abstract |
A COMPOUND OF FORMULA 1: WHEREIN A REPRESENTS: D REPRESENTS OXYGEN OR SULFUR; E REPRESENTS A SINGLE BOND, OXYGEN, SULFUR , OR NR10; R REPRESENTS HYDROGEN OR METHYL; AR1 REPRESENTS A 5- OR 6- MEMBERED AROMATIC OR HETEROAROMATIC RING CONTAINING ZERO TO THEREE NITROGEN ATOMS, ZERO OR ONE OXYGEN ATOM, AND ZERO OR ONE SULFUR ATOM; AR2 REPRESENTS A 5- OR 6-MEMBERED AROMATIC OR HETEROAROMATIC RING CONTAINING ZERO TO THREE NITROGEN ATOMS, ZERO OR ONE OXYGEN ATOM, AND ZERO OR ONE SULFUR ATOM OR; AN 8-, 9- OR 10- MEMBERED FUSED AROMATIC OR HETEROAROMATIC RING SYSTEM CONTAINING ZERO TO THREE NITROGEN ATOMS, ZERO TO ONE OXYGEN ATOM, AND ZERO TO ONE SULFUR ATOM; THE AROMATIC RINGS AR1 AND AR2 ARE OPTIONALLY SUBSTITUTED WITH ONE TO THREE SUBSTITUENTS SELECTED FROM: HALOGEN C1-4 ALKYL, C2-4 ALKYL, CN, NO2, NR1R2, CH2NR1R2, OR3, CH2OR3, CF3; R1, R2 AND R3 ARE INDEPENDENTLY C1-4 ALKYL , ARYL , HETEROARYL, C(O)R5, C(O)NHR6, C(O)R7, SO2R8 OR R1 AND R2 MAY TOGETHER BE (CH2)jG(CH2)k WHERE G IS OXYGEN, SULFUR, NR9, OR A BOND ; j IS 2 TO 4; k IS 0 TO 2: R4, R5, R6, R7, R8, R9 AND R10 ARE INDEPENDENTLY C1-4ALKYL, ARYL, OR HETEROARYL; OR AN ENANTIOMER THEREOF AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF; WITH THE PROVISOS THAT : (1) IF D REPRESENTS OXYGEN, E REPRESENTS A SINGLE BOND, AND A REPRESENTS: AND EITHER AR1 OR AR2 REPRESENTSA PYRAZOLE RING, THEN ALL OPTIONAL SUBSTITUENTS ON THE PYRAZOLE RING SHALL BE HYDROGEN; AND (2) IF AR1 REPRESENTS A PYRIDINE RING , AR2 REPRESENTS AN ARYL RING, AND A REPRESENTS: THEN ALL OPTIONAL SUBSTITUENTS ON THE PYRIDINE RING SHALL BE HYDROGEN; AND (3) FORMULA I DOES NOT REPRESENT: PROCESSES FOR PREPARING THEM, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN THERAPY, ESPECIALLY IN THE TREATMENT PROPHYLAXIS OF PSYCHOTIC AND INTELLECTUAL IMPAIRMENT DISORDERS. |