Derivatives of triazole, having antifungal activity

 

The invention relates to the field of organic chemistry and relates to compounds of formula (I) and their pharmaceutically acceptable salts and difficult ether derivativeswhere Ar represents a phenyl group which may be optionally substituted from 1 to 3 substituents selected from the group consisting of halogen atoms and triptorelin groups with antifungal activity. Compounds have high antifungal activity. 5 C. and 10 C.p. f-crystals, 2 ill., 3 table.

Description text in facsimile form (see graphic part).

Claims

1. The compound of formula (I) or its pharmaceutically acceptable salt or ester derivativewhere AG represents a phenyl group which may be optionally substituted from 1 to 3 substituents selected from the group consisting of halogen atoms or triptorelin groups.

2. The compound of formula (I) under item 1 or its pharmaceutically acceptable salt or ester derivative, where AG represents 2,4-differenly group or 2-florfenicol group.

3. The compound of formula (I) under item 1 or its pharmaceutically PR is of the formula (I) under item 1 or its pharmaceutically acceptable salt or ester derivative, where the aforementioned compound of formula (I) is a compound of formula (Ia)where AG represents a phenyl group which may be optionally substituted from 1 to 3 substituents selected from the group consisting of halogen atoms or triptorelin groups.

5. Connection on p. 1, representing the (2R, 3R)-3-[[TRANS-2-[(1E, 3E)-4-(4-cyano-2-forfinal)-1,3-butadiene-1-yl] -1,3-dioxane-5-yl] thio] -2-(2,4-differenl)-1-(1H-1,2,4-triazole-1-yl)-2-butanol or its pharmaceutically acceptable salt or ester derived.

6. Connection on p. 1, representing the (2R, 3R)-3-[[TRANS-2-[(1E, 3E)-4-(4-cyano-2-forfinal)-1,3-butadiene-1-yl] -1,3-dioxane-5-yl] thio] -2-(2,4-differenl)-1-(1H-1,2,4-triazole-1-yl)-2-butanol in crystalline form.

7. (2R, 3R)-3-[[TRANS-2-[(1E, 3E)-4-(4-cyano-2-forfinal)-1,3-butadiene-1-yl] -1,3-dioxane-5-yl] thio]-2-(2,4-differenl)-1-(1H-1,2,4-triazole-1-yl)-2-butanol in crystalline form on p. 6, having main peaks at distances in the lattice 3,14, 3,39, 3,71, 3,75, 4,21, 4,88, 5,28, 5,42, 5,89, 5,95, 6,79, 6,86, 8,03 anddetermined by x-ray diffraction powder method using Kradiation of copper.

8. (2R, 3R)-3-[[TRANS-2-[(1E, 3E)-4-(4-cyano-2-forfinal)-1,3-butadiene-1-yl]main peaks at distances in the lattice 3,62, 3,96, 4,54, 4,59, 4,79, 4,91, 5,32, 5,48, 6,18, 7,99 anddetermined by x-ray diffraction powder method using Kradiation of copper.

9. Pharmaceutical composition comprising an effective amount of the pharmacologically active compound together with its pharmaceutically acceptable carrier or diluent, where the aforementioned pharmacologically active compound is a compound of formula (I) or its pharmaceutically acceptable salt or complex ether derivative according to any one of paragraphs.1-8.

10. The compound of formula (I) or its pharmaceutically acceptable salt or ester derivative according to any one of paragraphs.1-8, for use as pharmaceuticals.

11. Agent containing the compound of formula (I) or its pharmaceutically acceptable salt or ester derivative according to any one of paragraphs.1-8, for use in the prevention or treatment of fungal infections.

12. The compound of formula (I) or its pharmaceutically acceptable salt or ester derivative according to any one of paragraphs.1-8, as an active ingredient of a medicinal product for the prevention or treatment of fungal infections.

13. A method of preventing or treating the fungus effective number of connections, possessing antifungal activity, where the specified compounds having antifungal activity, is a compound of formula (I) or its pharmaceutically acceptable salt or ester derivative according to any one of paragraphs.1-8.

14. The compound of formula (II) or its acetaline derived15. Connection on p. 14, having the formula (IIA)

Priority points and features:
PP.1, 2 and 4 have the second priority date of the application;
PP.3, 5-8, 14 and 15 have the date of the first priority application;
that part of the PP. 9-13, which depends on PP.1, 2 and 4 has the second priority date of the application;
that part of the PP.9-13, which depends on PP.3, 5-8 has the date of the first priority application.

 

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< / BR>
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