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    Selective agents for pain suppression
    1.
    发明授权
    Selective agents for pain suppression 有权
    选择性抑制剂

    公开(公告)号：US08835424B2

    公开(公告)日：2014-09-16

    申请号：US12779449

    申请日：2010-05-13

    Applicant: James Cook ,  Shengming Huang ,  Rahul Edwankar ,  Ojas A. Namjoshi ,  Zhi-Jian Wang

    Inventor： James Cook ,  Shengming Huang ,  Rahul Edwankar ,  Ojas A. Namjoshi ,  Zhi-Jian Wang

    IPC: A61K31/5517 ,  C07D487/02

    CPC classification number: C07D243/12 ,  C07D243/20 ,  C07D243/24 ,  C07D471/04 ,  C07D487/04 ,  C07D487/06 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

    Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.

    Abstract translation: 在优选的实施方案中，本发明提供治疗方法和用于抑制，缓解和预防常伴有炎性疾病和神经性损伤的常规慢性，严重和衰弱性疼痛的药物组合物，其通常对常规镇痛治疗无反应。 本发明的优选实施方案还涉及使用苯并二氮杂衍生物的治疗方法和药物组合物，其提供抑制，缓解和预防神经性疼痛，偏头痛相关疼痛和炎症性疼痛，同时具有降低的镇静和共济失调副作用。

    Short-acting benzodiazepines
    4.
    发明申请
    Short-acting benzodiazepines 有权
    短效苯二氮卓类

    公开(公告)号：US20070135420A1

    公开(公告)日：2007-06-14

    申请号：US11650636

    申请日：2007-01-05

    Applicant: Paul Feldman ,  David Jung ,  Istvan Kaldor ,  Gregory Pacofsky ,  Jeffrey Stafford ,  Jeffrey Tidwell

    Inventor： Paul Feldman ,  David Jung ,  Istvan Kaldor ,  Gregory Pacofsky ,  Jeffrey Stafford ,  Jeffrey Tidwell

    IPC: A61K31/5513 ,  C07D403/02 ,  C07D243/14

    CPC classification number: C07D243/20 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D487/04

    Abstract: 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.

    Abstract translation: 现已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描述的本发明化合物，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。

    Intermediates to produce imidazodiazepines
    8.
    发明授权
    Intermediates to produce imidazodiazepines 失效

    公开(公告)号：US4371468A

    公开(公告)日：1983-02-01

    申请号：US244511

    申请日：1981-03-16

    Applicant: Armin Walser ,  Rodney I. Fryer

    Inventor： Armin Walser ,  Rodney I. Fryer

    IPC: C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561 ,  C07D401/04

    CPC classification number: C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

    Abstract: Novel imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. As especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof. R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

    Imidazodiazepines and processes therefor
    9.
    发明授权
    Imidazodiazepines and processes therefor 失效
    咪唑二氮类及其制备方法

    公开(公告)号：US4280957A

    公开(公告)日：1981-07-28

    申请号：US905820

    申请日：1978-05-15

    Applicant: Armin Walser ,  Rodney I. Fryer

    Inventor： Armin Walser ,  Rodney I. Fryer

    IPC: C07D243/16 ,  C07D243/20 ,  C07D285/10 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

    CPC classification number: C07D285/10 ,  C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561 ,  Y10S514/906 ,  Y10S514/96

    Abstract: Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

    Abstract translation: 新型咪唑并二氮杂类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢，低级烷基优选是甲基; R3和R5是氢; R4是氢，硝基和卤素，最优选氯，最优选的实施方案中，当位于咪唑并二氮杂的稠合苯并部分位于其8-位时，R 6是苯基或卤素，硝基或低级烷基取代的 苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位，并且R 2是氢和低级烷基。

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