Hoffmann-la Roche Inc.

Nicolas Singewald

Wilhelm Klotzer

Renate Mussner

Helmut Link

Werner Schiestl

Marc Montavon

The imidazolium compounds of the formula ##STR1## wherein Q is arylene or heteroarylene, the group --NR.sup.1 R.sup.2 is a basic amino group, R.sup.3 is lower alkylthio, lower alkoxy or the group --(A).sub.n --Ra, R.sup.4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group, --N.dbd.CRc--Rb, --CHRcRd, --NH--CHRcRd, --NH--CO--Re or --CHRc--CO--Re, R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R.sup.6 is hydrogen or lower alkyl, Ra and Rb independently are aryl, heteroaryl or a basic amino group, Rc is hydrogen or lower alkyl, Rd is aryl or heteroaryl, Re is hydrogen, a saturated or partially unsaturated lower hydrocarbon group optionally attached via an oxygen atom, or an aryl, heteroaryl or basic amino group optionally attached via a lower alkyl group, A is vinylene or lower alkylene, n is the integer 0 or 1, the dotted line is an additional double bond and the symbol Y.sup.- is a pharmaceutically acceptable anion, and their pharmaceutically acceptable acid addition salts, which possess valuable pharmacological properties are described. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties and are especially active against parasitic protozoa and worms. The compounds of formula I can be prepared according to known methods.

1,3-disubstituted/imidazolium salts

Imidazole derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 each is lower alkyl, X is a residue of the formula ##STR2## R.sup.3 is hydrogen and R.sup.4 is hydrogen or lower alkyl or R.sup.3 and R.sup.4 taken together are an additional carbon-nitrogen bond; R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkylthio or a residue of the formula --NR.sup.7 R.sup.8 ; and R.sup.7 and R.sup.8 each is lower alkyl or taken together with the nitrogen atom are a 5- or 6-membered saturated heterocycle; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I possess valuable pharmacodynamic properties, especially inflammation-inhibiting and edema-inhibiting properties, so that they can be used for the control or prevention of illnesses, especially for the control or prevention of inflammations and edemas.

Imidazole derivatives

The imidazolium compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and their pharmaceutically acceptable acid addition salts, which possess valuable pharmacological properties are described. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties and are especially active against parasitic protozoa and worms. The compounds of formula I can be prepared according to known methods.

Growing community of inventors

Innsbruck, Austria

Nicolas Singewald