Pyrazolo[3,4-b]pyridine compounds, and their use as a PDE4 inhibitors
    7.
    发明申请
    Pyrazolo[3,4-b]pyridine compounds, and their use as a PDE4 inhibitors 审中-公开
    吡唑并[3,4-b]吡啶化合物,以及它们作为PDE4抑制剂的用途

    公开(公告)号:US20090131431A1

    公开(公告)日:2009-05-21

    申请号:US12067990

    申请日:2006-09-29

    CPC分类号: C07D471/04

    摘要: The invention provides a compound of formula (I) or a salt thereof: wherein R2 is H, C1-3alkyl, n-butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl-, —CN, or —CH2OH; R3 is inter alia optionally substituted C4-7cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); Ra is H, methyl or ethyl; Rb is H or methyl; R4 is H, methyl, ethyl, n-propyl, —C(O)-Me, or —C(O)—C1fluoroalkyl; and R5 is: —C(O)—(CH2)n—Ar, —C(O)-Het, —C(O)—C1-6alkyl, —C(O)—C1 fluoroalkyl, —C(O)—(CH2)2—C(O)—NR15bNR15b, —C(O)—CH2—C(O)—NR15bNR15b, —C(O)—NR15b—(CH2)m1—Ar, —C(O)—NR15b—Het, —C(O)—NR15b—C1-6alkyl, —C(O)—NR5aR5b, —S(O)2—(CH2)m2—Ar, —S(O)2-Het, —S(O)2—C1-6alkyl, or —CH2—Ar; or R4 and R5 taken together are —(CH2)p1—, —(CH2)2—X5—(CH2)2—, —C(O)—(CH2)p2—, —C(O)—N(R15)—(CH2)p3—; or NR4R5 is of sub-formula (y), (y1), (y2) or (y3). The invention provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as COPD and the like.

    摘要翻译: 本发明提供式(I)化合物或其盐:其中R2是H,C1-3烷基,正丁基,C1-2氟烷基,环丙基,环丁基,(环丙基)甲基,-CN或-CH2OH; R3特别是任选取代的C 4-7环烷基或任选取代的杂环基团(aa),(bb)或(cc); Ra是H,甲基或乙基; Rb是H或甲基; R 4是H,甲基,乙基,正丙基,-C(O)-Me或-C(O)-C 1-6氟烷基; 并且R 5是:-C(O) - (CH 2)n -Ar,-C(O)-Het,-C(O)-C 1-6烷基,-C(O)-C 1氟代烷基,-C(O) (CH 2)2 -C(O)-NR 15 b N R 15 b,-C(O)-CH 2 -C(O)-NR 15 b NR 15 b,-C(O)-NR 15 b - (CH 2)m -Ar,-C(O) C(O)-NR 15 b -C 1-6烷基,-C(O)-NR 5 R 5a,-S(O)2 - (CH 2)m -Ar,-S(O)2 -Het,-S(O) 2-C 1-6烷基或-CH 2 -Ar; 或(R 4)和R 5和R 5一起为 - (CH 2)p1 - , - (CH 2)2 -X 5 - (CH 2)2 - , - - (CH 2)p3-; 或NR4R5为子式(y),(y1),(y2)或(y3)。 本发明提供了化合物作为IV型磷酸二酯酶抑制剂(PDE4)和/或用于治疗和/或预防炎性和/或过敏性疾病如COPD等的用途。