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    6,7-ASYMMETRICALLY DISUBSTITUTED QUINOXALINECARBOXYLIC ACID DERI VATIVES, ADDITION SALTS THEREOF, AND PROCESSES FOR THE PREPARATION OF BOTH
    1.
    发明公开
    6,7-ASYMMETRICALLY DISUBSTITUTED QUINOXALINECARBOXYLIC ACID DERI VATIVES, ADDITION SALTS THEREOF, AND PROCESSES FOR THE PREPARATION OF BOTH 有权
    6,7-二取代的非对称喹喔啉羧酸衍生物，它们的加成盐及其制造方法TWO

    公开(公告)号：EP1020453A1

    公开(公告)日：2000-07-19

    申请号：EP98940594.9

    申请日：1998-08-28

    申请人： KYORIN PHARMACEUTICAL CO., LTD.

    发明人： TAKANO, Yasuo ,  SHIGA, Futoshi ,  TAKADOI, Masanori ,  UCHIKI, Hideharu ,  ASANO, Jun ,  ANRAKU, Tsuyoshi ,  FUKUCHI, Kazunori ,  UDA, Junichiro ,  ANDO, Naoki

    IPC分类号： C07D241/44 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/44 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

    摘要： The present invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor, having 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives and their addition salts as effective ingredients, and processes for preparing them, and relates to 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives represented by a general formula (1)
    [wherein, Q denotes a halogen atom, lower alkyl group which may be substituted with halogen atom, general formula (2)

             Ar-P-      (2)

    (wherein Ar denotes a phenyl group or naphthyl group which may have one or more substituents, and P denotes a lower alkylene, lower alkenylene, lower alkynylene, oxygen or sulfur atom), or general formula (3);

             L-A-      (3)



    R denotes a nitro group, trifluoromethyl group, amino group which may be substituted, or general formula (7),

    R 1 denotes an aralkyl group, phenyl group, naphthyl group, 5- or 6-membered heterocycle and its condensed ring (these may have one or more substituents on aromatic ring or heterocycle), hydrogen atom, lower alkyl group which may be substituted with halogen atom or cycloalkyl group, and R 2 denotes a hydroxyl group, lower alkoxy group or general formula (6)
    ], and their addition salts.

    摘要翻译： 本发明提供的化合物与抗兴奋性氨基酸受体拮抗作用，特别是AMPA受体，具有6,7-二取代的非对称喹喔啉羧酸衍生物及其加成盐作为有效成分，以及制备它们的方法，并且涉及6,7- 由通式（1）表示二取代的非对称喹喔啉羧酸衍生物 a其中，Q表示卤素原子，其可以是有卤原子取代的低级烷基，通式（2）中的Ar-P-（Ar表示苯基worin 可具有一个或多个取代基，P表示低级亚烷基，低级亚烯基，低级亚炔基，氧，硫原子），或通式（3）基团或萘基; LA-R表示硝基，三氟甲基，可以被取代的氨基，或通式（7）， - [R <1>表示在芳烷基，苯基，萘基，5元或6元杂环 及其稠环（论文可以具有芳香环或杂环上一个或多个取代基），氢原子，低级烷基可以被卤素原子或环烷基被substituiertem，且R <2>表示羟基，低级烷氧基或 通式（6） T，及其加成盐。

    NOVEL N-SUBSTITUTED PYRROLIDINE DERIVATIVES AND PROCESS FOR PREPARING THE SAME
    8.
    发明公开
    NOVEL N-SUBSTITUTED PYRROLIDINE DERIVATIVES AND PROCESS FOR PREPARING THE SAME 失效
    在DEREN HERSTELLUNGSVERFAHREN下，使用DERIVATE VON N-SUBSTITUIERTEN PYRROLIDIN DERIVATEN

    公开(公告)号：EP0948964A1

    公开(公告)日：1999-10-13

    申请号：EP97913443.4

    申请日：1997-11-26

    申请人： KYORIN PHARMACEUTICAL CO., LTD.

    发明人： MIYACHI, Hiroyuki ,  HOSHINO, Masato ,  ANDO, Naoki ,  KOBAYASHI, Fumiyoshi

    IPC分类号： A61K31/40 ,  C07D207/12

    CPC分类号： C07D207/12

    摘要： Novel N-substituted pyrrolidine derivatives having a highly selective and potent antagonism against smooth muscle muscarine receptors and being useful for the treatment of irritable bowel syndrome and the like, characterized by being represented by the general formula (1) (wherein R represents a hydrogen atom, a halogen atom, or a lower alkoxy group and a process for preparing the same.

    摘要翻译： 新型N-取代吡咯烷衍生物，其具有对平滑肌毒蕈碱受体的高度选择性和有效的拮抗作用，并且可用于治疗肠易激综合征等，其特征在于由通式（1）表示（其中R表示氢原子 ，卤素原子或低级烷氧基及其制备方法