1,5-benzothiazepine derivatives and preparation thereof

C - Chemistry – Metallurgy – 07 – D

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167/209, 260/238

C07D 281/02 (2006.01) A61K 31/55 (2006.01) C07D 281/10 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2023790

- 69 - Abstract of the disclosure: Novel 1,5-benzothiazepine derivatives of the formula: Image wherein X is hydrogen atom, a halogen atom or a lower alkyl group; R1 is a lower alkyl group or a lower alkoxy group; R2 is hydrogen atom, a lower alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenyl-lower alkyl group or a diphenyl-lower alkyl group; R3 is a lower alkyl group or a substituted or unsubstituted phenyl-lower alkyl group, Q is single bond, or an alkylene or lower alkenylene group which may optionally be substituted by a lower alkoxy group or oxo group; R4 is (i) hydrogen atom, (ii) a lower alkyl group, (iii) an N-phenyl- N-lower alkylamino group, (iv) a phenyl, phenyloxy, phenyl- thio, benzenesulfonylamino, 1,4-benzoquinonyl or benzylthio group which may optionally have substituent, or (v) a heterocyclic group which may optionally have substituent; and n is 2 or 3, or a pharmaceutically acceptable salt thereof, which are useful as a calcium antagonist, and the process for preparing thereof.

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