Estrogen receptor targeting antagonists

• Main Authors: MOTTAMAL MADHUSOODANAN, WANG GUANGDI, KANG BORUI
• Format: Patent
• Language: Chinese; English
• Published: 07.09.2021
• 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

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 method 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. 本公开涉及通过非共价或共价结合ER配体结合域而充当拮抗剂，或同时充当拮抗剂和ER蛋白降解剂的化合物，及其合成方法。此外本公开内容教导了这类化合物在治疗增殖性疾病中的用途，所述增殖性疾病包括癌症，特别是乳腺癌并且尤其是ER+乳腺癌。