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    Biaryl Substituted Pyrazinones as Sodium Channel Blockers
    6.
    发明申请
    Biaryl Substituted Pyrazinones as Sodium Channel Blockers 审中-公开
    二芳基取代的吡嗪酮作为钠通道阻断剂

    公开(公告)号：US20080280873A1

    公开(公告)日：2008-11-13

    申请号：US10594367

    申请日：2005-03-25

    申请人： Jun Liang ,  Prasun K. Chakravarty ,  Deborah E. Pan ,  William H. Parsons ,  Pengcheng P. Shao ,  Feng Yee ,  Bishan Zhou

    发明人： Jun Liang ,  Prasun K. Chakravarty ,  Deborah E. Pan ,  William H. Parsons ,  Pengcheng P. Shao ,  Feng Yee ,  Bishan Zhou

    IPC分类号： A61K31/4965 ,  C07D241/24

    CPC分类号： C07D241/24 ,  B05B1/02 ,  B05B1/14 ,  B05B1/34 ,  B65D83/20 ,  C07D241/18 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06

    摘要： Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

    摘要翻译： 由式I表示的二芳基取代的吡嗪酮化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症 ，焦虑，多发性硬化和双相性精神障碍，包括单独或与一种或多种其它治疗活性化合物组合施用有效量的本发明化合物。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

    3-substituted piperidines promote release of growth hormone
    10.
    发明授权
    3-substituted piperidines promote release of growth hormone 失效
    3-取代的哌啶促进生长激素的释放

    公开(公告)号：US5559128A

    公开(公告)日：1996-09-24

    申请号：US424750

    申请日：1995-04-18

    申请人： Prasun K. Chakravarty ,  Ravi Nargund ,  Robert W. Marquis ,  Arthur A. Patchett ,  Lihu Yang

    发明人： Prasun K. Chakravarty ,  Ravi Nargund ,  Robert W. Marquis ,  Arthur A. Patchett ,  Lihu Yang

    IPC分类号： C07D211/56 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  A61K31/445 ,  C07D209/04

    CPC分类号： C07D401/06 ,  C07D211/56 ,  C07D401/14 ,  C07D413/14

    摘要： The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing these compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及鉴定为以下结构式的3-取代哌啶的某些新化合物：其中R1，R1a，R2a，R4，R5，A，X和Y如本文所定义。 这些化合物促进人和动物中生长激素的释放。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。 还公开了含有这些化合物作为其活性成分的生长激素释放组合物。