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    3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
    54.
    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）。

    Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists
    55.
    发明授权
    Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists 失效
    吡咯并[2,3-d]嘧啶衍生物作为促肾上腺皮质激素释放因子拮抗剂

    公开(公告)号：US07462622B2

    公开(公告)日：2008-12-09

    申请号：US10480958

    申请日：2002-06-11

    申请人： Romano Di Fabio ,  Chiara Marchionni ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Bendetta Perini ,  Yves St-Denis

    发明人： Romano Di Fabio ,  Chiara Marchionni ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Bendetta Perini ,  Yves St-Denis

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P25/24 ,  A61P25/22

    CPC分类号： C07D487/04 ,  A61K51/0459 ,  C07B2200/05 ,  C07D239/70 ,  C07D239/94 ,  C07D471/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle;  wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; 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： 本发明提供式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素，C 1 -C 6 烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自以下的基团取代：C 1 -C 6烷氧基和羟基; R7独立于R6，具有相同的含义; X是碳或氮; 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因子（CRF）介导的病症的用途。

    Indole derivatives
    57.
    发明授权
    Indole derivatives 有权
    吲哚衍生物

    公开(公告)号：US6100289A

    公开(公告)日：2000-08-08

    申请号：US374982

    申请日：1999-08-16

    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

    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 where 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 .dbd.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，SO2R2或COR2的基团，其中R2 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。