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    Compounds having activity at 5ht2c receptor and uses thereof
    21.
    发明申请
    Compounds having activity at 5ht2c receptor and uses thereof 审中-公开

    公开(公告)号：US20070191457A1

    公开(公告)日：2007-08-16

    申请号：US10551904

    申请日：2004-04-05

    申请人： Giorgio Bonanomi ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Silvia Terreni

    发明人： Giorgio Bonanomi ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Silvia Terreni

    IPC分类号： A61K31/454 ,  C07D401/02

    CPC分类号： C07D209/46

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, —COOR3, —COR4, wherein R3 and R4 are independently hydrogen or C1-6alkyl, or —COR5, wherein R5 is amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; p is 0, 1, 2 or 3; Q is a 6-membered aromatic group or a 6-membered heteroaromatic group; A is —(CH2—CH2)—, —(CH═CH)—, or a group —(CHR7)— wherein R7 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R2 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is oxygen, sulfur, —CH2— or NR8 wherein R8 is hydrogen or C1-6alkyl; Y is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is an optionally substituted N-linked heterocyclic group or a C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, or Z is —NR9R10 where R9 and R10 are independently hydrogen or C1-6alkyl. Methods of preparation and uses thereof in therapy, such as for depression or anxiety, are also disclosed.

    3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
    23.
    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）。

    Triazolyl Derivatives of Azabicyclo [3.1.0] Hexane as Dopamine D3 Receptor Modulators
    24.
    发明申请
    Triazolyl Derivatives of Azabicyclo [3.1.0] Hexane as Dopamine D3 Receptor Modulators 失效

    公开(公告)号：US20080242715A1

    公开(公告)日：2008-10-02

    申请号：US12064118

    申请日：2006-08-18

    申请人： Anna Marie Capelli ,  Elettra Fazzolari ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Anna Marie Capelli ,  Elettra Fazzolari ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： C07D413/14 ,  A61K31/422 ,  A61P25/18

    CPC分类号： C07D413/14

    摘要： The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: 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; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; 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; with the proviso that when m5=m6=1, R7 is not chlorine; 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.

    AZABICYCLIC COMPOUNDS AS SEROTONIN, DOPAMINE AND NOREPINEPHRINE RE-UPTAKE INHIBITORS
    26.
    发明申请
    AZABICYCLIC COMPOUNDS AS SEROTONIN, DOPAMINE AND NOREPINEPHRINE RE-UPTAKE INHIBITORS 审中-公开
    作为丝氨酸，多巴胺和诺贝那韦再摄入抑制剂的化学式

    公开(公告)号：US20100029740A1

    公开(公告)日：2010-02-04

    申请号：US12519438

    申请日：2007-12-12

    申请人： Giorgio Bonanomi ,  Fabrizio Micheli ,  Silvia Terreni

    发明人： Giorgio Bonanomi ,  Fabrizio Micheli ,  Silvia Terreni

    IPC分类号： A61K31/403 ,  C07D209/52 ,  A61P25/00

    CPC分类号： C07D209/52

    摘要： Novel compounds of formula (I)′ and pharmaceutically acceptable salts, solvates and prodrugs thereof: wherein A is: K is a mono or bicyclic aryl group; R1 is selected from halogen, C1-4alkyl and C1-4alkoxy (R1 may assume different meanings on the basis of p value); p is an integer from 0 to 5; R2 is a group P: R3 is hydrogen, C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, haloC1-2alkyl or an optionally substituted phenyl group; X is oxygen, —NR8— or sulphur; n is 0 or 1; R7 is hydrogen or methyl; R8 is hydrogen or C1-4alkyl; R4 is hydrogen or methyl; R5 is hydrogen or C1-4alkyl; and R6 is hydrogen or C1-4alkyl; 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： 新的式（I）化合物及其药学上可接受的盐，溶剂合物和前药：其中A是：K是单或双环芳基; R1选自卤素，C1-4烷基和C1-4烷氧基（R1可以基于p值取代不同的含义）; p是0至5的整数; R2是基团P：R3是氢，C1-4烷基，C3-6环烷基，C3-6环烷基C1-3烷基，卤代C1-2烷基或任选取代的苯基; X是氧，-NR8-或硫; n为0或1; R7是氢或甲基; R8是氢或C1-4烷基; R4是氢或甲基; R5是氢或C1-4烷基; R6为氢或C1-4烷基; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，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应用。

    AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE
    29.
    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.

    AZABICYCLO [3.1.0] HEXYLPHENYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
    30.
    发明申请
    AZABICYCLO [3.1.0] HEXYLPHENYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
    亚氨基胆碱[3.1.0]作为DOPAMINE D3受体的调节剂的HEXYLPHENYL衍生物

    公开(公告)号：US20090030062A1

    公开(公告)日：2009-01-29

    申请号：US12064121

    申请日：2006-08-18

    申请人： Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Adolfo Prandi ,  Silvia Terreni

    发明人： Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Adolfo Prandi ,  Silvia Terreni

    IPC分类号： A61K31/403 ,  C07D209/52

    CPC分类号： C07D209/52

    摘要： The present invention relates to novel compounds of formula (IA) or a salt thereof: wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: —SO2NR5—, —SO2CR2R3—, —CR2R3SO2— and —NR5SO2—; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; 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： 本发明涉及式（IA）的新化合物或其盐：其中：A相对于环丙基在间位或对位与苯基连接，并且选自： - SO 2 NR 5 - ， - SO 2 CR 2 R 3 - ， - CR 2 R 3 SO 2 - 和-NR 5 SO 2 - ; R1是氢，C1-6烷基，卤代C 1-6烷基或C 2-6亚烷基; R2和R3独立地是氢或C1-6烷基; R 4是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R5是氢，C1-6烷基或任选被R4取代的苯基; 并且R 6是氢，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; 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。 治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。