Amino acid derivatives useful for treating high blood pressure

Details Amino acid derivatives useful for treating high blood pressure Amino acid derivatives useful for treating high blood pressure

1990-03-27

1994-01-11

Higel, Floyd D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514365, 514400, 514407, 514438, 514530, 514540, 514548, 514551, 514616, 514620, 514626, 548214, 5483355, 5483381, 5483731, 5483751, 5483365, 549 75, 549 76, 549 77, 560 19, 560 37, 560 38, 560155, 560157, 560159, 560169, 564164, 564192, 564193, 564194, 564196, 564197, A61K 3702, A61K 3743, C07K 506, C07K 508, C07C23308, C07C23502, C07C23702

Patent

active

052781488

ABSTRACT:
Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.-naphthyl, Y is a bivalent residue in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the control or prevention of high blood pressure and cardiac insufficiency.

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