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    Pyrazolo[3,4-b] pyridine compounds, and their use as phosphodiesterase inhibitors
    4.
    发明申请
    Pyrazolo[3,4-b] pyridine compounds, and their use as phosphodiesterase inhibitors 审中-公开
    吡唑并[3,4-b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途

    公开(公告)号：US20060089375A1

    公开(公告)日：2006-04-27

    申请号：US10527866

    申请日：2003-09-12

    申请人： David Allen ,  Diane Coe ,  Caroline Cook ,  Michael Dowle ,  Christophen Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Richard Knowles ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  Peter Ward

    发明人： David Allen ,  Diane Coe ,  Caroline Cook ,  Michael Dowle ,  Christophen Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Richard Knowles ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  Peter Ward

    IPC分类号： C07D471/02 ,  A61K31/4745

    CPC分类号： C07D471/04

    摘要： The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is C1-4alkyl, C1-3fluoroalkyl, —CH2CH2OH or —CH2CH2CO2C1-2alkyl; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

    摘要翻译： 本发明涉及式（I）化合物或其盐：其中：R 1是C 1-4烷基，C 1-3烷基， 氟代烷基，-CH 2 CH 2 OH或-CH 2 CH 2 CO 2， C 1-12烷基; R 2是氢原子（H），甲基或C 1氟代烷基; R 3是任选取代的C 3-8环烷基或任选取代的单不饱和C 5〜5-7环烯基或任选取代的杂环基 子公式（aa），（bb）或（cc）; 其中n 1和n 2独立地为1或2; 并且其中Y是O，S，SO 2或NR 10; 或R 3是双环基（dd）或（ee）：其中X是NR 4 R 5或OR 5a 。 这些化合物是磷酸二酯酶（PDE）抑制剂，特别是PDE4抑制剂。 还提供了式（I）化合物或其药学上可接受的盐在制备用于治疗和/或预防哺乳动物例如人的炎性和/或过敏性疾病的药物中的用途， 例如慢性阻塞性肺疾病（COPD），哮喘或过敏性鼻炎。