ESTRADIOL-16 alpha -CARBOXYLIC ACID ESTERS AS LOCALLY ACTIVE ESTROGENS

Title:

ESTRADIOL-16 alpha -CARBOXYLIC ACID ESTERS AS LOCALLY ACTIVE ESTROGENS

Document Type and Number:

WIPO Patent Application WO2002058634

Kind Code:

A3

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 16 alpha -carboxylic acid substituted steroids sand their esters 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: I Where R is H, a C1 to C5 alkyl, vinyl, CF3, CH2CH2F, CH2CHF2 or CH2CF3; and m is from 0-2, or a pharmaceutically acceptable salt thereof. Preferably, R is methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, pentyl, neo-pentyl, vinyl, CF3, CH2CH2F, CH2CHF2 or CH2CF <3? and m is 0. More preferbly, R is methyl, ethyl, CH>2222< or CH>22< and m is 0.

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Inventors:

HOCHBERG RICHARD B

Application Number:

PCT/US2002/001898

Publication Date:

February 27, 2003

Filing Date:

January 23, 2002

Export Citation:

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Assignee:

UNIV YALE (US)

International Classes:

A61K31/56; A61K31/59; C07J1/00; C07J5/00; C07J7/00; (IPC1-7): A61K31/56; A61K31/59; C07J1/00

Foreign References:

US3190895A	1965-06-22
US3045012A	1962-07-17
US3287356A	1966-11-22
DE864257C	1953-01-22

Other References:

POIRIER, D. ET AL.: "Inhibitors of type II, 17beta-hydroxysteroid dehydrogenase", MOLECULAR AND CELLULAR ENDOCRINOLOGY, vol. 171, no. 1-2, 29 January 2001 (2001-01-29), pages 119 - 128, XP001058494

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