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    Enantiomerically pure opioid diarylmethylpiperzine and methods of using same
    1.
    发明授权
    Enantiomerically pure opioid diarylmethylpiperzine and methods of using same 有权
    对映异构纯的阿片样二芳基甲基哌嗪及其使用方法

    公开(公告)号：US06924288B2

    公开(公告)日：2005-08-02

    申请号：US10254609

    申请日：2002-09-25

    申请人： Kwen-Jen Chang

    发明人： Kwen-Jen Chang

    IPC分类号： G01N33/50 ,  A61K31/496 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P1/14 ,  A61P9/04 ,  A61P11/00 ,  A61P11/06 ,  A61P11/14 ,  A61P17/00 ,  A61P17/06 ,  A61P17/10 ,  A61P19/02 ,  A61P25/04 ,  A61P25/18 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P29/00 ,  A61P37/06 ,  C07D333/20 ,  C07D409/06 ,  G01N33/15 ,  A61P1/12

    CPC分类号： C07D333/20

    摘要： An essentially pure compound of the formula: (−)3-((S)-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)(3-thienyl)methyl)phenol or a pharmaceutically acceptable salt thereof, having utility as a receptor-binding species, e.g., as a therapeutic agent for mediating analgesia; as a co-administered agent with various other bioactive compositions, including anesthetics, barbiturates, analgesics, etc.; for reducing, treating, reversing or preventing drug-mediated respiratory depression that may be directly or indirectly caused by use of such various bioactive compositions; as a conjugate in agonist/antagonist pairs for verifying/assaying receptor and neurotransmitter function; and as a therapeutic agent having utility in combating pain, cardiac disorders, mental and emotional disorders cough, diarrhea and gastro-intestinal disorders.

    摘要翻译： （ - ）3 - （（S） - （（2S，5R）-4-烯丙基-2,5-二甲基-1-哌嗪基）（3-噻吩基）甲基）苯酚或其药学上基本上纯的化合物 可接受的盐作为受体结合物质，例如用作介导镇痛的治疗剂; 作为具有各种其他生物活性组合物的共同给药剂，包括麻醉剂，巴比妥类，止痛剂等; 用于减少，治疗，逆转或预防可能由于使用这种各种生物活性组合物直接或间接引起的药物介导的呼吸抑制; 作为激动剂/拮抗剂对中的缀合物，用于验证/测定受体和神经递质功能; 并且作为用于对抗疼痛，心脏疾病，精神和情绪障碍咳嗽，腹泻和胃肠道疾病的治疗剂。

    Compositions and Methods for Reducing Respiratory Depression and Attendant SIde Effects of Mu Opioid Compounds
    2.
    发明申请
    Compositions and Methods for Reducing Respiratory Depression and Attendant SIde Effects of Mu Opioid Compounds 失效
    减少呼吸抑制和服用阿片类药物的成分和方法

    公开(公告)号：US20020111359A1

    公开(公告)日：2002-08-15

    申请号：US09974004

    申请日：2001-10-09

    申请人： Ardent Pharmaceuticals, Inc.

    发明人： Mr. Kwen-Jen Chang ,  Mr. Robert W. McNutt Jr. ,  Mr. Hugh O. Pettit ,  Mr. Michael J. Bishop

    IPC分类号： A61K031/495

    CPC分类号： A61K31/495 ,  A61K31/00 ,  A61K31/40 ,  A61K31/445 ,  A61K31/485 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06 ,  C07D295/096 ,  C07D295/155 ,  A61K2300/00

    摘要： Abstract of DisclosureA method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound. Preferred examples of such delta receptor agonist compound include diarylmethyl piperazine compounds and diarylmethyl piperidine compounds, and pharmaceutical compositions thereof, having utility in medical therapy for reducing respiratory depression associated with certain analgesics, such as mu opiates.

    摘要翻译： 公开摘要一种减少，治疗或预防动物中药物介导的呼吸抑制，肌肉僵硬或恶心/呕吐的方法，该方法涉及对所述动物施用混合物 delta / mu阿片样物质激动剂或呼吸抑制介导药物，包括向接受所述药物的动物施用有效量的δ受体激动剂化合物。 这种δ受体激动剂化合物的优选实例包括二芳基甲基哌嗪化合物和二芳基甲基哌啶化合物及其药物组合物，其在医学疗法中具有用于减少与某些镇痛药相关的呼吸抑制作用，例如阿片剂。