Orally active azole derivatives

Details Orally active azole derivatives Orally active azole derivatives

1995-10-13

1997-07-08

Morris, Patricia L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

5483401, C07D24908, C07D23361

Patent

active

056462948

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(.dbd.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(.dbd.O)R.sub.7, --NR.sub.8 R.sub.9, --NHC(.dbd.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(.dbd.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.
T. Tanaka et al., "Triazole Antifungals. V.) Synthesis and Antifungal Activities of Some Amides Related to 3-Acylamino-2-aryl-1-triazolyl-2-butanol." Chem. Pharm. Bull. 40(3) 661-665 (1992).
Chemical Abstract No. 139896j, "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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