abstract |
REFERS TO BENZOXAZINONE DERIVATIVES OF FORMULA I WHERE Y IS C or S; m IS 1 WHEN Y IS C and m IS 2 WHEN Y IS S; n IS 1 or 2; p ES 0-3; q IS 1-3; Z IS (CRaRb) r, or SO2; Ra AND Rb ARE H or ALKYL; r IS 0-2; X IS CH or N; R1 IS H, HALOGEN, ALKYL, HALOALKYL, HETEROALKYL, ALCOXY, CYANE, AMONG OTHERS; R2 IS ARYL OR HETEROARYL, BOTH OPTIONALLY REPLACED; R3 AND R4 ARE H or ALKYL, or BOTH TOGETHER WITH THEIR SHARED CARBONS FORM A 3-6 MEMBER CYCLOALKYL RING; R5, R6, R7, R8 AND R9 ARE H or ALKYL, OR ONE OF R5 AND R6 TOGETHER WITH ONE OF R7, R8 AND R9 AND THE ATOMS IN THE MIDDLE CAN FORM A RING OF 5-7 MEMBERS. PREFERRED COMPOUNDS ARE: 4-BENZYL-6-METHYL-8-PIPERAZIN-1-IL-4H-BENZO [1,4] OXAZIN-3-ONA; 4-BENZYL-6-METOXY-8-PIPERAZIN-1-IL-4H-BENZO [1,4] -OXAZIN-3-ONA; 4- (2-FLUORO-BENZYL) -6-METOXY-8-PIPERAZIN-1-IL-4H-BENZO [1,4] OXAZIN-3-ONA; AMONG OTHERS. IT ALSO REFERS TO A PROCESS TO PRODUCE SUCH COMPOUNDS AND A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS ARE MODULAR OF 5-HYDROXITRIPTAMINE (5-HT) AND ARE USEFUL TO TREAT OR PREVENT DISORDERS OF THE CENTRAL NERVOUS SYSTEM AND OF THE GASTROINTESTINAL TRACT |