Phosphoramidates useful as antitumor agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514426, 514447, 514472, 548119, 548413, 549 6, 549218, A61K 31415, A61K 3134, A61K 3138, A61K 3140

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active

053067274

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.

REFERENCES:
patent: 4908356 (1990-03-01), Borch et al.
patent: 5190929 (1993-03-01), Borch et al.
Richard F. Broch et al., "Synthesis of novel hypoxia-selective phosphoramidates", Abstract from 1993 ACCR meeting (published Mar. 1993).
CA 115(11):105438v Synthesis . . . 3'-azido-3'-deoxythymidine (AZT). Jones et al., p. 17, 1991.
CA 115(17):183451h Synthesis . . . analogs. Borch et al., p. 945, 1991.
CA 115(19):208082d Nitro . . . cells. Firestone et al., p. 1033, 1991.
CA 117(11);103588m Comparison . . . in vitro. Kinchington et al., p. 24, 1992.
CA 117(15):142890y Comparison . . . in vitro. Kinchington et al., p. 21, 1992.

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