New selective aromatase inhibiting 4(5)-imidazoles

Details New selective aromatase inhibiting 4(5)-imidazoles New selective aromatase inhibiting 4(5)-imidazoles

C - Chemistry, Metallurgy

07

D

C07D 233/64 (2006.01) A61K 31/415 (2006.01) C07D 233/54 (2006.01)

Patent

CA 2111469

2111469 9222537 PCTABS00018 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).

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