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发明授权
US4977277A Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof 失效
官能化肽基氨基二醇和三醇4-氨基-5-环己基-3-羟基-1,2-氧代戊烷及其衍生物

Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof
摘要：
The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected)-(alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, .alpha.-methylbenzyl, .alpha., .alpha.-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)-methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R.sub.1 is phenoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen; R.sub.3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R.sub.4 is lower-alkyl, cycloalkyl- methyl or benzyl; R.sub.2, R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl; X is O, NH or S; R.sub.7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R.sub.12 and R.sub.13 are independently hydrogen or loweralkyl, n is 0-2 and R.sub.14 is substituted or unsubstituted phenyl or heterocyclic; or XR.sub.7 together are loweralkylsulfonyl, N.sub.3 or Cl, and pharmaceutically acceptable salts thereof.
摘要（中）：

本发明涉及下式的肾素抑制化合物：其中A是氢; 低级烷基 芳烷基 OR 8或SR 8，其中R 8是氢，低级烷基或氨基烷基; NR 9 R 10其中R 9和R 10独立地选自氢，低级烷基，氨基烷基，氰基烷基和羟烷基; 其中B是NH，烷基氨基，S，O，CH 2或CHOH，R 11是低级烷基，环烷基，芳基，芳基烷基，烷氧基，烯氧基，羟基烷氧基，二羟基烷氧基，芳基烷氧基，芳基烷氧基烷基，氨基，烷基氨基，二烷基氨基，（羟基烷基） 烷基）氨基，（二羟基烷基）（烷基）氨基，羧酸取代的烷基，烷氧基羰基烷基，氨基烷基，N-保护的氨基烷基，烷基氨基烷基，二烷基氨基烷基，（N-保护的） - （烷基）氨基烷基，（杂环）烷基或取代或 未取代的杂环; R1是低级烷基，环烷基甲基，苄基，α-甲基苄基，α，α-二甲基苄基，4-甲氧基苄基，卤代苄基，（1-萘基） - 甲基，（2-萘基）甲基，（4-咪唑基）甲基，苯乙基，苯氧基， 噻吩氧基或苯胺基; 如果R1是苯氧基，硫代苯氧基或苯胺基，B是CH 2或CHOH或A是氢; R3是低级烷基，苄基或杂环取代的甲基; R4是低级烷基，环烷基 - 甲基或苄基; R2，R5和R6独立地是氢或低级烷基; X是O，NH或S; R 7为氢，低级烷基，烷酰基，烷基磺酰基，其中R 12和R 13独立地为氢或低级烷基，n为0-2，R 14为取代或未取代的苯基或杂环基; 或XR7一起是低级烷基磺酰基，N 3或Cl，及其药学上可接受的盐。

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