利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

82 条记录 (耗时 0.05 秒)

    Short-acting benzodiazepines
    45.
    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。

    Histone deacetylase inhibitors
    46.
    发明授权
    Histone deacetylase inhibitors 失效
    组蛋白脱乙酰酶抑制剂

    公开(公告)号：US07399884B2

    公开(公告)日：2008-07-15

    申请号：US11557402

    申请日：2006-11-07

    申请人： Jerome C. Bressi ,  Sheldon X. Cao ,  Jeffrey A. Stafford ,  Phong H. Vu

    发明人： Jerome C. Bressi ,  Sheldon X. Cao ,  Jeffrey A. Stafford ,  Phong H. Vu

    IPC分类号： C07C259/04 ,  C07C229/34 ,  C07D231/16 ,  C07D239/22 ,  C07D241/36

    CPC分类号： C07C259/06 ,  C07D231/16 ,  C07D239/38 ,  C07D241/44

    摘要： Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen;R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl;M is a substituent capable of complexing with a protein metal ion; andL is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.

    摘要翻译： 提供组蛋白脱乙酰酶抑制剂及其用途，其具有以下通式：其中R 1，R 2，R 3和R 4， / SUB>各自独立地选自氢，取代或未取代的直链C 1-12烷基，C 2-12-12氨基烷基或C 1 -C 12烷基， 2-12个氧杂烷基，以及取代和未取代的3,4,5,6,7或8元环，条件是R 3和R 4 不是氢; R 5选自羰基，取代或未取代的C 1-3烷基，取代或未取代的C 1-3烷基， 烷基-C（O），取代或未取代的-C（O）-C 1-3烷基和取代或未取代的-C（O）C（O）C 1-3烷基; M是能与蛋白质金属离子络合的取代基; L是包含连接M取代基与L取代基的α原子的3-12个原子的链的取代基。