| 摘要 |
PURPOSE: 2,4-Diaminopyridine derivatives; N-oxide forms, pharmaceutically acceptable acid additive salts and optical isomers thereof; and a preparation method thereof are provided, which exhibit more selective affinity to dopamine D4 receptor than to other receptors. CONSTITUTION: The derivatives are represented by the formula 1, wherein: Alk is an alkanediyl group of C1-C6 or an alkenediyl group of C3-C6; R1 is hydrogen or an alkyl group of C1-C4; R2 and R3 are independently hydrogen, an alkyl group of C1-C6 or a cycloalkyl group of C3-C7; or R2 and R3 also form a pyrrolidine, piperidine or perhydro azepine ring with the nitrogen atom to which they are attached; R4 is a hydrogen or halogen atom; Q is an aryl, aryloxy, di(aryl)methyl or heteroaryl group; the aryl group is an optionally substituted naphthyl or phenyl group; and the heteroaryl group is an optionally substituted quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl group. The derivatives of the formula 1 containing a radioactive isotope are used for marking dopamine D4 receptor sites and imaging an organ.
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