Orally active azole derivatives

Details Orally active azole derivatives Orally active azole derivatives

1994-03-15

1995-12-26

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142362, 544132, 544139, A01N 4384, A61K 31535, C07D41306

Patent

active

054788269

ABSTRACT:
The present invention relates to new orally active azole derivatives with antifungal activity of formula I ##STR1## wherein: X is CH or N; Ar represents phenyl substituted with halogen and/or trifluoromethyl; Z is --C(=O)-- or --SO.sub.2 --; R.sub.1 is CN, CO.sub.2 H, CO.sub.2 R.sub.7, CONR.sub.8 R.sub.9 or CH.sub.2 Y and then R.sub.3 is hydrogen, or R.sub.1 together with R.sub.3 forms a ring of formula I' ##STR2## wherein B is O, hydroxy or hydrogen; R.sub.4 is C.sub.1-4 alkyl; R.sub.5, R.sub.6, R.sub.8 and R.sub.9 are hydrogen or C.sub.1-4 alkyl; Y is --OH, --OR.sub.7, --OC(=O)R.sub.7, --NR.sub.8 R.sub.9, --NHC(=O)OR.sub.7 ; R.sub.7 is C.sub.1 -C.sub.4 -alkyl, phenyl-C.sub.1 -C.sub.4 -alkyl or optionally substituted phenyl; when Z is --C(=O)--, R.sub.2 is optionally susbtituted phenyl, or naphtyl; when Z is --SO.sub.2 --, R.sub.2 is C.sub.1-4 alkyl, phenyl-C.sub.1-4 -alkyl or optionally susbtituted phenyl.

REFERENCES:
patent: 5149707 (1992-09-01), Bartroli et al.
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Chemical Abstract No. 139186j, "Synthesis and antifungal activity of triazolylpropanol derivatives." 119(13), 875 (1993).
Konosu, Toshiyuki, Tajima, Yawara, Takeda, Noriko, Miyaoka, Takeo, Kasahara, Mayumi, Yasuda, Hiroshi and Oida, Sadao: Triazole Antifungals. II. Synthesis and Antifungal Activities of 3-Acyl-4-methyloxazolidine Derivatives. Chem. Pharm. Bull. 38(9) 2476-2486 (1990).
Evans, David A., Britton, Thomas C., Ellman, Jon A.: Contrasteric Carboximide Hydrolysis With Lithium Hydroperoxide. Tetrahedron Letters, vol. 28, No. 49, pp. 6141-6144, (1987).
Konosu, Toshiyuki, Tajima, Yawara, Takeda, Noriko, Miyaoka, Takeo, Kasahara, Mayumi, Yasuda, Hiroshi, Oida, Sadao: Triazole Antifungals. IV. Synthesis and Antifungal Activities of 3-Acylamino-2-aryl-2-butanol Derivatives. Chem. Pharm. Bull. 39(10):2581-2589 (1991).

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