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：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。

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：WO2013092791A1

公开(公告)日：2013-06-27

申请号：PCT/EP2012/076275

申请日：2012-12-20

Applicant: GALAPAGOS NV

Inventor： LABÉGUÈRE, Frédéric Gilbert ,  NEWSOME, Gregory John Robert ,  ALVEY, Luke Jonathan ,  SANIÈRE, Laurent Raymond Maurice ,  FLETCHER, Stephen Robert

IPC: C07D471/04 ,  A61K31/529 ,  A61P9/10

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: A compound according to Formula (Ia) wherein L 1 , and G, and R 1 are as described herein. The present invention relates to novel compounds according to Formula (I) that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

Abstract translation: 根据式（Ia）的化合物，其中L 1，G 1和R 1如本文所述。 本发明涉及拮抗参与炎性病症的G蛋白偶联受体GPR84的式（I）的新化合物，以及这些新化合物的制备方法，包含这些化合物的药物组合物，以及用于 预防和/或治疗炎性疾病（例如炎性肠病（IBD），类风湿性关节炎，血管炎，肺部疾病（例如慢性阻塞性肺疾病（COPD）和肺间质疾病（例如特发性肺纤维化（IPF）））， 神经炎症状况，感染性疾病，自身免疫性疾病，内分泌和/或代谢疾病，和/或涉及免疫细胞功能损害的疾病，通过施用本发明的化合物。