公开(公告)号：WO2018065921A1

公开(公告)日：2018-04-12

申请号：PCT/IB2017/056126

申请日：2017-10-04

Applicant: ABBVIE S.Á.R.L. ,  GALAPAGOS NV

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  GRESZLER, Stephen N. ,  KOENIG, John R. ,  KYM, Philip R. ,  LIU, Bo ,  SCANIO, Marc J. ,  SEARLE, Xenia ,  WANG, Xueqing ,  YEUNG, Ming C. ,  ZHAO, Gang

IPC: C07D207/16 ,  C07D401/12 ,  A61K31/4025 ,  A61K31/4439 ,  A61P11/00

Abstract: The invention discloses compounds of Formula (I) wherein R 1 , R 2 , R 2A , R 3 , R 3A , R 4 , and R 5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

Abstract translation: 本发明公开了式（I）的化合物，其中R 1，R 2，R 2，A，R 4，R 5， R 3，R 4，R 5和R 5如本文所定义。 本发明涉及化合物及其在治疗囊性纤维化中的用途，其制备方法，包含其的药物组合物，以及通过施用本发明化合物治疗囊性纤维化的方法。

公开(公告)号：WO2018154519A1

公开(公告)日：2018-08-30

申请号：PCT/IB2018/051160

申请日：2018-02-23

Applicant: ABBVIE S.À.R.L. ,  GALAPAGOS NV

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  GRESZLER, Stephen N. ,  KYM, Philip R. ,  LIU, Bo ,  MALAGU, Karine Fabienne ,  MERAYO MERAYO, Nuria ,  PIZZONERO, Mathieu Rafaël ,  SEARLE, Xenia B. ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing ,  YEUNG, Ming C. ,  ZHAO, Gang

IPC: C07C311/46 ,  A61P3/04 ,  A61K31/343 ,  C07D215/12 ,  C07D215/36 ,  C07D317/68 ,  C07D319/22 ,  C07D231/56 ,  C07D471/04 ,  C07D205/04 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D307/16

Abstract: The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention. In one embodiment, the compound is a compound of Formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein A 1 is selected from the group consisting of X 1 , X 2 , X 3 , X 4 ; R 1 , R 2A , R 2B , R 2C , R 2D , R 3 , R 4 ,R 5A , R 5B , R 5C , R 5D , R 6A , R 6B , R 6C , R 6D , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , and R 14 are as described herein.

公开(公告)号：WO2018154493A1

公开(公告)日：2018-08-30

申请号：PCT/IB2018/051125

申请日：2018-02-23

Applicant: ABBVIE S.À.R.L. ,  GALAPAGOS NV

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  GRESZLER, Stephen N. ,  KYM, Philip R. ,  LIU, Bo ,  MALAGU, Karine Fabienne ,  MERAYO MERAYO, Nuria ,  PIZZONERO, Mathieu Rafaël ,  SEARLE, Xenia B. ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing ,  YEUNG, Ming C. ,  ZHAO, Gang

IPC: C07D405/12 ,  C07D407/12 ,  C07D319/22 ,  C07D307/16 ,  A61P3/04 ,  A61K31/381 ,  A61K31/343

Abstract: The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention. Other embodiments of the invention include a pharmaceutical composition comprising a therapeutically effective amount of a compound of the present invention, or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier. In one aspect, the invention provides for compounds of Formula (I) (I) wherein A 1 is selected from the group consisting of and R 1 , R 2A , R 2B , R 2C , R 2D , R 3 , R 4 , R 5A , R 5B , R 5C , R 5D , R 6A , R 6B , R 6C , R 6D , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , and R 14 are as defined herein.

公开(公告)号：WO2018065962A1

公开(公告)日：2018-04-12

申请号：PCT/IB2017/056196

申请日：2017-10-06

Applicant: ABBVIE S.À.R.L. ,  GALAPAGOS NV

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  COUTY, Sylvain ,  DE LEMOS, Elsa ,  DESROY, Nicolas ,  DUTHION, Béranger ,  GFESSER, Gregory A. ,  GRESZLER, Stephen N. ,  HOUSSEMAN, Christopher Gaëtan ,  KOENIG, John R. ,  KYM, Philip R. ,  LIU, Bo ,  SCANIO, Marc J. ,  SEARLE, Xenia ,  WANG, Xueqing ,  YEUNG, Ming C. ,  ZHAO, Gang

IPC: C07D401/14 ,  C07D401/04 ,  C07D405/06 ,  C07D207/14 ,  C07D207/48 ,  A61P11/00 ,  A61K31/4025

Abstract: The invention discloses compounds of Formula (I), wherein R 1 , R 2 , R 2A , R 3 , R 3A , R 4 , R 4A , and R 5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

Abstract translation: 本发明公开了式（I）的化合物，其中R 1，R 2，R 2，R 4，R 5， 3，R 3A，R 4，R 4A和R 5为 如本文所定义的。 本发明涉及化合物及其在治疗囊性纤维化中的用途，其制备方法，包含其的药物组合物，以及通过施用本发明化合物治疗囊性纤维化的方法。