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US 5,346,898 AGranted
Anti-fungal uracil compounds
AssigneeSchering Corporation
InventorsAlan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
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Abstract
Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described. The compounds of formula I are useful as agents in the treatment of fungal infections.
Claims8
A compound of the formula:
- ##STR125## or pharmaceutically acceptable salts thereof, wherein Het is ##STR126## R is H, COOH;
- C.sub.1 -C.sub.12 alkyl;
- CHO;
- CN;
- CH.sub.2 OH;
- or CONH.sub.2 ;
- wherein R.sub.3 is ##STR127## wherein R.sub.8 is ##STR128## R.sub.2 is H;
- OH;
- F;
- C.sub.1 -C.sub.6 alkoxy;
- alkyl;
- SH;
- S-alkyl;
- or SO.sub.2 -alkyl;
- R.sub.4 is H;
- a natural amino acid attached by a peptide bond;
- or a metabolizable group;
- J is OH, H, Br, Cl, or F;
- K is OH, H, Br, Cl, or F;
- X and Y are the same or different and are independently selected from the group consisting of H;
- OH;
- O-C.sub.1 -C.sub.14 alkyl;
- F;
- Cl;
- Br;
- NO.sub.2, and alkyl;
- Z is R.sub.5 NR.sub.6 ;
- ##STR129## wherein Z' is R.sub.5 NR.sub.6, R.sub.5 is (CH.sub.2).sub.11 CH.sub.3 ;
- R.sub.6 is H;
- OH;
- O-benzyl;
- O-aryl;
- O-C.sub.4 -C.sub.14 alkyl;
- C.sub.1 -C.sub.12 alkyl;
- phenyl;
- substituted phenyl;
- or CO-R.sub.7 ;
- and
- R.sub.7 is H, C.sub.1 -C.sub.16 alkyl, aryl or alkylaryl;
- and
- n is an integer from 0 to 16.
38 more elements
Dependencies are inferred from the claim text.