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1. 发明授权

US5354767A Renin inhibiting polyhydroxy-monoamides 失效
标题翻译：肾素抑制多羟基 - 单酰胺
公开(公告)号：US5354767A
公开(公告)日：1994-10-11
申请号：US990779
申请日：1992-12-10
申请人： Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
发明人： Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
IPC分类号： C07C235/08 , C07C235/26 , C07C235/34 , C07D233/54 , C07D233/88 , C07D277/36 , C07D307/58 , A61K31/16
CPC分类号： C07D233/64 , C07C235/08 , C07C235/26 , C07C235/34 , C07D233/88 , C07D277/36 , C07D307/58 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：R1CH2CH（X）CH（Y）CH（Z）CHR2C（O）NHCHR3CH（OH）CH（OH）R4其中R1是末端单元，例如低级环烷基或苯基; R2是例如任选取代的烷基，环烷基甲基，苄基，4-咪唑基甲基，2-噻吩基甲基或4-噻唑基甲基; R3是烷基，环烷基甲基或任选取代的苄基; R4是烷基或环烷基; X和Y各自为羟基，Z为氢，或X和Z各自为羟基，Y为氢; 条件是（a）带有R2的碳原子具有“R”构型，除非R2是2-噻吩基甲基或2-噻唑基甲基，X和Y各自为羟基，Z为氢，则带有R2的碳原子具有“ S“配置; （b）含有R 3和R 4的碳原子各自具有“S”构型; 和（c）位于最后所述两个碳原子之间的碳原子具有“R”构型。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

2. 发明授权

US5859014A Pyrimidinedione, pyrimidinetrione, triazinedione and tetrahydroquinazolinedione derivatives as .alpha..sub.1 -adrenergic receptor antagonists 失效
标题翻译：嘧啶二酮，嘧啶四酮，三嗪二酮和四氢喹唑啉二酮衍生物作为α1-肾上腺素能受体拮抗剂
公开(公告)号：US5859014A
公开(公告)日：1999-01-12
申请号：US658774
申请日：1996-06-05
申请人： Gary W. Bantle , Todd R. Elworthy , Angel Guzman , Saul Jaime-Figueroa , Francisco J. Lopez-Tapia , David J. Morgans, Jr. , Arturo Perez-Medrano , Jurg R. Pfister , Eric B. Sjogren , Francisco X. Talamas
发明人： Gary W. Bantle , Todd R. Elworthy , Angel Guzman , Saul Jaime-Figueroa , Francisco J. Lopez-Tapia , David J. Morgans, Jr. , Arturo Perez-Medrano , Jurg R. Pfister , Eric B. Sjogren , Francisco X. Talamas
IPC分类号： C07D237/16 , C07D239/22 , C07D239/54 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D239/96 , C07D253/075 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/12 , C07F7/08 , C07D239/04 , A61K31/505 , C07D239/10
CPC分类号： C07D239/22 , C07D237/16 , C07D239/54 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D239/96 , C07D253/075 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/12 , C07F7/0812
摘要： Compounds of Formula I: ##STR1## where R.sup.5 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## and the pharmaceutically acceptable salts and N-oxides thereof, are .alpha..sub.1 -adrenergic receptor antagonists useful for the treatment of diseases involving directly or indirectly an obstruction of the lower urinary tract, such as benign prostatic hyperplasia.
摘要翻译：（a），（b），（c）和（d）所示的基团：其中R 5是选自式（a），（b），（c）和（d）的基团：）（d）及其药学上可接受的盐和N-氧化物是α1-肾上腺素能受体拮抗剂，可用于治疗直接或间接地阻塞下尿路的疾病，例如良性前列腺增生。

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