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US 5,225,437 AGranted
1,2,4-trioxane compounds having antimalarial activity
AssigneeThe Johns Hopkins University
InventorsGary Posner, Chang H. Oh
Life of this patent
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Abstract
Novel 1,2,4-trioxanes which possess anti-malarial activity.
Claims9
An anti-malarial 1,2,4-trioxane of the formula:
- ##STR30## and the enantiomers thereof, wherein:
- R.sup.1 is lower alkoxy, aryloxy or aralkoxy;
- R.sup.2 is lower alkyl, hydroxy substituted-lower alkyl or ester or ether derivatives of such hydroxy substituted-lower alkyl;
- R.sup.3 is --(CH.sub.2).sub.m Q where Q is halogen or --OR.sup.5 where
- R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl or heteroaralkyl, or
- R.sup.5 is ##STR31## where Y is C, S or P,
- Z is O or S,
- R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, lower alkoxy, aryloxy, aryl, aralkyl, mono- or di-lower alkylamino or mono- or di-arylamino;
- n is 1 or 2;
- y is 1 or 2;
- and
- m is 1, 2, 3 or 4;
- and
- R.sup.4 is hydrogen or one or two lower alkyl.
11 more elements
Dependencies are inferred from the claim text.