abstract |
A renin inhibiting compound of formula (I), wherein A is a substituent; W is C=O or CHOH; U is CH2? or NR2?, provided that when W is CHOH then U is CH2?; R1? 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; R2? is hydrogen or loweralkyl; R3? is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R4? is loweralkyl, cycloalkylmethyl or benzyl; R5? is vinyl, formyl, hydroxymethyl or hydrogen; R7? is hydrogen or loweralkyl; R8? and R9? are independently selected from OH and NH2?; and R6? is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R5? and R7? are both hydrogen and R8? and R9? are OH, the carbon bearing R5? is of the ''R'' configuration and the carbon bearing R6? 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. |