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    Di-and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
    1.
    发明授权
    Di-and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone 失效
    二取代和三取代的哌啶，吡咯烷和六氢-1H-吖庚因促进生长激素的释放

    公开(公告)号：US5721250A

    公开(公告)日：1998-02-24

    申请号：US600646

    申请日：1996-02-13

    申请人： Gregori J. Morriello ,  Lihu Yang ,  Arthur A. Patchett

    发明人： Gregori J. Morriello ,  Lihu Yang ,  Arthur A. Patchett

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/083 ,  A61K31/445 ,  C07D401/02 ,  C07D401/14 ,  C07D409/02

    CPC分类号： C07K5/0202 ,  C07K5/06034 ,  C07K5/06139 ,  C07K5/0808 ,  A61K38/00

    摘要： The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A, X, Y, and n 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 growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及鉴定为二 - 和三 - 取代的哌啶，吡咯烷和六氢-1H-吖庚因的一些新化合物，其通式为：其中R1，R4，R5，A，X，Y和 n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，并治疗由生长激素改善的医疗状况。 还公开了含有这种二取代和三取代的哌啶，吡咯烷酮和六氢-1H-吖庚因作为其活性成分的生长激素释放组合物。

    2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
    2.
    发明授权
    2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone 失效
    2-取代的哌啶，吡咯烷和六氢-1H-吖庚因促进生长激素的释放

    公开(公告)号：US5494919A

    公开(公告)日：1996-02-27

    申请号：US323994

    申请日：1994-10-17

    申请人： Gregori J. Morriello ,  Arthur A. Patchett ,  Lihu Yang

    发明人： Gregori J. Morriello ,  Arthur A. Patchett ,  Lihu Yang

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/083 ,  A61K31/445 ,  C07D209/04 ,  C07D401/06

    CPC分类号： C07K5/0202 ,  C07K5/06034 ,  C07K5/0808 ,  A61K38/00

    摘要： The present invention is directed to certain piperidine, pyrrolidine, and hexahydro-1H-azepine compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5, A, W, X, Y, and n axe 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 s are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及以下通式结构式的某些哌啶，吡咯烷和六氢-1H-吖庚因化合物：其中如本文所定义的R1，R3，R4，R5，A，W，X，Y和n ax 。 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，并且通过生长激素的合成代谢作用来治疗被改善的医疗状况。 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。

    Treatment of osteoporosis with substituted piperidines, pyrrolidines and hexahydro-1H-azepines in combination with bisphosphonates
    4.
    发明授权
    Treatment of osteoporosis with substituted piperidines, pyrrolidines and hexahydro-1H-azepines in combination with bisphosphonates 失效
    用取代的哌啶，吡咯烷和六氢-1H-吖庚因与双膦酸盐组合治疗骨质疏松症

    公开(公告)号：US5622973A

    公开(公告)日：1997-04-22

    申请号：US464982

    申请日：1995-06-05

    申请人： Gregori J. Morriello ,  Arthur A. Patchett ,  Lihu Yang

    发明人： Gregori J. Morriello ,  Arthur A. Patchett ,  Lihu Yang

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/083 ,  A61K31/445 ,  A61K31/41 ,  A61K31/425 ,  A61K31/505

    CPC分类号： C07K5/06139 ,  C07K5/0202 ,  C07K5/06034 ,  C07K5/0808 ,  A61K38/00

    摘要： The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A, X, Y, and n 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 such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及鉴定为二 - 和三 - 取代的哌啶，吡咯烷和六氢-1H-吖庚因的一些新化合物，其通式为：其中R1，R4，R5，A，X，Y和 n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。 还公开了含有这种二取代和三取代的哌啶，吡咯烷酮和六氢-1H-吖庚因作为其活性成分的生长激素释放组合物。

    Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
    5.
    发明授权
    Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone 失效
    二取代和三取代的哌啶，吡咯烷和六氢-1H-吖庚因促进生长激素的释放

    公开(公告)号：US5492916A

    公开(公告)日：1996-02-20

    申请号：US323988

    申请日：1994-10-17

    申请人： Gregori J. Morriello ,  Arthur A. Patchett ,  Lihu Yang

    发明人： Gregori J. Morriello ,  Arthur A. Patchett ,  Lihu Yang

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/083 ,  A61K31/445 ,  C07D209/04 ,  C07D401/06

    CPC分类号： C07K5/06139 ,  C07K5/0202 ,  C07K5/06034 ,  C07K5/0808 ,  A61K38/00

    摘要： The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A,X,Y, and n 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 such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.

    摘要翻译： 本发明涉及鉴定为二 - 和三 - 取代的哌啶，吡咯烷和六氢-1H-吖庚因的一些新化合物，其通式为：其中R1，R4，R5，A，X，Y和 n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。 还公开了含有这种二取代和三取代的哌啶，吡咯烷酮和六氢-1H-吖庚因作为其活性成分的生长激素释放组合物。

    Somatostatin agonists
    10.
    发明授权
    Somatostatin agonists 失效
    生长抑素激动剂

    公开(公告)号：US6117880A

    公开(公告)日：2000-09-12

    申请号：US181590

    申请日：1998-10-28

    申请人： Liangquin Guo ,  Ralph T. Mosley ,  Alexander Pasternak ,  Arthur A. Patchett ,  Lihu Yang

    发明人： Liangquin Guo ,  Ralph T. Mosley ,  Alexander Pasternak ,  Arthur A. Patchett ,  Lihu Yang

    IPC分类号： A61K31/438 ,  C07D221/20

    CPC分类号： C07D401/14 ,  C07D221/20 ,  C07D401/12

    摘要： This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are also orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostastin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. Further objects will become apparent from reading the following description.

    摘要翻译： 本发明涉及对受体亚型2具有高选择性的生长抑素激动剂化合物。该化合物在治疗糖尿病，癌症，肢端肥大症和视网膜病变中提供改进的治疗指数。 许多化合物也是口服活性的。 因此，本发明的目的是描述这些化合物。 进一步的目的是描述生长激素激动剂的具体优选的立体异构体。 另一个目的是描述制备这些化合物的方法。 另一个目的是描述使用这些化合物作为其活性成分的方法和组合物。 通过阅读以下描述，其他目的将变得显而易见。