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公开(公告)号：EP3283114A1
公开(公告)日：2018-02-21
申请号：EP16712378.5
申请日：2016-03-31
申请人： Galapagos NV
CPC分类号： A61K31/541 , A61K31/54 , A61K45/06 , A61P3/06 , A61P9/10
摘要： The present invention discloses compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate or the salt of a solvate thereof, pharmaceutical compositions comprising the same, and methods of treatment using the same, for use in the prophylaxis and/or treatment of cardiovascular disorders and/or dyslipidemia, by administering the compound according to Formula (I).
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42.发明公开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 - [（哌嗪-1-基）-3-氧代 - 丙基] - 咪唑并吡啶-2,4-二酮衍生物作为ADAMTS抑制剂治疗骨关节炎的药物
公开(公告)号：EP3237406A1
公开(公告)日：2017-11-01
申请号：EP15813831.3
申请日：2015-12-18
发明人： 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分类号： C07D403/06 , A61K31/496 , A61P19/02 , A61P19/04
CPC分类号： C07D233/78 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/12 , C07D417/12
摘要： The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a 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，R 2，R 3a，R 3b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用于预防和/或治疗涉及软骨降解和/或软骨内稳态破坏的炎症和/或疾病的方法。
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43.发明授权NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF CYSTIC FIBROSIS 有权新型化合物及其药物组合物用于治疗囊性纤维化
公开(公告)号：EP2994463B1
公开(公告)日：2017-10-25
申请号：EP14726516.9
申请日：2014-05-06
申请人： Galapagos NV
发明人： VAN DER PLAS, Steven , MAMMOLITI, Oscar , MENET, Christel , TRICARICO, Giovanni , DE BLIECK, Ann , JOANESSE, Caroline , DE MUNCK, Tom , KELGTERMANS, Hans
IPC分类号： C07D333/36 , A61K31/381 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , A61P43/00
CPC分类号： 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
摘要： The present invention discloses compounds according to Formula I: wherein R1, R2, R3, 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.
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公开(公告)号：EP3212184A1
公开(公告)日：2017-09-06
申请号：EP15854248.0
申请日：2015-10-29
申请人： Abbvie S.a.r.l. , Galapagos NV
发明人： KYM, Philip R. , WANG, Xueqing , SEARLE, Xenia B. , LIU, Bo , YEUNG, Ming C.
IPC分类号： A61K31/36 , A61K31/351 , A61P11/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts or radiolabelled forms thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and m are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
摘要翻译： 其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12和m如说明书中所定义的式（I）化合物及其药学可接受的盐或放射标记的形式是有用的 用于治疗由囊性纤维化跨膜电导调节剂（CFTR）蛋白阻止或改善的病症或障碍。 描述了制备这些化合物的方法。 还描述了式（I）化合物的药物组合物，以及使用这些化合物和组合物的方法。
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45.发明公开MOLECULAR TARGETS AND COMPOUNDS, AND METHODS TO IDENTIFY THE SAME, USEFUL IN THE TREATMENT OF DISEASES ASSOCIATED WITH EPITHELIAL MESENCHYMAL TRANSITION 审中-公开分子靶点的化合物和方法IT中的用途疾病的诊治上皮 - 间质转化相关的识别
公开(公告)号：EP2972381A2
公开(公告)日：2016-01-20
申请号：EP14708867.8
申请日：2014-03-07
申请人： Galapagos NV
CPC分类号： G01N33/5073 , A01K67/027 , A01K2207/10 , A01K2207/30 , A01K2227/105 , A01K2267/03 , C07K16/18 , C07K16/40 , C12N15/111 , C12N15/113 , C12N15/1137 , C12N15/1138 , C12N2310/11 , C12N2310/111 , C12N2310/12 , C12N2310/14 , C12N2310/141 , C12N2310/531 , C12N2320/10 , C12N2320/12 , C12N2320/30 , C12Q1/6883 , C12Q1/6886 , C12Q2600/158 , C12Y204/0203 , C12Y207/11001 , C12Y207/11015 , C12Y207/12001 , G01N33/5011 , G01N33/5044 , G01N2333/70596 , G01N2333/78 , G01N2333/96486 , G01N2500/04 , G01N2500/10
摘要： The present invention relates to methods and assays for identifying agents useful in the treatment of diseases associated with epithelial mesenchymal transition(EMT), in particular fibrotic diseases and cancer. The invention provides polypeptide and nucleic acid TARGETs, siRNA sequences based on these TARGETs and antibodies against the TARGETs. The invention is further related to pharmaceutical composition comprising siRNA sequences based on the TARGETs and antibodies against the TARGETs for use in the treatment of diseases associated withepithelial mesenchymal transition, in particular fibrotic disease and cancer. The invention further provides
in vitro methods for inhibition of epithelial mesenchymal transition.-
公开(公告)号：EP3649119B1
公开(公告)日：2021-11-03
申请号：EP18732777.0
申请日：2018-06-21
发明人： 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分类号： C07D401/14 , C07D405/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D471/04 , A61K31/502 , A61P29/00
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公开(公告)号：EP3416983B1
公开(公告)日：2021-04-07
申请号：EP17705873.2
申请日：2017-02-17
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48.发明授权
公开(公告)号：EP3102575B1
公开(公告)日：2021-01-13
申请号：EP15704974.3
申请日：2015-02-04
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公开(公告)号：EP3212189B1
公开(公告)日：2020-09-09
申请号：EP15854320.7
申请日：2015-10-28
发明人： KYM, Philip R. , WANG, Xueqing , SEARLE, Xenia B. , LIU, Bo , YEUNG, Ming C. , ALTENBACH, Robert J. , VOIGHT, Eric , BOGDAN, Andrew , KOENIG, John R. , GRESZLER, Stephen N.
IPC分类号： A61K31/44 , C07D471/04 , C07D311/58 , A61K31/397 , A61K31/4025 , A61K31/435 , A61K31/436 , A61K31/4433 , A61K31/453 , A61K31/5377 , A61P11/00
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公开(公告)号：EP3286191B1
公开(公告)日：2020-07-29
申请号：EP16720370.2
申请日：2016-04-19
申请人： Galapagos NV
发明人： MENET, Christel, Jeanne, Marie , DOYON, Julien, Georges, Pierre-Olivier , CLAES, Pieter, Isabelle, Roger , ALLART, Brigitte , DE WACHTER, Maxim, Maria, Paul , TRICARICO, Giovanni, Alessandro
IPC分类号： C07D471/04 , C07D519/00 , A61K31/4375 , A61P29/00
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