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    • 69. 发明授权
    • Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    • 环烷基取代的芳基哌嗪,哌啶和四氢吡啶作为血清素能药
    • US07049330B2
    • 2006-05-23
    • US10340087
    • 2003-01-10
    • Wayne E. ChildersMichael G. KellyYvette L. PalmerEdward J. Podlesny
    • Wayne E. ChildersMichael G. KellyYvette L. PalmerEdward J. Podlesny
    • A61K31/445C07D211/26
    • C07D239/42C07D209/08C07D211/22C07D213/74C07D217/22C07D277/82C07D295/125C07D295/13C07D319/20
    • This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5–7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1–C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.
    • 本发明涉及具有下式的化合物,其具有作为5-HT 1A激动剂和拮抗剂的活性,其可用于治疗焦虑,抑郁,认知缺陷和前列腺癌,其中:X为 选自以下的基团:n选自整数1至5; R 1是任选取代的芳基或单或双环杂芳基,条件是杂芳基不是噻二唑; R 2是H或烷基; R 3是H,COR 5,COOR 5和CONR 5 R 6 O / >; R 4是H,烷基,烯基,炔基,芳基,单或双环杂芳基,芳烷基和单或双环杂芳烷基,其中芳基或杂芳基任选被取代; R 5和R 6是H,烷基,烯基,炔基,环烷基,环烯基,金刚烷基和去月桂外基或R 5和R 共同组合可以形成5-7元的氮杂环,任选地含有选自O,S或NR 4的另外的杂原子。 当R 5或R 6选自环烷基或环烯基时,环状基团可以任选地在1位被C 1〜 -C 3烷基; 或光学异构体; 或其药学上可接受的盐。