Hoffmann-La Roche Inc.

Ivan Kompis

Guido Zanetti

Ekkehard Weiss

Rita Locher

Gerald Rey-Bellet

Alexander E Wick

Synese Jolidon

Pierre-Charles Wyss

Hans Maag

Christian N Hubschwerlen

Jean-Luc Specklin

Martin Karpf

Markus Schlageter

Rudolf L Then

Alfredo Guerrato

G/e/ Rald Rey-Bellet

Hanny K Berger

Pharmaceutical preparations containing an antibacterially-active synergistic combination of epiroprim and dapsone are useful in the treatment or control of infections caused by mycobacteria, Actinomycetes and toxoplasmosis pathogens.

Antibiotic combination

The present invention relates to novel substituted pyrimidobenzimidazole derivatives of the formula ##STR1## wherein the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The products have an inhibitory action on the DNA-gyrase activity in bacteria. They can accordingly be used for the prevention or control of bacterial infections.

Amino substituted pyrimido[1,6-2]benzimidazoles

Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Quinoline derivatives

Methyl 4-dimethylamino-3,5-dimethoxybenzoate, an intermediate in the preparation of the antibacterially active aditoprim, is obtained from 4-amino-3,5-dibromobenzoic acid by replacement of the bromine atoms by methoxy groups and subsequent methylation.

Process for the methyl-4-(dimethylamino)-3,5-dimethoxybenzoate

Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.

2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.

2,4-diamino-5[4-amino (or dimethylamino)-3,5-dimethoxybenzyl]pyrimidine

The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present, are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.

Pyrimidine derivatives for treating malaria

The compounds of the formula ##STR1## wherein one of the symbols Q and Q' is the group --CH.dbd. and the other is the group --CH.dbd. or --N.dbd., R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or halogen and n is the integer 0, 1 or 2, and their pharmaceutically acceptable acid addition salts, which have valuable antimycotic properties and can be used for the control of infections caused by pathogenic fungi, are described.

Intermediates for the preparation of substituted 2-phenyl-1,3-dioxolanes

Intermediates for benzylpyrimidines

Substituted 2-phenyl-1,3-dioxolanes

Aqueous solutions of antibacterially active sulfonamides and sulfonamide potentiators, which are suitable for parenteral administration and which contain no organic solvent, are prepared by reacting a sulfonamide RH with an aldehyde R.sup.1 CHO to give a compound of the formula R.sup.1 CH(R).sub.2 and dissolving said compound in water together with the sulfonamide potentiator.

Process for the preparation of aqueous solutions of potentiated

2,4-diamino-[4-piperidinyl]pyrimidines useful as antibacterial agents,

Pharmaceutical compositions of sulfonamide and sulfonamide-potentiator are disclosed. These compositions, which are suitable for injection administration, comprise an aldehyde in addition to the sulfonamide and its potentiator.

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Oberwil, Switzerland

Ivan Kompis