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US 5,472,956 AGranted
Phosphoramidates useful as antitumor agents
AssigneeResearch Corporation Technologies, Inc.
InventorsRichard F. Borch, James P. Schmidt
Life of this patent
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Abstract
Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.
Claims12
A method of treating a solid tumor in a mammalian host comprising administering to said host a pharmaceutical unit dosage form comprising an amount of a compound of the formula:
- ##STR17## wherein R.sup.1 and R.sup.2 are individually (C.sub.2 -C.sub.6)alkyl, optionally substituted with halogen, (C.sub.1 -C.sub.4)alkoxy, (C.sub.6 -C.sub.12)aryloxy, cyano, (C.sub.1 -C.sub.4)alkoxycarbonyl, (C.sub.1 -C.sub.4)alkylsulfonyl, (C.sub.6 -C.sub.12)arylsulfonyl, (C.sub.1 -C.sub.4)perfluoroalkylsulfonyl, (C.sub.1 -C.sub.C.sub.4)alkylsulfinyl, (C.sub.6 -C.sub.12)arylsulfinyl, or R.sup.1 and R.sup.2 taken together with N are a morpholino ring;
- R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are individually H;
- and Ar is a sulfur- or oxygen-containing heteroaromatic ring;
- in combination with a pharmaceutically acceptable vehicle, which amount is effective to inhibit the growth of said solid tumor, wherein said tumor is a lung adenocarcinoma, a breast tumor, an ovarian tumor, a malignant melanoma or a colon tumor.
1 more element
Dependencies are inferred from the claim text.