Mixtures of substituted benzimidazoles with polyether antibiotic

Details Mixtures of substituted benzimidazoles with polyether antibiotic Mixtures of substituted benzimidazoles with polyether antibiotic

1997-11-19

2000-03-07

Cook, Rebecca

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514395, 514629, A61K 31415

Patent

active

060341165

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to mixtures of substituted benzimidazoles with a polyether antibiotic or a synthetically prepared coccidiostat as compositions to control parasitic protozoa and, in particular, coccidia, and fish parasites and insect parasites.
Substituted benzimidazoles and their use as insecticides, fungicides and herbicides have already been disclosed (EP-OS (European Published Specifications) 87 375, 152 360, 181 826, 239 508, 260 744, 266 984, U.S. Pat. Nos. 3,418,318, 3,472,865, 3,576,818, 3,728,994).
Halogenated benzimidazoles and their effect as anthelmintics, coccidiostats and pesticides have been disclosed (DE-OS (German Published Specification) 2 047 369, DE-OS (German Published Specification) 4 237 617). Mixtures of nitro-substituted benzimidazoles and polyether antibiotics have been disclosed as coccidiostats (U.S. Pat. No. 5,331,003). Their effect is as yet unsatisfactory in all cases.
Coccidiosis is a disease caused by single-cell parasites (protozoa). It may cause great losses in particular in poultry rearing. In order to avoid this, the stocks are treated prophylactically with coccidiostats. The development of resistance to the compositions used results after only a relatively few years in serious problems. On the other hand, it is possible by using chemically completely new coccidiostats, in particular combinations, to control even polyresistant parasite strains.
The present invention relates to mixtures of substituted benzimidazoles of the formula (I) ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R4 each, independently of one another, represent hydrogen, halogen, represent in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, represent optionally substituted fused-on dioxyalkylene, but where at least one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is different from hydrogen and halogen, more times, identically or differently, by OH, CN, NH.sub.2, alkyl, cycloalkyl, alkenyl, alkinyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, alkenoxy, alkinoxy, aminocarbonyl, optionally substituted alkylcarbonyl, optionally substituted (het-)arylcarbonyl, optionally substituted alkoxycarbonyl (AlkO--CO--), optionally substituted alkoxycarbonyloxy (AlkOCOO--), aminosulphonyl (SO.sub.2 NH.sub.2), optionally substituted mono- or dialkylaminosulphonyl, acylated amino (AlkCON(R.sub.7)-- or AlkOCON(R.sub.7)--), where R.sub.7 is equal to hydrogen, alkyl or cycloalkyl, or optionally substituted alkylsulphonylamino (AlkylSO.sub.2 NH--), or alkylsulphonyl-N-alkylamino (ArylSO.sub.2 NAlkyl--), optionally substituted arylsulphonylamino (ArylSO.sub.2 NH--) or arylsulphonyl-N-alkylamino (ArylSO.sub.2 NAlk--) optionally substituted dialkylamino, furthermore R.sub.5 represents optionally substituted alkoxycarbonyl, optionally substituted (het-)aryloxycarbonyl. alkylsulphonyl, alkenylsulphonyl, (het-)arylsulphonyl, or --SO.sub.2 NR.sub.8 R.sub.9, --CONR.sub.8 R.sub.9 or --P(O)(NR.sub.8 R.sub.9).sub.2, where R.sub.8 and R.sub.9 represent H or alkyl which is optionally substituted by one or more radicals,
Polyether antibiotics such as maduramycin, lasalocid, monensin, narasin, salinomycin or synthetic coccidiostats such as


______________________________________ 1(-(4-Amino-2-n-propyl-5-pyrimidinylmethyl)-2- Amprolium picolinium chloride 1(-(4-Amino-2-n-propyl-5-pyrimidinylmethyl)-2- Amprolium + picolinium chloride + sulfaquinoxaline sulfaquinoxaline 1(-(4-Amino-2-n-propyl-5-pyrimidinylmethyl)-2- Amprolium + picolinium chloride + sulfaquinoxaline + ethopabate sulfaquinoxaline + ethopabate 4,4-Dinitrocarbanilide + 2-hydroxy-4,6-dimethyl- Nicarbazin pyrimidine 3,5-Dichloro-2,6-dimethyl-4-pyridinol Clopidol 3,5-Dichloro-2,6-dimethyl-4-pyridinol + methyl Clopidol + 7-benzyloxy-6-butyl-1,4-dihydro-4-oxylquinoline- methylbenzoquate 3-carboxylate Ethyl 6-n-decyloxy-7-ethoxy-4-hydroxyquinoline-3- Decoquinate carboxylate 9-(2-Chloro-6-fluorophenylmethyl)-9H-purin-6- Arprinocid amine (.+-.)-2,6-Dichl

REFERENCES:
patent: 5331003 (1994-07-01), O'Doherty
patent: 5482956 (1996-01-01), Lunkenheimer

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