Amino acid derivatives useful for treating high blood pressure

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United States of America Patent

PATENT NO 5278148
SERIAL NO

07499852

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Abstract

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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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Patent Owner(s)

  • HOFFMANN-LA ROCHE INC.

International Classification(s)

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Branca, Quirico Basel, CH 19 373
Marki, Hans P Basel, CH 6 147
Neidhart, Werner Freiburt im Breisgau, DE 91 695
Ramuz, Henri Birsfelden, CH 44 674
Wostl, Wolfgang Grenzach-Wyhlen, DE 59 750

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