5-}2-HYDROXY-3-`1-(3-TRIFLUOROMETHYLPHENYL)-CYCLOPROPYL!-PROPIONYLAMINO}-PHTALIDE AND RELATED COMPOUNDS WITH PROGESTERONE RECEPTOR MODULATING A CTIVITY FOR USE IN FERTILITY CONTROL AND HORMONE REPLACEMENT THERAPY

摘要

The present invention relates to non-steroidal progestins of the generalformula (I) wherein R1 and R2 are independently of each other -H or -F, R3 is -CH3 or -CF3, and Ar is (a) or (b), or a pharmaceutically acceptable derivativeor analogue thereof. These progestins are suitable for selectively modulatingprogesterone receptor mediated effects in different target tissues,particularly in uterine tissue versus breast tissue. Therefore, the progestinsof the present invention, optionally in combination with estrogens, may beused for contraception (in particular in estrogen-free oral contraceptives),hormone replacement therapy and the treatment of gynecological disorders. Thepresent invention furthermore relates to methods for selectively modulatingprogesterone receptor mediated effects in different target tissues or organs.