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10 条记录 (耗时 0.033 秒)

    Benzimidazole and its ribonucleoside
    3.
    发明授权
    Benzimidazole and its ribonucleoside 有权
    苯并咪唑及其核糖核苷

    公开(公告)号：US06307043B1

    公开(公告)日：2001-10-23

    申请号：US09489098

    申请日：2000-01-21

    申请人： Stanley Dawes Chamberlain ,  Jeffrey H. Tidwell

    发明人： Stanley Dawes Chamberlain ,  Jeffrey H. Tidwell

    IPC分类号： C07H1904

    CPC分类号： C07D235/30 ,  C07H19/052

    摘要： The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.

    摘要翻译： 本发明涉及苯并咪唑衍生物及其在药物治疗中的用途，特别是用于治疗或预防诸如由疱疹病毒引起的病毒感染的病毒感染。 本发明还涉及苯并咪唑衍生物的制备和含有它们的药物制剂。

    Benzimidazole derivatives for the treatment of viral infections
    5.
    发明授权
    Benzimidazole derivatives for the treatment of viral infections 失效
    苯并咪唑衍生物用于治疗病毒感染

    公开(公告)号：US06413938B1

    公开(公告)日：2002-07-02

    申请号：US09367260

    申请日：1999-08-25

    申请人： Jeffrey H. Tidwell ,  Stanley D. Chamberlain ,  George A. Freeman ,  Joseph H. Chan ,  George W. Koszalka ,  Leroy B. Townsend ,  John C. Drach

    发明人： Jeffrey H. Tidwell ,  Stanley D. Chamberlain ,  George A. Freeman ,  Joseph H. Chan ,  George W. Koszalka ,  Leroy B. Townsend ,  John C. Drach

    IPC分类号： A61K3170

    CPC分类号： C07H19/052 ,  A61K31/7056 ,  Y10S514/934

    摘要： According to a first aspect of the invention there is provided compounds of formula (I): wherein: R1 is hydroxy; O-acetyl; or a halo atom; R2 is hydroxy; O-acetyl; or a halo atom; R3 is hydrogen; a halo atom; azido; C2-6alkenyl; C2-6alkynyl; C6-14aryl C2-6alkenyl; C6-14arylC2-6alkynyl —NR8R9 (where R8 and R9 may be the same or different and are hydrogen, C1-8alkyl, cyanoC1-8alkyl, hydroxyC1-8alkyl, haloC1-8alkyl, C3-7cycloalkyl, C1-8alkylC3-7cycloalkyl, C2-6alkenyl, C3-7cycloalkylC1-8alkyl, C2-6alkynyl, C6-14aryl, C6-14arylC1-8alkyl, heterocycleC1-8alkyl, C1-8alkylcarbonyl, C6-14arylsulfonyl, C1-8alkysulfonyl, or R8R9 together with the N atom to which they are attached form a 3,4,5 or 6 membered heterocyclic ring); —OR10 (where R10 is hydrogen, C1-8alkyl, C6-14aryl, or C6-14arylC1-8alkyl, C2-6alkenyl, C2-6alkynyl, C6-14aryl C2-6alkenyl or C6-14arylC2-6alkynyl); or —SR11 (where R11 is hydrogen, C1-8alkyl, C6-14aryl, or C6-14arylC1-8alkyl).

    摘要翻译： 根据本发明的第一方面，提供式（I）的化合物：其中：R 1是羟基; O-乙酰基; 或卤原子; R 2为羟基; O-乙酰基; 或卤素原子; R 3是氢; 卤素原子 叠氮 C2-6烯基; C 2-6炔基; C6-14芳基C2-6烯基; C 6-14芳基C 2-6炔基-NR 8 R 9（其中R 8和R 9可以相同或不同，为氢，C 1-8烷基，氰基C 1-8烷基，羟基C 1-8烷基，卤代C 1-8烷基，C 3-7环烷基，C 1-8烷基C 3-7环烷基， C 1-6烷基，C 3-7环烷基C 1-8烷基，C 2-6炔基，C 6-14芳基，C 6-14芳基C 1-8烷基，杂环C 1-8烷基，C 1-8烷基羰基，C 6-14芳基磺酰基，C 1-8炔基磺酰基或R 8 R 9与它们所连接的N原子一起 形成3,4,5或6元杂环）; -OR 10（其中R 10是氢，C 1-8烷基，C 6-14芳基或C 6-14芳基C 1-8烷基，C 2-6烯基，C 2-6炔基，C 6-14芳基C 2-6烯基或C 6-14芳基C 2-6炔基）; 或-SR 11（其中R 11是氢，C 1-8烷基，C 6-14芳基或C 6-14芳基C 1-8烷基）。

    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。