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    NITROGENATED BICYCLIC AROMATIC HETEROCYCLIC COMPOUND
    3.
    发明公开
    NITROGENATED BICYCLIC AROMATIC HETEROCYCLIC COMPOUND 有权
    NITROGENIERTE BICYCLISCHE AROMATISCHE HETEROCYCLISCHE VERBINDUNG

    公开(公告)号：EP2840083A1

    公开(公告)日：2015-02-25

    申请号：EP13777902.1

    申请日：2013-04-17

    申请人： Astellas Pharma Inc.

    发明人： NAKAJIMA, Yutaka ,  IMADA, Sunao ,  TAKASUNA, Yuji ,  AOYAMA, Naohiro ,  NIGAWARA, Takahiro ,  SHIRAKAMI, Shohei ,  SHIRAI, Fumiyuki ,  SATO, Junji ,  NAKANISHI, Keita ,  KUBO, Kaori

    IPC分类号： C07D487/04 ,  C07D473/00 ,  A61K31/519 ,  A61K31/5377 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

    CPC分类号： A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  C07D473/00 ,  C07D487/04

    摘要： [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided.
    [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

    摘要翻译： [问题]基于组织蛋白酶S抑制效果，提供了用于治疗或预防自身免疫性疾病，过敏性疾病，器官，骨髓或组织的移植物排斥，系统性红斑狼疮等的优异的药剂。 [解决方案]发现含氮双环杂环化合物具有优异的组织蛋白酶S抑制作用，从而完成了本发明。 本发明的化合物具有组织蛋白酶S抑制作用，可用作预防和/或治疗自身免疫性疾病，过敏性疾病，器官移植排斥反应，骨髓或组织，系统性红斑狼疮等的药剂 。

    N-HYDROXYACRYLAMIDE COMPOUNDS
    4.
    发明公开
    N-HYDROXYACRYLAMIDE COMPOUNDS 有权
    N-羟基丙烯酰胺化合物

    公开(公告)号：EP1981877A1

    公开(公告)日：2008-10-22

    申请号：EP07708338.4

    申请日：2007-02-06

    申请人： Astellas Pharma Inc.

    发明人： SHIRAI, Fumiyuki ,  TSUTSUMI, Hideo ,  ITANI, Hiromichi ,  KOZUKI, Yoshihiro ,  EIKYU, Yoshiteru ,  MASUNAGA, Taro

    IPC分类号： C07D403/12 ,  C07D401/12 ,  A61K31/496 ,  A61P35/00

    CPC分类号： C07D409/14 ,  C07D401/12 ,  C07D403/12

    摘要： This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof . More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC- related disease.

    摘要翻译： 本发明涉及式（I）的新型N-羟基丙烯酰胺化合物及其药学上可接受的盐。 更具体地说，本发明涉及作为HDAC抑制剂的新型N-羟基丙烯酰胺化合物及其药学上可接受的盐，包含其的药物组合物，以及涉及治疗和/或预防HDAC-相关 疾病。

    N-HYDROXYACRYLAMIDE COMPOUNDS
    5.
    发明公开
    N-HYDROXYACRYLAMIDE COMPOUNDS 审中-公开
    N-羟基丙烯酰胺化合物

    公开(公告)号：EP2099756A1

    公开(公告)日：2009-09-16

    申请号：EP07851012.0

    申请日：2007-12-14

    申请人： Astellas Pharma Inc.

    发明人： INOUE, Yoshikazu ,  EIKYU, Yoshiteru ,  SHIRAI, Fumiyuki

    IPC分类号： C07D213/74 ,  C07D241/20 ,  A61K31/44 ,  A61K31/4965

    CPC分类号： C07D213/74 ,  C07D241/20 ,  C07D405/12

    摘要： A compound having the following formula (I) : wherein - R1 is hydrogen, optionally substituted lower alkyl, cyclo (lower) alkyl, cyclo (higher) alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo (lower) alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with -OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.

    摘要翻译： 具有下式（I）的化合物：其中-R 1是氢，任选取代的低级烷基，环（低级）烷基，环（高级）烷基，任选取代的芳基，任选取代的杂环基或芳基稠合的环（低级） ，R2是氢或卤素，Z是CH或N，X是式（II）R3是可以被-OH取代的低级烷基或任选取代的芳基或低级烷酰基，R4是氢或低级烷基，Y是任选取代的 低级亚烷基或其盐。 该化合物可用作组蛋白脱乙酰酶抑制剂。