公开(公告)号：WO2017211668A1

公开(公告)日：2017-12-14

申请号：PCT/EP2017/063273

申请日：2017-06-01

Applicant: GALAPAGOS NV ,  LES LABORATOIRES SERVIER

Inventor： LABÉGUÈRE, Frédéric, Gilbert ,  HENG, Rama ,  DE CEUNINCK, Frédéric, André ,  ALVEY, Luke, Jonathan ,  AMANTINI, David ,  BREBION, Franck, Laurent ,  DEPREZ, Pierre, Marc, Marie, Joseph ,  GOSMINI, Romain, Luc, Marie ,  JARY, Hélène ,  PEIXOTO, Christophe ,  POP-BOTEZ, Iuliana, Ecaterina ,  VARIN, Marie, Laurence, Claire ,  COMAS MARTINEZ, Daniel

IPC: C07D233/95 ,  A61K31/496 ,  A61K31/4178 ,  A61P19/02

Abstract: The present invention discloses (5R)-5-[3-[(3S)-4-(4-chloro-3-methoxy-5-methyl-phenyl)-3-methyl-piperazin-l-yl]-3-oxo-propyl]-5-methyl-imidazolidine-2,4-dione according to Formula (I). The present invention relates to the compound of formula (I) inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or disruption of cartilage homeostasis, such as e.g. osteoarthritis.

Abstract translation: 本发明公开了（5R）-5- [3 - [（3S）-4-（4-氯-3-甲氧基-5-甲基 - 苯基）-3-甲基 - 哌嗪-1-基] 哌啶-1-基] -3-氧代 - 丙基] -5-甲基 - 咪唑烷-2,4-二酮。 本发明涉及抑制ADAMTS 4和5的式（I）化合物用于预防或治疗涉及软骨退化或软骨动态平衡破坏的疾病或疾病，例如， 骨关节炎。

公开(公告)号：WO2020173739A1

公开(公告)日：2020-09-03

申请号：PCT/EP2020/054122

申请日：2020-02-17

Applicant: GALAPAGOS NV

Inventor： BEAUMONT, Stéphane, Nicolas, Alain ,  BOCK, Xavier, Marie ,  COMAS MARTINEZ, Daniel ,  JONCOUR, Agnès, Marie ,  LABÉGUÈRE, Frédéric, Gilbert ,  LÓPEZ RAMOS, Miriam ,  TEMAL-LAÏB, Taoues

IPC: C07D471/04 ,  A61P3/00 ,  A61P5/00 ,  A61P9/00 ,  A61K31/437

Abstract: The present invention discloses compounds according to Formula I: wherein R 1 , R 2 , R 3a , R 3b , Het, X and the subscript n 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 endocrine, nutritional, metabolic, and/or cardiovascular diseases by administering the compound of the invention.