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18 条记录 (耗时 0.031 秒)

    Process for the preparation of chemical compounds
    1.
    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。

    CHEMICAL COMPOUNDS
    2.
    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
    3.
    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
    9.
    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。