The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jan. 11, 1994

Filed:

Mar. 27, 1990
Applicant:
Inventors:

Quirico Branca, Basel, CH;

Hans P Marki, Basel, CH;

Werner Neidhart, Freiburt im Breisgau, DE;

Henri Ramuz, Birsfelden, CH;

Wolfgang Wostl, Grenzach-Wyhlen, DE;

Assignee:

Hoffmann-La Roche Inc., Nutley, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ; A61K / ; C07K / ; C07K / ; C07C / ; C07C / ; C07C / ;
U.S. Cl.
CPC ...
514 19 ; 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 ;
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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