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1. 发明授权

US06063796A Somatostatin agonists 失效
公开(公告)号：US06063796A
公开(公告)日：2000-05-16
申请号：US53299
申请日：1998-04-01
申请人： Lihu Yang , Arthur A. Patchett , Alexander Pasternak , Scott Berk , Meng Hsin Chen , David Johnston , Kevin Chapman , Ravi Nargund , James R. Tata , Liangqin Guo
发明人： Lihu Yang , Arthur A. Patchett , Alexander Pasternak , Scott Berk , Meng Hsin Chen , David Johnston , Kevin Chapman , Ravi Nargund , James R. Tata , Liangqin Guo
IPC分类号： A61P25/04 , A61K31/454 , A61P1/00 , A61P3/10 , A61P9/00 , A61P25/24 , A61P27/02 , A61P35/00 , A61P43/00 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/445 , C07D211/14 , C07D211/40
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. Compounds of the formula: ##STR1## including pharmaceutically acceptable salts and hydrates thereof are disclosed. These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome, pain and diabetic retinopathy. Many of the compounds are also orally active.

2. 发明授权

US06025372A Somatostatin agonists 失效
标题翻译：生长抑素激动剂
公开(公告)号：US06025372A
公开(公告)日：2000-02-15
申请号：US53373
申请日：1998-04-01
申请人： Lihu Yang , Arthur A. Patchett , Alexander Pasternak , Kevin Chapman , James R. Tata , Liangqin Guo
发明人： Lihu Yang , Arthur A. Patchett , Alexander Pasternak , Kevin Chapman , James R. Tata , Liangqin Guo
IPC分类号： A61P25/04 , A61K31/454 , A61K31/4545 , A61K31/496 , A61P1/00 , A61P3/10 , A61P9/00 , A61P25/24 , A61P27/02 , A61P35/00 , A61P43/00 , C07D401/14 , C07D405/14 , A61K31/445 , C07D401/12 , C07D40/10
CPC分类号： C07D401/14 , C07D405/14
摘要： Somatostatin agonist compounds of formula I are disclosed: ##STR1## including pharmaceutically acceptable salts and hydrates thereof These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome and pain. The compounds are potent with high selectivity toward the receptor subtype 2.Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：公开了式I的生长抑素激动剂化合物：包括其药学上可接受的盐和水合物。这些化合物可用于治疗糖尿病，癌症，肢端肥大症，再狭窄，抑郁症，肠易激综合征和疼痛。该化合物对于受体亚型2具有高选择性。药物组合物和治疗方法也包括在内。

3. 发明授权

US5965565A Piperidines promote release of growth hormone 失效
标题翻译：皮质激素促进生长激素的释放
公开(公告)号：US5965565A
公开(公告)日：1999-10-12
申请号：US988816
申请日：1997-12-11
申请人： Meng H. Chen , Zhijian Lu , Ravi Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang , Mu Tsu Wu
发明人： Meng H. Chen , Zhijian Lu , Ravi Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang , Mu Tsu Wu
IPC分类号： C07D401/06 , C07D413/14 , C07D471/10 , C07D495/10 , C07D209/04 , A61K31/445 , C07D211/00
CPC分类号： C07D401/06 , C07D413/14 , C07D471/10 , C07D495/10
摘要： The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, 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 such compounds as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及一般结构式的某些哌啶，吡咯烷和六氢-1H-吖庚因：其中B选自：和R1，R1a，R2a，R3a，R3b，R4，R4a，R4b，R4c，R5， D，X，Y，n，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。

4. 发明授权

US5536716A Spiro piperidines and homologs which promote release of growth hormone 失效
标题翻译： Spiro哌啶和促进生长激素释放的同系物
公开(公告)号：US5536716A
公开(公告)日：1996-07-16
申请号：US147226
申请日：1993-11-03
申请人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
发明人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
IPC分类号： A61K38/00 , C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07D519/00 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/55 , A61K31/44 , C07D401/04 , C07D451/00
CPC分类号： C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07K5/021 , C07K5/06026 , C07K5/06034 , C07K5/06147 , C07K5/06191 , A61K38/00 , Y10S514/825
摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which 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 spiro compounds as the active ingredient thereof are also disclosed.
摘要翻译：已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。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。还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

5. 发明授权

US5804578A Piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone 失效
标题翻译：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：US5804578A
公开(公告)日：1998-09-08
申请号：US828606
申请日：1997-03-31
申请人： Prasun K. Chakravarty , Meng H. Chen , Ravi Nargund , Arthur A. Patchett , James R. Tata , Mu Tsu Wu , Lihu Yang
发明人： Prasun K. Chakravarty , Meng H. Chen , Ravi Nargund , Arthur A. Patchett , James R. Tata , Mu Tsu Wu , Lihu Yang
IPC分类号： A61K38/00 , C07K5/02 , C07K5/08 , C07K5/083 , A01N43/54 , C07D215/00 , C07D413/00 , C07D453/02
CPC分类号： C07K5/0802 , C07K5/021 , C07K5/0806 , A61K38/00
摘要： The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, 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 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：其中B选自：其中R 1，R 1a，R 2a，R 3a，R 3b，R 4，R 4a， R4b，R4c，R5，D，X，Y，n，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。

