IMIDAZOPYRIDINES

摘要

Novel imidazopyridine derivatives of formula I: <IMAGE> I wherein R is <IMAGE> R1 is A, alkenyl or alkynyl each having up to 6 C atoms, R2 is H, COOH, COOA, CN, NO2, NHCOR5, NHSO2R5 or 1H-tetrazol-5-yl, R3 is R5-CO-alkyl, Ar-CO-alkyl, Het-CO-alkyl or Het-alkyl each having 1-6 C atoms in the alkyl moiety, R4 is H or Hal, R5 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=C(COOH)-, -CH=C(CN)- OR -CH=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 R5, OR5, COOH, COOA, CN, NO2, NH2, NHCOR5, NHSO2R5 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, and Hal 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.