Orally active derivatives of 1,3,5(10)-estratriene

Details Orally active derivatives of 1,3,5(10)-estratriene Orally active derivatives of 1,3,5(10)-estratriene

1993-09-17

1996-09-10

Kestler, Kimberly J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

552618, 552626, A61K 3156, C07J 100

Patent

active

055546030

ABSTRACT:
The invention presents 17.beta.-nitro and 11.beta., 17.beta.-dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.

REFERENCES:
patent: Re34136 (1992-12-01), Crowe
patent: 3980681 (1976-09-01), Sykes
patent: 4859370 (1989-08-01), Crowe
Sykes, P. J., et al. (1971) "Oxidation of Ring A-Aromatic Steroids To 9,11.beta.-Diol 11-Nitrates Wtih Ceric Ammonium Nitrate", Tetrahedron Letters, 37:3393-3396.
Pellicciari, Roberto, et al. (1987) "An Efficient Procedure For The Regiospecific Preparation of D-Homo-Steroid Derivatives" Steroids 49:433-441.
Peters, Richard H., et al. (1989) "11.beta.-Nitrate Estrane Analogues: Potent Estrogens" J. Med. Chem. 32:2306-2310.
Hasrat Ali, et al. (1993) "7.alpha.-Methyl- and 11.beta.-Ethoxy-Substitution of [.sup.125 I]-16.alpha.-Iodoestradiol: Effect on Estrogen Receptor-Mediated Target Tissue Uptake" J. Med. Chem. 36:264-271.
Chemical Abstracts, vol. 83, No. 1, Jul. 7, 1975, Columbus, Ohio, USA, Abstract No. 1164g, I. Kun, "Estrogenic Action of Some New Nitrate Esters of Estradiol", p. 18, col. 2; see abstract & Rev.Med., vol. 20, No. 2, 1974, ROM pp. 190-193.

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