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26 条记录 (耗时 0.012 秒)

    2,6,7,8-Substituted quinazolines, process for production thereof, and use thereof
    21.
    发明授权
    2,6,7,8-Substituted quinazolines, process for production thereof, and use thereof 失效
    2,6,7,8-取代的喹唑啉，其制备方法及其用途

    公开(公告)号：US4517189A

    公开(公告)日：1985-05-14

    申请号：US519235

    申请日：1983-08-02

    申请人： Masayuki Ishikawa ,  Hiroshi Azuma ,  Akiko Sugimoto ,  Noriko Takahashi ,  Yoshimi Takashima

    发明人： Masayuki Ishikawa ,  Hiroshi Azuma ,  Akiko Sugimoto ,  Noriko Takahashi ,  Yoshimi Takashima

    IPC分类号： C07D239/74 ,  A61K31/505

    CPC分类号： C07D239/74

    摘要： A 2,6,7,8-substituted quinazoline represented by the following formula ##STR1## wherein R.sub.1 and R.sub.3 each represent a lower alkyl group, R.sub.2 represents a lower alkoxy-carbonyl group, and A represents a lower alkyl group, or a phenyl or benzyl group which is unsubstituted or substituted by a substituent selected from the class consisting of halogen atoms, a trifluoromethyl group and lower alkyl groups, or its acid addition salt. The said compound can be prepared by reacting a compound represented by the following formula ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and A are as defined, with ammonia. A pharmaceutical composition comprising the said compound as an active ingredient is useful for the treatment of disorders of the circulatory system.

    摘要翻译： 由下式[IMAGE]表示的2,6,7,8-取代喹唑啉其中R1和R3各自表示低级烷基，R2表示低级烷氧基 - 羰基，A表示低级烷基或苯基 或未取代或被选自卤素原子，三氟甲基和低级烷基的取代基取代的苄基或其酸加成盐。 所述化合物可以通过使下式（其中R 1，R 2，R 3和A如上所定义）与氨反应的化合物制备。 包含所述化合物作为活性成分的药物组合物可用于治疗循环系统疾病。

    Drug target that promotes secretory granule-granule fusion
    22.
    发明申请
    Drug target that promotes secretory granule-granule fusion 审中-公开
    促进分泌颗粒 - 颗粒融合的药物靶标

    公开(公告)号：US20120058931A1

    公开(公告)日：2012-03-08

    申请号：US12796035

    申请日：2010-09-03

    申请人： Haruo Kasai ,  Noriko Takahashi ,  Vesa Olkkonen ,  Herbert Y. Gaisano ,  Patrick Lam

    发明人： Haruo Kasai ,  Noriko Takahashi ,  Vesa Olkkonen ,  Herbert Y. Gaisano ,  Patrick Lam

    IPC分类号： A61K38/00 ,  G01N33/566 ,  C07K2/00

    CPC分类号： G01N33/68 ,  G01N33/6872 ,  G01N2500/00

    摘要： Munc18 proteins facilitate formation of SNARE complexes known to mediate membrane fusion. Much is known about the fusion of secretory granule (SG) to plasma membrane, mediated by Munc18a-SNARE complexes. It has been found that another Munc18 isoform, Munc18b, mediates SG-SG fusion which causes potentiation of secretion. The present invention has identified specific site mutations within Munc18b which further increased (called KR mutant) or reduced (called E59K mutant) SG-SG fusion compared to wild type (WT) Munc18b, causing amplification or reduction of insulin secretion, respectively. Compounds identified that mimic the actions of Munc18b-WT and Munc18b-KR mutant which increase SG-SG fusion, and those which mimic Munc18b-E59K mutant that block SG-SG fusion, are useful for treating and/or preventing diseases and/or conditions, whose underlying bases are a deficiency or excess of SG-SG fusion, respectively. These compounds also include conserved domains in Munc18a and Munc18c that mimic the KR and E59K sites in Munc18b.

    摘要翻译： Munc18蛋白有助于形成已知介导膜融合的SNARE复合物。 已知关于由Munc18a-SNARE复合物介导的分泌颗粒（SG）与质膜的融合。 已经发现另一种Munc18同种型Munc18b介导导致分泌增强的SG-SG融合物。 本发明鉴定了与野生型（WT）Munc18b相比分别进一步增加（称为KR突变体）或降低（称为E59K突变体）SG-SG融合物的Munc18b中的特异性位点突变，分别导致胰岛素分泌的扩增或降低。 鉴定出模拟Munc18b-WT和Munc18b-KR突变体增加SG-SG融合物的作用的化合物，以及模拟阻断SG-SG融合物的Munc18b-E59K突变体的化合物可用于治疗和/或预防疾病和/或病症 ，其基础分别为SG-SG融合体的缺乏或过量。 这些化合物还包括Munc18a和Munc18c中的保守结构域，其模拟Munc18b中的KR和E59K位点。