| 摘要 |
Novel phenylpyridylpiperazine compounds, a preparation process thereof and pharmaceutical compositions containing the same compounds are provided to treat cognitive deficiencies associated with cerebral aging and neurodegenerative diseases, mood disorders, convulsive attacks, attention deficit hyperactivity syndrome, obesity, pain and narcoleptic states. The phenylpyridylpiperazine compounds represented by the formula(I), its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base are provided, wherein X is C(O) or SO2 group; R1 is aryl group or NR3R4 group; R2 is linear or branched (C1-C6) alkyl group, (C3-C8) cycloalkyl group or (C3-C8) cycloalkyl-(C1-C6) alkyl group, wherein alkyl is linear or branched; and R3 and R4 are identical or different, and each independently hydrogen atom, linear or branched (C1-C6) alkyl group, (C3-C8) cycloalkyl group or (C3-C8) cycloalkyl-(C1-C6) alkyl group, wherein alkyl is linear or branched. The phenylpyridylpiperazine compounds represented by the formula(I) is prepared by condensing compounds represented by the formula(II) in the presence of palladium(O) with compounds represented by the formula(III), wherein R and R' are identical or different, and each independently hydrogen atom or linear or branched (C1-C6) alkyl group or form together with linear or branched (C1-C6) alkylene ring; and Hal is halogen atom.
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