方法和中间体。

公开(公告)号：WO2018165395A1

公开(公告)日：2018-09-13

申请号：PCT/US2018/021492

申请日：2018-03-08

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： FATHEREE, Paul R. ,  BRANDT, Gary E.L. ,  SMITH, Cameron ,  SULLIVAN, Steven D.E. ,  VAN ORDEN, Lori Jean ,  KLEINSCHEK, Melanie A. ,  CRATER, Glenn D.

IPC分类号： C07D471/04 ,  A61P11/00 ,  A61K31/437

摘要： The invention provides compounds of formula (I): (I) where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：WO2018165392A1

公开(公告)日：2018-09-13

申请号：PCT/US2018/021489

申请日：2018-03-08

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： FATHEREE, Paul R. ,  BRANDT, Gary E.L. ,  SMITH, Cameron ,  SULLIVAN, Steven D.E. ,  VAN ORDEN, Lori Jean ,  KLEINSCHEK, Melanie A. ,  CRATER, Glenn D.

IPC分类号： C07D471/04 ,  A61P11/00 ,  A61K31/437 ,  A61K31/397

摘要： The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：WO2016191524A1

公开(公告)日：2016-12-01

申请号：PCT/US2016/034243

申请日：2016-05-26

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： HUDSON, Ryan ,  KOZAK, Jennifer ,  FATHEREE, Paul R. ,  PODESTO, Dante D. ,  BRANDT, Gary E.L. ,  FLEURY, Melissa ,  BEAUSOLEIL, Anne-Marie ,  HUANG, Xiaojun ,  THALLADI, Venkat R.

IPC分类号： C07D519/00 ,  A61K31/439 ,  A61P1/04

CPC分类号： C07D519/00 ,  A61K31/46 ,  A61K45/06 ,  C07B2200/13

摘要： The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat inflammatory bowel diseases, and processes and intermediates useful for preparing such compounds.

摘要翻译： 本发明提供式（I）化合物：其中变量在本说明书中定义，或其药学上可接受的盐，其为JAK激酶抑制剂。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗炎症性肠病的方法，以及可用于制备这些化合物的方法和中间体。