QUINAZOLIN-4-ONE AMPA ANTAGONIST

PROBLEM TO BE SOLVED: To obtain the subject new compound useful for a pharmaceutical composition for treating a neurodegenerative, psychotropic and drug- and alcohol-induced disease of central nervous system and peripheral nervous system. SOLUTION: This antagonist is a compound of formula I [A is a...

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Hauptverfasser: CHENARD BERTRAND LEO, WELCH WILLARD MCKOWAN, REINHOLD ANTHONY RONALD
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain the subject new compound useful for a pharmaceutical composition for treating a neurodegenerative, psychotropic and drug- and alcohol-induced disease of central nervous system and peripheral nervous system. SOLUTION: This antagonist is a compound of formula I [A is a benzo-fusion aromatic ring or the like; B is phenyl or the like; X is N or CH; Y-Z is CH2 NH or the like; R is H, a (fluoro)alkyl or the like; R is a halo, cyano or the like; R to R are each H, an alkyl or the like], e.g. 2- [3-(2-chloro-pyridin-3-yl)-6- fluoro-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-amino}-benzonitrile. The compound of formula I is obtained, for example, by reacting a compound of formula II with acetic anhydride, and further reacting the obtained compound with an amine of formula III to provide a compound of formula IV, reacting the compound of formula IV with dimethylformamide dimethylacetal complex to provide the corresponding amines, reacting the corresponding amines with sodium periodade and further carrying out a reductive amination of the obtained product by an amine of formula V.