DIARYL COMPOUNDS AS NON-STEROIDAL INHIBITORS OF 17-BETA HYDROXYSTEROID DEHYDROGENASE AND/OR STEROID SULPHATASE FOR THE TREATMENT OF OESTROGEN-RELATED DISEASES SUCH AS HORMONE DEPENDENT BREAST CANCER

摘要

There is provided a compound of Formula (I): wherein R₃, R₄, R₅, R₆, R₇, R₉, and R₁₀, are independently selected from -H, -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO₂), and halogens; wherein ring A is optionally further substituted wherein X is a bond or a linker group wherein (A) (i) R₉ is selected from alkyl and halogen groups; and (ii) R10 is selected from -OH, oxyhydrocarbyl and -OSO₂NR₁R₂; wherein R₁ and R₂ are independently selected from H and hydrocarbyl or (B) at least one of R₃, R₄, R₅, R₆ and R₇ is the group -C(=0)-CR₁₁ R₁₂-R₈ wherein R₈ is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group (vii) =N-O-alkyl or =N-O-H group (viii) branched alkenyl (ix) alkyl-alcohol group or alkenyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is -CH₂- or - CH₂CH₂-, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO, or together with another of R₃, R₄, R₅, R₆ and R₇ the enol tautomer thereof wherein R₁₁ and R₁₂ are independently selected from H and hydrocarbyl; or (C) at least one of R₃, R₄, R₅, R₆ and R₇ together with another of R₃, R₄, R₅, R₆ and R₇ forms a ring containing -C(=O)-; or (D) at least one of R₃, R₄, R₅, R₆ and R₇ is selected from alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, and heteroaryl groups or (E) at least one of R₃, R₄, R₅, R₆ and R₇ is selected from -CN, -C(R₁₃)=N-O-alkyl group, - C(R₁₄)=N-O-H group, optionally substituted pyrazole, optionally substituted thiazole, optionally substituted oxazole, optionally substituted isoxazole, optionally substituted pyridine, and optionally substituted pyrimidine, or together with another of R₃, R₄, R₅, R₆ and R₇ forms a nitrogen containing ring; wherein R₁₃ and R₁₄ are independently selected from H and hydrocarbyl.