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711 条记录 (耗时 0.05 秒)

    IMIDAZOL-2-ONE COMPOUNDS USEFUL IN THE TREATMENT OF VARIOUS DISORDERS
    3.
    发明授权
    IMIDAZOL-2-ONE COMPOUNDS USEFUL IN THE TREATMENT OF VARIOUS DISORDERS 有权
    参与各种疾病的治疗咪唑-2-酮化合物适合

    公开(公告)号：EP1753739B1

    公开(公告)日：2010-04-28

    申请号：EP05750479.7

    申请日：2005-06-07

    申请人： GLAXO GROUP LIMITED

    发明人： ALVARO, Giuseppe ,  GHIRLANDA, Damiano

    IPC分类号： C07D401/04 ,  A61K31/4166

    CPC分类号： C07D401/04

    摘要： A compound of formula (I) wherein: R represents a group selected from: i) ii) iii) or iv) in which R6 is halogen, cyano, C1-4 alkyl or trifluoromethyl and p is 2 or 3 or R6 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or trifluoromethyl and p is 0 or 1; R1 represents hydrogen, halogen, cyano, C2-4 alkenyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 represents hydrogen or (CH2)qR7; R3 and R4 each independently are hydrogen or C1-4 alkyl; R5 represents : phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen, S(O)rC1-4 alkyl or a phenyl substituted by a 5 or 6 membered heteroaryl group optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC1-4 alkyl; naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC1-4 alkyl; a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC1-4 alkyl or R5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC1-4alkyl; R7 is hydrogen, C3-7 cycloalkyl, C1-4 alkoxy, amine, C1-4 alkylamine, (C1-4 alkyl)2amine, OC(O)NR8R9 or C(O)NR8R9; R8 and R9 each independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; A-B is a bivalent radical of formula (v) -CH=C(R11)- (vi) -C (R10)=CH- or (vii) -C(R12)(R10)-C(R11)(R13)- wherein R10, R11, R12 and R13 each independently are hydrogen or C1-4 alkyl; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof, process for their preparation and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.

    COMPOUNDS POSSESSING AFFINITY AT 5HT1-TYPE RECEPTORS AND USE THEREOF IN THERAPY OF CNS DISORDERS
    10.
    发明授权
    COMPOUNDS POSSESSING AFFINITY AT 5HT1-TYPE RECEPTORS AND USE THEREOF IN THERAPY OF CNS DISORDERS 有权
    用亲和链接到受体5HT-1类和它们在CNS障碍的治疗

    公开(公告)号：EP1480972B1

    公开(公告)日：2007-04-11

    申请号：EP03727261.4

    申请日：2003-02-17

    申请人： GLAXO GROUP LIMITED

    发明人： SMITH, Paul, W., GlaxoSmithKline ,  THEWLIS, Kevin, Michael, GlaxoSmithKline ,  VONG, Antonio, Kuok, Keong, GlaxoSmithKline ,  WARD, Simon, E., GlaxoSmithKline

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12 ,  C07D215/20 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (I) wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R1 is halogen, hydroxy, cyano, C1-6alkyl, haloC1-6alkyl or C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 and R3, together with the nitrogen atom to which they are attached, form a nitro group or an optionally substituted 3 to 7 membered heterocyclic group, or R2 and R3 are independently hydrogen, aroyl, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl, arylC1-6alkyl or a group CO(CH2)bNR4R5 wherein b is 1, 2, 3 or 4 and R4 and R5 are independently hydrogen or C1-6alkyl, or R4 and R5, together with the nitrogen atom to they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.