1-phenylpiperazine derivative as modulators of dopamine neurotransmission
    2.
    发明公开
    1-phenylpiperazine derivative as modulators of dopamine neurotransmission 有权
    1-Phenylpiperazin-Derivaten als Modulatoren der Dopamin-Neurotransmission

    公开(公告)号:EP1428822A2

    公开(公告)日:2004-06-16

    申请号:EP03027033.4

    申请日:2000-12-22

    IPC分类号: C07D295/096 C07D295/08

    摘要: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula 1:
    wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R 1 is OSO 2 CF 3 , OSO 2 CH 3 , SOR 3 , SO 2 R 3 , COR 3 , NO 2 , or CONHR 3 and when X is CH or C R 1 may also be CF 3 , CN, F, Cl, Br, or I; R 2 is a C 1 -C 4 alkyl, an allyl, CH 2 SCH 3 , CH 2 CH 2 OCH 3 , CH 2 CH 2 CH 2 F, CH 2 CF 3 , 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or -(CH 2 )-R 4 ; R 3 is a C 1 -C 3 alkyl, CF 3 , or N(R 2 ) 2 ; R 4 is a C 3 -C 6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.
       Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

    摘要翻译: 新的3-取代的4-(苯基-N-烷基) - 哌嗪和式1的4-(苯基-N-烷基) - 哌啶化合物:其中XN,CH或C,但当化合物包含 虚线双键; R 1是OSO 2 CF 3,OSO 2 CH 3,SOR 3,SO 2 R 3,COR 3,NO 2或CONHR 3,当X是CH或CR 1也可以是CF 3,CN,F,Cl, Br或I; R 2是C 1 -C 4烷基,烯丙基,CH 2 SCH 3,CH 2 CH 2 OCH 3,CH 2 CH 2 CH 2 F,CH 2 CF 3,3,3,3-三氟丙基,4,4 ,4-三氟丁基或 - (CH 2)-R 4; R 3是C 1 -C 3烷基,CF 3或N(R 2)2; R 4是C 3 -C 6环烷基,2-四氢呋喃或3-四氢呋喃,以及其药学上可接受的盐。 公开了包含上述化合物的药物组合物和其中上述化合物用于治疗中枢神经系统疾病的方法。

    4-Phenylpiperidine derivatives as modulators of dopamine neurotransmission
    3.
    发明公开
    4-Phenylpiperidine derivatives as modulators of dopamine neurotransmission 有权
    4-苯基哌啶衍生物多巴胺神经递质

    公开(公告)号:EP1419773A2

    公开(公告)日:2004-05-19

    申请号:EP03027034.2

    申请日:2000-12-22

    摘要: New substituted 4-(phenyl-N-alkyl)-piperidine compounds of Formula 1:
    wherein X is CH; R 1 is CF 3 , OSO 2 CF 3 , OSO 2 CH 3 , SOR 7 , SO 2 R 7 , COR 7 , CN, OR 3 , NO 2 , CONHR 3 , 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R 2 is F, Cl, Br, I, CN, CF 3 , CH 3 , OCH 3 , OH, and NH 2 ; R 3 and R 4 are H; R 5 is a C 1 -C 4 alkyl, an allyl, CH 2 SCH 3 , CH 2 CH 2 OCH 3 , CH 2 CH 2 CH 2 F, CH 2 CF 3 , 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or -(CH 2 )-R 6 ; R 6 is a C 3 -C 6 cycloalkyl, 2-tetrahydrofurane, or 3-tetrahydrofurane; R 7 is a C 1 -C 3 alkyl, CF 3 , or N(R 4 ) 2 , and pharmaceutically acceptable salts thereof are disclosed.
    Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

    摘要翻译: 新的取代的4-(苯基-N-烷基) - 哌啶化合物的式1:其中X是CH; R1是CF3,OSO2CF3,OSO2CH3,SOR7,SO2R7,COR7,CN,OR3,NO2,CONHR3,3噻吩,2-噻吩,3-呋喃,2-呋喃,F,Cl,Br或I; R2是F,Cl,Br,I,CN,CF3,CH3,OCH3,OH和NH2; R3和R4是H; R5是C1-C4烷基,烯丙基,CH2SCH3,CH2CH2OCH3,CH2CH2CH2F,CH2CF3,3,3,3-三氟丙基,4,4,4-三氟丁基或 - (CH2)-R6; R6是C3-C6环烷基,2-四氢呋喃或3-四氢呋喃; R 7是C 1 -C 3烷基,CF 3或N(R 4)2,并且其药学上可接受的盐被公开。 还公开了包含上述化合物的药物组合物和其中上述化合物用于治疗中枢神经系统疾病的方法。