Benzothiazepine derivatives and their methods of preparation
US4539150A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 28, 1984 |
| Grant date | Sep 3, 1985 |
| Priority date | — |
| Expiry date | Jun 28, 2004 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D281/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.