SUBSTITUTED 2- AMIDOQUINAZOL-4-ONES AS MATRIX METALLOPROTEINASE-13 INHIBITORS
    1.
    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

    IPC分类号: C07D495/04

    摘要: 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.

    摘要翻译: 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。