CHEMICAL COMPOUNDS
    44.
    发明申请
    CHEMICAL COMPOUNDS 失效
    化学化合物

    公开(公告)号:US20080114049A1

    公开(公告)日:2008-05-15

    申请号:US11851459

    申请日:2007-09-07

    申请人: Romano Di Fabio

    发明人: Romano Di Fabio

    IPC分类号: A61K31/403 C07D209/02

    CPC分类号: C07D221/04

    摘要: The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; 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(1S,6R)-6-(3,4-二氯苯基)-1 - [(甲氧基)甲基] -3-氮杂双环[4.1.0]庚烷,其药学上可接受的盐,前药或溶剂合物; 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。

    CRF receptor antagonists
    45.
    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

    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 as NMDA antagonists
    48.
    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

    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。