Peptidylaminodiols

Details Peptidylaminodiols Peptidylaminodiols

1991-06-10

1992-02-25

Ramsuer, Robert W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

564336, 564507, C07C21103, C07C27112

Patent

active

050915754

ABSTRACT:
A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sup.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl; phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl; lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

REFERENCES:
Chemical Abstracts 79-105010: Pansevich-Kolyada et al, Oxide Compounds Vesdi Akad. Navok Belaros. SSR, Ser. Khim., Navuk 1973.
Chemical Abstracts 87-38779: Stel'tsov et al., Studies on Eopxy Compounds, Vesti Akad Navuk Belarus, SSR, Ser. Khim. Navuk, 1977.

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