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    TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE
    3.
    发明申请
    TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE 失效
    三唑吡啶衍生物及其治疗用途

    公开(公告)号：US20120088763A1

    公开(公告)日：2012-04-12

    申请号：US13201716

    申请日：2010-02-16

    Applicant: Harry Finch ,  John Montana ,  Monique Bodil Van Niel ,  Chi-Kit Woo ,  Jamie Knight ,  Bohdan Waszkowycz

    Inventor： Harry Finch ,  John Montana ,  Monique Bodil Van Niel ,  Chi-Kit Woo ,  Jamie Knight ,  Bohdan Waszkowycz

    IPC: A61K31/5377 ,  A61P11/00 ,  A61P11/06 ,  C07D471/04 ,  A61K31/437

    CPC classification number: C07D471/04

    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(═O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as defined in the claims.

    Abstract translation: 式（I）化合物是p38MAP激酶的抑制剂，其可用作治疗特别是呼吸道疾病的抗炎剂，其中： R 1是C 1 -C 6烷基，C 3 -C 6环烷基，任选取代的苯基，任选被取代的5-或6-元单环杂芳基，或其中n是1或2的式（II）基团，R 3和R 4是 独立地是H或C 1 -C 6烷基，或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6元杂环; Y是-O-或-S（O）p - ，其中p是0,1或2; A是任选取代的二价亚芳基，或单环或双环亚杂芳基或具有5或6个环原子的C 3 -C 6二价亚环烷基或哌啶子基，其中环氮连接至R 2 NHC（= O）W - ; W是键，-NH-或-C（RA）（RB），其中RA和RB独立地是H，甲基，乙基，氨基，羟基或卤素; 并且R 2是如权利要求中所定义的基团。

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