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18 条记录 (耗时 0.026 秒)

    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    8.
    发明授权
    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
    环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药

    公开(公告)号：US06376494B1

    公开(公告)日：2002-04-23

    申请号：US09723478

    申请日：2000-11-28

    申请人： Wayne E. Childers ,  Michael G. Kelly ,  Yvette L. Palmer ,  Edward J. Podlesny

    发明人： Wayne E. Childers ,  Michael G. Kelly ,  Yvette L. Palmer ,  Edward J. Podlesny

    IPC分类号： A61K31496

    CPC分类号： C07D239/42 ,  C07D209/08 ,  C07D211/22 ,  C07D213/74 ,  C07D217/22 ,  C07D277/82 ,  C07D295/125 ,  C07D295/13 ,  C07D319/20

    摘要： 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.

    摘要翻译： 本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物，其可用于治疗具有下列基团的焦虑，抑郁，认知缺陷和前列腺癌：X是选自以下的部分：n是 从整数1到5中选择; R1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; R2是H或烷基; R3是H，COR5，COOR5和CONR5R6; 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; R5和R6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环，任选地含有选自O，S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时，环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。

    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    10.
    发明授权
    Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
    环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药

    公开(公告)号：US06518272B2

    公开(公告)日：2003-02-11

    申请号：US10107866

    申请日：2002-03-27

    申请人： Wayne E. Childers ,  Michael G. Kelly ,  Yvette L. Palmer ,  Edward J. Podlesny

    发明人： Wayne E. Childers ,  Michael G. Kelly ,  Yvette L. Palmer ,  Edward J. Podlesny

    IPC分类号： A61K3150

    CPC分类号： C07D239/42 ,  C07D209/08 ,  C07D211/22 ,  C07D213/74 ,  C07D217/22 ,  C07D277/82 ,  C07D295/125 ,  C07D295/13 ,  C07D319/20

    摘要： 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.

    摘要翻译： 本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物，其可用于治疗具有下列基团的焦虑，抑郁，认知缺陷和前列腺癌：X是选自以下的部分：n是 从整数1到5中选择; 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; R2是H或烷基; R3是H，COR5，COOR5和CONR5R6; 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; R5和R6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环，任选地含有选自O，S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时，环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。