| 摘要 |
<p>A compound of formula (I) or pharmaceutically acceptable slats of formula (I), where R1 is H, C¿1?-C3 alkyl, -(CH2)nCONH2 where n is 2 to 6, (CH2)n-1-(4,4-dimethylpiperidine-2,6-dione-yl), cyclopropylmethyl; R?2¿ is hydrogen, C¿1?-C8 alkyl, C3-C8 cycloalkyl or combined with R?1¿ to form a C¿3?-C8 cycloalkyl, C2-C8 alkenyl, C2-C8 alkynyl, (CH2)n-X-Ar where X is O, S, or NH, 3,3,3-trifluoropropyl, -(CH2)m-R?9¿ where m is 2 or 3 and R9 is phenyl, 2-thiophenyl or 3-thiophenyl; R3 is C1-C3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH2OR2, C(O)C(O)Y where Y is OR?1 or NR1R2¿, -(CH¿2?)q-NR?1R2¿ where q is 0 to 5, C=NOR2,2(4,5-dihydro)oxazolyl, or COR10 where R10 is H, R?1, NR1R2¿ or CF¿3?; R?4 is C¿1-C3 alkyl, cyclopropylmethyl, CF3, 2,2,2-trifluoroethyl, CN, CONR1R2, =O, 2(4,5-dihydro)imidazolyl, 2(4,5-dihydro)oxazolyl, 2-oxazolyl, 3-oxadiazolyl, or 3,3,3-trifluoropropyl; R5 is hydrogen, R1, OCH3, C(O)CH3 or C(O)OR1; X is (a) a valence bond, (b) CH¿2?, (c) O, S or NR?5¿ where R5 is H, C¿1?-C8 alkyl, C3-C8 cycloalkyl, benzyl, COR?6¿ where R6 is a C¿1?-C3 alkyl, phenyl, or CONR?7R8¿ where R?7 and R8¿ are independently H or C¿1?-C3 alkyl; and Z is a hydrogen or halogen. The compounds of formula (I) are suitable for treating disorders of the central nervous system, particularly as 5-HT1A receptor agonists.</p> |
