PURPOSE: To provide a platelet coagulation inhibitor containing a specific 1,5- benzothiazepine derivative or its acid addition salt as an active component, having excellent platelet coagulation inhibiting activity, keeping the effect for a long period even by oral administration and useful for the remedy and prevention of thrombosis.
CONSTITUTION: The objective platelet coagulation inhibitor contains the 1,5- benzothiazepine derivative of formula I (R1 is lower alkyl; R2 is H or lower alkanoyl; R3 is lower alkyl; one of R4 and R5 is H and the other is Cl) or its acid addition salt as an active component. The compound of formula I has excellent platelet coagulation inhibiting activity and useful for the remedy, amelioration and prevention of thrombosis such as cerebral infarction, transient cerebral ischemia, myocardial infarction, etc. The compound of formula I can be produced by condensing the compound of formula II with the compound of formula III (Q is H or protecting group; X1 is halogen) in a solvent such as acetone in the presence of a base at 25W100°C.
OISHI ATSUO
NAKAJIMA HIROMICHI
NAGAO HIROSHI
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