2,4-DIAMINOPYRIMIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION, THEIR USE FOR THE PREPARATION OF DOPAMINE D4 ANTAGONIST PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN LABELING DOPAMINE D4 RECEPTOR

摘要

Antipsychotic compounds of the formula N-oxide forms, pharmaceutically acceptable acid addition salts or stereochemically isomeric forms thereof, wherein Alk is C1-6 alkanediyl or C3-6 alkenediyl; R1 is hydrogen or C1-4 alkyl; R2 and R3 each independently are hydrogen, C1-6 alkyl or C3-7 cycloalkyl; or R2 and R3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R4 is hydrogen; Q is aryl, aryloxy, di (aryl) methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted with one, two or three substituents selected from halo, hydroxy, C1-4 alkyl, C1-4 alkyloxy, C1-4 alkylcarbonyl, halo C1-4 alkyl, nitro, amino, cyano and phenyl; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4- benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted with one, two or three substituents selected from halo, hydroxy, C1-4 alkyl, C1-4 alkyloxy, C1-4 alkylcarbonyl, halo C1-6 alkyl and phenyl. 3795 ט' בשבט התשס" ג - January 12, 20