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    Triazole derivatives as modulators of dopamine D3 receptors
    11.
    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。

    TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
    12.
    发明申请
    TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 有权
    作为DOPAMINE D3受体的调节剂的三唑衍生物

    公开(公告)号：US20090221593A1

    公开(公告)日：2009-09-03

    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： A61K31/422 ,  C07D413/14 ,  A61K31/4709 ,  A61K31/423 ,  A61K31/498 ,  A61K31/506

    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。

    SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS
    17.
    发明申请
    SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS 失效

    公开(公告)号：US20100063078A1

    公开(公告)日：2010-03-11

    申请号：US12297253

    申请日：2007-04-24

    申请人： Barbara Bertani ,  Romano Di Fabio ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Luca Tarsi ,  Silvia Terreni

    发明人： Barbara Bertani ,  Romano Di Fabio ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Luca Tarsi ,  Silvia Terreni

    IPC分类号： A61K31/506 ,  C07D413/14 ,  C07D417/14 ,  C07D409/14 ,  A61K31/427 ,  A61K31/422 ,  A61P25/00

    CPC分类号： C07D403/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/10

    摘要： The present invention relates to novel compounds of formula (I) or salts thereof: wherein A is a substituent selected in the group consisting of P, P1, P2 and P3 wherein P is P1 is P2 is P3 is p is an integer ranging from 0 to 4; R4 is selected in the group consisting of halogen, hydroxy, cyano, C1-4 alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl, SF5 and a 5- or 6-membered monocyclic heteroaryl group; and when p is an integer ranging from 2 to 4, each R4 may be the same or different; R2 is hydrogen or C1-4alkyl; q is 3, 4 or 5; n is 0, 1 or 2; X is —CR1R3— or —O—; R1 is selected in the group consisting of hydrogen, C1-4 alkyl and fluorine; R3 is selected in the group consisting of hydrogen, C1-4alkyl and fluorine; R5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR′R″; or R5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R6 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR′R″; or R6 is a phenyl group, a 5-14 membered heterocyclic group and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R7 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4 alkoxy, C1-4 alkanoyl and NR′R″; or R7 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R8 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4 alkoxy, C1-4 alkanoyl and NR′R″; or R8 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R9 is selected in the group consisting of hydrogen, a phenyl group, a heterocyclyl group, a 5- or 6-membered monocyclic heteroaryl group, and a 8- to 11-membered heteroaryl bicyclic, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4 alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R10 is C1-4alkyl; R11 is hydrogen or C1-4alkyl; R′ is H, C1-4 alkyl or C1-4 alkanoyl; R″ is defined as R′; R′ and R″ taken together with the interconnecting nitrogen atom may form a 5-, 6-membered saturated or unsaturated heterocyclic ring; wherein R5, R6, R7 and R8 are not simultaneously other than hydrogen; wherein only one R2 group ma be different from hydrogen and wherein when n is 0, X is a group —CR1R3—; 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, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or to enhance cognition.

    3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
    19.
    发明申请
    3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION 审中-公开
    3-AZABICYCLO [4。 1. 0]用于治疗呕吐的HEPTANE衍生物

    公开(公告)号：US20090281135A1

    公开(公告)日：2009-11-12

    申请号：US12440821

    申请日：2007-09-07

    申请人： Romano Di Fabio ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Romano Di Fabio ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： A61K31/439 ,  C07D221/22 ,  A61P25/24

    CPC分类号： C07D221/04

    摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: wherein G is selected from the group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, and a 8- to 11-membered heteroaryl bicyclic group; wherein G may be substituted by (R2)p, which can be the same or different; R1 is hydrogen or C1-4 alkyl; R2 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to R8; R5 is hydrogen or C1-4 alkyl; R6 is hydrogen or C1-4 alkyl; R7 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to X, X1, X2 or X3; wherein X corresponds to: X1 corresponds to: X2 corresponds to: X3 corresponds to: R3 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R4 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R9 is C1-4alkyl; R10 is hydrogen, C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-3alkyl; R11 is haloC1-2alkyl; p is an integer from 0 to 5; and n is 1 or 2; and processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

    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，溶剂合物或前药：其中G选自：苯基，5-或6-元单环杂芳基，和8- 11元杂芳基双环基; 其中G可以被（R 2）p取代，其可以相同或不同; R1是氢或C1-4烷基; R 2是卤素，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R8; R5是氢或C1-4烷基; R6是氢或C1-4烷基; R 7选自：氢，氟和C 1-4烷基; 或对应于X，X1，X2或X3; 其中X对应于：X1对应于：X2对应于：X3对应于：R 3是氢或C 1-4烷基; 或对应于X或X1; R4是氢或C1-4烷基; 或对应于X或X1; R8是5-6元杂环基团，其可以被一个或两个选自以下的取代基取代：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; R9为C1-4烷基; R 10是氢，C 1-4烷基，C 3-6环烷基或C 3-6环烷基C 1-3烷基; R11是卤代C 1-2烷基; p是0至5的整数; n为1或2; 再生摄取抑制剂，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5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE）。

    AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE
    20.
    发明申请
    AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE 审中-公开

    公开(公告)号：US20100035914A1

    公开(公告)日：2010-02-11

    申请号：US12440852

    申请日：2007-09-07

    申请人： Barbara Bertani ,  Romano Di Fabio ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Barbara Bertani ,  Romano Di Fabio ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： A61K31/435 ,  C07D221/02 ,  A61P25/24

    CPC分类号： C07D221/04

    摘要： The present invention relates to novel compounds of formula (I)′, and pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R1 is hydrogen or C1-4 alkyl; R2 is a group A, K or W wherein A is K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R18, each of them being the same or different; and W is and wherein G is a 5,6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; wherein G may be substituted by (R15)p, which can be the same or different; p is an integer from 0 to 5; R3 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to a group X or X1; R4 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to a group X or X1; R5 is hydrogen or C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; or is a group X, X1, X2 or X3; wherein X is X1 is X2 is and X3 is R6 is hydrogen or C1-4 alkyl; or is a group X or X1; R9 is C1-4alkyl; R10 is selected from the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R11 is selected from the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R12 is selected from the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R13 is selected from the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R14 is selected from the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R15 is selected from the group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R16 is hydrogen, C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-3alkyl; R17 is hydrogen or C1-4alkyl; R18 is selected from the group consisting of: halogen, cyano, and C1-4alkyl; R19 is haloC1-2alkyl; and n is 1 or 2; with the proviso that: if R2 is A, R3, R4, R5, R6, R7, R10, R11, R13, and R14 are hydrogen, and R12 is fluorine, R1 is C1-4 alkyl; if R2 is A, R3, R4, R5, R6, R7, R10, R11, R13, and R14 are hydrogen, and R1 is methyl, R12 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R8; and processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.