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    SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS
    6.
    发明申请
    SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS 审中-公开
    作为基质金属蛋白酶-13抑制剂取代2-氨基喹唑啉-4-酮

    公开(公告)号：US20150329556A1

    公开(公告)日：2015-11-19

    申请号：US14812351

    申请日：2015-07-29

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Jun Terauchi ,  Hiroshi Nara ,  Hideyuki Oki ,  Kenjiro Sato

    IPC: C07D495/04

    CPC classification number: C07D495/04 ,  C07D217/26 ,  C07D239/90 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

    Abstract: The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR1 (R1 is a hydrogen atom or an optionally substituted hydrocarbon group), is a single bond or a double bond, R2 is a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X′ is S, O, SO, or CH2), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]2 hydroxypropyl}5,6 dimethyl 4 oxo 1,4 dihydrothieno[2,3-d]pyrimidine-2-carboxamide is excluded, or a salt thereof.

    Abstract translation: 本发明提供具有基质金属蛋白酶抑制活性的新型酰胺衍生物，可用作药剂，其为式（I）表示的化合物，其中环A为任选取代的含氮杂环，环B为任选的 取代的单环同环或任选取代的单环杂环，Z是N或NR1（R1是氢原子或任选取代的烃基）是单键或双键，R2是氢原子或任选取代的烃基， X是任选取代的具有1-6个原子的间隔基，环C是（1）任选取代的杂环，或（2）除（II）表示的环以外的任选取代的杂环（X'是S，O，SO或 CH2），并且环B和环C中的至少一个具有取代基，条件是N - {（1S，2R）-1-（3,5-二氟苄基）-3 - [（3-乙基苄基）氨基] 2羟丙基} 5,6二甲基4氧代1,4-二氢噻吩并[2,3-d]嘧啶-2 - 甲酰胺或其盐。

    HETEROCYCLIC COMPOUND
    7.
    发明申请
    HETEROCYCLIC COMPOUND 有权
    杂环化合物

    公开(公告)号：US20150141406A1

    公开(公告)日：2015-05-21

    申请号：US14404126

    申请日：2013-05-31

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Hiroshi Nara ,  Masaki Daini ,  Akira Kaieda ,  Taku Kamei ,  Toshihiro Imaeda ,  Fumiaki Kikuchi

    IPC: C07D471/04

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 本发明提供具有优异的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，干燥综合征，白塞病，多发性硬化，系统性红斑狼疮， 等），癌症（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，其中每个符号如说明书中所定义，或其盐。

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