发明公开
EP0230266A3 Functionalized peptidyl aminodiols and -triols 失效
功能性磷酸二肽和 -

Functionalized peptidyl aminodiols and -triols
摘要:
The invention relates to renin inhibiting compounds of the formula
wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl;
wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ 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; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-di­methylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)­methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R₄ is lower­alkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl.
wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted penyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
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