Thieno-pyrimidine, thieno-oxazine and thienyl oxamate derivs. - useful as antiallergic agents with high oral activity

摘要

Thienopyrimidine, thienooxazine and thienyl oxamate derivs. of formulae (I), (II) and (III) are new. In the formulae, R2 is COOR3, CH=CHCOOR3, CH2OH, CH2OCOH, CH2OCOR, 5-tetrazolyl, N-(5-tetrazolyl)carbamoyl or CHO; where R is 1-8C alkyl. R3 is H, 1-8C alkyl or M; where M is a cation. R5 and R6 are H, halogen, 1-8C alkyl, 3-6C alkenyl, 1-6C alkoxy, OH, NO2, NH2, phenyl or 2-6C alkanoyl; R5 and R6 can also form an opt. R-substd. 5-7C cycloalkane ring. A is a direct bond or CH=CH. L and B are H, 1-8C alkyl, 3-6C alkenyl, phenyl or 2-6C alkanoyl, or together form an opt. R-substd. 5-7C cycloalkene ring). Cpds. (I)-(III) are antiallergic agents with high oral activity (e.g. with ID50 values of 3.1-34 mg/kg, rat, in PCA test) and low toxicity (e.g. with LD50 >1600mg/kg). Cpds. (II) and (III) are also useful as intermediates for (I).