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31.
公开(公告)号:US20150087826A1
公开(公告)日:2015-03-26
申请号:US14556914
申请日:2014-12-01
申请人: Ying-Zi Xu , Dean R. Artis , Simeon Bowers , Roy K. Hom , Hing L. Sham , Shendong Yuan
发明人: Ying-Zi Xu , Dean R. Artis , Simeon Bowers , Roy K. Hom , Hing L. Sham , Shendong Yuan
IPC分类号: C07D513/10
CPC分类号: C07D513/10 , C07D265/12 , C07D265/18 , C07D279/08 , C07D279/16 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/10
摘要: Compounds are provided having a structure according to Formula (I): wherein A1, A2, A3, Y, R1, R2, R3, R4, R5, R6, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
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32.Acetyl-CoA carboxylase (ACC) inhibitors and their use in diabetes, obesity and metabolic syndrome 有权
标题翻译: 乙酰辅酶A羧化酶(ACC)抑制剂及其在糖尿病,肥胖症和代谢综合征中的应用公开(公告)号:US08207350B2
公开(公告)日:2012-06-26
申请号:US12259090
申请日:2008-10-27
申请人: Robert F. Keyes , Yu Gui Gu , Hing L. Sham
发明人: Robert F. Keyes , Yu Gui Gu , Hing L. Sham
IPC分类号: A61K31/428 , C07D277/64 , C07D277/74
CPC分类号: C07D277/68 , C07D277/82 , C07D417/12
摘要: The present invention relates to compounds of formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
摘要翻译: 本发明涉及抑制乙酰辅酶A羧化酶(ACC)的式(I)化合物,可用于预防或治疗人类代谢综合征,II型糖尿病,肥胖症,动脉粥样硬化和心血管疾病。
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33.Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) 失效
标题翻译: 药物组合物作为二肽基肽酶-IV(DPP-IV)的抑制剂公开(公告)号:US07348346B2
公开(公告)日:2008-03-25
申请号:US11075319
申请日:2005-03-08
申请人: Irini Akritopoulou-Zanze , Daria Darczak , Jürgen Dinges , Stevan W. Djuric , Ethan D. Hoff , Hana A. Kopecka , Jyoti R. Patel , Zhonghua Pei , Qi Shuai , Kathy Sarris , Hing L. Sham , Paul E. Wiedeman
发明人: Irini Akritopoulou-Zanze , Daria Darczak , Jürgen Dinges , Stevan W. Djuric , Ethan D. Hoff , Hana A. Kopecka , Jyoti R. Patel , Zhonghua Pei , Qi Shuai , Kathy Sarris , Hing L. Sham , Paul E. Wiedeman
IPC分类号: A61K31/426 , A61K31/4025 , C07D277/04
CPC分类号: C07D417/14 , C07D207/09 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/06
摘要: The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
摘要翻译: 本发明涉及抑制二肽基肽酶IV(DPP-IV)的式(I)化合物,其可用于预防或治疗糖尿病,特别是II型糖尿病,以及高血糖症,X综合症,高胰岛素血症,肥胖症, 动脉粥样硬化和各种免疫调节疾病。
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公开(公告)号:US5905068A
公开(公告)日:1999-05-18
申请号:US718882
申请日:1996-09-24
申请人: Xiaoqi Chen , Brian E. Green , Dale J. Kempf , Lin Li , Daniel W. Norbeck , Hing L. Sham
发明人: Xiaoqi Chen , Brian E. Green , Dale J. Kempf , Lin Li , Daniel W. Norbeck , Hing L. Sham
IPC分类号: C07D333/32 , C07D333/48 , C07D335/02 , C07D493/04 , C07D519/00 , A61K38/05 , A61K39/00
CPC分类号: C07D333/48 , C07D333/32 , C07D335/02 , C07D493/04 , Y10S514/885
摘要: A compound of the formula: ##STR1## is disclosed as a retroviral protease inhibitor compound. Also disclosed are methods and compositions for inhibiting an HIV infection.
