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31. 发明授权

US06294534B1 Spiropiperidine derivatives as melanocortin receptor agonists 失效
公开(公告)号：US06294534B1
公开(公告)日：2001-09-25
申请号：US09329814
申请日：1999-06-10
申请人： Ravi P. Nargund , Brenda L. Palucki , Zhixiong Ye , Raman K. Bakshi , Arthur A. Patchett , Leonardus H. T. Van Der Ploeg
发明人： Ravi P. Nargund , Brenda L. Palucki , Zhixiong Ye , Raman K. Bakshi , Arthur A. Patchett , Leonardus H. T. Van Der Ploeg
IPC分类号： A61K3144
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/06191
摘要： Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

32. 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.

33. 发明授权

US5721250A Di-and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone 失效
标题翻译：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。

34. 发明授权

US5656606A Camphor compounds promote release of growth hormone 失效
标题翻译：樟脑化合物促进生长激素的释放
公开(公告)号：US5656606A
公开(公告)日：1997-08-12
申请号：US390328
申请日：1995-02-17
申请人： Ravi Nargund , Arthur A. Patchett
发明人： Ravi Nargund , Arthur A. Patchett
IPC分类号： C07D211/60 , C07D401/12 , C07D453/02 , A61K31/16 , A61K31/445 , A61K31/495 , A61K38/22
CPC分类号： C07D401/12 , C07D211/60 , C07D453/02 , C07C2102/42
摘要： The present invention is directed to certain novel compounds identified as camphor derivatives of the general structural formula: ##STR1## wherein A, X, Y, R.sup.2a, R.sup.4, and R.sup.5 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：本发明涉及鉴定为以下通式结构式的樟脑衍生物的某些新化合物：其中A，X，Y，R 2a，R 4和R 5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。

35. 发明授权

US5412097A Heterocyclic compounds bearing acidic functional groups as angiotensin II antagonists 失效
标题翻译：带有酸性官能团的杂环化合物作为血管紧张素II拮抗剂
公开(公告)号：US5412097A
公开(公告)日：1995-05-02
申请号：US940267
申请日：1992-09-02
申请人： Prasun K. Chakravarty , William J. Greenlee , Dooseop Kim , Nathan B. Mantlo , Arthur A. Patchett , Ralph A. Rivero
发明人： Prasun K. Chakravarty , William J. Greenlee , Dooseop Kim , Nathan B. Mantlo , Arthur A. Patchett , Ralph A. Rivero
IPC分类号： C07D471/04 , C07D473/08 , C07D473/32 , C07F9/6561 , A61K31/435 , A61K31/52 , C07D473/00
CPC分类号： C07D471/04 , C07D473/08 , C07D473/32 , C07F9/6561
摘要： Heterocyclic compounds of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
摘要翻译：结构式的杂环化合物：其中A，B，C和D独立地为碳原子或氮原子，可用于治疗高血压和充血性心力衰竭的血管紧张素II拮抗剂。

36. 发明授权

US5254682A Cyclic renin inhibitors containing 3(S)-amino-4-cyclohexyl-2(R)-hydroxy-butanoic acid or 4-cyclo-hexyl-(2R, 3S)-dihydroxybutanoic acid or related analogs 失效
标题翻译：含有3（S） - 氨基-4-环己基-2（R） - 羟基 - 丁酸或4-环己基 - （2R，3S） - 二羟基丁酸或相关类似物的环状肾素抑制剂
公开(公告)号：US5254682A
公开(公告)日：1993-10-19
申请号：US714114
申请日：1991-06-11
申请人： Daljit S. Dhanoa , Arthur A. Patchett , William J. Greenlee , William H. Parsons , Thomas A. Halgren , Ann E. Weber , Lihu Yang
发明人： Daljit S. Dhanoa , Arthur A. Patchett , William J. Greenlee , William H. Parsons , Thomas A. Halgren , Ann E. Weber , Lihu Yang
IPC分类号： A61K31/335 , A61K31/357 , A61K31/39 , A61K31/395 , A61K31/40 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61K38/00 , A61P5/38 , A61P9/00 , A61P9/12 , A61P27/02 , A61P27/06 , A61P31/12 , A61P43/00 , C07D225/02 , C07D245/02 , C07D267/00 , C07D273/00 , C07D273/01 , C07D273/02 , C07D281/00 , C07D285/00 , C07D291/02 , C07D313/00 , C07D321/00 , C07D323/00 , C07D327/00 , C07D327/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D411/12 , C07D413/12 , C07D417/12 , C07D419/12 , C07D453/02 , C07D487/04 , C07F9/6527 , C07F9/6558 , C07F9/6561 , C07K5/02 , C07K5/065 , C07K5/078 , C07K5/097 , C07D225/00
CPC分类号： C07K5/0823 , C07D245/02 , C07D273/00 , C07D273/02 , C07D281/00 , C07D291/02 , C07D401/12 , C07D405/12 , C07D413/10 , C07D419/12 , C07D453/02 , C07D487/04 , C07F9/6527 , C07F9/65586 , C07F9/6561 , C07K5/0202 , C07K5/06078 , C07K5/06139 , A61K38/00
摘要： Compounds of the formula: ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.
摘要翻译：公开了下式的化合物：（I）。这些化合物抑制天然蛋白水解酶肾素的血管紧张素原切割作用，并且可用于治疗，预防或控制肾素相关性高血压，醛固酮增多症，充血性心力衰竭和青光眼。

