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    • 12. 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。
    • 14. 发明授权
    • Diazole derivatives as serotonergic agents
    • 二唑衍生物作为血清素能药剂
    • US06239134B1
    • 2001-05-29
    • US09515049
    • 2000-02-25
    • Annmarie L. SabbRobert L. VogelMichael G. KellyYvette L. PalmerWayne E. Childers
    • Annmarie L. SabbRobert L. VogelMichael G. KellyYvette L. PalmerWayne E. Childers
    • A61K31496
    • C07D285/10C07D417/12
    • The present invention provides compounds of the general formula (1): wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, phenoxy, thiophenoxy, phenyl or substituted phenyl; A is C, CH, or N; R1 is aryl, heteroaryl, or cycloalkyl groups, optionally substituted by from 1 to 3 substituents selected from C1-C6 alkyl, C1-C6 alkoxy; CF3, Cl, Br, F, CN, or CO2CH3; R2is H or alkyl R3 is C1-C6 alkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heteroaryl, C3 to C8 cycloalkyl optionally substituted by C1-C6 alkyl, or a 3 to 8-membered heterocyclic ring containing one or more heteroatoms selected from O, S or N; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders using these compounds.
    • 本发明提供通式(1)的化合物:其中X,Y或Z的两个原子是氮,第三个原子是硫或氧; R是H,卤素,OH,SH,C 1 -C 6烷基, C 1 -C 6烷氧基,C 1 -C 6硫代烷基,苯氧基,硫代苯氧基,苯基或取代的苯基; A是C,CH或N; R 1是芳基,杂芳基或环烷基,任选地被1至3个选自C1- C6烷基,C1-C6烷氧基; CF 3,Cl,Br,F,CN或CO 2 CH 3; R 2为H或烷基R 3为C 1 -C 6烷基,任选取代的芳基,任选取代的5或6元杂芳基,任选被C 1 -C 6烷基取代的C 3至C 8环烷基, 含有一个或多个选自O,S或N的杂原子的3至8元杂环; 或其药学上可接受的盐,以及使用这些化合物治疗中枢神经系统疾病的药物组合物和方法。
    • 15. 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
    • US06376494B1
    • 2002-04-23
    • US09723478
    • 2000-11-28
    • Wayne E. ChildersMichael G. KellyYvette L. PalmerEdward J. Podlesny
    • Wayne E. ChildersMichael G. KellyYvette L. PalmerEdward J. Podlesny
    • A61K31496
    • 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。