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69 条记录 (耗时 0.046 秒)

    Indole derivatives as NMDA antagonists
    41.
    发明授权
    Indole derivatives as NMDA antagonists 失效
    吲哚衍生物作为NMDA拮抗剂

    公开(公告)号：US5962496A

    公开(公告)日：1999-10-05

    申请号：US86522

    申请日：1998-05-29

    申请人： Alfredo Cugola ,  Romano Di Fabio ,  Giorgio Pentassuglia

    发明人： Alfredo Cugola ,  Romano Di Fabio ,  Giorgio Pentassuglia

    IPC分类号： A61K31/395 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/475 ,  A61K31/50 ,  A61P25/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/06 ,  C07D413/14 ,  C07D231/04

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/06 ,  Y02P20/55

    摘要： This invention relates to compounds of formula ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group=O;R.sub.3 represents hydrogen, alkyl or a nitrogen protecting group;n is zero or an integer from 1 to 2;p is zero or an integer from 1 to 3;q is zero or an integer from 1 to 3 with the proviso that the sum of p+q is 1, 2 or 3, which are antagonists of excitatory amino acids, to processes for the preparation and to other use in medicine.

    摘要翻译： 本发明涉及式或其盐或其代谢不稳定酯的化合物，其中R表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲基，三氟甲氧基，硝基，氰基，SO 2 R 2或COR 2的基团，其中R 2 表示羟基，甲氧基，氨基，烷基氨基或二烷基氨基; m为零或整数1或2; R 1表示环烷基，桥连环烷基，杂芳基，桥连杂环或任选取代的苯基或稠合双环碳酰基; A表示C 1-4亚烷基链或链（CH 2）p Y（CH 2）q，其中Y是O，S（O）n或NR 3，哪些链可以被选自任选被羟基取代的C 1-6烷基中的一个或两个基团取代 ，氨基，烷基氨基或二烷基氨基，或哪些链可以被基团= O取代; R3表示氢，烷基或氮保护基; n为0或1至2的整数; p为0或1至3的整数; q为0或1至3的整数，条件是p + q的和为1,2或3，它们是兴奋性氨基酸的拮抗剂，用于制备和在医药中的其它用途。

    Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors
    43.
    发明授权
    Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors 有权
    可用作多巴胺D3受体调节剂的氮杂双环（3.1.0。）己烷衍生物

    公开(公告)号：US07855298B2

    公开(公告)日：2010-12-21

    申请号：US10598200

    申请日：2005-02-21

    申请人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： C07D215/38

    CPC分类号： C07D495/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: 1. wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N -pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2 -pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; or a salt thereof which are useful as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

    摘要翻译： 本发明涉及新的式（I）化合物或其药学上可接受的盐：1.其中G选自：苯基，吡啶基，苯并噻唑基，吲唑基; p为0〜5的整数。 R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代 选自：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; R5是选自以下的部分：异恶唑基，-CH 2 -N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷基，任选地被一个或多个 选自以下的两个取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; 当R1为氯且p为1时，该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时，p为1; 或其盐，其可用作多巴胺D3受体的调节剂，例如， 治疗药物依赖或作为抗精神病药。

    Triazole derivatives as modulators of dopamine D3 receptors
    45.
    发明授权
    Triazole derivatives as modulators of dopamine D3 receptors 有权
    三唑衍生物作为多巴胺D3受体的调节剂

    公开(公告)号：US07799815B2

    公开(公告)日：2010-09-21

    申请号：US12064128

    申请日：2006-08-18

    申请人： Giorgio Bonanomi ,  Romano Di Fabio ,  Elettra Fazzolari ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Silvia Terreni

    发明人： Giorgio Bonanomi ,  Romano Di Fabio ,  Elettra Fazzolari ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Silvia Terreni

    IPC分类号： A01N43/64 ,  A61K31/41 ,  C07D249/08 ,  C07D249/00 ,  C07D249/12

    CPC分类号： C07D403/14 ,  C07D413/14

    摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.

    摘要翻译： 本发明涉及新的式（I）化合物或其盐：其中：G是5-或6-元杂芳族基团，或是含有一个或两个独立选择的杂原子的9或10元双环杂芳族基团 氮和氧，其中G不是吡啶基，吲唑基或苯并噻唑基; p为0〜4的整数。 R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基或SF 5; 或对应于R5组; R2是氢或C1-4烷基; n为2或3; X是S或-CH 2 - ; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代 选自：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; R5是异恶唑基，-CH2-N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基或2-吡咯烷基，其中每个基团任选被一个或两个选自以下的取代基取代：卤素，氰基，C1 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。 治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。

    Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors
    46.
    发明申请
    Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors 有权
    可用作多巴胺D3受体调节剂的氮杂双环（3.1.0）己烷衍生物

    公开(公告)号：US20100160336A1

    公开(公告)日：2010-06-24

    申请号：US12639282

    申请日：2009-12-16

    申请人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： A61K31/50 ,  C07D403/14

    CPC分类号： C07D495/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.

    摘要翻译： 本发明涉及新的式（I）化合物或其药学上可接受的盐：其中G选自：苯基，吡啶基，苯并噻唑基，吲唑基; p为0〜5的整数。 R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代 选自：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; R5是选自以下的部分：异恶唑基，-CH 2 -N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基，任选地被一个或多个 选自以下的两个取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; 当R1为氯且p为1时，该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时，p为1; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。 治疗药物依赖或作为抗精神病药。

    Tetrahydroquinoline derivatives as glycine antagonists
    49.
    发明授权
    Tetrahydroquinoline derivatives as glycine antagonists 失效
    四氢喹啉衍生物作为甘氨酸拮抗剂

    公开(公告)号：US06362199B1

    公开(公告)日：2002-03-26

    申请号：US09719188

    申请日：2001-02-15

    申请人： Romano Di Fabio

    发明人： Romano Di Fabio

    IPC分类号： A61K31495

    CPC分类号： C07D401/04 ,  C07D401/14 ,  Y02P20/55

    摘要： The present invention provides compounds of formula (I) or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the same and to their use in medicine.

    摘要翻译： 本发明提供式（I）化合物或其盐或无毒的代谢不稳定酯，其制备方法，含有该化合物的药物组合物及其在医药中的用途。