Peptidylaminodiols

Details Peptidylaminodiols Peptidylaminodiols

C - Chemistry, Metallurgy

07

D

167/211, 260/292

C07D 295/20 (2006.01) A61K 31/395 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07D 233/54 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) C07K 5/08 (2006.01) C07K 5/083 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1340940

A renin inhibiting compound of the formula: (see 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, loweralkenyl, 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.

527514

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