YU54292A - NEW 4 (5) -IMIDAZOLES THAT SELECTIVELY INHIBIT AROMATASE - Google Patents

Abstract

NOVI 4(5)-IMIDAZOLI KOJI SELEKTIVNO INHIBIRAJU AROMATAZU, novi derivati 4(5)-imidazola formule u kojoj je R1 CN, R2 je H, CH3, OCH3, NO2, CN, CF3, CHF2, CH2F ili halogen; R' je H ili gde je R3 H, CH3 ili halogen; R4 je H i R5 je H ili R4 i R5 zajedno obrazuju vezu i n je 1 do 2 i u kojoj su R1 i R2 CN ili je R1 ili R2 CN a drugi je H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F ili halogen; R' je H ili gde je R3 H, CH3 ili halogen; R4 je H i R5 je H ili R4 i R5 zajedno obrazuju vezu i y je 0 do 2, njihovi stereo izomeri i njihove netoksične farmaceutski prihvatljive adicione soli kiselina ispoljavaju selektivna svojstva kočenja aromataze, uporedjena sa njihovim svojstvima koja koče dezmolazu. Jedinjenja pronalaska su vredna u lečenju bolesti koje zavise od estrogena, na pr. rak dojki ili benigna hiperplazija prostate (BHP).NEW 4 (5) -IMIDAZOLES SELECTIVELY INHIBITING AROMATASE, new 4 (5) -imidazole derivatives of the formula wherein R1 is CN, R2 is H, CH3, OCH3, NO2, CN, CF3, CHF2, CH2F or halogen; R 'is H or where R 3 is H, CH 3 or halogen; R4 is H and R5 is H or R4 and R5 together form a bond in 1 to 2 and in which R1 and R2 are CN or R1 or R2 are CN and the other is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2 , CH 2 F or halogen; R 'is H or where R 3 is H, CH 3 or halogen; R4 is H and R5 is H or R4 and R5 together form a bond and y is 0 to 2, their stereo isomers and their non-toxic pharmaceutically acceptable acid addition salts exhibit selective aromatase inhibitory properties compared to their desmolase inhibitory properties. The compounds of the invention are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer or benign prostatic hyperplasia (BHP).