5-PHENYL-1,3,4-OXADIAZOL-2(3H)-ONE DERIVATIVES AND THEIR USE AS 5-HT4 LIGANDS

摘要

The invention concerns compounds of general formula (I) in which R1 represents H, an alkyl or a cycloalkylmethyl, X1 represents H or an alkoxy, or OR1 and X1 together represent a -OCH2O-, -O(CH2)2-, -O(CH2)3-, O(CH2)2O- or -O(CH2)3O- group, X2 represents H, an amino group or a -NHCO2R group in which R represents an alkyl or a phenylalkyl, X3 represents H or a halogen, n represents number 0, 1, 2, or 3, and Het represents either a pyrrolidin-1-yl group, or a piperidin-1-yl group optionally substituted, or a 1H-hexahydroazepin-1-yl group, or an 8-azabicyclo{3.2.1}oct-8-yl group, or a 4-(phenylmethyl)piperazin-1-yl group, or a 4-methyl-hexahydro-1,4-diazepin-1-yl group, or a 1,2,3,4-tetrahydrisoquinolin-2-yl group, or a 1-azabicyclo{2.2.2}oct-3-yl group. The invention is applicable in therapy. Said compounds are useful for preventing disorders in which 5-HT4 receptors are involved, whether in the central nervous, the gastrointestinal, the cardiovascular or the urinary system.