Phosphoramidates useful as antitumor agents

Details Phosphoramidates useful as antitumor agents Phosphoramidates useful as antitumor agents

1994-01-21

1995-12-05

McKane, Joseph K.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514 90, 514 91, 514 94, 514 99, 5142315, 5142322, 5142358, 514398, 514426, 514472, 514447, 544 84, 544139, 544146, 544152, 548119, 548413, 549 6, 549218, C07F 902

Patent

active

054729564

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: 4997822 (1991-05-01), Hohorst et al.
patent: 5190929 (1993-03-01), Borch et al.
CA 69(19):76898u Benzyl phosphorodiamidates. Kawakami et al., p. 7180, 1968.
CA 112(21):198797n Phosphoramides useful as antitumor agents. Borch et al., p. 754, 1990.
CA 115(17):183451h Synthesis . . . analogs. Borch et al., p. 945, 1991.
CA 115(19):208082d Nitro . . . cells. Firestone et al., p. 1033, 1991.
84th Annual Meeting of the American Association for Cancer Research, Orlando, Fla., USA, May 19-22, 1993, Proc. Am. Assoc. Cancer Res. Annu. Meet. 34, Mar. 1993, p. 267, Abstract 1987, R. F. Borch et al., "Synthesis and Cytotoxicity of Novel Hypoxia-Selective Phosphoramidates".

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