Compounds and compositions for inhibiting estrogen sulfotransfer

Details Compounds and compositions for inhibiting estrogen sulfotransfer Compounds and compositions for inhibiting estrogen sulfotransfer

1983-07-19

1985-01-29

Roberts, Elbert L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

2603974, 2603975, 2603973, 514178, 514177, A61K 3156

Patent

active

044965559

ABSTRACT:
The present invention concerns the novel compounds having fluoro, amino, nitro or hydroxy monosubstituted at the 2- or 4- position on deoxyestrone as well as deoxyestra-17-ol. The compounds are useful as estrogen sulfotransferase inhibitors. Such estrogen sulfotransferase inhibition provides the novel use for treating a female mammal to prevent implantation of a blastocyst. Additionally, the invention concerns the novel synthesis and novel intermediates in the synthesis of the estrogen sulfotransferase inhibiting compound of the present invention.

REFERENCES:
patent: 4340602 (1982-07-01), Brooks
Rozhin et al., J. Biol. Chem., 1977, 252, 7214.
Musliner et al., "The Replacement of Phenolic Hydroxyl Groups by Hydrogen", J. Am. Chem. Soc. 88:18, pp. 4271-4273 (Sep. 20, 1966).
Morrow et al., "The Trienes", J. Med. Chem. 1966, vol. 9, pp. 249-251.
Yagupol'skii et al., "Aryl Trifluoromethanesulfoantes", Institute of Organic Chemistry, Academy of Sciences of the Ukranian SSR. Translation from Zhurnal Organicheskoi Khimii, vol. 7, No. 5, pp. 996-1001, May 1971.
L. R. Subramanian et al., "Perfluoroalkane Sulfonic Esters, Methods of Preparation and Applications in Organic Chemistry", Synthesis, 85-125 (1982).
J. Org. Chem., 1968, 33, pp. 2469-2473.
Tomson, A. J. and Horowitz, J. P. Org. Chem. 24, pp. 2056-2058 (1959).

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