Hoffmann-la Roche Inc.

Marc Montavon

Roland Reiner

Erika Bohni

Helmut Link

Hermann Bretschneider

Wilhelm Klotzer

Renate Mussner

Urs Brombacher

Karl Bernauer

Janos Borgulya

Nicolas Singewald

Gunter Weis

Kraft Hohenlohe-Oehringen

Joachim Schantl

Wolfgang Turk

Eva M Karpitschka

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

Compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and the pharmaceutically acceptable acid addition salts thereof, possess pharmacological properties. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties.

Antimicrobial imidazolium derivatives

The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro,

Schistosomicidal acridanone hydrazones

Acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of the substituents R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond and R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl substituted by halogen or lower alkoxy, and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical compositions based thereon, are described. The compounds of formula I are useful as schistosomicidal agents.

There are presented cephalosporin derivatives of the formula ##STR1## wherein X is the group ##STR2## R is hydrogen or a readily hydrolyzable ester or ether group and n stands for 1 or 2, as well as salts of these compounds and hydrates of these compounds and salts.

Cephalosporin derivatives

Cephalosporins represented by the formula

Cephalosporins

Acyl derivatives of the formula ##STR1## wherein R signifies hydrogen or a protective group which can be split off, R.sup.1 signifies lower alkyl and X signifies the group ##STR2## wherein one of the residues R.sup.2 and R.sup.3 represents hydrogen and the other represents alkyl and R.sup.4 represents lower alkyl the easily hydrolyzable esters and ethers thereof, the salts and hydrates of the above compounds, esters, ethers and salts.

Thiazolylacelamide cephalosporins

There is presented cephalosporin derivatives which are the readily hydrolysable esters and ethers of compounds of the general formula ##STR1## wherein R represents furyl, thienyl or phenyl optionally substituted by halogen, hydroxy, lower alkoxy or lower alkyl, R.sub.1 represents lower alkyl or aminocarbonylmethyl and X represents a group of the formula ##STR2## in which one of the two symbols R.sub.2 and R.sub.3 represents hydrogen and the other represents lower alkyl and R.sub.4 represents lower alkyl, as well as salts of said esters and ethers and hydrates of said esters, ethers and salts.

The acyl derivatives provided by the present invention are compounds of the general formula ##STR1## wherein R represents furyl, thienyl or phenyl optionally substituted by halogen, hydroxy, lower alkoxy or lower alkyl, R.sub.1 represents alkyl or aminocarbonylmethyl and X represents a group of the formula ##STR2## in which one of the two symbols R.sub.2 and R.sub.3 or R.sub.4 and R.sub.5 represents hydrogen

Derivatives of 7 [-substituted oxyimins acetamido] cephalosporins

Compositions comprising N-sulfanilyl-1-ethylcytosine and a sulfonamide potentiator, which are useful as antibacterial agents, are described.

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Basel, Switzerland

Marc Montavon