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 general formula (I) wherein R1 and R2 are independently of each other -H or -F, R3 i s - CH3 or -CF3, and Ar is (a) or (b), or a pharmaceutically acceptable derivati ve or analogue thereof. These progestins are suitable for selectively modulatin g progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progesti ns of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. Th e present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs .