| abstract |
Esters, of polar acidic metabolites of atropine, siopolamine etc. of formula (I) and having anticholinergic or mydriatic properties are new. where R' = esterification residue of a pharmaceutically acceptable, non-toxic, opt. substd. cyclic or opt.branched 1-8C alcohol (R'-OH) such that COOR1 is metabolically hydrolysable to R'-OH and a non-toxic metabolite of (I) following admin. R2 =opt. substd. aryl, cycloalkyl or alkyl of 1-8C; R3 = H or R2; n = 0-4; X = -O-CO-; -NR8-CO-, -CO-, -CR9R10-, -S-, -O- or -NH-; R8 = H or opt. branched 1-5C alkyl; R9, R10 = H or 1-5C alkyl; m = 0-4; R4 = bicyclic amine gp. formula (a), (b) or (c), -NR6R6, -NR5R6R7(+), o, m- or p-substd. alkyl pyridine, or non-toxic quat. ammonium salt gp. (-N(B)3(+)X(-)); R5, R6, R7 = 1-5C aklyl; X(-)=anion. |