| abstract |
Compounds of formula (I) in which A represents a direct bond, C1-C4 alkyl, or C1-C4 alkenyl; n is 0, 1 or 2; R1 represents hydrogen, C1-C6 alkyl, aryl, C1-C3 alkylaryl, C1-C3 alkylheteroaryl, or - (CH2) mR6; W, X, Y and Z each independently represent oxygen, sulfur, nitrogen or carbon, provided that at least one of W, X, Y or Z represents nitrogen; R2, R3, R4 and R5 each independently represent hydrogen, C1-C6 alkyl, aryl, C1-C3 arylaryl, C1-C3 alkylheteroaryl, halogen, cyano, trifluoromethyl, nitro, -OR7, -NR7R8, - (CH2) sOR7, - SR7, -SO2NR7R8, -NR7SO2R8, -NR7CO2R8, -CONR7R8, or -CO2R7; R2 and R3, or R3 and R4, or R4 and R5 can together form an alkyl nucleus containing 5 to 7 elements, an aryl nucleus with six elements, a heteroalkyl nucleus containing from 5 to 7 elements as well as 1 or 2 heteroatoms of N, O or S; R6 represents cyano, trifluoromethyl or -OR9; R7, R8 and R9 each independently represent hydrogen, C1-C6 alkyl, - (CH2) mR10, C1-C3 alkylaryl or aryl; R7 and R8 can together form a C4-C7 alkyl ring; R10 represents cyano, trifluoromethyl, or C1-C4 alkoxy; R11 represents hydrogen, -OR12 or -NHCOR12; R12 represents C1-C6 alkyl, aryl or C1-C3 alkyl-aryl; m is 1, 2 or 3; s is 0, 1, 2 or 3; and the aryl groups and the aryl fractions mentioned above of the alkylaryl groups are independently chosen between phenyl and substituted phenyl, said substituted phenyl being able to be substituted with one to three groups chosen from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro and C1 to C4 alkoxy, and their pharmaceutically acceptable salts. These compounds are useful as psychotherapeutic substances, are potent serotonin (5-HT) antagonists and can be used in the treatment of depression, anxiety, eating disorders, obesity, drug dependence , headache, migraine, pain, and chronic paroxysmal hemicrania and headache associated with vascular disorders as well as others |