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    • 6. 发明申请
    • MACROCYCLIC COMPOUNDS AS IRAK4 INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISEASES
    • 作为IRAK4抑制剂治疗炎性疾病的大环化合物
    • WO2014143672A1
    • 2014-09-18
    • PCT/US2014/027722
    • 2014-03-14
    • BIOGEN IDEC MA INC.
    • JENKINS, TracyVESSELS, Jeffery
    • C07D498/18C07D498/22C07D513/18C07D513/22C07D471/22A61K31/439A61P29/00
    • C07D513/22C07D471/22C07D498/18C07D498/22C07D513/18
    • Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein i.a. Ring A is phenylene or 5- to 6-membered heteroarylene; Ring B is phenylene, 5- to 6-membered heterocycloalkylene or 5- to 6-membered heteroarylen; R 4 is absent, heteroarylene, arylene, C1-3 alkylene, or R 4 and R 3 taken together with the nitrogen to which they are bound form a 3- to 7-membered heterocycloalkyl ring; R 5 is absent, C(0)NR 51 , NR 52 or 0; R 6 is C2-10 alkylene or alkenylene, wherein one or two of the carbon atoms in the alkylene chain is optionally replaced by an 0, S, SO, SO 2 or NR 61 , and wherein two of the carbon atoms in the alkylene chain are optionally connected by a two or three carbon atom alkylene chain to form a 5- to 7-membered ring; R 7 is absent, NR 71 or O. The compounds are IRAK4 inhibitors useful for the treatment of inflammatory diseases.
    • 提供式(I)的化合物或其药学上可接受的盐,其中i.a. 环A是亚苯基或5-至6-元杂亚芳基; 环B是亚苯基,5-至6-元杂环亚烷基或5-至6-元杂芳基; R4不存在,杂亚芳基,亚芳基,C 1-3亚烷基,或者R 4和R 3与它们所连接的氮一起形成3-至7-元杂环烷基环; R5不存在,C(0)NR51,NR52或0; R 6是C 2-10亚烷基或亚烯基,其中亚烷基链中的一个或两个碳原子任选被0,S,SO,SO 2或NR 61取代,并且其中亚烷基链中的两个碳原子任选连接 通过两个或三个碳原子的亚烷基链形成5-至7-元环; R7不存在,NR71或O.化合物是可用于治疗炎性疾病的IRAK4抑制剂。