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US 4,731,369 AGranted
Amides and esters of 2-(N-(hydroxypiperidinoalkyl) and (hydroxypyrrolidinoalkyl)-aminosulfonyl)-6-nitrobenzoic acids useful as adjuncts to radiation therapy
AssigneeMerck & Co., Inc.
InventorsEdward L. Engelhardt, Walfred S. Saari
Life of this patent
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Abstract
Amides and esters of 2-[N-(hydroxypiperidinoalkyl) and (hydroxypyrrolidinoalkyl) aminosulfonyl]-6-nitrobenzoic acids are disclosed to have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds, pharmaceutical compositions including such compounds and methods of treating patients in need of therapeutic radiation with effective amounts of such compounds.
Claims7
A compound of the formula:
- ##STR6## wherein:
- R.sub.1 is hydroxy(loweralkoxy), lower alkoxy, allyloxy, amino, alkylamino, di(loweralkyl)amino, (hydroxyalkyl)amino, di(hydroxy-alkyl)amino or allylamino;
- R.sub.2 is hydrogen, lower alkyl from 1-4 carbon atoms, hydroxyloweralkyl, allyl;
- n is 2 or 3;
- m is 0, 1 or 2;
- p is 1 or 2 and pharmaceutically acceptable salts thereof.
3 more elements
Dependencies are inferred from the claim text.