| 摘要 |
Novel piperidinyl compounds of formula (I) in which X and Y are independently selected from hydrogen, halogen and C1-6 alkoxy, R1 is selected from five- and six-membered heteroaryl rings containing from 1-3 heteroatoms selected from nitrogen, oxygen, and sulfur, and benz derivatives thereof, which may bear 1-2 substituents selected from C1-6 alkyl, hydroxy, C1-6 alkoxy which may bear a trifluoromethyl group, C1-6 alkoxycarbonyl, C1-6 hydroxyalkyl, benzyloxy, halo, C1-3 alkylaminocarbonyl, C1-3 alkyl, aminocarbonyl having the formula: CONR<c>R<d> wherein R<c> and R<d> are independently selected from hydrogen, 2-pyrrolidinyl, and C1-6 alkyl or wherein R<c> and R<d> together with the nitrogen atom to which each is attached form a 5- or 6-membered heterocyclic ring in which said nitrogen is the only heteroatom, R<e>S(O)n, R<f>NH, and R<g>S wherein R<e> and R<f> are independently selected from hydrogen and C1-6 alkyl and n is 0, 1 or 2 and R<g> is selected from C1-3 alkylcarbonylaminophenyl and di(C1-3)alkylamino(C1-6)alkyl wherein at least one of the substituents on the five- and/or six-membered heteroaryl ring is a chiral sulfoxide of the formula C1-4alkylSO, and their pharmaceutically acceptable salts, are useful as dopamine antagonists and are particularly useful as antipsychotic agents in humans. The compounds may also be useful in other neurological and psychiatric disorders including schizophrenia. Processes for preparing the piperidinyl compounds are also described as well as their use in medecine. |
