FUNCTIONALIZED PEPTIDYL AMINODIOLS AND TRIOLS

    公开(公告)号:AU6759887A

    公开(公告)日:1987-07-23

    申请号:AU6759887

    申请日:1987-01-15

    Applicant: ABBOTT LAB

    Abstract: 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, alpha -methylbenzyl, alpha , alpha -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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