NEW MODULATORS OF DOPAMINE NEUROTRANSMISSION
    2.
    发明公开
    NEW MODULATORS OF DOPAMINE NEUROTRANSMISSION 审中-公开
    多巴胺神经传递的新调节剂

    公开(公告)号:EP1240143A1

    公开(公告)日:2002-09-18

    申请号:EP00989163.1

    申请日:2000-12-22

    摘要: New substituted 4-(phenyl N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bind at the dotted line; R1 is CF3, OSO2CF3, OSO2CH3, SOR7, SO2R7, COR7, CN, OR3, NO2, CONHR3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, and NH2; R3 and R4 are independently H or a C1-C4 alkyl; R5 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or -(CH2)-R6; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetrahydrofurane; R7 is a C1-C3 alkyl, CF3, or N(R4)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.

    NEW MODULATORS OF DOPAMINE NEUROTRANSMISSION
    3.
    发明公开
    NEW MODULATORS OF DOPAMINE NEUROTRANSMISSION 有权
    多巴胺神经递质的新调节剂

    公开(公告)号:EP1240141A1

    公开(公告)日:2002-09-18

    申请号:EP00989161.5

    申请日:2000-12-22

    摘要: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR5, SO2R5, COR5, CN, NO2, CONHR5, CF3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or -(CH2)-R6; R3 and R4 are independently selected from the group consisting of H and C1-C4 alkyls, however both R3 and R4 cannot be H at the same time; R5 is C1-C3 alkyls, CF3, or N(R2)2; R6 is a C3-C6 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 are disclosed.

    摘要翻译: 其中X是N,CH或C的新的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,然而X可以仅为C 该化合物在虚线处包含双键; R1是OSO2CF3,OSO2CH3,SOR5,SO2R5,COR5,CN,NO2,CONHR5,CF3,3-噻吩,2-噻吩,3-呋喃,2-呋喃,F,Cl,Br或I; R2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; R3和R4独立地选自H和C1-C4烷基,然而R3和R4不能同时为H; R5是C1-C3烷基,CF3或N(R2)2; R 6是C 3 -C 6环烷基,2-四氢呋喃或3-四氢呋喃及其药学上可接受的盐。 还公开了包含上述化合物和其中使用上述化合物的方法的药物组合物。

    1-phenylpiperazine derivative as modulators of dopamine neurotransmission
    9.
    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
    10.
    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。