公开(公告)号：EP3523293A1

公开(公告)日：2019-08-14

申请号：EP17794779.3

申请日：2017-10-06

申请人： Abbvie S.a.r.l. ,  Galapagos N.V.

发明人： 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分类号： C07D401/14 ,  C07D401/04 ,  C07D405/06 ,  C07D207/14 ,  C07D207/48 ,  A61P11/00 ,  A61K31/4025

公开(公告)号：EP3585784A1

公开(公告)日：2020-01-01

申请号：EP18710151.4

申请日：2018-02-23

申请人： Abbvie S.a.r.l. ,  Galapagos NV

发明人： 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分类号： C07D405/12 ,  C07D407/12 ,  C07D319/22 ,  C07D307/16 ,  A61P3/04 ,  A61K31/381 ,  A61K31/343

公开(公告)号：EP3523277A1

公开(公告)日：2019-08-14

申请号：EP17794414.7

申请日：2017-10-04

申请人： Abbvie S.a.r.l. ,  Galapagos NV

发明人： 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分类号： C07D207/16 ,  C07D401/12 ,  A61K31/4025 ,  A61K31/4439 ,  A61P11/00

公开(公告)号：EP3269716A1

公开(公告)日：2018-01-17

申请号：EP17177371.6

申请日：2014-03-07

申请人： Galapagos N.V.

发明人： DESROY, Nicolas ,  HECKMANN, Bertrand ,  BRYS, Reginald, Christophe, Xavier ,  JONCOUR, Agnès, Marie ,  PEIXOTO, Christophe ,  BOCK, Xavier, Marie

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00 ,  A61P25/28 ,  A61P11/00 ,  A61P9/00

摘要： The present invention discloses compounds according to Formula I:

Wherein R 1a , R 1b , R 2 , R 4 , R 5 , R 6a , R 6b , R 7 , R 8 , W, X, Cy, and the subscript a are as defined herein.
The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), 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, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

摘要翻译： 本发明公开了根据式I的化合物：其中R 1a，R 1b，R 2，R 4，R 5，R 6a，R 6b，R 7，R 8，W，X，Cy和下标a如本文所定义。 本发明涉及抑制autotaxin的化合物（NPP2或ENPP2），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，用于预防和/或治疗涉及纤维化疾病，增殖性疾病，炎症 疾病，自身免疫疾病，呼吸系统疾病，心血管疾病，神经退行性疾病，皮肤病学和/或异常血管生成相关疾病。

公开(公告)号：EP3736270A1

公开(公告)日：2020-11-11

申请号：EP20183402.5

申请日：2018-09-13

申请人： AbbVie Overseas S.à r.l. ,  Galapagos N.V.

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

摘要： Compounds of Formula (I) are disclosed:

wherein A 1 , R 1 , R 2 , R 3 , R 4 , and n are as defined herein. Also disclosed is the use of the compounds in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering the compounds.

公开(公告)号：EP3269716B1

公开(公告)日：2020-09-16

申请号：EP17177371.6

申请日：2014-03-07

申请人： Galapagos N.V.

发明人： DESROY, Nicolas ,  HECKMANN, Bertrand ,  BRYS, Reginald, Christophe, Xavier ,  JONCOUR, Agnès, Marie ,  PEIXOTO, Christophe ,  BOCK, Xavier, Marie

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00 ,  A61P25/28 ,  A61P11/00 ,  A61P9/00

公开(公告)号：EP3865474A1

公开(公告)日：2021-08-18

申请号：EP21164249.1

申请日：2018-09-13

申请人： AbbVie Overseas S.à r.l. ,  Galapagos N.V.

发明人： ALTENBACH, Robert J ,  BOGDAN, Andrew ,  COUTY, Sylvain ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  HOUSSEMAN, Christopher Gaëtan ,  KYM, Philip R. ,  LIU, Bo ,  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. ,  MAI, Thi Thu Trang

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

摘要： 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 and pharmaceutical compositions comprising the same. Also disclosed are methods for their production and methods of treating cystic fibrosis by administering the compounds.

公开(公告)号：EP3760630A1

公开(公告)日：2021-01-06

申请号：EP20189787.3

申请日：2014-03-07

申请人： Galapagos N.V.

发明人： DESROY, Nicolas ,  HECKMANN, Bertrand ,  BRYS, Reginald, Christophe, Xavier ,  JONCOUR, Agnès, Marie ,  PEIXOTO, Christophe ,  BOCK, Xavier, Marie

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00 ,  A61P25/28 ,  A61P11/00 ,  A61P9/00

摘要： The present invention discloses compounds according to Formula I:

Wherein R 1a , R 1b , R 2 , R 4 , R 5 , R 6a , R 6b , R 7 , R 8 , W, X, Cy, and the subscript a are as defined herein.
The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), 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, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

公开(公告)号：EP3736267A1

公开(公告)日：2020-11-11

申请号：EP20183405.8

申请日：2018-09-13

申请人： AbbVie Overseas S.à r.l. ,  Galapagos N.V.

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

摘要： Compounds of Formula (I) are disclosed:

wherein A 1 , R 1 , R 2 , R 3 , R 4 , and n are as defined herein. Also disclosed is the use of the compounds in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering the compounds.

公开(公告)号：EP3976189A1

公开(公告)日：2022-04-06

申请号：EP20728465.4

申请日：2020-05-25

申请人： Galapagos N.V.

发明人： ALVEY, Luke, Jonathan ,  BUCHER, Denis ,  DESROY, Nicolas ,  JARY, Hélène, Marie ,  PEIXOTO, Christophe ,  TEMAL-LAÏB, Taoues ,  TIRERA, Amynata ,  BONNATERRE, Florence, Marie-Emilie ,  DUTHION, Béranger

IPC分类号： A61P29/00 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04 ,  A61P11/00 ,  A61K31/437 ,  A61P9/00 ,  A61P37/00