Functionalized peptidyl aminodiols and -triols 4-amino-5-cyclohexyl-3-hydroxy-1,2-oxopentane and derivatives thereof

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United States of America Patent

PATENT NO 4977277
SERIAL NO

07361522

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; OR.sub.8 or SR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or aminoalkyl; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; ##STR2## wherein B is NH, alkylamino, S, O, CH.sub.2 or CHOH and R.sub.11 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; R.sub.1 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 R.sub.1 is phenoxy, thiophenoxy or anilino, B is CH.sub.2 or CHOH or A is hydrogen; R.sub.3 is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R.sub.4 is lower-alkyl, cycloalkyl-methyl or benzyl; R.sub.2, R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl; X is O, NH or S; R.sub.7 is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl ##STR3## wherein R.sub.12 and R.sub.13 are independently hydrogen or loweralkyl, n is 0-2 and R.sub.14 is substituted or unsubstituted phenyl or heterocyclic; or XR.sub.7 together are loweralkylsulfonyl, N.sub.3 or Cl, and pharmaceutically acceptable salts thereof.

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Patent Owner(s)

Patent OwnerAddress
ABBOTT LABORATORIES A CORP OF ILNORTH CHICAGO IL

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Luly, Jay R Libertyville, IL 68 1277
Plattner, Jacob J Libertyville, IL 140 2666
Rosenberg, Saul H Libertyville, IL 34 1439

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