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公开(公告)号:EP3312170A1
公开(公告)日:2018-04-25
申请号:EP16814361.8
申请日:2016-06-21
IPC分类号: C07D401/12 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号: C07C233/88 , A61P35/02 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1') wherein ring Q 1 is optionally-substituted C 6-10 aryl group, etc.; R 1 and R 2 are independently hydrogen atom, etc.; W 1 is optionally-substituted C 1-4 alkylene group; W 2 is -NR 3a C(O)- wherein R 3a is hydrogen atom or C 1-6 alkyl group, etc.; ring Q 2 is 5- to 10-membered heteroaryl group, etc.; W 3 is optionally-substituted C 1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R 4 is independently halogen atom, optionally-substituted C 1-6 alkyl group, etc.; R 5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.
摘要翻译: 本发明提供了式(1')的1,4-二取代的咪唑衍生物,其中环Q1是任选取代的C6-10芳基等。 R 1和R 2独立地为氢原子等; W 1是任选取代的C 1-4亚烷基; W2为-NR3aC(O) - ,其中R3a为氢原子或C1-6烷基等; 环Q2为5至10元杂芳基等; W3是任选取代的C1-4亚烷基等; n是1,2,3,4或5; R4独立地为卤素原子,任选取代的C1-6烷基等; R5是羟基等; 及其药理学上可接受的盐,其对癌细胞的球形成能力具有有效的抑制作用,并且可用作口服可用的抗肿瘤剂。
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公开(公告)号:EP3450433A1
公开(公告)日:2019-03-06
申请号:EP17789569.5
申请日:2017-04-25
IPC分类号: C07D473/22 , A61K31/52 , A61K31/5377 , A61P37/06 , A61P43/00 , C07D487/04 , C07D519/00
摘要: The present invention relates to a substituted purine derivative of formula (1) wherein R 1 is alkoxy or the like, R 2 is alkyl or the like, Ring Q 1 is aryl or the like, W 1 is alkylene or the like, Ring Q 2 is aromatic carbocyclyl or the like, n is 1 - 4, R 3 is hydrogen atom or the like, X 1 is single bond or the like, W 2 is alkylene or the like, and R 4 is hydrogen atom or the like, or a pharmaceutically acceptable salt thereof, which has a potent inhibitory effect against TLR7, and thereby is useful for treating autoimmune disease.
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