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54 条记录 (耗时 0.03 秒)

    7-Pyrazolylbenzazepines Having Affinity For D3 Receptor
    31.
    发明申请
    7-Pyrazolylbenzazepines Having Affinity For D3 Receptor 失效
    具有D3受体亲和性的7-吡唑基苯并吖庚因

    公开(公告)号：US20080312213A1

    公开(公告)日：2008-12-18

    申请号：US11570623

    申请日：2005-06-17

    申请人： Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco

    发明人： Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco

    IPC分类号： A61K31/55 ,  C07D401/14

    CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D413/14

    摘要： Compounds of formula (I) or a salt thereof are disclosed: wherein R1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C1-4alkyl and haloC1-4alkyl; R2 is hydrogen or methyl; and R3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C1-4alkyl or haloC1-4alkyl. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.

    摘要翻译： 公开了式（I）化合物或其盐：其中R 1是被两个或三个独立地选自卤素，C 1-4烷基和卤代C 1-4烷基的取代基取代的吡唑基; R2是氢或甲基; 并且R 3是喹啉基，恶唑基或苯基，其各自任选被一个或两个卤素，C 1-4烷基或卤代C 1-4烷基取代。 还公开了用于药物中化合物的制备和用途的方法，例如用于治疗精神分裂症或药物依赖性。

    Compounds having activity at 5ht2c receptor and uses thereof
    32.
    发明申请
    Compounds having activity at 5ht2c receptor and uses thereof 审中-公开

    公开(公告)号：US20060205788A1

    公开(公告)日：2006-09-14

    申请号：US10548118

    申请日：2004-02-24

    申请人： Federica Damiani ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Giovanna Tedesco

    发明人： Federica Damiani ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Giovanna Tedesco

    IPC分类号： A61K31/454 ,  C07D403/02

    CPC分类号： C07D207/26 ,  C07D207/273 ,  C07D207/38

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ═ is a double bond and m is 1 when ═ is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, 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 —(CH2—CH2)—, —(CH═CH)—, —(CH2)3—, —C(CH3)2—, —(CH═CH—CH2)—, —(CH2-CH═CH)— or a group —(CHR5)— wherein R5 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R3 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, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio or COOR6, CONR7R8 or COR9 wherein R6, R7, R8 and R9 are independently hydrogen or C1-6alkyl; p is 0, 1 or 2 or 3; R4 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; Y is oxygen, sulfur, —CH2— or NR10 wherein R10 is hydrogen or C1-6alkyl; D is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is —NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and anxiety, are also disclosed.

    7-pyrazolylbenzazepines having affinity for D3 receptor
    34.
    发明授权
    7-pyrazolylbenzazepines having affinity for D3 receptor 失效
    对D3受体具有亲和性的7-吡唑基苯并吖庚因

    公开(公告)号：US08003638B2

    公开(公告)日：2011-08-23

    申请号：US11570623

    申请日：2005-06-17

    申请人： Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco

    发明人： Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco

    IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D413/14

    摘要： Compounds of formula (I) or a salt thereof are disclosed: wherein R1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C1-4alkyl and haloC1-4alkyl; R2 is hydrogen or methyl; and R3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C1-4alkyl or haloC1-4alkyl. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.

    摘要翻译： 公开了式（I）化合物或其盐：其中R 1是被两个或三个独立地选自卤素，C 1-4烷基和卤代C 1-4烷基的取代基取代的吡唑基; R2是氢或甲基; 并且R 3是喹啉基，恶唑基或苯基，其各自任选被一个或两个卤素，C 1-4烷基或卤代C 1-4烷基取代。 还公开了用于药物中化合物的制备和用途的方法，例如用于治疗精神分裂症或药物依赖性。

    Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors
    35.
    发明授权
    Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors 失效
    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：US07875643B2

    公开(公告)日：2011-01-25

    申请号：US11911229

    申请日：2006-04-13

    申请人： Dieter Hamprecht ,  Caterina Mazzoni ,  Fabrizio Micheli

    发明人： Dieter Hamprecht ,  Caterina Mazzoni ,  Fabrizio Micheli

    IPC分类号： A61K31/41 ,  C07D249/08

    CPC分类号： C07D403/12

    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 and 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 and SF5; or corresponds to a group R5; each R2 is independently hydrogen or C1-4alkyl; n is 2, 3, 4 or 5; 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 and SF5; R5 is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; 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, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.

    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，苯并噻唑基和吲唑基; 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烷酰基和SF 5; 或对应于R5组; 每个R 2独立地是氢或C 1-4烷基; n为2，3，4或5; 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烷酰基和SF 5; R5选自：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，吡啶基和2-吡咯烷基，并且该基团任选被一个或两个取代基取代 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; 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。 治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

    CRF receptor antagonists
    37.
    发明授权
    CRF receptor antagonists 失效
    CRF受体拮抗剂

    公开(公告)号：US07329667B2

    公开(公告)日：2008-02-12

    申请号：US10476441

    申请日：2002-04-30

    申请人： Romano Di Fabio ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Yves St. Denis

    发明人： Romano Di Fabio ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Yves St. Denis

    IPC分类号： A01N43/54 ,  C07D239/00

    CPC分类号： C07D471/06 ,  C07D487/06

    摘要： The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    摘要翻译： 本发明涉及式（I）的三环嘧啶化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放介导的病症 因子（CRF）。

    Indole derivatives
    40.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US5686461A

    公开(公告)日：1997-11-11

    申请号：US507384

    申请日：1995-09-18

    申请人： Alfredo Cugola ,  Giovanni Gaviraghi ,  Fabrizio Micheli

    发明人： Alfredo Cugola ,  Giovanni Gaviraghi ,  Fabrizio Micheli

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/435 ,  A61P25/00 ,  A61P43/00 ,  C07D209/42 ,  C07D453/02 ,  A61K31/44

    CPC分类号： C07D209/42 ,  C07D453/02

    摘要： The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2; A represents an ethynyl group or an optionally substituted ethenyl group; X represents a bond or a C.sub.1-4 alkylene chain; R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.

    摘要翻译： PCT No.PCT / EP94 / 00614 Sec。 371 1995年9月18日第 102（e）1995年9月18日PCT PCT 1994年3月3日PCT公布。 公开号WO94 / 20465 日期：1994年9月15日本发明涉及式（I）化合物。 其中R 1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 3或COR 3中的基团，其中R 3表示 羟基，甲氧基或氨基; m为零或整数1或2; A表示乙炔基或任选取代的乙烯基; X表示键或C1-4亚烷基链; R 2表示桥连环烷基或桥连杂环基; 它们是兴奋性氨基酸的拮抗剂，其制备方法及其在医学中的应用。