37. 发明授权

US5236928A Imidazole derivatives bearing acidic functional groups at the 5-position, their compositions and methods of use as angiotensin II antagonists 失效
标题翻译：在5位含有酸性官能团的咪唑衍生物，其作为血管紧张素II拮抗剂的组合物和用途
公开(公告)号：US5236928A
公开(公告)日：1993-08-17
申请号：US891668
申请日：1992-05-29
申请人： Prasun K. Chakravarty , William J. Greenlee , Arthur A. Patchett
发明人： Prasun K. Chakravarty , William J. Greenlee , Arthur A. Patchett
IPC分类号： C07D233/84 , C07D233/90 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/12
CPC分类号： C07D403/10 , C07D233/84 , C07D233/90 , C07D403/12 , C07D403/14 , C07D413/10
摘要： There are disclosed substituted imidazole derivatives of Formula I bearing acidic functional groups which are useful as angiotensin II antagonists. ##STR1##
摘要翻译：公开了具有酸性官能团的式I的取代咪唑衍生物，其可用作血管紧张素II拮抗剂。我

38. 发明授权

US5147867A Phosphorus containing enzyme inhibitors 失效
标题翻译：含磷酶抑制剂
公开(公告)号：US5147867A
公开(公告)日：1992-09-15
申请号：US824738
申请日：1992-01-21
申请人： William H. Parsons , William R. Schoen , Arthur A. Patchett
发明人： William H. Parsons , William R. Schoen , Arthur A. Patchett
IPC分类号： A61K31/40 , C07F9/30 , C07F9/58
CPC分类号： C07F9/582 , A61K31/40 , C07F9/301 , C07F9/302 , C07F9/303 , C07F9/306
摘要： Dipeptide mimics which contain phosphorus and their pharmaceutical use and preparation are disclosed. The compounds have dehydropeptidase (DHP) enzyme inhibitor activity.
摘要翻译：公开了含有磷的二肽模拟物及其药物用途和制剂。该化合物具有脱氢肽酶（DHP）酶抑制剂活性。

39. 发明授权

US5122511A Immunosuppressive cyclosporin analogs with modified amino acids at position-8 失效
标题翻译：在位置-8上具有改性氨基酸的免疫抑制CYCLOSPORIN模拟物
公开(公告)号：US5122511A
公开(公告)日：1992-06-16
申请号：US485920
申请日：1990-02-27
申请人： Arthur A. Patchett , David Taub , Robert T. Goegelman
发明人： Arthur A. Patchett , David Taub , Robert T. Goegelman
IPC分类号： A61K38/00 , A61P37/06 , C07K1/02 , C07K1/113 , C07K7/64 , C07K14/195 , C07K14/41
CPC分类号： B82Y15/00 , C07K7/645 , A61K38/00
摘要： New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala].sup.8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.

40. 发明授权

US4602002A N-carboxymethyl substituted lysyl and .alpha.-(.epsilon.-aminoalkyl) glycyl amino acid antihypertensive agents 失效
标题翻译： N-羧甲基取代的赖氨酰和α-（ε-氨基烷基）甘氨酰氨基酸抗高血压药
公开(公告)号：US4602002A
公开(公告)日：1986-07-22
申请号：US463412
申请日：1983-02-07
申请人： Arthur A. Patchett , Mu T. Wu
发明人： Arthur A. Patchett , Mu T. Wu
IPC分类号： A61K38/00 , C07K5/02 , A61K31/405 , A61K37/02 , C07D207/08
CPC分类号： C07K5/0222 , A61K38/00
摘要： Compounds of the formula: ##STR1## wherein R.sup.2 is --(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3 ; wherein k is 0 to 3, j is 1 or 2; X is F or OH; and, R.sup.3 is hydrogen; loweralkyl or loweraralkyl which may be substituted by hydroxy, carboxy, carbamoyl, or carbalkoxy; or, acyl; and, a pharmaceutically acceptable salt thereof; are inhibitors of angiotensin I converting enzyme useful as antihypertensive agents.
摘要翻译：下式的化合物：其中R 2是 - （CH 2）k -X-（CH 2）j -NHR 3; 其中k为0至3，j为1或2; X是F或OH; R3为氢; 可被羟基，羧基，氨基甲酰基或烷氧基取代的低级烷基或低级烷基; 或酰基; 及其药学上可接受的盐; 是用作抗高血压药的血管紧张素I转化酶的抑制剂。

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