Estrogen receptor targeted antagonists

• Main Authors: WANG GUANGDI, KANG BORUI, MOTAMARE, MADHUSUDANAN
• Format: Patent
• Language: Chinese; English
• Published: 31.10.2023
• 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 by non-covalently or covalently binding ER ligand binding domains, or both as antagonists and ER protein degradation agents, and methods of synthesis thereof. In addition, the present disclosure teaches the use of such compounds in the treatment of proliferative diseases, including cancer, in particular 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。