Piperidinderivater som NMDA-reseptorantagonister

• Main Authors: DOMANY GYORGY, BIELIK ATTILA, SZENDREI GYORGYI IGNACZNE, BOZO EVA KOVACSNE, FARKAS SANDOR, BORZA ISTVAN, KOLOK SANDOR, NAGY JOZSEF, SZALAI GIZELLA BARTANE, VAGO ISTVAN, KESERU GYORGY, HORVATH CSILLA
• Format: Patent
• Language: Norwegian
• Published: 23.03.2004
• Edition: 7

The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, 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-C4 alkyl, -S or -SH groups; W: is -CO-, -CH2- or -CH2-(C1-C4 alkyl)-; X: is -CO-; Y: is -O-, C1-C4 alkylene, C1-C4 alkynylene, cycloalkylene, aminocarbonyl, -NH-, -N(C1-C4 alkyl)-, -C1-C4 alkylene-N(C1-C4 alkyl)-, -CH2O-, -CH(OH)- or -OCH2-; Z: is hydrogen, halogen, nitro, amino, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluoromethyl, hydroxyl or carboxyl; R1 and R2: are hydrogen, or together form a C1-C3 bridge; and n 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.