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AssigneeMitsui Toatsu Chemicals, Inc.
InventorsTsutomu Katakami, Nobuyuki Fukazawa, Hajime Iizuka, Takashi Nishina, Isao Shirakawa
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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.
A benzothiazepine compound of the following formula ##STR8## wherein K is hydrogen or a --CH.sub.2 COOR.sub.2 group where R.sub.2 is hydrogen or a lower alkyl having 1 to 4 carbon atoms;
A process for preparing benzothiazepine compound of the following formula ##STR9## wherein Z is hydrogen or phenyl and Y' is hydrogen, an acyl group being alkanoyl having 1 to 5 carbon atoms including trifluoroacetyl and trichloroacetyl or benzoyl, a --COO(CH.sub.2)nR.sub.4 group where R.sub.4 is an acyl group being phenyl, tolyl or xylyl and n is a whole number of 1 to 10, benzyloxycarbonyl group having a substitute or substitutes of P-methoxy, P-chloro, P-nitro, 3,5-dimethoxy or 3,4,5-trimethoxy, or an alkoxycarbonyl group being t-butoxycarbonyl, which comprises reacting a compound of the following formula ##STR10## wherein Z is as previously defined, Y.sup.2 is the same as defined in Y' except that hydrogen is excluded and R.sub.5 is hydrogen, with 2-aminobenzenethiol to form a compound of the following formula ##STR11## wherein Z, Y.sup.2 and R.sub.5 are as previously defined;
A process for preparing benzothiazepine compound of the following formula ##STR12## wherein Z is hydrogen or phenyl, R.sub.1 is hydrogen or a lower alkyl group having 1 to 4 carbon atoms, R.sub.2 is hydrogen or a lower alkyl group 1 to 4 carbon atoms, and R.sub.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, an aralkyl group being benzyl or phenethyl or an aryl-lower alkyl group where aryl is tolyl or xylyl and lower alkyl has 1 to 4 carbon atoms, which comprises reacting a compound of the following formula
Dependencies are inferred from the claim text.