abstract |
1,4-di-substituted piperidine muscarinic antagonists of the above formula or an isomer, pharmaceutically acceptable salt, ester or solvate thereof, wherein X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR7)2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH2-, -CH(C1-C6 alkyl)-, -C(C1-C6 alkyl)2-, -CONR17-, -NR17CO-, -O-C(O)NR17-, -NR17C(O)-O-, -SO2NR17- or -NR17SO2-; R is C3-C6 cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl; R2 is H, alkyl, optionally substituted cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted piperidinyl; and the remaining R variables are as defined in the specification, are disclosed. Compounds of the above formula are useful for treating cognitive disorders such as Alzheimer's disease. Also disclosed are pharmaceutical compositions, methods of preparation and combinations of compounds (kits) of the above formula with Acetylcholinesterase inhibitors and pharmaceutically acceptable carriers. |