Imidazopyridines
    4.
    发明授权
    Imidazopyridines 失效
    咪唑吡啶

    公开(公告)号:US5242928A

    公开(公告)日:1993-09-07

    申请号:US991888

    申请日:1992-12-17

    CPC分类号: C07D471/04

    摘要: Novel imidazopyridine derivatives of formula I: ##STR1## wherein R is ##STR2## R.sup.1 is A, alkenyl or alkynyl each having up to 6 C atoms, R.sup.2 is H, COOH, COOA, CN, NO.sub.2, NHCOR.sup.5, NHSO.sub.2 R.sup.5 or 1H-tetrazol-5-yl,R.sup.3 is R.sup.5 --CO--alkyl, Ar--CO--alkyl, Het--CO--alkyl or Het-alkyl each having 1-6 C atoms in the alkyl moiety,R.sup.4 is H or Hal,R.sup.5 is alkyl having 1-6 C atoms, wherein one or more H atoms can also be replaced with F,X is absent or is --NH--CO--, --CO--NH--, --O--CH(COOH)--, --NH--CH(COOH)--, --NA--CH(COOH)--, --CH.dbd.C(COOH)--, --CH.dbd.C(CN)-- OR --CH.dbd.C(1H-tetrazol-t-yl)--,Y is O or S,A is alkyl having 1-6 C atoms,Ar is unsubstituted phenyl or phenyl monosubstituted by R.sup.5, OR.sup.5, COOH, COOA, CN, NO.sub.2, NH.sub.2, NHCOR.sup.5, NHSO.sub.2 R.sup.5 or 1H-tetrazol-5-yl,Het is a five- or six-membered heteroaromatic radical having 1 to 3 N, O and/or S atoms, which can also be fused with a benzene or pyridine ring, andHal is F, Cl, Br or I,and their salts, exhibit antagonistic properties towards angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and increased intraocular pressure, and of disorders of the central nervous system.

    摘要翻译: 式I的新型咪唑并吡啶衍生物:其中R为R 1为各自具有至多6个C原子的链烯基或炔基,R 2为H,COOH,COOA,CN,NO 2,NHCOR 5,NHSO 2 R 5或1H- 四唑-5-基,R 3是在烷基部分中具有1-6个C原子的R 5 -CO-烷基,Ar-CO-烷基,Het-CO-烷基或Het-烷基,R 4是H或Hal,R 5是烷基 具有1-6个C原子,其中一个或多个H原子也可被F取代,X不存在或是-NH-CO-,-CO-NH-,-O-CH(COOH) - , - NH-CH (COOH) - ,-NA-CH(COOH) - , - CH = C(COOH) - , - CH = C(CN) - 或-CH = C(1H-四唑-T-基) - ,Y为O 或S,A是具有1-6个C原子的烷基,Ar是未取代的苯基或被R5,OR5,COOH,COOA,CN,NO2,NH2,NHCOR5,NHSO2R5或1H-四唑-5-基单取代的苯基,Het是 具有1至3个N,O和/或S原子的5或6元杂芳族基团,其也可以与苯或吡啶环稠合,Hal是F,Cl,Br或I,并且它们的盐表现出拮抗作用 对血管紧张素II的特性,可用于治疗h 高血压,醛固酮增多症,心功能不全和眼压升高以及中枢神经系统疾病。