1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors

US8022224B2 · kind B2 · utility

Assignee

• Sterix Limited · GB

Inventors

• Lok Wai Lawrence Woo · Slough, GB
• Toby Jackson · Slough, GB
• Atul Purohit · Slough, GB
• Michael John Reed · London, GB
• Barry Victor Lloyd Potter · Slough, GB

Key dates

• Filing date: Jun 13, 2008
• Grant date: Sep 20, 2011
• Expiry date: Dec 14, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/10
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

There is provided a compound of Formula Iwherein R3, R4, R5, R6 and R7 are independently selected from H and —Y—R8; wherein each R8 is independently selected from —OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2), H-bond acceptors, and halogens; wherein at least one of R3, R4, R5, R6 and R7 is —Y—R8 wherein R8 is selected from substituted and unsubstituted heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further substituted; wherein R9 is selected from H, —OH and —OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is —Y—R8; OR (b) R9 is —OSO2NR1R2 or —OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is —Y—R8. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.