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 and 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:
##STR1##
Where R is H, a C.sub.1 to C.sub.5 alkyl, vinyl, CF.sub.3, CH.sub.2
CH.sub.2 F, CH.sub.2 CHF.sub.2 or CH.sub.2 CF.sub.3 ; 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, CF.sub.3, CH.sub.2 CH.sub.2 F, CH.sub.2 CHF.sub.2 or
CH.sub.2 CF.sub.3 and m is 0. More preferably, R is methyl, ethyl,
CH.sub.2 CH.sub.2 F, CH.sub.2 CHF.sub.2 or CH.sub.2 CF.sub.3 and m is 0.
La actual invención se relaciona con los análogos del estradiol, que, en su encarnación preferida, acto como localmente estrógenos activos sin la acción systemic significativa. Una serie de esteroides substituidos ácido 16.alpha.-carboxylic y de sus ésteres se presenta que exhiban la actividad biológica excelente para el uso en las composiciones farmacéuticas para el tratamiento del symptomology asociado a menopausia. La actual invención por lo tanto se dirige a los compuestos según la estructura: ## del ## STR1 Donde está H R, un C.sub.1 C.sub.5 al alkyl, vinilo, CF.sub.3, CH.sub.2 CH.sub.2 F, CH.sub.2 CHF.sub.2 o CH.sub.2 CF.sub.3; y m es a partir de la 0-2, o de una sal farmacéutico aceptable de eso. Preferiblemente, R es metilo, etilo, propyl, iso-propyl, butilo, isobutílico, pentyl, neo-pentyl, vinilo, CF.sub.3, CH.sub.2 CH.sub.2 F, CH.sub.2 CHF.sub.2 o CH.sub.2 CF.sub.3 y m es 0. Preferiblemente, R es metilo, etilo, CH.sub.2 CH.sub.2 F, CH.sub.2 CHF.sub.2 o CH.sub.2 CF.sub.3 y m es 0.
