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    • 48. 发明授权
    • Triazolopyridine derivatives and their therapeutic use
    • 三唑并吡啶衍生物及其治疗用途
    • US08557797B2
    • 2013-10-15
    • US13201716
    • 2010-02-16
    • Harry FinchJohn MontanaMonique Bodil Van NielChi-Kit WooJamie KnightBohdan Waszkowycz
    • Harry FinchJohn MontanaMonique Bodil Van NielChi-Kit WooJamie KnightBohdan Waszkowycz
    • A61K31/535A01N43/54C07D413/04C07D239/02
    • C07D471/04
    • 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.
    • 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。