PIPERIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS

• Main Authors: BIELIK ATTILA, HORVÁTH CSILLA, BARTÁNÉ SZALAI GIZELLA, KESERÜ GYÖRGY, KOLOK SÁNDOR, NAGY JÓZSEF, VÁGÓ ISTVÁN, IGNÁCZNÉ SZENDREI GYÖRGYI, DOMÁNY GYÖRGY, KOVÁCSNÉ BOZÓ ÉVA, BORZA ISTVÁN, FARKAS SÁNDOR
• Format: Patent
• Language: English; Polish
• Published: 30.04.2014
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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.