SUBSTITUTED TETRAHYDRO-3-PYRIDINE-CARBOXYLIC ACID, ESTER, AND AMIDE CHOLINERGIC AGENTS

摘要

1,2,3,6-Tetrahydro- and 1,2,5,6-tetrahydropyridine-3-car-boxylic acids, esters, and amides having structural formula I …… wherein the dashed lines indicate the presence of only one carbon-carbon double bond either between carbon atoms numbers 3 and 4 or between carbon atoms numbers 4 and 5; R1 = hydrogen: C1-C6-alkyl, C2-C6 alkenyl, alkoxycarbonyl of from 2 to 5 C, C4-C8-cycloalkyl or phenyl-(C1-C6)-alkyl, wherein the phenyl ring may be substituted; R3 = -COOR, wherein R = hydrogen, C1-C6-alkyl, C2-C6-alkenyl; C3-C8-cycloalkyl or phenyl, which may be substituted; -CONR min R sec , wherein R min and R sec are independently hydrogen or cycloalkyl, benzyloxy or phenyl-(C1-C6)-alkyl, wherein the phenyl ring may be substituted, or R min and R sec when taken together with the nitrogen atom to which they are attached from a 5 to 7 membered heterocyclic ring which may contain another heteroatom selected from N,0 or S; R4 = C1-C6-alkyl, C2-C6-alkenyl,C3-C8-cycloalkyl, 2- or 3-thienyl, phenyl, which may be substituted or phenyl-(C1-C6)-alkyl, wherein the phenyl group may be substituted, and the pharmaceutically acceptable salts thereof, possessing muscarinic binding activity, having utility for the treatment of the symptoms of senile cognitive decline are disclosed. Pharmaceutical compositions and pharmaceuticals are also disclosed.