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Generated: September 22, 2017

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Title: Method for treatment of equine protozoal myeloencephalitis with thiazolides
Abstract:A method for treatment or prevention of equine protozoal myeloencephalitis, a condition for which there is presently no effective treatment. The method comprises administering to the infected horse an amount of one or more 2-benzamido-5-nitro-thiazole compounds sufficient to eradicate Sarcocystis spp.
Inventor(s): Rossignol; Jean-Fran.cedilla.ois (Clearwater, FL), Ayers; Marc S. (Tampa, FL)
Assignee: Romark Laboratories, L.C. (Tampa, FL)
Application Number:09/007,653
Patent Claims: 1. A process for treating a horse afflicted with, or at risk of being afflicted with, equine protozoal myeloencephalitis which comprises administering to the infected animal an amount of one or more 2-benzamido-5-nitro-thiazole compounds of the formula (I): ##STR5## wherein at least one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represents an acyloxy group or an hydroxy group and the remaining symbols represent hydrogen or one of the remaining symbols represents an alkoxy group or an hydroxy group, such amount being sufficient to eradicate Sarcocystis spp.

2. A process as in claim 1, wherein said acyloxy group is selected from the group consisting of an acetoxy group and a propionyloxy group.

3. A process as in claim 1, wherein only one of the symbols R.sub.1, R.sub.2, R.sub.3, R4 and R.sub.5 represents an acyloxy group.

4. A process as in claim 1, wherein two of the symbols R.sub.1, R.sub.2, R.sub.3, R4 and R.sub.5 represent an acyloxy group.

5. A process as in claim 1, wherein only one of the symbols R.sub.1, R.sub.2, R.sub.3, R4 and R.sub.5 represents an hydroxy group.

6. A process as in claim 1, wherein two of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represents an hydroxy group.

7. A process as in claim 1, wherein the dosage of said 2-benzamido-5-nitro-thiazole compounds averages from 25 to 200 mg/kg of body weight during the period of treatment.

8. A process as in claim 1, wherein said process is carried out over a period of from 5 days to 3 months.

9. A process as in claim 1, wherein said process is carried out over a period of from 7 days to 30 days.

10. The process of claim 1, wherein the 2-benzamido-5-nitro-thiazole compound is 2-(2'-acetoxy)-benzamido-5-nitro-thiazole.

11. The process of claim 1, wherein the 2-benzamido-5-nitro-thiazole compound is 2-(2'-propionyloxy)-benzamido-5-nitro-thiazole.

12. The process of claim 1, wherein the 2-benzamido-5-nitro-thiazole compound is 2-(2'-hydroxy)-benzamido-5-nitro-thiazole.

13. A method as in claim 1, wherein said 2-benzamido-5-nitro-thiazole compound is in the form of particles with a mean particle size of between 10 and 200 .mu.m.

14. A method as in claim 13, wherein said 2-benzamido-5-nitro-thiazole compound is in the form of particles with a mean particle size of between 20 and 50 .mu.m.

15. A method as in claim 13, wherein less than 10% of said solid particles have a particle size larger than 100 .mu.m.

16. A method as in claim 13, wherein said 2-benzamido-5-nitro-thiazole compound is administered in the form of a pharmaceutical composition comprising said 2-benzamido-5-nitro-thiazole compound, and wherein said pharmaceutical composition further contains at least one pharmaceutically acceptable acid.

17. A method as in claim 16, wherein said pharmaceutically acceptable acid is selected from the group consisting of citric acid, glutamic acid, succinic acid, ethanesulfonic acid, acetic acid, tartric acid, ascorbic acid, methanesulfonic acid, fumaric acid, adipic acid, malic acid and mixtures thereof.

18. A method as in claim 16, wherein the ratio of the weight of pharmaceutically acceptable acid/the weight of said solid particles is between 0.01 and 0.5.

19. A method as in claim 16, wherein said particles of active agent include a granulating agent selected from the group consisting of polyvinylpyrrolidone, water, alcohol, sucrose hydroxyl cellulose and mixture thereof.

20. A method as in claim 1, wherein said 2-benzamido-5-nitro-thiazole agent is a mixture of 2-(2'-acetolyloxy)-benzamido-5-nitro-thiazole and 2-(2'-hydroxy)-benzamido-5-nitro-thiazole.

21. A process for treating a horse afflicted with a protozoal or helminth infection, said process comprising administering to the infected horse an eradicating effective amount of one or more 2-benzamido-5-nitro-thiazole compounds of the formula (I): ##STR6## wherein at least one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represents an acyloxy group or a hydroxy group and the remaining symbols represent hydrogen or one of the remaining symbols represents an alkoxy group.

22. A process as in claim 21, wherein said acyloxy group is selected from the group consisting of an acetoxy group and a propionyloxy group.

23. A process as in claim 21, wherein the dosage of said 2-benzamido-5-nitro-thiazole compounds averages from 25 to 200 mg/kg body weight during the period of treatment.

24. A process as in claim 21, wherein said process is carried out over a period of from 5 days to 3 months.

25. A process as in claim 21, wherein said process is carried out over a period of from 7 days to 30 days.

26. A process as in claim 21, wherein the 2-benzamido-5-nitro-thiazole compound is 2-(2'-acetoxy)-benzamido-5-nitro-thiazole.

27. A process as in claim 21, wherein the 2-benzamido-5-nitro-thiazole compound is 2-(2'-propionyloxy)-benzamido-5-nitro-thiazole.

28. A process as in claim 21, wherein the 2-benzamido-5-nitro-thiazole compound is 2-(2'-hydroxy)-benzamido-5-nitro-thiazole.

29. A process for treating a horse infected with Sarcocystis spp., which comprises administering to the infected animal an amount of one or more 2-benzamido-5-nitro-thiazole compounds of the formula (I): ##STR7## wherein at least one of the symbols R.sub.1, R.sub.2, R.sub.3, R4 and R.sub.5 represents an acyloxy group or an hydroxy group and the remaining symbols represent hydrogen or one of the remaining symbols represents an alkoxy group or an hydroxy group, such amount being sufficient to eradicate Sarcocystis spp.
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