Benzothiazepine derivatives and their methods of preparation

Details Benzothiazepine derivatives and their methods of preparation Benzothiazepine derivatives and their methods of preparation

1984-06-28

1985-09-03

Bond, Robert T.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07D28102

Patent

active

045391505

ABSTRACT:
This invention relates to benzothiazepine derivatives of the general formula ##STR1## where K is hydrogen or a --CH.sub.2 COOR.sub.2 group where R.sub.2 is hydrogen or a lower alkyl group, Z is hydrogen or phenyl except when both K and Z are hydrogen, and Y is hydrogen, a --CHR.sub.3 --COOR.sub.1 group, an alkanoyl group or a --COO(CH.sub.2).sub.n R.sub.4 group where R.sub.1 is hydrogen or a lower alkyl group, R.sub.3 is hydrogen, an alkyl group, an alkylphenyl group or an aryl-lower alkyl group, R.sub.4 is an aryl group and n is a whole number of 1 to 10, and to their methods of preparation.
The benzothiazepine derivatives of this invention, including their salts, have a powerful inhibitory effect on the angiotensin converting enzyme and exert a marked depressor effect in such models of hypertension as spontaneously occurring hypertensive rats and the like, so that they are useful as drugs for the treatment of hypertension and other cardiovascular diseases. In addition, these compounds are also useful as intermediates for the synthesis of coronary dilators, psychotropic drugs and the like.

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