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公开(公告)号：WO2019105886A1
公开(公告)日：2019-06-06
申请号：PCT/EP2018/082537
申请日：2018-11-26
Applicant: GALAPAGOS NV
Inventor： ALVEY, Luke, Jonathan , ANNOOT, Denis, Maurice , BONNATERRE, Florence, Marie-Emilie , BUCHER, Denis , DUTHION, Béranger , JARY, Hélène , PEIXOTO, Christophe , TEMAL-LAIB, Taoues , TIRERA, Amynata
IPC: C07D403/04 , C07D471/04 , A61K31/437 , A61P9/00 , A61P37/00
Abstract: The present invention discloses compounds according to Formula (I): wherein R 1 , R 2 , R 3a , R 3b , X, Y 1 , Y 2 , Y 3 , and Z 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 inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of TNFα, interferons, IL-6, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
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Patent Agency Ranking
公开(公告)号：WO2020239658A1
公开(公告)日：2020-12-03
申请号：PCT/EP2020/064368
申请日：2020-05-25
Applicant: GALAPAGOS NV
Inventor： ALVEY, Luke, Jonathan , BUCHER, Denis , DESROY, Nicolas , JARY, Hélène, Marie , PEIXOTO, Christophe , TEMAL-LAÏB, Taoues , TIRERA, Amynata , BONNATERRE, Florence, Marie-Emilie , DUTHION, Béranger
IPC: A61P29/00 , A61P35/00 , C07D471/04 , C07D487/04 , A61P11/00 , A61K31/437 , A61P9/00 , A61P37/00
Abstract: The present invention discloses compounds according to Formula (I), wherein R 1a , R 1b , R 1c , R 2a , W 1 , W 2 , X 1 , X 2 , X 3 , Y, and Z 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 inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
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3.发明申请5-[3-[PIPERIDIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS 审中-公开5- [3- [哌啶-1-基] -3-氧代 - 丙基] - 咪唑并吡啶-2,4-二酮衍生物作为ADAMTS 4和5抑制剂用于治疗E.G. 骨性关节炎
公开(公告)号：WO2017211667A1
公开(公告)日：2017-12-14
申请号：PCT/EP2017/063272
申请日：2017-06-01
Applicant: GALAPAGOS NV , LES LABORATOIRES SERVIER
Inventor： LABÉGUÈRE, Frédéric, Gilbert , HENG, Rama , ALVEY, Luke, Jonathan , AMANTINI, David , BREBION, Franck, Laurent , DE CEUNINCK, Frédéric, André , DEPREZ, Pierre, Marc, Marie, Joseph , GOSMINI, Romain, Luc, Marie , JARY, Hélène , PEIXOTO, Christophe , POP-BOTEZ, Iuliana, Ecaterina , VARIN, Marie, Laurence, Claire
IPC: C07D401/06 , A61K31/4439 , A61K31/4178 , A61P19/02
Abstract: The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R 1 , R 2 , R 3a , R 3b , R 6a , R 6b , the subscript n and Cy are as defined herein. The present invention relates to compounds 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: 本发明公开了根据式（I）的5- [3- [哌嗪-1-基] -3-氧代 - 丙基] - 咪唑烷-2,4-二酮衍生物， R 1，R 2，R 3，R 3，R 3，R 6a，R 5，R 6，R 6， 下标n和Cy如本文所定义。 本发明涉及抑制ADAMTS 4和5的化合物，用于预防或治疗涉及软骨退化或软骨动态平衡破坏的炎性疾病或疾病，例如， 骨关节炎。
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4.发明申请5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS 审中-公开5 - [（PIPERAZIN-1-YL）-3-氧代丙基] - 咪达唑烷-2,4-二酮衍生物作为治疗OSTEOARTHRITIS的ADAMTS抑制剂
公开(公告)号：WO2016102347A1
公开(公告)日：2016-06-30
申请号：PCT/EP2015/080430
申请日：2015-12-18
Applicant: GALAPAGOS NV , LES LABORATOIRES SERVIER
Inventor： BREBION, Franck, Laurent , ALVEY, Luke, Jonathan , AMANTINI, David , DEPREZ, Pierre, Marc, Marie, Joseph , GOSMINI, Romain, Luc, Marie , JARY, Helène, Marie , PEIXOTO, Christophe , VARIN, Marie, Laurence, Claire , DE CEUNINCK, Frédéric, André , POP-BOTEZ, Iuliana, Ecaterina
IPC: C07D403/06 , A61K31/496 , A61P19/02 , A61P19/04
CPC classification number: C07D233/78 , A61K31/496 , A61K31/5377 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/12 , C07D417/12
Abstract: The present invention discloses compounds according to Formula (I), wherein R, R 2 , R 3a , R 3b , and Cy are as defined herein. The present invention discloses compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same and methods for the prophylaxis and/or treatment of inflammatory conditions and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis.
Abstract translation: 本发明公开了根据式（I）的化合物，其中R，R2，R3a，R3b和Cy如本文所定义。 本发明公开了抑制ADAMTS的化合物，其制备方法，包含其的药物组合物以及预防和/或治疗软骨降解和/或破坏软骨体内平衡的炎性病症和/或疾病的方法。
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5.发明申请(5R)-5-[3-[(3S)-4-(4-CHLORO-3-METHOXY-5-METHYL-PHENYL)-3-METHYL-PIPERAZIN-1-YL]- 3-OXO-PROPYL]-5-METHYL-IMIDAZOLIDINE-2,4-DIONE AS ADAMTS 4 AND 5 INHIBITOR FOR TREATING E.G. OSTEOARTHRITIS 审中-公开（5R）-5- [3 - [（3S）-4-（4-氯-3-甲氧基-5-甲基 - 苯基）-3-甲基 - 哌嗪-1-基] -3-氧代 - 丙基] - 作为ADAMTS 4和5抑制剂的5-甲基咪唑啉-2,4-二酮用于治疗EG 骨性关节炎
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。
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6.发明申请5-[3-[PIPERAZIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS 审中-公开5- [3- [哌嗪-1-基] -3-氧代 - 丙基] - 咪唑并吡啶-2,4-二酮衍生物作为ADAMTS 4和5抑制剂用于治疗E.G. 骨性关节炎
公开(公告)号：WO2017211666A1
公开(公告)日：2017-12-14
申请号：PCT/EP2017/063271
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
IPC: C07D233/95 , A61K31/496 , A61K31/4178 , A61P19/02
Abstract: The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R 1 , R 2 , R 3a , R 3b , R 6a , R 6b , the subscript n and Cy are as defined herein. The present invention relates to compounds 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: 本发明公开了根据式（I）的5- [3- [哌嗪-1-基] -3-氧代 - 丙基] - 咪唑烷-2,4-二酮衍生物， R 1，R 2，R 3，R 3，R 3，R 6a，R 5，R 6，R 6， 下标n和Cy如本文所定义。 本发明涉及抑制ADAMTS 4和5的化合物，用于预防或治疗涉及软骨退化或软骨动态平衡破坏的炎性疾病或疾病，例如， 骨关节炎。
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