Quinolone carboxamide Calpain inhibitors
    1.
    发明授权
    Quinolone carboxamide Calpain inhibitors 失效
    喹诺酮羧酰胺钙蛋白酶抑制剂

    公开(公告)号:US5622967A

    公开(公告)日:1997-04-22

    申请号:US450961

    申请日:1995-05-25

    CPC分类号: C07D401/04

    摘要: A compound of the formula ##STR1## wherein: Z is aryl, substituted aryl, phenyl-lower-alkyl, hetero-aryl, substituted heteroaryl, heterocycloalkyl, heterocyclocalkyl-lower-alkyl, hetero-aryl-lower-alkyl wherein one or more hydrogens of aryl and heteroaryl is optionally replaced by A and B;Y is lower cycloalkyl, aryl, phenyl-lower-alkyl, hetero-aryl, heterocycloalkyl, heterocyclocalkyl-lower-alkyl, hetero-aryl-lower-alkyl wherein one or more hydrogens of aryl and heteroaryl is optionally replaced by A and B;X is CONH.sub.2, CONHOH, tetrazole, SO.sub.2 N(R).sub.2, PO(OH).sub.2, CON(R).sub.2, or CONR--CHR--CO--A or CONR--(CHR).sub.n --A;A and B is independently H, OH, OR, halo, CF.sub.3, lower alkyl, N(R).sub.2, CON(R).sub.2, SR, NHSO.sub.2 R, hydroxy-lower-alkyl, NHCOR, NRSO.sub.2 CF.sub.3, OSO.sub.2 CF.sub.3, or CN;R is H, lower-alkyl, phenyl-lower-alkyl, hydroxy-lower-alkyl, CO-lower-alkyl, or CO--(CH.sub.2).sub.n --aryl; andn is 1, 2, or 3, and a pharmaceutically acceptable salt thereof.

    摘要翻译: 式(I)的化合物,其中:Z是芳基,取代的芳基,苯基 - 低级 - 烷基,杂芳基,取代的杂芳基,杂环烷基,杂环烷基 - 低级 - 烷基,杂 - 芳基 - 低级烷基,其中一个 或更多的芳基和杂芳基的氢任选地被A和B取代; Y是芳基和杂芳基的一个或多个氢任选地被A和B取代的低级环烷基,芳基,苯基 - 低级烷基,杂芳基,杂环烷基,杂环烷基 - 低级烷基,杂芳基 - 低级烷基, X是CONH 2,CONHOH,四唑,SO 2 N(R)2,PO(OH)2,CON(R)2或CONR-CHR-CO-A或CONR-(CHR)n-A; A和B独立地是H,OH,OR,卤素,CF 3,低级烷基,N(R)2,CON(R)2,SR,NHSO 2 R,羟基 - 低级烷基,NHCOR,NRSO 2 CF 3,OSO 2 CF 3或CN; R为H,低级烷基,苯基 - 低级 - 烷基,羟基 - 低级 - 烷基,CO-低级 - 烷基或CO-(CH2)n-芳基; 和n为1,2或3及其药学上可接受的盐。