Piperidine derivatives as NMDA receptor antagonists

Details Piperidine derivatives as NMDA receptor antagonists Piperidine derivatives as NMDA receptor antagonists

2004-01-21

2008-10-14

Chang, Celia (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C514S230500, C514S322000, C514S323000, C544S106000, C546S198000, C546S199000, C546S201000

Reexamination Certificate

active

07435744

ABSTRACT:
The present invention relates to a compound of formula (I):wherein: V and U are hydrogen, halogen, C1-C4alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more:(a) hydrogen atoms;(b) carbon atoms;(c) —CH═ groups;(d) —CH2— groups; or(e) additional heteroatoms of the same or different type;or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C1-C4alkyl, ═S or —SH groups;W: is —CO—, —CH2— or —CH2—(C1-C4alkyl)-;X: is —CO—;Y: is —O—, C1-C4alkylene, C1-C4alkynylene, cycloalkylene, aminocarbonyl, —NH—, —N(C1-C4alkyl)-, -C1-C4alkylene-N(C1-C4alkyl)-, —CH2O—, —CH(OH)— or —OCH2—;Z: is hydrogen, halogen, nitro, amino, C1-C4alkyl, C1-C4alkoxy, cyano, trifluoromethyl, hydroxyl or carboxyl;R1and R2: are hydrogen, or together form a C1-C3bridge; andn and m: independently are 0-3, wherein n and m cannot each be 0;or an optical antipode, racemate or pharmaceutically-acceptable salt thereof. The carboxylic acid amide derivatives of formula (I) are highly effective and selective antagonists of the NMDA receptor.

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