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    1,2,3,4-TETRAHYDROQUINOXALINEDIONE DERIVATIVE
    1.
    发明公开
    1,2,3,4-TETRAHYDROQUINOXALINEDIONE DERIVATIVE 失效
    1,2,3,4-四氢喹喔啉二酮衍生物

    公开(公告)号：EP0784054A1

    公开(公告)日：1997-07-16

    申请号：EP95932217.3

    申请日：1995-09-25

    申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

    发明人： SHISHIKURA, Jun-ichi ,  INAMI, Hiroshi ,  SAKAMOTO, Shuichi ,  TSUKAMOTO, Shin-ichi ,  SASAMATA, Masao ,  OKADA, Masamichi ,  FUJII, Mitsuo

    IPC分类号： C07D403/04 ,  C07D471/04 ,  C07D241/44 ,  A61K31/495

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/44 ,  C07D249/08

    摘要： A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier.
    wherein symbols in the above formula represent the following meanings, respectively:

    X: N, CH,
    R: an imidazolyl group or a di-lower alkylamino group,
    R 1 :

    (1) a halogen atom, a nitro group, a cyano group, a carboxyl group, an amino group, a mono- or di-lower alkylamino group, a lower alkanoyl group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group or a carbamoyl group,
    (2) a lower alkyl group or lower alkoxyl group which may be substituted by a halogen atom, a carboxyl group or an aryl group,
    (3) a phenyloxy group which may be substituted by a lower alkoxycarbonyl group or a carboxyl group,

    R 2 : a hydroxyl group, a lower alkoxyl group, an amino group or a mono- or di-lower alkylamino group,
    A: a lower alkylene group which may be substituted or a group represented by the formula -O-B-, and
    B: a lower alkylene group,
       with the proviso that the case wherein R represents an imidazolyl group, R 1 represents a cyano group, A represents an ethylene group and R 2 represents a hydroxyl group is excluded.

    摘要翻译： 由下式（I）表示的1,2,3,4-四氢喹喔啉二酮衍生物或其盐，含有该衍生物或盐的NMDA-甘氨酸受体和/或AMPA受体拮抗剂或海人藻酸神经毒性抑制剂。 另外，包含所述化合物和药学上可接受的载体的药物组合物。 其中上式中的符号分别表示以下含义：X：N，CH，R：咪唑基或二低级烷基氨基，R1：（1）卤素原子，硝基，氰基， 羧基，氨基，一或二低级烷基氨基，低级烷酰基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基或氨基甲酰基，（2）低级烷基或低级烷基 可以被卤素原子，羧基或芳基取代的烷氧基，（3）可以被低级烷氧基羰基或羧基取代的苯氧基，R2：羟基，低级烷氧基， 氨基或一或二低级烷基氨基，A：可被取代的低级亚烷基或由式-OB-表示的基团，和B：低级亚烷基，条件是其中 R表示咪唑基，R 1表示氰基，A表示亚乙基 并且R2代表羟基被排除。

    KAINIC ACID NEURONOTOXICITY INHIBITORS AND PYRIDOTHIAZINE DERIVATIVES
    3.
    发明公开
    KAINIC ACID NEURONOTOXICITY INHIBITORS AND PYRIDOTHIAZINE DERIVATIVES 失效
    抑制剂KAINSÄURE-NEUROTOXIZITÄTSOWIE PYRIDOTHIAZINDERIVATE

    公开(公告)号：EP0878196A1

    公开(公告)日：1998-11-18

    申请号：EP96938464.3

    申请日：1996-11-14

    申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.

    发明人： SHISHIKURA, Jun-ichi ,  INAMI, Hiroshi ,  YASUNAGA, Tomoyuki ,  HIRANO, Masaaki ,  SAKAMOTO, Shuichi ,  OHNO, Kazushige ,  OKADA, Masamichi ,  TSUKAMOTO, Shin-ichi

    IPC分类号： A61K31/54 ,  C07D513/04

    CPC分类号： A61K31/5415

    摘要： Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R 1 , R 2 , R 3 , R 4 and R 5 are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R 2 and R 3 together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.

    摘要翻译： 神经元保护剂，其基础是抑制红藻氨酸的神经毒性和用作此类药物的化合物。 通式（I）表示的吡唑并噻嗪衍生物或其药学上可接受的盐和含有这些化合物或其药学上可接受的盐的活性成分的神经毒性抑制剂，其中A表示吡啶环; 式（II）表示式（III）或式（IV）; 和R 1，R 2，R 3，R 4和R 5相同或不同，各自表示氢，任选取代的低级烷基，环烷基，烯基，芳基，羧基或低级烷氧基羰基 或不存在，或R 2和R 3一起形成任选具有氮原子作为另一杂原子的含氮杂环，与苯环稠合或被低级烷基取代。