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 Method for inhibiting uterine fibroid disease with 1,1,2-triphenylbut-1-ene derivatives

Details
Inventors: Fontana, Steven A.;
Assignee: Eli Lilly and Company (Indianapolis, IN)
Primary Examiner: Jordan; Kimberly
Assistant Examiner:
Attorney, Agent or Firm: Sales; James J., Boone; David E.

The present invention provides novel methods of inhibiting uterine fibroid disease and endometriosis in women comprising administering to a woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is a benzyl group, or a pharmaceutically acceptable salt thereof.

DETAILED DESCRIPTION OF THE INVENTION The present invention concerns methods for inhibiting uterine fibroid disease and endometriosis in women.
The term "inhibit" is defined to include its generally accepted meaning which includes prophylactically treating a subject from incurring one or more of these disease states, holding in check the symptoms of such a disease state, and/or treating such symptoms.
Thus, the present methods include both medical therapeutic and/or prophylactic treatment, as appropriate.
The methods of this invention are practiced by administering to a woman in need of treatment an effective amount of a compound of formula I ##STR3## wherein R.
sup.
1 and R.
sup.
2 may be the same or different provided that, when R.
sup.
1 and R.
sup.
2 are the same, each is a methyl or ethyl group, and, when R.
sup.
1 and R.
sup.
2 are different, one of them is a methyl or ethyl group and the other is a benzyl group; or a pharmaceutically acceptable salt thereof.
Compounds of formula I are known in the art and essentially are prepared via the methods described in U.
S.
Pat.
No.
5,047,431 which is herein incorporated by reference.
A preferred formula I compound is that in which R.
sup.
1 and R.
sup.
2 each are methyl.
This preferred compound is known as droloxifene which previously has been described as an antiestrogenic agent and is useful for the treatment of hormone-dependent mammary tumors (U.
S.
Pat.
No.
5,047,431) and for the relief of bone diseases caused by the deficiency of estrogen or the like (U.
S.
Pat.
No.
5,254,594).
Furthermore, droloxifene is known to have less of a uterotrophic effect than other antiestrogenic compounds such as tamoxifen.
Although the free-base form of formula I compounds can be used in the methods of the present invention, it is preferred to prepare and use a pharmaceutically acceptable salt form.
Thus, the compounds used in the methods of this invention form pharmaceutically acceptable acid and base addition salts with a wide variety of inorganic and, preferrably, organic acids and bases, and include the physiologically acceptable salts which are often used in pharmaceutical chemistry



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