선택적 에스트로겐 수용체 분해제

• Main Authors: PRAJAPATI KAUSHIK DHANJIBHAI, PAL RANJAN KUMAR, PATHAK SANDEEP PANKAJKUMAR, SAMANTA BISWAJIT, ARADHYE JAYRAJ DILIPBHAI, CHITTURI TRINADHA RAO, PANCHAL BHAVESH MOHANBHAI
• Format: Patent
• Language: Korean
• Published: 14.04.2022
• Subjects: 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

선택적 에스트로겐 수용체 분해제(SERD)인, 화합물 3-(3,5-디플루오로페닐)-2-[4-[(E)-3-[3-(플루오로메틸)아제티딘-1-일]프로프-1-에닐]페닐]-4-메틸-2H-크로멘-7-올, 및 이의 S 거울상 이성질체인, (2S)-3-(3,5-디플루오로페닐)-2-[4-[(E)-3-[3-(플루오로메틸)아제티딘-1-일]프로프-1-에닐]페닐]-4-메틸-2H-크로멘-7-올, 또는 이의 약학적으로 허용 가능한 염. 또한, 이들의 제조를 위한 프로세스가 제공된다. 또한, ER-양성 유방암과 같은 에스트로겐 수용체의 조절과 관련된 질환의 치료를 위한 이들 화합물의 용도가 제공된다. A selective estrogen receptor degrader (SERD), a compound 3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol, and its S enantiomer, (2S)-3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol, or pharmaceutically acceptable salts thereof. Also provided are processes for their preparation. Also provided for is the use of these compounds for the treatment of diseases which are related to modulation of estrogen receptors, such as ER-positive breast cancer.