1,5-benzothiazepine derivative and processes for preparing...

C - Chemistry – Metallurgy – 07 – D

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260/238.6

C07D 281/10 (2006.01)

Patent

CA 1218992

- 1 - ABSTRACT OF DISCLOSURE The invention provides novel 1/5-benzothiazepine derivatives of the formula: Image (I) wherein R1 and R4 are: a) R1 is lower alkyl or lower alkoxy, and R4 is lower alkyl, lower alkoxy, fluorine, benzyloxy, hydroxy or lower alkylthio, or b) R1 is lower alkyl, and R4 is hydrogen, or c) R1 is hydroxy, and R4 is lower alkyl, fluor- ine, hydroxy or lower alkylthio; R2 is hydrogen, lower alkanoyl or benzoyl; and R3 is lower akyl; and a pharmaceutically acceptable acid ad- dition salt thereof. The derivatives (I) and their salts have a potent platelet aggregation-inhibiting activity and are thus useful for the therapeutic treatment of thrombosis.

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