| abstract |
The present invention relates to compounds of the general formula R 1 wherein R 1 - R 4 is independently hydrogen, -CF 3> -OCF 3, OCHF 2, -OCH 2 F, lower alkyl, lower alkoxy, halogen, hydroxy, phenyl, benzyl, amino, nitro, pyrrole-1- yl, lower alkylsulfonyl, lower alkylsulfanyl, cyano or benzyloxy; or R 2 and R 3 may be together -O- (CH 2) 2 -O-, -O-CH 2 -O-, -O- (CH 2) 2-, - (CH 2) 3- or -CH = CH-CH = CH -; X is -N =, - N (R8) -or-CH =; Y means -N =, = N-, -N (R8) - or -CH =; wherein one of X or Y has to be nitrogen; R5 means the group v wherein R6 and R7 independently represent hydrogen, lower alkyl, -C (O)-lower alkyl, hydroxy-lower alkyl, lower alkenyl, -C (O) CH2OH or R6 and R7 may be together with the N atom - (CH 2) n -, - (CH 2) 2 -O- (CH 2) 2-, -CH 2 -CH = CH-CH 2, -CH 2 -CH [OC (O) CH 3] - (CH 2) 2, - CH2-CH [NHC (O) CH3] - (CH2) 2, -O- (CH2) 3-, -CH2-CH (OCH3) - (CH2) 2-, -CH2-CH (halogen) - (CH2) 2-, - (CH2) 2-CH (O-phenyl) - (CH2) 2-, - (CH2) 2-N (CHO) - (CH2) 2-, - (CH2) 2-N (COCH3HCH2) 2 -, -CH2-CH (OH> (CH2) 3-, - (CH2) 2 -CH (OH) - (CH2) 2- or - (CH2) 2-N (benzyl) -CH:) 2-; n means 3 to 5; and R8 is hydrogen, lower alkyl, lower alkenyl, lower alkinyl, - (CH2) mO-lower alkyl, - (CH2) m-OH, - (CH2) m-CHF2, - (CH2) m -CH2F, - (CH2 ) mC (O)-lower alkyl, - (CH 2) mC (O) O-lower alkyl, - (CH 2) m-CH (OH)-lower alkyl, - (CH 2) m-CH (OH) - (CH 2) mOH, - (CH2) m -C6H5, which phenyl ring is optionally substituted with lower alkyl, lower alkoxy or hydroxy, - (CH2) mC (= CH2)-lower alkyl, - (CH2) m-cycloalkyl) - (CH2) m -CN, - (CH2) m-pyridin-4-yl, - (CH2) m-pyridin-3-yl or - (CH2) m-pyridin-2-yl; m means 0 to 4; and their pharmaceutically acceptable acid addition salts. These compounds can be used for the treatment of diseases related to NMDA receptor subtype selective blocking agents. |