N-(3-PYRROLIDINYL)BENZAMIDE DERIVATIVE
    2.
    发明公开
    N-(3-PYRROLIDINYL)BENZAMIDE DERIVATIVE 失效
    N-(3-吡咯烷基)BENZAMID-衍生金融

    公开(公告)号:EP0757985A1

    公开(公告)日:1997-02-12

    申请号:EP95917462.4

    申请日:1995-04-26

    IPC分类号: C07D207/14 A61K31/40

    CPC分类号: C07D207/14

    摘要: N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D 3 and/or D 4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof.
    (wherein each symbol in the formula has the following meaning,

    R 1 : hydrogen, lower alkyl, aralkyl, or cycloalkyl or cycloalkyl-lower alkyl having 3 to 8 ring atoms,
    R 2 : bicyclic or tricyclic bridged hydrocarbon ring of 4 to 16 ring atoms which may have lower alkyl,
    R 3 : lower alkoxy, amino or mono- or di-lower alkylamino,
    R 4 : hydrogen, halogen, lower alkyl which may have hydroxyl, lower alkoxy, cyano, nitro, amino, mono- or di-lower alkylamino, acyl or a group represented by -S(O) m -R 5 ,
    R 5 : lower alkyl, amino or mono- or di-lower alkylamino,
    m: 0, 1 or 2,
    X: a bond or a group represented by -O-, -S(O) n -, -NH- or -CONH-, and
    n: 0, 1 or 2,
    with the proviso that, when R 1 is cycloalky, the cases wherein X is -CONH-, R 3 is lower alkoxy and R 4 is halogen are excluded.)

    摘要翻译: 具有对多巴胺D3和/或D4受体具有强效和选择性拮抗作用并且可用作精神药物,精神分裂症治疗剂等的由以下通式(I)表示的N-(3-吡咯烷基)苯甲酰胺衍生物,或 其药学上可接受的盐或其药物制剂。 (其中式中的每个符号具有以下含义:R 1:氢,低级烷基,芳烷基或具有3至8个环原子的环烷基或环烷基 - 低级烷基,R 2:双环或三环桥连 具有4至16个环原子的烃环,其可具有低级烷基,R 3:低级烷氧基,氨基或单 - 或二 - 低级烷基氨基,R 4:氢,卤素,可具有羟基的低级烷基,低级烷氧基 ,氰基,硝基,氨基,一或二低级烷基氨基,酰基或由-S(O)m R 5表示的基团,R 5:低级烷基,氨基或单 - 或二 - 低级烷基氨基,m :0,1或2,X:由-O - , - S(O)n-,-NH-或-CONH-表示的键或基团,n:0,1或2,条件是, 当R 1为环烷基时,其中X为-CONH-,R 3为低级烷氧基且R 4为卤素的情况除外)

    NOVEL BISOXADIAZOLIDINE DERIVATIVE
    3.
    发明授权
    NOVEL BISOXADIAZOLIDINE DERIVATIVE 失效
    新型双二唑二唑衍生物

    公开(公告)号:EP0696585B1

    公开(公告)日:1998-12-16

    申请号:EP94913821.8

    申请日:1994-04-26

    CPC分类号: C07D271/07 C07D413/14

    摘要: A bisoxadiazolidinedione derivative of general formula (I) useful as an insulin-sensitivity improver, a pharmaceutically acceptable salt thereof, and a medicinal composition thereof, wherein (a) and (b) may be the same or different from each other and each represent an optionally substituted phenylene group, and L represents: (1) an oxygen atom, (2) a group of formula (II) (R1 being a hydrogen atom or a lower alkyl group), (3) a group of the formula: -S(O)¿n?- (n being 0, 1 or 2), (4) a group of the formula: -CO-, (5) a group of formula (III) or (IV) (R?2¿ being a hydrogen atom or a lower alkyl group), or (6) an alkylene or alkenylene group which may be substituted and interrupted by an oxygen atom and/or a sulfur atom, and the like.

    摘要翻译: 用作胰岛素敏感性改进剂的通式(I)的双恶二唑烷二酮衍生物,其药学上可接受的盐及其药用组合物,其中(a)和(b)可以彼此相同或不同,并且各自表示 (1)氧原子,(2)式(II)的基团(R 1为氢原子或低级烷基),(3)下式的基团:-S (O)n - (n为0,1或2),(4)式-CO-的基团,(5)式(III)或(IV)的基团 氢原子或低级烷基),或(6)可以被氧原子和/或硫原子取代和插入的亚烷基或亚烯基等。

    NOVEL BISOXADIAZOLIDINE DERIVATIVE
    5.
    发明公开
    NOVEL BISOXADIAZOLIDINE DERIVATIVE 失效
    新型双二唑二唑衍生物

    公开(公告)号:EP0696585A1

    公开(公告)日:1996-02-14

    申请号:EP94913821.8

    申请日:1994-04-26

    CPC分类号: C07D271/07 C07D413/14

    摘要: A bisoxadiazolidinedione derivative of general formula (I) useful as an insulin-sensitivity improver, a pharmaceutically acceptable salt thereof, and a medicinal composition thereof, wherein (a) and (b) may be the same or different from each other and each represent an optionally substituted phenylene group, and L represents: (1) an oxygen atom, (2) a group of formula (II) (R¹ being a hydrogen atom or a lower alkyl group), (3) a group of the formula: -S(O) n - (n being 0, 1 or 2), (4) a group of the formula: -CO-, (5) a group of formula (III) or (IV) (R² being a hydrogen atom or a lower alkyl group), or (6) an alkylene or alkenylene group which may be substituted and interrupted by an oxygen atom and/or a sulfur atom, and the like.

    摘要翻译: 用作胰岛素敏感性改进剂的通式(I)的双恶二唑烷二酮衍生物,其药学上可接受的盐及其药用组合物,其中(a)和(b)可以彼此相同或不同,并且各自表示 (1)氧原子,(2)式(II)的基团(R 1为氢原子或低级烷基),(3)下式的基团:-S (O)n-(n为0,1或2),(4)式-CO-的基团,(5)式(III)或(IV)的基团(R 2为氢原子或 低级烷基)或(6)可被氧原子和/或硫原子取代和插入的亚烷基或亚烯基等。