2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations

Abstract

The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:

1 . A method of treating vasomotor symptoms in a menopausal woman in need thereof which comprises administering to said woman an effective amount of a composition comprising 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol and conjugated estrogens. 
     
     
         2 . The method of  claim 1 , wherein the composition comprises conjugated estrogens in the amount of about 0.3 mg to about 2.5 mg and the 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol or a pharmaceutically acceptable salt thereof is present in an amount from about 1 mg to about 150 mg. 
     
     
         3 . The method of  claim 2 , wherein the composition comprises about 0.45 mg of conjugated estrogens and about 20 mg of 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol or a pharmaceutically acceptable salt thereof. 
     
     
         4 . A method of preventing postmenopausal osteoporosis in a woman with a uterus which comprises administering to said woman an effective amount of a composition comprising conjugated estrogens in the amount of about 0.3 mg to about 2.5 mg and the 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol or a pharmaceutically acceptable salt thereof is present in an amount from about 1 mg to about 150 mg. 
     
     
         5 . The method of  claim 4 , wherein the composition comprises about 0.45 mg of conjugated estrogens and about 20 mg of 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol or a pharmaceutically acceptable salt thereof.