Muscarinic antagonists for treating memory loss

Details Muscarinic antagonists for treating memory loss Muscarinic antagonists for treating memory loss

1997-07-08

1999-09-14

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514314, 514320, 514321, 514323, 546152, 546179, 546193, 546196, 546197, 546201, A61K 31445, C07D40104

Patent

active

059523492

ABSTRACT:
1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, --O--, --SO.sub.0-2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 --C.sub.6 alkyl)--, --C(C.sub.1 --C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --; R is C.sub.3 --C.sub.6 cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl; R.sup.1 is H, --CN, --CF.sub.3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, --COR.sup.15, --COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or --CON(R.sup.13).sub.2 ; R.sup.2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; and R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.13, R.sup.15 and R.sup.17 are as defined in the specification are disclosed as being useful for treating cognitive disorders such as Alzheimer's disease; also disclosed are pharmaceutical compositions, methods of preparation and combinations of compounds of formula I capable of enhancing ACh release with ACh'ase inhibitors.

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