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    HETEROCYCLIC COMPOUND
    6.
    发明公开
    HETEROCYCLIC COMPOUND 审中-公开
    杂环化合物

    公开(公告)号：EP2857400A1

    公开(公告)日：2015-04-08

    申请号：EP13797604.9

    申请日：2013-05-31

    申请人： Takeda Pharmaceutical Company Limited

    发明人： NARA, Hiroshi ,  DAINI, Masaki ,  KAIEDA, Akira ,  KAMEI, Taku ,  IMAEDA, Toshihiro ,  KIKUCHI, Fumiaki

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61P1/04 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00

    CPC分类号： C07D471/04

    摘要： The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof.
    The present invention relates to a compound represented by the formula

    wherein each symbol is as defined in the specification, or a salt thereof.

    摘要翻译： 本发明提供具有优越的JAK抑制作用的化合物，其可用作预防或治疗自身免疫性疾病（类风湿性关节炎，牛皮癣，炎性肠病，舍格伦综合征，贝切特氏病，多发性硬化症，系统性红斑狼疮， （白血病，子宫平滑肌肉瘤，前列腺癌，多发性骨髓瘤，恶病质，骨髓纤维化等）等，或其盐。 本发明涉及由下式表示的化合物或其盐，其中每个符号如说明书中所定义。

    NOVEL THIOL DERIVATIVE, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
    7.
    发明公开
    NOVEL THIOL DERIVATIVE, PROCESS FOR PRODUCING THE SAME AND USE THEREOF 审中-公开
    消除琐事，VERFAHREN ZU DESSEN HERSTELLUNG UND DESSEN VERWENDUNG

    公开(公告)号：EP1500658A1

    公开(公告)日：2005-01-26

    申请号：EP03719194.7

    申请日：2003-04-24

    申请人： Takeda Pharmaceutical Company Limited

    发明人： KAJINO, Masahiro ,  TAKIZAWA, Masayuki ,  NOTOYA, Kohei ,  NARA, Hiroshi ,  IKEMOTO, Tomomi ,  NISHIGUCHI, Atsuko

    IPC分类号： C07D401/06 ,  C07D401/14 ,  A61K31/4439 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P19/02 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00

    CPC分类号： C07D401/14 ,  A61K31/4439 ,  C07D401/06

    摘要： The present invention provides a novel thiol derivative [I] which has an excellent matrix metalloprotease inhibiting activity and is useful as a pharmaceutical composition, particularly a therapeutic agent or prophylactic agent for osteoarthritis and rheumatoid arthritis and a salt thereof, the thiol derivative being a compound represented by the formula [I]:
       wherein ring A represents an optionally substituted aromatic heterocyclic ring;
       ring B represents an optionally substituted homocyclic or heterocyclic ring;
       R 1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR 2 (wherein R 2 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group);
       X represents an optionally substituted divalent C 1-3 aliphatic hydrocarbon group;
       Y represents an optionally substituted hydrocarbon group, a halogen atom, a carboxy group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR 3 (wherein R 3 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group), an oxo group, a thioxo group, an optionally substituted imino group, a nitro group or a cyano group; and
       q represents an integer of 0 to 5.

    摘要翻译： 本发明提供了一种具有优异的基质金属蛋白酶抑制活性的新型硫醇衍生物，可用作药物组合物，特别是用于骨关节炎和类风湿性关节炎及其盐的治疗剂或预防剂，硫醇衍生物是由 其中环A表示任选取代的芳族杂环; 环B表示任选取代的杂环或杂环; R 1表示氢原子，任选取代的烃基，酰基，任选取代的杂环基或SR 2（其中R 2表示氢原子，任选取代的烃基，酰基或 任选取代的杂环基）; X表示任选取代的二价C 1-3脂族烃基; Y表示任选取代的烃基，卤素原子，羧基，酰基，任选取代的羟基，任选取代的氨基，SR 3（其中R 3表示氢原子，任选取代的 烃基，酰基或任选取代的杂环基），氧代基，硫代基，任选取代的亚氨基，硝基或氰基; q表示0〜5的整数。