Aromatase inhibiting 4(5)-imidazoles

C - Chemistry – Metallurgy – 07 – D

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

Patent

CA 1329616

ABSTRACT OF THE DISCLOSURE Novel imidazole derivatives and processes for their preparation are provided herein. Such novel imidazole derivatives have the Formula Image wherein R1, R2, R'1 and R'2, which can be the same or different, are H, CH3, C2H5, OCH3, OH, CH2OH, NH2 or halogen; R' is H or Image . where R3 is H, CH3 or halogen; R4 is H, R5 is H or OH, and R6 is H or OH; or R4 and R5 together form a bond; or R4 and R6 together form a bond and X and Y, which can be the same or different, are a bond, a straight C1-2-alkyl or the corres- ponding alkenyl. Novel pharmaceutical compositions comprising at least one of such compounds or their salts are also provided, The compounds and their non-toxic salts exhibit valuable pharma- cological properties, especially aromatase-inhibiting effects, and are useful in the treatment of estrogen dependent diseases, e.g. breast cancer. Antimycotic and antifungal properties have also been found.

578192

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