Estrogenic compounds, process for their production and pharmaceutical uses thereof

摘要

The presently disclosed and claimed inventive concept(s) provides new estrogenic compounds of the general formula;
and pharmaceutical compositions containing them. The compounds of the presently disclosed and claimed inventive concept(s) are useful, for example, in hormone replacement therapies (HRT/ERT), and as contraceptives, and estrogenic hormone therapies. Also provided is a process for synthesizing the compounds of the presently disclosed and claimed inventive concept(s).

主权项

1. A method for hormone replacement therapy in a subject, comprising administering to said subject an effective amount of a compound of Formula I, or a pharmaceutically acceptable salt, ester or solvate thereof: where R1 is H, halogen or CH3; R2 is H, halogen or CH3; R4 is H, halogen or CH3; R5 is H, halogen CF3, C1-C5 alkyl, CH2OH, CH2OAc, CH2CH2OH, CH2CH2OAc, CH2-aryl, CH2-heteroaryl, CH═CH2, CH2CH2SCH3, CH2CH2SC2H5, CH2CH2SCH2Ar, CH2CH2SCH2-heteroaryl, OH, OCH3, OC2H5, OCH2Ar, OCH2-heteroaryl, OAc, SCH3, SC2H5, SCH2Ar, SCH2-heteroaryl, SOCH3, SOC2H5, SOCH2Ar, SOCH2-heteroaryl, SO2CH3, SO2C2H5, SO2CH2Ar, SO2CH2-heteroaryl, CN, CHO, COCH3, COC2H5, CO2H, CO2CH3, CO2C2H5, CO2CH2Ar, CO2CH2-heteroaryl, CONH2CON(CH3)2, CON(CH2)4, CON(CH2)5, or NO2; R9 is absent, H or OH; and R17 is H or C2H.