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：WO2017009804A1

公开(公告)日：2017-01-19

申请号：PCT/IB2016/054219

申请日：2016-07-14

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

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  COWART, Marlon D. ,  ESMIEU, William Ramesh ,  GFESSER, Gregory A. ,  GRESZLER, Stephen N. ,  KOENIG, John R. ,  KYM, Philip R. ,  LIU, Bo ,  MALAGU, Karine Fabienne ,  PATEL, Sachin V. ,  SCANIO, Marc J. ,  SEARLE, Xenia B. ,  VOIGHT, Eric ,  WANG, Xueqing ,  YEUNG, Ming C.

IPC: C07D317/70 ,  C07D405/12 ,  C07D407/12 ,  C07D493/04 ,  C07D519/00 ,  A61K31/36 ,  A61K31/404 ,  A61K31/426 ,  A61K31/433 ,  A61K31/443 ,  A61K31/4184 ,  A61K31/501 ,  A61K31/497 ,  A61P11/00

CPC classification number: C07D493/04 ,  A61K31/357 ,  A61K31/397 ,  A61K31/433 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/5377 ,  A61K45/06 ,  C07D317/70 ,  C07D405/12 ,  C07D407/12 ,  C07D519/00

Abstract: The present invention provides for compounds of formula (I) wherein X, Y, and R 1 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract translation: 本发明提供式（I）化合物，其中X，Y和R 1具有说明书中定义的任何值及其药学上可接受的盐，其可用作治疗由 CFTR，包括囊性纤维化，Siegren综合征，胰腺功能不全，慢性阻塞性肺病和慢性阻塞性气道疾病。 还提供了由一种或多种式（I）化合物组成的药物组合物。

公开(公告)号：WO2019193062A1

公开(公告)日：2019-10-10

申请号：PCT/EP2019/058417

申请日：2019-04-03

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

Inventor： DESROY, Nicolas ,  DE LEMOS, Elsa ,  COUTY, Sylvain ,  PICOLET, Olivier Laurent ,  WANG, Xueqing ,  SEARLE, Xenia B ,  LIU, Bo ,  YEUNG, Ming C. ,  ALTENBACH, Robert J ,  GFESSER, Gregory A. ,  KYM, Phillip R.

IPC: C07D403/04 ,  C07D403/06 ,  C07D407/06 ,  C07D207/16 ,  A61K31/4025 ,  A61P11/00

Abstract: The invention discloses compounds of Formula (I) wherein R 1 , R 2 , 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.

公开(公告)号：WO2017187321A1

公开(公告)日：2017-11-02

申请号：PCT/IB2017/052349

申请日：2017-04-24

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

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  CHAN, Vincent ,  GRIEME, Timothy A. ,  KOENIG, John R. ,  KYM, Philip R. ,  LIU, Bo ,  MALAGU, Karine Fabienne ,  PATEL, Sachin V. ,  SCANIO, Marc ,  SEARLE, Xenia B. ,  SHEKHAR, Shashank ,  WANG, Xueqing ,  YEUNG, Ming C.

IPC: C07D311/58 ,  A61K31/352 ,  C07D311/60 ,  C07D407/12 ,  C07D407/14 ,  A61P11/00

Abstract: The present invention provides for compounds of formula (I), wherein R 1 , m, Z, G 1 , R 2 , and R 3 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract translation: 本发明提供了式（I）的化合物，其中R 1，m，Z，G 1，R 2， R 3和R 3具有本说明书中定义的任何值及其药学上可接受的盐，其可用作治疗由CFTR介导和调节的疾病和病症的试剂，包括 囊性纤维化，SJ氏综合征，胰腺功能不全，慢性阻塞性肺病和慢性阻塞性气道疾病。 还提供了由一种或多种式（I）化合物组成的药物组合物。

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：WO2019053634A1

公开(公告)日：2019-03-21

申请号：PCT/IB2018/057020

申请日：2018-09-13

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

Inventor： ALTENBACH, Robert J. ,  BOGDAN, Andrew ,  COUTY, Sylvain ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  HOUSSEMAN, Christopher Gaëtan ,  KYM, Philip R. ,  LIU, Bo ,  MAI, Thi Thu Trang ,  MALAGU, Karine Fabienne ,  MERAYO MERAYO, Nuria ,  PICOLET, Olivier Laurent ,  PIZZONERO, Mathieu Rafaël ,  SEARLE, Xenia B. ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing ,  YEUNG, Ming C.

IPC: C07D213/71 ,  C07D215/36 ,  C07D231/56 ,  C07D401/12 ,  C07D235/28 ,  C07D471/04 ,  C07D213/64 ,  C07C311/45 ,  A61P11/00 ,  A61K31/4709

Abstract: The invention discloses compounds of Formula (I), wherein A 1 , R 1 , R 2 , R 3 , R 4 , and n 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.

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。