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Generated: April 23, 2018

DrugPatentWatch Database Preview

Details for Patent: 5,278,175

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Title: Triazole antifungal agents
Abstract:The invention provide antifungal compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ; R.sup.1 is C.sub.1 -C.sub.4 alkyl; R.sup.2 is H or C.sub.1 -C.sub.4 alkyl; X is CH or N; and Y is F or Cl.
Inventor(s): Ray; Stephen J. (Groton, CT), Richardson; Kenneth (Groton, CT)
Assignee: Pfizer Inc. (New York, NY)
Filing Date:Oct 05, 1992
Application Number:07/956,569
Claims:1. A compound of the formula: ##STR48## or a pharmaceutically acceptable salt thereof, wherein R is phenyl substituted 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;

R.sup.1 is C.sub.1 -C.sub.4 alkyl;

R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;

X is CH; and

Y is F or Cl.

2. A compound of claim 1, wherein R is phenyl substituted by 1 or 2 substituents each independently selected from fluoro and chloro.

3. A compound of claim 2, wherein R is 2-fluorophenyl, 2,4-difluorophenyl, 2-chlorophenyl or 2,4-dichlorophenyl.

4. A compound of claim 3, wherein R.sup.1 is methyl.

5. A compound of claim 4, wherein R.sup.2 is hydrogen or methyl.

6. The compound of claim 5, wherein R.sup.2 is hydrogen, R is 2,4-difluorophenyl, and Y is fluoro.

7. The compound of claim 5, of the formula ##STR49## wherein R.sup.2 is hydrogen, R is 2,4-difluorophenyl, and Y is fluoro.

8. A method of treating a fungal infection in a mammal which comprises administering to said mammal an antifungal effective amount of a compound of the formula ##STR50## or a pharmaceutically acceptable salt thereof, wherein R is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;

R.sup.1 is C.sub.1 -C.sub.4 alkyl;

R.sup.2 is H or C.sub.1 -C.sub.4 alkyl; X is C; and Y is F or Cl.

9. A method of claim 8, wherein R is phenyl substituted by 1 or 2 substituents each independently selected from fluoro and chloro.

10. A method of claim 9, wherein R is 2-fluorophenyl, 2,4-difluorophenyl, 2-chlorophenyl or 2,4-dichlorophenyl.

11. A method of claim 10, wherein R.sup.1 is methyl.

12. A method of claim 11, wherein R.sup.2 is hydrogen or methyl.

13. A method of claim 12, wherein R.sup.2 is hydrogen, R is 2,4-difluorophenyl, X is CH and Y is fluoro.

14. A method of claim 12, wherein the compound has the formula ##STR51## wherein R is 2,4-difluorophenyl, X is CH and Y is fluoro.

15. A method of claim 14, wherein the fungal infection is caused by the Aspergillus sp fungi.

16. A method of claim 15, wherein the Aspergillus sp fungi is Aspergillus fumigatus.

17. A pharmaceutical composition in unit dosage form for treating a fungal infection in a human which comprises a fungically effective amount of a compound according to claim 1, together with a pharmaceutically acceptable diluent or carrier.

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