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Claims for Patent: 5,135,943

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Claims for Patent: 5,135,943

Title: 1H-imidazole derivative compounds and pharmaceutical compositions containing the same
Abstract:The 1H-imidazole derivative compound of formula I: ##STR1## and its nontoxic addition salts, particularly the nitrate addition salt, are more effective as antimycotic agents and are unexpectedly safer than the corresponding prior art compounds, especially the compound in which the sulfur atom of the benzothiophene ring of the above compound is replaced by an oxygen atom. Pharmaceutical compositions containing an effective amount of the compound of formula I, e.g. 1 to 5% by weight, in a pharmaceutical carrier are safer, more effective, and, in some cases, more reliable with fewer side effects than currently used antimycotic preparations.
Inventor(s): Foguet; Rafael (Barcelona, ES), Moreno; Marcial (Barcelona, ES), Raga; Manuel (Barcelona, ES), Cuberes; Rosa M. (Barcelona, ES), Castello; Jose M. (Barcelona, ES), Ortiz; Jose A. (Barcelona, ES)
Assignee: Ferrer Internacional S.A. (Barcelona, ES)
Application Number:07/649,764
Patent Claims: 1. A 1H-imidazole derivative compound of formula I: ##STR17## or a nontoxic addition salt thereof.

2. A pharmaceutical composition for treating infections caused by fungi or yeasts in humans and pets, comprising said compound of claim 1 in an effective amount and in combination with a pharmaceutically acceptable carrier.

3. A pharmaceutical composition according to claim 2, in dosage unit form including 100 to 800 mg of said compound.

4. A pharmaceutical composition according to claim 3 for topical application, wherein said compound is present in a concentration from 0.1 to 5 %.

5. A pharmaceutical composition composed of 0.1 to 5 % by weight of said compound of claim 1 in a pharmaceutically acceptable carrier, said compound being present in an amount of from 100 to 800 mg.

6. Method of treating infection caused by fungi or yeast in humans and pet animals, comprising administering an effective amount of the composition according to claim 2.

7. Method of claim 6, wherein said effective amount comprises a daily dose of 100 to 800 mg of said compound.

8. Method of claim 6, wherein said administering comprises oral, injection, rectal, vaginal or topical route administering.

9. Method of treating disease caused by fungi or yeast in crops, comprising applying onto or within the locus of said crops, an effective amount of a compound of claim 1 in combination with carrier means.

10. Method of claim 9, wherein said effective amount comprises 0.1 to 15 kg per hectare of soil.

11. Method of claim 9, wherein said applying comprises watering, atomizing, spraying, dusting or pasting.

12. Compound according to claim 1, wherein said acid addition salt is a nitrate salt.

13. A pharmaceutical composition for treating fungal and yeast infections in humans and pets, comprising 100 to 800 mg of a member selected from the group consisting of a 1H-imidazole derivative compound of formula I: ##STR18## and nontoxic addition salts thereof in a pharmaceutically acceptable carrier.

14. A pharmaceutical composition according to claim 13, wherein said nontoxic addition salts include a mononitrate addition salt of said 1H-imidazole derivative compound.
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