Parasiticidal compositions comprising benzimidazole derivatives, methods and uses thereof

Patent metadata

Field	Value
Publication number	US-9359305-B2
Application number	US-201514627595-A
Country	US
Kind code	B2
Filing date	Feb 20, 2015
Priority date	Apr 20, 2012
Publication date	Jun 7, 2016
Grant date	Jun 7, 2016

Abstract

The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.

First claim

What is claimed is:

1. A compound of the formula:

wherein:
R 10 is H;
R 11 is (C 2 -C 6 )-alkyl, (C 2 -C 5 )-alkenyl, or (C 2 -C 5 )-alkynyl, (C 1 -C 6 )-alkoxy, tetralin ether, aryl, aryl ether, sulfonylaryl, sulfoxyaryl, thioaryl, or (C 3 -C 6 )-cycloalkyl, or;
wherein the last six substituents may be unsubstituted or substituted with one or more of (C 1 -C 6 )-alkyl, halogen, (C 1 -C 3 )-haloalkyl, or (C 1 -C 3 )-haloalkoxy;
R 12 is H or halogen;
R 13 is H.

2. A compound according to claim 1 wherein aryl is naphthyl, biphenyl or phenyl.

3. A compound according to claim 1 wherein R 11 is phenoxy substituted with one or more halogens.

4. A compound according to claim 1 that is 6-chloro-5-(2,3-dichlorophenoxy)-2-trifluoromethylthiobenzimidazole.

5. A compound according to claim 1 that is 6-chloro-5-(4-chlorophenyl)-2-trifluoromethylthiobenzimidazole.

6. A compound according to claim 1 that is 6-chloro-5-(3-chlorophenyl)-2-trifluoromethylthiobenzimidazole.

7. A compound according to claim 1 that is 6-chloro-5-(2-butyl)-cyclopropyl-2-trifluoromethylthiobenzimidazole.

8. A composition for treating helminth infestation comprising an anthelmintically effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier.

9. A composition for treating helminth infestation according to claim 8 wherein the composition of formula (I) is combined with an additional active agent.

10. A composition for treating helminth infestation according to claim 9 wherein the active agent is a macrocyclic lactone.

11. A composition for treating helminth infestation according to claim 10 wherein the macrocyclic lactone is selected from the group consisting of abamectin, dimadectin, doramectin, emamectin, eprinomectin, ivermectin, latidectin, lepimectin, selamectin and ML-1,694,554.

12. A composition for treating helminth infestation according to claim 9 wherein the composition of formula (I) is combined with verapamil.

13. A method for treating helminth infestation comprising the step of administering an anthelmintically effective amount of the compound of claim 1 to an animal in need thereof.

14. A method according to claim 13 in which the step of administering an anthelmintically effective amount of the compound to an animal in need thereof comprises an animal in which the helminths are trematodes.

15. A method according to claim 14 in which the step of administering an anthelmintically effective amount of the compound to an animal in need thereof comprises an animal in which the helminths are Fasciola hepatica.

Assignees

• Merial Ltd
• Merial Inc

Inventors

• Meng Charles Q

Classifications

• A61P33/00

  Antiparasitic agents · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P33/14

  Ectoparasiticides, e.g. scabicides · CPC title

• A61P33/10

  Anthelmintics · CPC title

• A61P33/12

  Schistosomicides · CPC title