Cardioprotective agents
AssigneeMerrell Pharmaceuticals Inc.
InventorsJ. Martin Grisar, Margaret A. Petty, Frank Bolkenius
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Abstract
This invention relates to certain hydroxy derivatives of 3,4-dihydro-2,5,7,8-tetraalkyl-2H-1-benzopyran-2-carboxylic acids and the lactones thereof, to the processes and intermediates useful for their preparation and to their use as free radical scavengers useful in the treatment of tissue damage implicated with free oxygen radicals.
Claims31
A compound of the formulae ##STR5## their individual stereoisomers and mixtures thereof, or the pharmaceutically acceptable salts thereof wherein
- R is H or C.sub.1-4 alkyl,
- R.sub.1 is C.sub.1-4 alkyl,
- R.sub.2 is H or C(O)R.sub.3,
- R.sub.3 is H or C.sub.1-9 alkyl,
- R.sub.4 is OR or N(R).sub.2,
- R.sub.5 is H, --C(O)R or C.sub.1-4 alkyl, and
- n is zero or one.
The process of making a compound of the formulae ##STR6## their individual stereoisomers and mixtures thereof, or the pharmaceutically acceptable salts thereof wherein
- R is H or C.sub.1-4 alkyl,
- R.sub.1 is C.sub.1-4 alkyl,
- R.sub.2 is H or C(O)R.sub.3,
- R.sub.3 is H or C.sub.1-9 alkyl,
- R.sub.4 is OR or N(R).sub.2,
- R.sub.5 is H, --C(O)R or C.sub.1-4 alkyl, and
- n is zero or one.
- by dihydroxylation of the following compound ##STR7## with an appropriate hydroxylating agent to give either the cisor trans compound having the formula ##STR8## or when the 4-hydroxy group is cis to the acid function, that is when R.sub.4 represents OH, to produce the lactone having the formula ##STR9##
Dependencies are inferred from the claim text.