发明名称 RENIN INHIBITING N-(2-AMINO-2-OXOETHYL)BUTANEDIAMIDE DERIVATIVES
摘要 Disclosed herein are compounds of the formula: A-N(R1)C(O)CH2CHR2C(O)-B, wherein A is R3R4NC(O)CH2 wherein, for example, R3 is hydrogen or alkyl and R4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R3 and R4 together with the nitrogen atom to which they are attached form a pyrroli dino, piperidino, morpholino or thiomorpholino; R1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethy l; R2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, ¢1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl! amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure .
申请公布号 CA2143300(C) 申请公布日期 1998.04.21
申请号 CA19932143300 申请日期 1993.09.15
申请人 BOEHRINGER INGELHEIM (CANADA) LTD./ BOEHRINGER INGELHEIM (CANADA) LTEE. 发明人 SIMONEAU, BRUNO;LAVALEE, PIERRE
分类号 C07D295/18;A61K31/16;A61K31/165;A61K31/40;A61K31/4015;A61K31/415;A61K31/44;A61K31/4402;A61K31/4418;A61P9/12;A61P43/00;C07C233/18;C07C237/22;C07D207/26;C07D213/40;C07D233/64;C07D277/28;C07D277/30;C07D277/40;C07D295/185;C07D295/215;C07D417/12;(IPC1-7):C07C237/22;C07D417/00;C07D409/12;C07D413/12;C07D277/20;C07D333/24;C07D207/27;A61K31/33 主分类号 C07D295/18
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