Vinylogous hydroxamic acids and derivatives thereof as 5-lipoxygenase inhibitors
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorsRonald L. Magolda, Stephen W. Wright
Life of this patent
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Abstract
The present invention relates to vinylogous hydroxamic acids, processes for their manufacture, pharmaceutical preparations containing them, and their use in the treatment of various disorders.
Claims30
A compound having the formula:
- ##STR14## the sterioisomers and pharmaceutically acceptable salts thereof, wherein:
- X is O;
- R.sub.1 is phenyl;
- phenyl optionally substituted with a total of 1 to 3 substituents each of which is independently selected from Br, Cl, F, I, CF.sub.3, C.sub.1 to C.sub.14 alkyl, NO.sub.2, phenyl naphthyl, C.sub.1 to C.sub.14 alkyl;
- or cycloalkyl of 3 to 6 carbon atoms;
- R.sub.3 and R.sub.4 independently represent H, C.sub.1 to C.sub.4 alkyl;
- phenyl;
- phenyl optionally substituted with 1 to 3 substituents each of which is independently selected from Br, Cl, F, I, CF.sub.3, C.sub.1 to C.sub.14 alkyl, NO.sub.2, phenyl, naphthyl, C.sub.1 to C.sub.14 alkyl, cycloalkyl of 3 to 6 carbon atoms;
- R.sub.5 is H, phenyl, benzyl, (C.sub.1 to C.sub.6 alkyl)phenyl, naphthyl, C.sub.1 to C.sub.12 alkyl, or C.sub.3 to C.sub.8 cycloalkyl;
- R.sub.7 is H, or a pharmaceutically acceptable cation;
A compound of the formula ##STR15## and pharmaceutically acceptable salts thereof wherein R.sub.1 is lower alkyl, lower alkoxy, phenyl, 4-O.sub.2 NC.sub.6 H.sub.4, 4-ClC.sub.6 H.sub.4 or Ph C.sub.6 H.sub.4 ;
- R.sub.3 is hydrogen, lower alkyl, phenyl, or 4-FC.sub.6 H.sub.4 ;
- R.sub.4 is hydrogen;
- R.sub.5 is lower alkyl, phenyl, benzyl, n-C.sub.10 H.sub.21, c-C.sub.6 H.sub.11, CH.sub.2 (2-naphthyl), CH(CH.sub.3)(2-naphthyl) or CH.sub.2 C.sub.6 H.sub.4 -4-C.sub.6 H.sub.5 ;
- and
- X is O.
A compound of the formula ##STR16## and pharmaceutically acceptable salts thereof wherein R.sub.1 is 4-chlorophenyl, 4-fluorophenyl, 4-nitrophenyl or 4-(phenyl)phenyl;
- R.sub.3, R.sub.4 and R.sub.7 are each hydrogen;
- and
- R.sub.5 is CH.sub.3 or CH.sub.2 C.sub.6 H.sub.5.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim and a pharmaceutically acceptable carrier.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.