Selective aromatase inhibiting 4(5)-imidazoles

摘要

PCT No. PCT/FI92/00184 Sec. 371 Date May 9, 1994 Sec. 102(e) Date May 9, 1994 PCT Filed Jun. 12, 1992 PCT Pub. No. WO92/22537 PCT Pub. Date Dec. 23, 1992 <IMAGE> (Ia) <IMAGE> (Ib) <IMAGE> (II) New 4(5)-imidazole derivatives of formula (Ia) and (Ib) wherein one of R1 and R2 is CN and the other one is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F or halogen; R' is H or (II) where R3 is H, CH3 or halogen; R4 is H and R5 is H or R4 and R5 together form a bond, n is 1 or 2 and y is 0 to 2, their stereoisomers and their non-toxic pharmaceutically acceptable acid addition salts exhibit selective aromatase inhibiting properties, compared with their desmolase inhibiting properties. The compounds of the invention are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer or benign prostatic hyperplasia (BPH).