2.beta.,19-ethylene bridged steroids as aromatase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

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514178, 514182, 552510, A61K 31565, C07J 5300

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active

051662019

ABSTRACT:
The present invention is directed to a group of androstane compounds which contain an ethylene radical bridging the 2- and 19-positions. These compounds are useful as aromatase inhibitors and they are prepared by the cyclization of a 19-[2-(4-toluenesulfonyloxy)ethyl]androst-4-ene-3,17-dione using a strong base.

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Eggleston et al. Chemical Abstracts, vol. 109, 1988 Abstract 139666j.
Johnston et al., Endocrinology 115(2), 1984 pp. 776-785.
Lan-Hargest et al. Tetrahedron Letters, 28 (49) pp. 6117-6120, 1987.
Greway et al., Biochemistry International, 20, 591 (1990).
Burkhart et al., Steroids 45:357, 1985.

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