专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:WO-2025067239-A1 优先权日:2023-09-26 标 题 :Kinesin kif18a inhibitor, and application thereof 发明人:XIAO YISONG; GU XIAOHUI; LAI KUNMIN; WANG MINGHUA; HU MIN 权利人:SHANGHAI APEIRON THERAPEUTICS COMPANY LTD 摘要:A KIF18 inhibitor, and a synthesis method therefor, capable of adjusting a KIF18A protein, so as to affect cell cycle and cell proliferation processes, in order to treat cancers and cancer-related diseases. Also provided are a pharmaceutical composition including the KIF18 inhibitor compound, and a method for treating KIF18A activity-related conditions.
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 376. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22.