Bayer Aktiengesellschaft

Hans Peter Schulz

Herbert Thomas

Arno Widdig

Peter Andrews

Hartmund Wollweber

Ekkehard Niemers

Heinrich Kolling

Engelbert Kuhle

Herbert Voege

A new class of N'-(aminoacylaminophenyl) acetamidines: ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, alkyl, aryl or the substituted derivatives thereof or, together with the nitrogen atom to which they are attached, an heterocyclic ring; and R.sup.3 is hydrogen, alkyl, aryl, aralkyl, or a heterocyclic moiety including the substituted derivatives thereof. The products have utility as anthelmintics. The products are obtained by treating a suitable amino-acid or a carbonyl-activated amino-acid, with the appropriate N'-(4-aminophenyl)-N,N-dimethylacetamidine. In addition, the products are obtained by treating a suitable N'-(haloacylaminophenylacetamidine with an appropriate amine.

N'-(Aminoacylaminophenyl) acetamidines

Helmintic infestations can be treated with an N-carbalkoxy-N'-(2-amido-5-alkylphenyl)-S-substituted-isothiourea. A typical embodiment is the treatment of Bunostomum trigonocephalum in sheep utilizing N-methoxycarbonyl-N'-(2-butyramido-5-n-butylphenyl)-S-methylisothiourea. Compositions adapted for this use are also described.

Anthelmintic compositions and uses employing amidophenylisothioureas

New 4-acylaminophenylacetamidines of the formula: ##STR1## in which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides. The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.

4-Acylaminophenylacetamidines and a method for their preparation

Pour-on veterinary compositions are prepared which comprise an anthelmintically effective amount of tetramisole, levamisole or an acid addition salt thereof in combination with a diluent suitable for pour-on formulations for use on animals. These compositions are used to treat helminthic infestations in animals by the pour-on method of application.

Tetramisole and levamisole pour-on anthelmintic compositions and methods

New 4-acylaminophenylacetamidines of the formula: ##SPC1## In which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides. The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.

Benzoylphenylisothioureas of the formula: ##SPC1## Wherein

Benzoylphenylisothioureas

Benzoylphenylguanidines of the formula ##SPC1## Wherein

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Wuppertal, Germany

Hans Peter Schulz