NOVEL SUBSTITUTED 6,7-DIHYDRO-5H-BENZO[7]ANNULENE COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF

• Main Authors: BOISNARD, Sabine, TABART, Michel, NICOLAI, Eric, EL-AHMAD, Youssef, VIVET, Bertrand, FETT, Eykmar, TERRIER, Corinne, HALLEY, Frank
• Format: Patent
• Language: English; French; German
• Published: 11.10.2023
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to a compound of the formula (i) wherein Ar represents a phenyl or a 6-membered heteroaryl group, R1 and R2 represent independently a hydrogen atom or a deuterium atom, R3 represents (1) a -COR4 group, (2) a -BOR5OR6 group, (3) a -X-Z group, (4) a (C1-C6)alkyl group or a (C1-C6)alkenyl group, (5) a -X-S(O)n(R7)p(R8)q group, (6) a halogen atom, a -NH2 group or a -CN group, (7) a -O-R11 group, (8) a -NH-COR9 group, (9) a -C(═NH)NHOH group, (10) a -NH-C(NH)-R9′ group, or (11) a -NHCOCOOR12 group or a -NHCOCONR12′R12″ group, X represents abond, a -NH- group, a -CONH- group or a -CO- group, Z represents a 4 or 5-membered cycloalkyl, a 4 or 5-membered heterocylcloalkyl group, a 4 or 5-membered heteroaryl group or a phenyl group or a pharmaceutically acceptable salt thereof. The present invention further relates to a medicament comprising said compound of formula (I) and to said compound of formula (I) for use as an inhibitor and degrader of estrogen receptors.