15α-substituted estradiol carboxylic acid esters as...

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

Reexamination Certificate

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C552S629000

Reexamination Certificate

active

07015211

ABSTRACT:
The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15α-estradiol ester compounds is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause. The present invention is therefore directed to compounds according to the structure:where X isR is H, a C1to C5alkyl group, optionally substituted with at least one halogen group, such as CH2CH2F, or other group (e.g., CH2CHF2, CH2CF3or CF3group); andm is from 0–5, preferably from 0–2.

REFERENCES:
Linder et al., “Preparation of Estrone and Estradiol Antigens through Carbon 15 of these Estrogens” Steroids, 1977, vol. 29(2), pp. 161-170.
Linder et al. “Preparation of Estrone and Estradiol Antigens through Carbon 15 of these Estrogens”Steroids. Feb. 1977, vol. 29, No. 2, pp. 161-170.

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