Synthetic vincamines and benzoic acid deriv. compsns. - opt. contg. ascorbic acid for treating thrombosis esp. of the brain

摘要

Therapeutic vincamine-type compsns. contg. (i) =1 cpd. of formulae (I) or (II): (where Z is (a) an ether gp. R.A.O.CH2- where A is 1-5C alkylene; R is the gp. where R1 and R2 are H or 1-5C alkyl; a 5-7 membered N-heterocycle opt. contg. a second heteroatom (O, N or S); a phenyl gp. where R3, R4 and R5 are H, halo, NO2, 1-3C alkyl, 1-3C haloalkyl or 1-3C alkoxy; (b) an ester gp. R6.O2C- where R6 is a 2-10C alkyl R7, or a gp. of formula: where R8 and R9 are H or Me; R10 is 1-4C alkyl or the gp. where m is is 1-5; n is 2-7; or the gp. Z is a gp. of formula: where R11, R12 and R13 are H or Me); (ii) =1 benzoic acid derivs., namely, salicylamide, 2-acetoxybenzoic acid and its salt esters and amides, and the isomeric diacetoxybenzoic aceds, their salts, esters and amides), are new. The compsns. of cerebral vasodilator (i) and inhibitors of blood platelet aggregation (ii) are partic. for treating thrombotic episodes, esp. in the brain, in man and animals. Addn. of ascorbic acid to the compns. potentiates the activity by increasing the absorption of (I) and (II).