摘要翻译: 公开了下式的化合物作为逆转录病毒蛋白酶抑制剂化合物。 还公开了用于抑制HIV感染的方法和组合物。
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公开(公告)号:US5625072A
公开(公告)日:1997-04-29
申请号:US415827
申请日:1995-04-03
申请人: Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham , Chen Zhao
发明人: Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham , Chen Zhao
IPC分类号: A61K31/425 , A61K31/427 , A61K38/00 , A61K45/06 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07D521/00 , C07K5/06 , C07K5/065
CPC分类号: C07D207/08 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/59 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
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公开(公告)号:US5621109A
公开(公告)日:1997-04-15
申请号:US455922
申请日:1995-05-31
申请人: Daniel W. Norbeck , Hing L. Sham , Dale J. Kempf , Chen Zhao
发明人: Daniel W. Norbeck , Hing L. Sham , Dale J. Kempf , Chen Zhao
IPC分类号: A61K31/42 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P35/00 , A61P43/00 , C07C281/02 , C07C281/06 , C07D213/30 , C07D213/38 , C07D213/40 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/24 , C07D277/28 , C07D307/52 , C07D309/04 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D263/34 , C07D277/54
CPC分类号: C07D213/30 , C07C281/02 , C07C281/06 , C07D213/38 , C07D213/40 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/24 , C07D277/28 , C07D307/52 , C07D309/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07C2101/14
摘要: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.
摘要翻译: 公开了下式的逆转录病毒蛋白酶抑制化合物:其中本文定义术语R1,R2,R5,R6,Y,Y',m和n。
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37.Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane 失效
标题翻译: 制备取代的2,5-二氨基-3-羟基己烷的方法公开(公告)号:US5541328A
公开(公告)日:1996-07-30
申请号:US415385
申请日:1995-04-03
申请人: Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao , David Scarpetti
发明人: Timothy L. Stuk , Michael S. Allen , Anthony R. Haight , Francis A. Kerdesky , Denton C. Langridge , M. Robert Leanna , Linda M. Lijewski , Laura Melcher , Howard E. Morton , Daniel W. Norbeck , Daniel S. Reno , Timothy A. Robbins , Hing L. Sham , Thomas J. Sowin , Jien-Heh J. Tien , Chen Zhao , David Scarpetti
IPC分类号: C07C213/00 , C07C215/28 , C07C225/16 , C07C227/18 , C07C229/36 , C07C231/12 , C07C233/35 , C07C251/40 , C07C255/27 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07D221/14 , C07C251/78 , C07C209/44 , C07C221/14
CPC分类号: C07D221/14 , C07C213/00 , C07C215/28 , C07C225/16 , C07C251/40 , C07C255/42 , C07C269/06 , C07C271/20 , C07D209/44 , C07B2200/07
摘要: A substantially pure compound of formula: ##STR1## wherein R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.l are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; andR.sub.g is hydrogen, loweralkyl or benzyl; or an acid addition salt thereof.
摘要翻译: (I)其中R a和R b独立地选自氢,低级烷基和苯基,R c,R d和R 10独立地选自氢,低级烷基 ,三氟甲基,烷氧基,卤素和苯基; (ii)其中萘基环是未取代的或被一个,两个或三个独立地选自低级烷基,三氟甲基,烷氧基和卤素的取代基取代; 或R 6如上所定义,且R 7为R 7aa(O) - ,其中R 7a为低级烷基; 或者R 6和R 7与它们所键合的氮原子一起是其中R f,R g,R h和R 1独立地选自氢,低级烷基,烷氧基,卤素和三氟甲基; R g为氢,低级烷基或苄基; 或其酸加成盐。
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公开(公告)号:US5539122A
公开(公告)日:1996-07-23
申请号:US410996
申请日:1995-03-27
申请人: Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham
发明人: Dale J. Kempf , Daniel W. Norbeck , Hing L. Sham
IPC分类号: A61K31/425 , A61K31/427 , A61K38/00 , A61K45/06 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D233/54 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07D521/00 , C07K5/06 , C07K5/065
