公开(公告)号：WO2016193812A1

公开(公告)日：2016-12-08

申请号：PCT/IB2016/000821

申请日：2016-05-25

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

Inventor： ALTENBACH, Robert, J. ,  COWART, Marlon, D. ,  DE MUNCK, Tom, Roger Lisette ,  DROPSIT MONTOVERT, Sebastien Jean, Jacques Cedric ,  GFESSER, Gregory, A. ,  KELGTERMANS, Hans ,  MARTINA, Sebastien, Laurent Xavier ,  VAN DER PLAS, Steven, Emiel ,  WANG, Xueqing

IPC: C07D213/81 ,  A61K31/44 ,  A61P11/00

CPC classification number: C07D213/81 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D491/107

Abstract: The invention discloses compounds of Formula (I) wherein X, R 1 , R 2 , and R 3 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X，R 1，R 2和R 3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：WO2017060873A1

公开(公告)日：2017-04-13

申请号：PCT/IB2016/056028

申请日：2016-10-07

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

Inventor： AKKARI, Rhalid ,  ALVEY, Luke Jonathan ,  BOCK, Xavier Marie ,  CLAES, Pieter Isabelle Roger ,  COWART, Marlon D. ,  DE LEMOS, Elsa ,  DESROY, Nicolas ,  DUTHION, Béranger ,  GFESSER, Gregory A. ,  GOSMINI, Romain Luc Marie ,  HOUSSEMAN, Christopher Gaëtan ,  JANSEN, Koen Karel ,  JI, Jianguo ,  KYM, Philip R. ,  LEFRANCOIS, Jean-Michel ,  MAMMOLITI, Oscar ,  MENET, Christel Jeanne Marie ,  NEWSOME, Gregory John Robert ,  PALISSE, Adeline Marie Elise ,  PATEL, Sachin V. ,  PIZZONERO, Mathieu Rafaël ,  SHRESTHA, Anurupa ,  SWIFT, Elizabeth C. ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing

IPC: C07D471/04 ,  A61K31/437 ,  A61P11/12 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00 ,  A61K2300/00

Abstract: The present invention provides for compounds of formula (I), wherein R 1 , R 2 , R 3 , and R 4 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R 1，R 2，R 3和R 4具有说明书中定义的任何值及其药学上可接受的盐，其可用作治疗疾病和病症的药剂 并通过CFTR调节，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。