Substituted 6,7-dihydro-5H-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof

US10570090B2 · kind B2 · utility

Assignee

• Sanofi · FR

Inventors

• Monsif BOUABOULA · Paris, FR
• Maurice Brollo · Paris, FR
• Victor CERTAL · Paris, FR
• Youssef El-Ahmad · Créteil, FR
• Bruno Filoche-Romme · Paris, FR
• Frank Halley · Romford, GB
• Gary MCCORT · Paris, FR
• Laurent Schio · Paris, FR
• Michel Tabart · Paris, FR
• Corinne Terrier · Livry-Gargan, FR
• Fabienne Thompson · Paris, FR

Key dates

• Filing date: Jun 5, 2017
• Grant date: Feb 25, 2020
• Expiry date: Jun 5, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F7/0812
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.