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    Chemical Compounds
    1.
    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）。

    CHEMICAL COMPOUNDS
    5.
    发明申请
    CHEMICAL COMPOUNDS 失效
    化学化合物

    公开(公告)号：US20090143366A1

    公开(公告)日：2009-06-04

    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： A61K31/5513 ,  C07D401/10

    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。

    Short-acting benzodiazepines
    6.
    发明授权
    Short-acting benzodiazepines 有权
    短效苯二氮卓类

    公开(公告)号：US07528127B2

    公开(公告)日：2009-05-05

    申请号：US11650636

    申请日：2007-01-05

    申请人： Paul L. Feldman ,  David Kendall Jung ,  Istvan Kaldor ,  Gregory J. Pacofsky ,  Jeffrey A. Stafford ,  Jeffrey H. Tidwell

    发明人： Paul L. Feldman ,  David Kendall Jung ,  Istvan Kaldor ,  Gregory J. Pacofsky ,  Jeffrey A. Stafford ,  Jeffrey H. Tidwell

    IPC分类号： A61P25/20 ,  A61K31/5517 ,  C07D487/02

    CPC分类号： C07D243/20 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D487/04

    摘要： It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.

    摘要翻译： 现在已经发现，如在含有羧酸酯部分的式（I）的苯并二氮杂衍生物中所述的本发明化合物，由此能够在器官非依赖性消除机制中被非特异性组织酯酶灭活，从而提供更可预测和 可重现的药效学特征。 本发明的化合物适用于治疗目的，包括镇静催眠，抗焦虑药，肌肉松弛剂和抗惊厥药物，并可用于在以下临床环境中静脉内施用：术前镇静，抗焦虑和围手术期的遗忘用途; 短期诊断，手术或内窥镜手术中有意义的镇静; 作为全身麻醉的诱导和维持的组成部分，先前和/或伴随其他麻醉剂的施用; ICU镇静。

    Benzodiazepine derivatives that inhibit rock
    10.
    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。