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：WO2019007696A1

公开(公告)日：2019-01-10

申请号：PCT/EP2018/066548

申请日：2018-06-21

Applicant: GALAPAGOS NV

Inventor： MAMMOLITI, Oscar ,  JANSEN, Koen, Karel ,  MENET, Christel, Jeanne, Marie ,  PALISSE, Adeline, Marie, Elise ,  TRICARICO, Giovanni, Alessandro ,  EL BKASSINY, Sandy ,  JAUNET, Alexis, Patrick, Claude ,  ALLART, Brigitte ,  DUTHION, Béranger ,  BREBION, Franck Laurent

IPC: C07D401/14 ,  C07D405/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D471/04 ,  A61K31/502 ,  A61P29/00

Abstract: The present invention discloses compounds according to Formula (I) Wherein R 1 , R 2 , L, A 1 , A 2 , A 3 , Cy and the subscript n are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phosphate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, respiratory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.

公开(公告)号：WO2015110378A1

公开(公告)日：2015-07-30

申请号：PCT/EP2015/050850

申请日：2015-01-19

Applicant: GALAPAGOS NV

Inventor： MENET, Christel, Jeanne, Marie ,  MAMMOLITI, Oscar ,  BLANC, Javier ,  ORŠULIC, Mislav ,  ROŠCIC, Maja

IPC: C07D235/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  A61K31/4184 ,  A61K31/4439 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08

CPC classification number: C07D235/08 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14

Abstract: The present invention discloses compounds according to Formula (I) wherein Cy, R 1 , L 1 R 3 , R 4 , R 5 , L a, and R a are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

Abstract translation: 本发明公开了式（I）的化合物，其中Cy，R 1，L 1，R 3，R 4，R 5，La和R a如本文所定义。 公开了根据式（I）的能够抑制JAK的新型苯并咪唑，这些化合物可以制备为药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括通过非 - 过敏性疾病，炎性疾病，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损伤的疾病，先天性软骨畸形和/或与IL6分泌过高或干扰素分泌过多相关的疾病。

公开(公告)号：WO2014180562A1

公开(公告)日：2014-11-13

申请号：PCT/EP2014/001202

申请日：2014-05-06

Applicant: GALAPAGOS NV

Inventor： VAN DER PLAS, Steven ,  MAMMOLITI, Oscar ,  MENET, Christel ,  TRICARICO, Giovanni ,  DE BLIECK, Ann ,  JOANESSE, Caroline ,  DE MUNCK, Tom ,  KELGTERMANS, Hans

IPC: C07D333/36 ,  A61K31/381 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  A61P43/00

CPC classification number: A61K31/381 ,  A61K31/397 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/435 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/536 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/553 ,  C07D333/36 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

Abstract: The present invention discloses compounds according to Formula (I), wherein R 1 , R 2 , R 3 , L, and the subscript m 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, and methods of treatment using the same, for the treatment of 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R1，R2，R3，L和下标m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，药物组合物和使用其的治疗方法，用于通过施用本发明的化合物治疗囊性纤维化。

公开(公告)号：WO2020200900A1

公开(公告)日：2020-10-08

申请号：PCT/EP2020/058064

申请日：2020-03-24

Applicant: GALAPAGOS NV

Inventor： MAMMOLITI, Oscar ,  JARY, Hélène, Marie ,  ORSULIC, Mislav ,  VRBAN, Denana ,  KOMAC, Marijana ,  BRYS, Reginald, Christophe, Xavier ,  AKKARI, Rhalid

IPC: C07D471/04 ,  A61P31/18 ,  A61K31/662

Abstract: The present invention discloses compounds according to Formula (I): (I). Wherein R 1 , R 2 , R 5 and Cy are as defined herein. The present invention relates to compounds, methods for the production of said compounds, pharmaceutical compositions comprising said compounds and methods for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, pain, fibrosis and/or proliferative diseases by administering said compounds.

