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    Benzodiazepine derivatives that inhibit rock
    11.
    发明授权
    Benzodiazepine derivatives that inhibit rock 失效
    抑制岩石的苯二氮卓衍生物

    公开(公告)号：US07888503B2

    公开(公告)日：2011-02-15

    申请号：US11577444

    申请日：2005-10-18

    申请人： Michael John Alberti ,  David Kendall Jung

    发明人： Michael John Alberti ,  David Kendall Jung

    IPC分类号： C07D243/14 ,  A61K31/5513

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D409/14

    摘要： The present invention relates to dihydrobenzodiazepine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dihydrobenzodiazepine derivatives are useful in the treatment of diseases associated with inappropriate ROCK kinase.

    摘要翻译： 本发明涉及二氢苯并二氮杂衍生物，含有它们的组合物和药物，以及这些化合物，组合物和药物的制备和用途的方法。 这样的二氢苯并二氮杂衍生物可用于治疗与不适当的ROCK激酶相关的疾病。

    Process for the preparation of chemical compounds
    15.
    发明授权
    Process for the preparation of chemical compounds 失效
    化合物的制备方法

    公开(公告)号：US06756498B2

    公开(公告)日：2004-06-29

    申请号：US10258679

    申请日：2002-10-25

    申请人： Russ N. Fitzgerald ,  David Kendall Jung ,  John F Eaddy

    发明人： Russ N. Fitzgerald ,  David Kendall Jung ,  John F Eaddy

    IPC分类号： C07D47104

    CPC分类号： C07D401/04 ,  C07D471/04

    摘要： The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulfonyl, C1-6alkoxy substituted by one or more fluorine atoms, halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is H or phenyl substituted by SO2C1-6alkyl or SO2NH2; R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups R6, or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring R6 is halogen, C1-6alkyl, C1-6alkoxy or C1-6alkoxy substituted by one or more fluorine atoms; which comprises rearrangement of an azirine of formula (II)  wherein R0 to R3 are as defined for formula (I), or a protected derivative thereof, in the presence of a catalyst and a solvent.

    摘要翻译： 本发明提供了制备式（I）化合物及其药学上可接受的衍生物的方法，其中：R 0和R 1独立地选自H，卤素，C 1-6烷基，C 1-6烷氧基或C 1-6烷氧基 被一个或多个氟原子取代; R 2是H，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（ O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，卤素，CN，CONR 4 R 5，CO 2 H，CO 2 C 1-6烷基或NHSO 2 R 4; R 3， 是H或被SO 2 C 1-6烷基或SO 2 NH 2取代的苯基; R 4和R 5独立地选自H，C 1-6烷基，苯基，被一个或多个原子或基团R 6取代的苯基，或与 它们所连接的氮原子形成饱和的4至8元环R 6是卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基;其包括将式 II）其中R 0至R 3为 如式（I）所定义，或其保护的衍生物在催化剂和溶剂的存在下反应。

    PYRIDOPYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USES AS ANTI-CANCER AND ANTI-DIABETE DRUGS
    16.
    发明申请
    PYRIDOPYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USES AS ANTI-CANCER AND ANTI-DIABETE DRUGS 审中-公开
    吡咯并吡嗪化合物及其作为抗癌剂和抗糖尿病药物的用途

    公开(公告)号：US20090054471A1

    公开(公告)日：2009-02-26

    申请号：US11815798

    申请日：2006-02-09

    申请人： David Kendall Jung ,  Michael John Alberti

    发明人： David Kendall Jung ,  Michael John Alberti

    IPC分类号： A61K31/519 ,  C07D471/14

    CPC分类号： C07D471/14

    摘要： The present invention relates to pyridopyrazolopyrimidine derivatives that are useful pharmacological agents through the inhibition or antagonism of protein kinases, and to processes for the preparation and use of the same. In particular, the present invention relates to compounds that demonstrate protein tyrosine kinase and/or protein serine/threonine kinase inhibition.

    摘要翻译： 本发明涉及通过抑制或拮抗蛋白激酶而成为有用的药理学的吡哆吡唑并嘧啶衍生物及其制备和使用方法。 特别地，本发明涉及证明蛋白酪氨酸激酶和/或蛋白丝氨酸/苏氨酸激酶抑制的化合物。

    Chemical Compounds
    17.
    发明申请
    Chemical Compounds 审中-公开
    化学化合物

    公开(公告)号：US20080275062A1

    公开(公告)日：2008-11-06

    申请号：US10597473

    申请日：2005-01-28

    申请人： David Harold Drewry ,  David Kendall Jung ,  James Andrew Linn ,  Robert Neil Hunter ,  Dennis Lee ,  Robert A. Stavenger ,  Clark Sehon

    发明人： David Harold Drewry ,  David Kendall Jung ,  James Andrew Linn ,  Robert Neil Hunter ,  Dennis Lee ,  Robert A. Stavenger ,  Clark Sehon

    IPC分类号： A61K31/4409 ,  C07D213/04 ,  A61K31/415 ,  C07D231/10 ,  C07D239/42 ,  A61K31/505 ,  C07D239/24 ,  C07D231/56 ,  C07D401/10

    CPC分类号： C07D213/56 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D239/42 ,  C07D403/04

    摘要： There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-4alkyl, C1-4alkanoyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy and C1-4alkoxycarbonyl; and X is indazolyl, pyrazolyl or a group: wherein G is CH or N; and Y1 and Y2 are independently hydrogen, halogen and a group NR5R6 (wherein R5 and R6 are independently hydrogen, C1-6alkyl or C2-6alkenyl).

    摘要翻译： 提供式（I）化合物及其盐，溶剂化物和生理功能衍生物：其中R1是氢或C 1-6烷基; n为1,2,3或4; R2是芳基，任选地被一个或两个选自卤素，羟基，氰基，C 1-4烷基，C 1-4烷氧基，C 1-4烷基， 烷基，卤代C 1-4烷基，卤代C 1-4烷氧基，芳基，芳氧基，C 1-4烷基， 烷氧基羰基，C 1-4烷基磺酰基和基团R 3 R 4 NSO 2（其中R 3和R 4独立地是氢或C 1-4烷基 ）和5-或6-元杂芳基; 或n为0，并且R 1和R 2与它们连接的氮原子一起形成5-或6-元单环杂环或9-或10-元双环杂环，其中至少含有 R 1和R 2连接的氮原子是非芳族的，其中5或6元单环杂环或9或10元双环杂环任选被一个或两个选自以下的基团取代： 卤素，羟基，氰基，氧代，C 1-4烷基，C 1-4烷酰基，C 1-4烷氧基，卤代C 1-4烷基， 烷基，卤代C 1-4烷氧基，芳基，芳氧基和C 1-4烷氧基羰基; 并且X是吲唑基，吡唑基或基团：其中G是CH或N; 和Y 1和Y 2独立地是氢，卤素和基团NR 5 R 6（其中R 5和R 6独立地是氢，C 1-6烷基 或C 2-6烯基）。