Imidazopyridines

US5242928A · kind A · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Werner Mederski · Zwingenberg, DE
• Dieter Dorsch · Ober-Ramstadt, DE
• Norbert Beier · Reinheim, DE
• Pierre Schelling · Mühltal, DE
• Ingeborg Lues · Darmstadt, DE
• Klaus-Otto Minck · Ober-Ramstadt, DE

Key dates

• Filing date: Dec 17, 1992
• Grant date: Sep 7, 1993
• Expiry date: Dec 17, 2012

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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, PA0 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, PA0 R.sup.4 is H or Hal, PA0 R.sup.5 is alkyl having 1-6 C atoms, wherein one or more H atoms can also be replaced with F, PA0 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)--, PA0 Y is O or S, PA0 A is alkyl having 1-6 C atoms, PA0 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, PA0 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 PA0 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 i…