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    HETEROCYCLE-FUSED BENZOTHIAZINE DERIVATIVES
    1.
    发明公开
    HETEROCYCLE-FUSED BENZOTHIAZINE DERIVATIVES 审中-公开
    异丁基苯乙烯 - 苯乙烯苯并三唑衍生物

    公开(公告)号：EP1057830A1

    公开(公告)日：2000-12-06

    申请号：EP99906524.6

    申请日：1999-02-26

    申请人： Eisai Co., Ltd. ,  Yamada, Sumiyo ,  Yamada, Ryoko

    发明人： YAMADA, Koji ,  MIYAMOTO, Mitsuaki ,  YOSHIUCHI, Tatsuya ,  SATO, Keizo ,  SOEJIMA, Motohiro ,  SATO, Takashi ,  KIKUCHI, Koichi, Gardenhills Hisamatsu 302 ,  YOSHIMURA, Hiroyuki ,  MORIYA, Katsuhiro ,  SAKUMA, Yoshinori ,  AKASOFU, Shigeru

    IPC分类号： C07D513/04 ,  A61K31/54 ,  A61K31/645

    CPC分类号： C07D513/04

    摘要： The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like. Further, the heterocyclic ring condensed benzothiazine compound of the present invention, its pharmacologically acceptable salt or hydrates thereof is represented by the following formula:
    In the formula, the ring Het represents an unsaturated heterocyclic ring; R 1 and R 2 are the same as or different from each other, and each represents halogen atom, a lower alkyl group that may be substituted with a halogen atom, a lower alkoxy group that may be substituted with a halogen atom, a lower alkyl lower alkoxy group, cyano group; D represents a lower alkylene group and the like that may have a substituent; Q represents, for example, the formula -NR 20 R 21 (in the formula, R 20 and R 21 are the same as or different from each other, and each represents hydrogen atom, a lower alkyl group that may be substituted with a halogen atom, an aryl group that may have a substituent, an arylalkyl group that may have a substituent, a heteroaryl group that may have a substituent or a heteroarylalkyl group that may have a substituent, or R 20 and R 21 may form a 3- to 8-membered ring along with the nitrogen atom to which they are bound); and x represents an integer of from 1 to 2.

    摘要翻译： 本发明提供一种新颖的杂环稠合苯并噻嗪化合物，其对组胺，白细胞三烯等参与的疾病的预防或治疗有效。 本发明的杂环稠合苯并噻嗪化合物或其药理学上可接受的盐对于预防或治疗其中化学介质如组胺，白三烯等参与的疾病是有效的，例如哮喘，过敏性鼻炎， 特应性皮炎，荨麻疹，花粉症，胃肠过敏，食物过敏等。 此外，本发明的杂环稠合苯并噻嗪化合物，其药理学上可接受的盐或其水合物由下式表示：式中，环Het表示不饱和杂环; R 1和R 2彼此相同或不同，各自表示卤素原子，可被卤素原子取代的低级烷基，可被卤素原子取代的低级烷氧基 ，低级烷基低级烷氧基，氰基; D表示可以具有取代基的低级亚烷基等; Q表示例如式-NR 20 R 21（式中，R 20和R 21彼此相同或不同，各自表示氢原子，低级烷基 可以被卤素原子取代的基团，可以具有取代基的芳基，可以具有取代基的芳烷基，可以具有取代基的杂芳基或可以具有取代基的杂芳基烷基，或者R 20 并且R 21可以与它们所结合的氮原子一起形成3至8元环; x表示1〜2的整数。