SPIRO[HETEROZYCLISCHE-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZIN]-4'-ONE, IHRE HERSTELLUNG UND DIESE ENTHALTENDE ARZNEIMITTEL

PCT No. PCT/FR95/01430 Sec. 371 Date Jun. 30, 1997 Sec. 102(e) Date Jun. 30, 1997 PCT Filed Oct. 30, 1995 PCT Pub. No. WO96/14318 PCT Pub. Date May 17, 1996Compounds of formula (I): (I) wherein R3 and R4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine...

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Hauptverfasser: AUDIAU, FRANCOIS, F-94220 CHARENTON-LE-PONT, FR, MIGNANI, SERGE, F-92290 CHATENAY-MALABRY, FR, JIMONET, PATRICK, F-78450 VILLEPREUX, FR, DAMOUR, DOMINIQUE, F-75014 PARIS, FR, GENEVOIS-BORELLA, ARIELLE, F-94320 THIAIS, FR, BARREAU, MICHEL, F-91230 MONTGERON, FR, ALOUP, JEAN-CLAUDE, F-94290 VILLENEUVE-LE-ROI, FR, RIBEILL, YVES, F-91360 VILLEMOISSON-SUR-ORGE, FR
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Zusammenfassung:PCT No. PCT/FR95/01430 Sec. 371 Date Jun. 30, 1997 Sec. 102(e) Date Jun. 30, 1997 PCT Filed Oct. 30, 1995 PCT Pub. No. WO96/14318 PCT Pub. Date May 17, 1996Compounds of formula (I): (I) wherein R3 and R4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl, -CHO, -COOR11, -CO-alk-COOR6, -CO-alk-NR6R12, -CO-alk-CONR6R8, -CO-COOR6, -CO-CH2-O-CH2-COOR6, -CO-CH2-S-CH2-COOR6, -CO-CH=CH-COOR6, CO-alk, -CO-Ar'', -CO-alk-Ar'', -CO-NH-Ar'', -CO-NH-alk-Ar'', -CO-Het, -CO-alk-Het, -CO-NH-Het, -CO-NH-alk-Het, -CO-NH2, -CO-NH-alk, -CO-N(alk)alk', -CS-NH2, -CS-NH-alk, -CS-NH-Ar'', -CS-NH-Het, -alk-Het, -alk-NR6R8, -alk-COOR6, -alk-CO-NR6R8, -alk-Ar'', -SO2-alk or -SO2-Ar radical, or a -CO-cycloalkyl radical where the cycloalkyl is optionally 2-substituted by a carboxyl radical; or (b) a 2-pyrrolidin-5-one ring. The compounds of formula (I) have useful pharmacological properties and are alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and especially NMDA receptor glycine modulation site ligands.