ESTROGEN RECEPTOR TARGETING ANTAGONISTS

The present disclosure relates to compounds that act as antagonists via binding to the ER ligand binding domain non-covalently or covalently, or act as both antagonists and ER protein degraders, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds...

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Bibliographic Details
Main Authors MOTTAMAL, Madhusoodanan, KANG, Borui, WANG, Guangdi
Format Patent
LanguageEnglish
French
Published 19.03.2020
Subjects
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
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
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Summary:The present disclosure relates to compounds that act as antagonists via binding to the ER ligand binding domain non-covalently or covalently, or act as both antagonists and ER protein degraders, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds in a treatment for proliferative diseases, including cancer, particularly breast cancer, and especially ER+ breast cancer. La présente invention concerne des composés qui agissent en tant qu'antagonistes par liaison au domaine de liaison de ligand ER de manière non covalente ou covalente, ou agissent en tant qu'antagonistes et agents de dégradation de protéine ER, et la synthèse de ceux-ci. En outre, la présente invention concerne l'utilisation de tels composés dans un traitement de maladies prolifératives, notamment le cancer, en particulier le cancer du sein, et spécialement le cancer du sein ER+.
Bibliography:Application Number: WO2019US50573