1,5-benzothiazepine derivatives, their preparation and their...

C - Chemistry – Metallurgy – 07 – D

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C07D 281/10 (2006.01) A61K 31/55 (2006.01) C07D 417/04 (2006.01) C07D 417/06 (2006.01) C07D 417/10 (2006.01)

Patent

CA 1336712

Compounds of formula (I): Image (I) [in which: R1 is aryl or aromatic heterocyclic; R2 and R3 are hydrogen, alkyl, alkoxy, halogen, phenyl, phenoxy, C1 - C6 alkylthio, phenylthio, C1 - C6 haloalkyl, cyano or nitro, or together are alkylene optionally containing oxygen; R4 is hydrogen, aliphatic acyl, cycloalkylcarbonyl, cycloalkoxycarbonyl, aromatic acyl, alkoxycarbonyl or benzyloxycarbonyl; R5 and R6 are alkyl; and X is oxygen, sulfur or methylene] have calcium channel blocking activity and can serve for the treatment or prophylaxis of cardiovascular diseases and disorders. They may be prepared by reacting a corresponding compound where R4 is hydrogen and the aminoethyl group is replaced by hydrogen with a compound providing the aminoethyl group and then, if required, acylating the product.

606525

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