Novel selective aromatase inhibiting compounds

Details Novel selective aromatase inhibiting compounds Novel selective aromatase inhibiting compounds

C - Chemistry, Metallurgy

07

D

C07D 233/61 (2006.01) A61K 31/41 (2006.01) A61K 31/505 (2006.01) C07D 231/12 (2006.01) C07D 239/26 (2006.01) C07D 249/02 (2006.01) C07D 257/04 (2006.01) C07D 261/08 (2006.01) C07D 263/32 (2006.01) C07D 275/02 (2006.01) C07D 277/30 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2150904

New compounds of formula (I) wherein R1 is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F or halogen, R2 is a heterocyclyl radical selected from 1-imidazolyl, triazolyl, pyrazolyl, pyrimidinyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl, R3 is H or OH, R4 is H, R5 is H or OH; or R4 is H and R3 and R5 combined form a bond; or R3 is H and R4 and R5 combined form ? O; R6 is methylene, ethylene, -CHOH-, -CH2-CHOH-, -CHOH-CH2-, -CH=CH- or -C(=O-)-; or R4 is H and R5 and R6 combined is ?CH- or =CH-CH2-; stereoisomers thereof and non-toxic pharmaceutically acceptable acid addition salts thereof exhibit selective aromase 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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