abstract |
IT REFERS TO COMPOUNDS OF FORMULA (I), WHERE: R1 AND R2 ARE INDEPENDENTLY H, F, Cl, NITRILE, ETOXY, CARBOXYL, C1-C4 ALKYL, HYDROXYL, AMONG OTHERS; R3 AND R4 ARE H OR R3 IS HYDROXYL, F, METHOXY OR ETHOXY AND R4 IS H OR R3 IS H AND R4 IS HYDROXYL, F, METOXY OR ETHOXY; R5 AND R6 ARE H OR R5 IS F, HYDROXYL, METHOXY OR ETHOXY AND R6 IS H OR R5 IS H AND R6 IS F; R7 IS H, C1-C4 ALKYL, C3-C6 CYCLOALKYL, CYCLOPROPYLMETHYL, AMONG OTHERS; R8 IS -CRaRb-COOH, WHERE Ra AND Rb ARE INDEPENDENTLY H, METHYL OR ETHYL OR Ra AND Rb ARE TOGETHER -CH2-NH-CH2-, -CH2-N (CH3) -, AMONG OTHERS. THE PREFERRED COMPOUNDS ARE: ACID 1 - [({[17- (5-FLUOROPYRIDIN-3-IL) ESTRA-1,3,5 (10), 16-TETRAEN-3-IL] CARBONYL} AMINO) METHYL] CYCLOPROPAN-1 -CARBOXYL; N - {[17- (5-FLUOROPYRIDIN-3-IL) ESTRA-1,3,5 (10), 16-TETRAEN-3-IL] CARBONYL} -L-PROLIN; AMONG OTHERS. SAID COMPOUNDS ARE INHIBITORS OF THE ENZYME ALDO-CETORREDUCTASE 1C3 (AKR1C3) BEING USEFUL FOR THE TREATMENT OF ENDOMETRIOSIS, ACNE, ALOPECIA, BREAST CANCER, RENAL CANCER |