公开(公告)号：WO2019110352A1

公开(公告)日：2019-06-13

申请号：PCT/EP2018/082540

申请日：2018-11-26

Applicant: GALAPAGOS NV

Inventor： MAMMOLITI, Oscar ,  JOANNESSE, Caroline, Martine, Andrée, Marie ,  PALISSE, Adeline, Marie, Elise ,  VAN DER PLAS, Steven, Emiel ,  CATANA, Cornel ,  JAUNET, Alexis, Patrick, Claude ,  LARUELLE, Chris, Ronan ,  DE MUNCK, Tom, Roger, Lisette ,  DE BLIECK, Ann ,  DUTHION, Béranger

IPC: C07D491/052 ,  A61P31/20 ,  A61P31/12 ,  A61K31/436

Abstract: The present invention discloses compounds according to Formula (I), wherein R 1 , R 2a , R 2b , R 3 , R 4 , and R 5 are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving hepatitis B by administering the compound of the invention.

公开(公告)号：WO2017148787A1

公开(公告)日：2017-09-08

申请号：PCT/EP2017/054139

申请日：2017-02-23

Applicant: GALAPAGOS NV

Inventor： MAMMOLITI, Oscar ,  JANSEN, Koen, Karel ,  PALISSE, Adeline, Marie, Elise ,  JOANNESSE, Caroline, Martine, Andrée-Marie ,  MENET, Christel, Jeanne, Marie ,  ALLART, Brigitte ,  EL BKASSINY, Sandy

IPC: C07D401/14 ,  C07D403/04 ,  A61P35/00

Abstract: The present invention discloses compounds according to Formula I, wherein R 1a , R 1b , R 2a , R 2b , R 3 , R 4 , R 5 , R 6a , X, Cy 1 , Cy 2 , and the subscript n and m are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phosphate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.

Abstract translation: 本发明公开了根据式I的化合物，其中R 1a，R 1b，R 2a，R 3，R 5， 2b，R 3，R 4，R 5，R 6a，X ，Cy 1，Cy 2，以及下标n和m如本文所定义。 本发明涉及鞘氨醇1-磷酸（S1P）受体的拮抗剂化合物，其制备方法，包含其的药物组合物以及使用其的药物组合物的治疗方法，用于预防和/或治疗涉及纤维化疾病，炎症 疾病，自身免疫性疾病，代谢性疾病，心血管疾病和/或增殖性疾病，通过施用本发明的化合物。

公开(公告)号：WO2020200899A1

公开(公告)日：2020-10-08

申请号：PCT/EP2020/058063

申请日：2020-03-24

Applicant: GALAPAGOS NV

Inventor： MAMMOLITI, Oscar ,  BRYS, Reginald, Christophe, Xavier ,  NEWSOME, Gregory, John, Robert ,  BABEL, Marielle, Gilles

IPC: C07D471/04 ,  A61P31/18 ,  A61K31/662

Abstract: The present invention discloses compounds according to Formula I: Wherein R 1 , R 2 , R 5 and Cy are as defined herein. The present invention relates to compounds, methods for the production of said compounds, pharmaceutical compositions comprising said compounds and methods for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, pain, fibrosis and/or proliferative diseases by administering said compounds.

公开(公告)号：WO2017067848A1

公开(公告)日：2017-04-27

申请号：PCT/EP2016/074662

申请日：2016-10-14

Applicant: GALAPAGOS NV

Inventor： BRYS, Reginald, Christophe, Xavier ,  GENEY, Raphaël, Jean, Joël ,  JONCOUR, Agnès, Marie ,  DOYON, Julien, Georges, Pierre-Olivier ,  LABÉGUÈRE, Frédéric, Gilbert ,  LEFRANCOIS, Jean-Michel ,  MAMMOLITI, Oscar ,  SCHMITT, Benoît, Antoine ,  VAN DER PLAS, Steven, Emiel ,  MENET, Christel, Jeanne, Marie

IPC: C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D471/04

Abstract: The present invention discloses compounds according to Formula (I): wherein R 1 , R 2 , and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases and/or proliferative diseases by administering the compound of the invention.

Abstract translation: 本发明公开了根据式（I）的化合物：其中R 1，R 2和Cy如本文所定义。 本发明涉及抑制IRAK家族激酶的化合物，其制备方法，包含其的药物组合物，以及使用该化合物的治疗方法，其通过给药来预防和/或治疗炎性疾病，自身免疫性疾病和/或增殖性疾病 本发明的化合物。

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。