CPC分类号: C07D207/08 , A61K31/425 , A61K31/427 , A61K45/06 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/59 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/26 , C07D213/30 , C07D213/34 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/61 , C07D213/75 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/14 , C07D235/16 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/56 , C07D295/13 , C07D295/205 , C07D295/215 , C07D303/36 , C07D307/42 , C07D333/16 , C07D401/12 , C07D413/12 , C07D417/12 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
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公开(公告)号:US5151438A
公开(公告)日:1992-09-29
申请号:US675780
申请日:1991-03-27
申请人: Hing L. Sham , Daniel W. Norbeck , Dale J. Kempf , Chen Zhao
发明人: Hing L. Sham , Daniel W. Norbeck , Dale J. Kempf , Chen Zhao
IPC分类号: A61K38/00 , C07C33/46 , C07C43/164 , C07C43/174 , C07C43/205 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/56 , C07C45/59 , C07C45/62 , C07C45/67 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C217/48 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C381/00 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/30 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/70 , C07D213/81 , C07D213/82 , C07D215/16 , C07D217/16 , C07D217/26 , C07D233/84 , C07D239/38 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/36 , C07D277/42 , C07D277/56 , C07D295/088 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D303/04 , C07D303/22 , C07D303/36 , C07D303/48 , C07D417/12 , C07D487/04 , C07D521/00 , C07F9/32 , C07F9/53 , C07K5/02 , C07K5/06
CPC分类号: C07D213/30 , C07C211/27 , C07C215/18 , C07C215/20 , C07C215/28 , C07C217/48 , C07C229/08 , C07C229/26 , C07C229/34 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/12 , C07C235/34 , C07C235/78 , C07C237/10 , C07C237/20 , C07C237/22 , C07C239/10 , C07C239/18 , C07C239/20 , C07C247/10 , C07C251/40 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/13 , C07C311/18 , C07C317/10 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/25 , C07C33/46 , C07C381/00 , C07C43/164 , C07C43/1742 , C07C43/2055 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/315 , C07C45/004 , C07C45/29 , C07C45/567 , C07C45/59 , C07C45/62 , C07C45/673 , C07C45/74 , C07C53/134 , C07C69/34 , C07C69/65 , C07C69/732 , C07D207/08 , C07D207/24 , C07D209/42 , C07D211/62 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/70 , C07D213/81 , C07D213/82 , C07D215/16 , C07D217/16 , C07D217/26 , C07D231/12 , C07D233/56 , C07D233/84 , C07D239/38 , C07D249/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D277/36 , C07D277/42 , C07D277/56 , C07D295/088 , C07D295/15 , C07D295/155 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D303/04 , C07D303/22 , C07D303/36 , C07D303/48 , C07D417/12 , C07D487/04 , C07F9/3241 , C07F9/5333 , C07K5/021 , C07K5/06043 , C07K5/06052 , C07K5/06191 , A61K38/00
摘要: Compounds are disclosed which are retroviral protease inhibitors. Also disclosed are methods of using the compounds and compositions for inhibiting a retroviral protease and for treating an HIV infection.
摘要翻译: 公开了作为逆转录病毒蛋白酶抑制剂的化合物。 还公开了使用化合物和组合物抑制逆转录病毒蛋白酶和治疗HIV感染的方法。
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公开(公告)号:US4725584A
公开(公告)日:1988-02-16
申请号:US830614
申请日:1986-02-19
申请人: Jay R. Luly , Jacob J. Plattner , Hing L. Sham
发明人: Jay R. Luly , Jacob J. Plattner , Hing L. Sham
IPC分类号: A61K38/00 , C07K5/065 , A61K31/65 , A61K37/43 , C07C103/20 , C07C125/06 , C07K5/06 , C07K7/02
CPC分类号: C07K5/06078 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要: The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are independently selected from loweralkyl or lipophilic or aromatic amino acid side chains; and R.sub.4 is hydrogen, loweralkyl, loweralkylmercapto or loweralkylsulfonyl.
摘要翻译: 本发明涉及下式的肾素抑制化合物,其中A是N-保护基; R1,R2,R3和R5独立地选自低级烷基或亲油或芳族氨基酸侧链; R4是氢,低级烷基,低级烷基巯基或低级烷基磺酰基。
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