Aromatase inhibiting 4(5)-imidazoles

Details Aromatase inhibiting 4(5)-imidazoles Aromatase inhibiting 4(5)-imidazoles

C - Chemistry, Metallurgy

07

D

167/237, 260/314

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

Patent

CA 2013395

Abstract Novel imidazole derivatives of the formula Image (Ia) wherein R1, R2, R'1 and R'2, which can be the same or different, are H, CH3, C2H5, C3H7, OCH3, OH, CH2OH, NO2, NH2, CN, CF3, CHF2, CH2F or halogen; R' is H or Image where R3 is H, CH3 or halogen; R4 is H, R5 is H or OH, R6 is H or OH and R7 is H or R4 and R6 together form a bond or R5 and R7 together form a bond; X and Y, which can be the same or different, are a bond, a straight C1-2-alkyl or the corresponding alkenyl and z is 0 to 2 and Image (Ib) wherein R1, R2, R'1, R'2 and R' are as defined before, R4 is H or OH and R5 is H or R4 and R5 together form a bond and y is 0 to 4, and their non-toxic salts exhibit aromatase and desmolase inhibiting properties. Very selective aromatase inhibiting compounds are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer.

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