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    Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors
    7.
    发明申请
    Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors 失效
    吡唑并[3,4-b]吡啶化合物及其作为PDE4抑制剂的用途

    公开(公告)号：US20080058369A1

    公开(公告)日：2008-03-06

    申请号：US11831325

    申请日：2007-07-31

    Applicant: David Allen ,  Rodger Barnett ,  Reshma Chudasama ,  Caroline Day ,  Christopher Edlin ,  Leanda Kindon

    Inventor： David Allen ,  Rodger Barnett ,  Reshma Chudasama ,  Caroline Day ,  Christopher Edlin ,  Leanda Kindon

    IPC: A61K31/437 ,  A61P29/00 ,  A61P37/08 ,  C07D471/04

    CPC classification number: C07D471/04

    Abstract: The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-4-({8-[(2-hydroxyethyl)(methyl)amino]octanoyl}amino)benzamide, whose formula is , or a salt thereof, such as the monohydrochloride salt thereof. The invention also provides the use of the compound or salt as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, or rhinitis (e.g. allergic and/or non-allergic rhinitis).

    Abstract translation: 本发明提供N - {[1,6-二乙基-4-（四氢-2H-吡喃-4-基氨基）-1H-吡唑并[3,4-b]吡啶-5-基]甲基} -4 - （{ 8 - [（2-羟乙基）（甲基）氨基]辛酰基}氨基）苯甲酰胺或其盐，如其一盐酸盐。 本发明还提供了化合物或盐作为磷酸二酯酶IV（PDE4）的抑制剂和/或用于治疗和/或预防炎性和/或过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘或 鼻炎（例如过敏性和/或非过敏性鼻炎）。

    Azaindoles
    9.
    发明授权
    Azaindoles 有权
    楝树

    公开(公告)号：US06770643B2

    公开(公告)日：2004-08-03

    申请号：US10178667

    申请日：2002-06-24

    Applicant: Paul J Cox ,  Tahir N. Majid ,  Justine Y. Q. Lai ,  Andrew D. Morley ,  Shelley Amendola ,  Stephanie D. Deprets ,  Christopher Edlin

    Inventor： Paul J Cox ,  Tahir N. Majid ,  Justine Y. Q. Lai ,  Andrew D. Morley ,  Shelley Amendola ,  Stephanie D. Deprets ,  Christopher Edlin

    IPC: C07D47104

    CPC classification number: A61K31/4985 ,  A61K31/437 ,  C07D471/04 ,  C07D487/04

    Abstract: The invention is directed to compositions containing physiologically active compounds of general formula (I): wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, —Z1R8, —C(═O)—NY3Y4, —CO2R8, —NY3Y4, —N(R6)—C(═O)—R7, —N(R6)—C(═O)—NY3Y4, —N(R6)—C(═O)—OR7, —N(R6)—SO2—R7, —N(R6)—SO2—NY3Y4 and one or more halogen a toms ; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, —C(═O)—OR5 or —C(═O)—NY3Y; and X1 represents N, CH, C-halo, C—CN, C—R7, C—NY3Y4, C—OH, C—Z2R7, C—C(═O)—OR5, C—C(═O)—NY3Y4, C—N(R8)—C(═O)—R7, C—SO2—NY3Y4, C—N(R8)—SO2—R7, C-alkenyl, C-alkynyl or C—NO2; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

    Abstract translation: 本发明涉及含有通式（I）的生理活性化合物的组合物：其中R 1是芳基或杂芳基; R 2表示氢，酰基，氰基，卤素，低级烯基或任选被选自氰基，杂芳基，杂环烷基，-Z 1 R 8，-C（= O）-NY 3，Y 4，-CO 2 R 8，-NY 3 Y 4，-N（R 6）-C（= O）-R 7，-N（R 6） ）-C（= O）-NY 3 Y 4，-N（R 6）-C（= O）-OR 7，-N（R 6）-SO 2 -R 7，-N（R 6）-SO 2 -NY 3 Y 4和一个或多个卤素; R 3表示氢，芳基，氰基，卤素，杂芳基，低级烷基，-C（= O）-OR 5或-C（= O）-NY 3 Y; 并且X 1表示N，CH，C - 卤素，C-CN，CR 7，C-NY 3 Y 4，C-OH，CZ 2 R 7，CC（= O）-OR 5，CC（= O）-NY 3 Y 4，CN（R 8）-C（= O）-R 7，C-SO 2 -YN 3， Y 4，CN（R 8）-SO 2 -R 7，C-烯基，C - 炔基或C-NO 2; 和它们的前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物性质，特别是抑制蛋白激酶的能力。

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