Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.
Patent
1991-11-18
1993-05-25
Griffin, Ronald W.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Tripeptides, e.g., tripeptide thyroliberin , etc.
560115, 564336, 564507, C07C21103, C07C27112
Patent
active
052141292
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.sub.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, loweralkenyl, 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:
patent: 4548926 (1985-10-01), Matsueda et al.
patent: 4657931 (1987-04-01), Baran et al.
patent: 5091575 (1992-02-01), Luly et al.
Chemical Abstracts 79:105010. Pansevich-Kolyada et al., Oxide Compounds Vesdi Akad. Navok Belaros. SSR, Ser, Khim., Navuk, 1973.
Chemical Astracts 87:38779. Stel'tsov et al., Studies on Epoxy Compounds, Vesti Akad Navuk Belarus, SSR, Ser. Khim. Navuk, 1977.
Kempf Dale J.
Luly Jay R.
Plattner Jacob J.
Abbott Laboratories
Crowley Steven R.
Griffin Ronald W.
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