公开(公告)号：WO2017060874A1

公开(公告)日：2017-04-13

申请号：PCT/IB2016/056029

申请日：2016-10-07

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

Inventor： AKKARI, Rhalid ,  ALVEY, Luke Jonathan ,  BOCK, Xavier Marie ,  BROWN, Brian S. ,  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 ,  MERAYO, Nuria Merayo ,  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 ,  DE BLIECK, Ann

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

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

Abstract: The present invention provides for compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 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，R 4，R 5和R 6具有说明书中定义的任何值及其药学上可接受的盐，其可用作治疗疾病的试剂 和由CFTR介导和调节的病症，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：WO2022008383A1

公开(公告)日：2022-01-13

申请号：PCT/EP2021/068377

申请日：2021-07-02

Applicant: GALAPAGOS NV

Inventor： JONCOUR, Agnès Marie ,  PIZZONERO, Mathieu Rafaël ,  MAI, Thi Thu Trang ,  MODRIC, Marina ,  QUINTON, Evelyne Martine ,  STIMSON, Christopher Charles ,  BARBEAU, Olivier Remi

IPC: C07D217/26 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4725 ,  A61P9/00 ,  A61P11/00 ,  A61P29/00 ,  A61P35/00

Abstract: The present invention discloses compounds according to Formula (I) wherein R1, R2, R3, L1, L2, and L3 are as defined herein. The present invention relates to compounds inhibiting discoidin domain receptors (DDRs), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, inflammatory diseases, respiratory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering a compound of the invention.

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：WO2017060879A1

公开(公告)日：2017-04-13

申请号：PCT/IB2016/056035

申请日：2016-10-07

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

Inventor： AKKARI, Rhalid ,  ALVEY, Luke Jonathan ,  BOCK, Xavier Marie ,  BROWN, Brian S. ,  CLAES, Pieter Isabelle Roger ,  COWART, Marlon D. ,  CONRATH, Katja E. ,  CYR, Douglas ,  DE LEMOS, Elsa ,  DE WILDE, Gert Jules Hector ,  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 ,  MERAYO, Nuria Merayo ,  NEWSOME, Gregory John Robert ,  PALISSE, Adeline Marie Elise ,  PATEL, Sachin V. ,  PIZZONERO, Mathieu Rafaël ,  SHRESTHA, Anurupa ,  SWIFT, Elizabeth C. ,  TSE, Chris ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61P11/00 ,  G01N33/68

CPC classification number: A61K31/4545 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  G01N33/5023 ,  G01N2800/382

Abstract: A corrector agent capable of stabilizing a newly synthesized cystic fibrosis transmembrane conductance regulator (CFTR) protein, useful in the treatment of cystic fibrosis.

Abstract translation: 能够稳定新合成的囊性纤维化跨膜电导调节蛋白（CFTR）蛋白的修正剂，可用于治疗囊性纤维化。

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。