5-(2-HIDROXY-3-/1-(3-TRIFLUOROMETHYLPHENYL)-CYCLOPROPYL/-PROPIONYLAMINO)-PHTALIDE AND RELATED COMPOUNDS WITH PROGESTERONE RECEPTOR MODULATING ACTIVITY FOR USE INE FERTILITY CONTROL AND HORMONE REPLACEMENT THERAPY

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 is -CH3 or -CF3, and Ar is (a) or (b), or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins 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. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs. Sadašnji pronalazak se odnosi na ne-steroidne progestine opšte formule (I) pri čemu su R1 i R2 nezavisno jedan od drugog -H ili -F, R3 je -CH3 ili -CF3, i Ar je (a) ili (b), ili njihov farmaceutski prihvatljiv derivat ili analog. Ovi progestini su pogodni za selektivno moduliranje sa progesteron receptorom posredovanih dejstva u različitim ciljanim tkivima, posebno u materičnom tkivu spram tikiva dojke. Prema tome, progestini sadašnjeg pronalaska, opciono u kombinaciji sa estrogenima, mogu biti upotrebljeni za kontracepciju (posebno u od estrogena oslobođenim kontraceptivnim sredstvima), terapiji zamene hormona i lečenju ginekoloških poremećaja. Sadašnji pronalazak se dalje odnosi na postupke za selektivno moduliranje sa progesteron receptorom posredovanih dejstava u različitim ciljanim tkivima ili organima.