6. 发明授权

US5652235A Method of using spiro piperidines to promote the release of growth hormone 失效
标题翻译：使用螺哌啶促进生长激素释放的方法
公开(公告)号：US5652235A
公开(公告)日：1997-07-29
申请号：US641311
申请日：1996-04-30
申请人： Meng-Hsin Chen , Ravi P. Nargund , David B. R. Johnston , Arthur A. Patchett , James R. Tata , Lihu Yang
发明人： Meng-Hsin Chen , Ravi P. Nargund , David B. R. Johnston , Arthur A. Patchett , James R. Tata , Lihu Yang
IPC分类号： A61K31/435 , A61K31/438 , A61K31/445 , A61K31/47 , A61K38/00 , A61K38/04 , A61P3/00 , A61P19/10 , A61P43/00 , C07D221/20 , C07D401/10 , C07D471/10 , C07D491/10 , C07D491/107 , C07D495/10 , C07D495/20 , C07D519/00 , C07K1/00 , C07K5/02 , C07K5/06 , C07K5/078 , C07K14/00 , A61K31/55 , A61K31/44
CPC分类号： C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07K5/021 , C07K5/06034 , C07K5/06147 , C07K5/06191 , A61K38/00 , Y02P20/55
摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which 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 spiro compounds as the active ingredient thereof are also disclosed.
摘要翻译：已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。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。还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

7. 发明授权

US5578593A Spiro piperidines and homologs promote release of growth hormone 失效
标题翻译： Spiro哌啶和同系物促进生长激素的释放
公开(公告)号：US5578593A
公开(公告)日：1996-11-26
申请号：US146848
申请日：1993-11-03
申请人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
发明人： Meng-Hsin Chen , David B. R. Johnston , Ravi P. Nargund , Arthur A. Patchett , James R. Tata , Lihu Yang
IPC分类号： A61K38/00 , C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07D519/00 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/55 , A61K31/44 , C07D401/00 , C07D471/00
CPC分类号： C07D401/10 , C07D471/10 , C07D491/10 , C07D495/10 , C07K5/021 , C07K5/06026 , C07K5/06034 , C07K5/06147 , C07K5/06191 , A61K38/00 , Y10S514/825
摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which 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 spiro compounds as the active ingredient thereof are also disclosed.
摘要翻译：已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。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。还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

8. 发明授权

US06420376B1 Amido spiropiperidines promote the release of growth hormone 有权
标题翻译：酰胺丙哌啶促进生长激素的释放
公开(公告)号：US06420376B1
公开(公告)日：2002-07-16
申请号：US09614193
申请日：2000-07-10
申请人： James R. Tata , Arthur A. Patchett
发明人： James R. Tata , Arthur A. Patchett
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/34 , C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention is directed to certain spiropiperidines of the general structural formula: wherein R1, R2, R3, R3a, R3b, R4 and R5 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 compounds as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及一般结构式的某些螺哌啶：其中R1，R2，R3，R3a，R3b，R4和R5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。

9. 发明授权

US5731317A Bridged piperidines promote release of growth hormone 失效
标题翻译：桥连的哌啶促进生长激素的释放
公开(公告)号：US5731317A
公开(公告)日：1998-03-24
申请号：US401849
申请日：1995-03-10
申请人： Zhijian Lu , Arthur A. Patchett , James R. Tata
发明人： Zhijian Lu , Arthur A. Patchett , James R. Tata
IPC分类号： C07D451/02 , A61K31/445 , A61K31/46
CPC分类号： C07D451/00 , C07D451/02
摘要： The present invention is directed to certain novel compounds identified as bridged piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.3, R.sup.3a,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 such compounds as the active ingredient thereof are also disclosed.
摘要翻译：本发明涉及确定为通式结构式的桥连哌啶的某些新化合物：其中R1，R1a，R2a，R3，R3a，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。

10. 发明申请

US20090054423A1 Niacin receptor agonists, compositions containing such compounds and methods of treatment 审中-公开
标题翻译：烟酸受体激动剂，含有这些化合物的组合物和治疗方法
公开(公告)号：US20090054423A1
公开(公告)日：2009-02-26
申请号：US11918270
申请日：2006-04-07
申请人： Jason E. Imbriglio , Steven L. Colletti , James R. Tata , Rui Liang , Subharekha Raghavan , Darby R. Schmidt , Abigail L. Smenton , Sook Yee Chan
发明人： Jason E. Imbriglio , Steven L. Colletti , James R. Tata , Rui Liang , Subharekha Raghavan , Darby R. Schmidt , Abigail L. Smenton , Sook Yee Chan
IPC分类号： A61K31/538 , C07D257/04 , A61K31/41 , C07D231/54 , A61K31/416 , C07D261/06 , A61K31/42 , C07D403/02 , A61P9/10 , A61P3/10 , A61K31/506 , C07D401/02 , A61K31/4439 , C07D277/20 , A61K31/426 , A61K31/497 , A61K31/437
CPC分类号： C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括可用于治疗血脂异常的式I化合物及其药学上可接受的盐和水合物。还包括药物组合物和使用方法。

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