专利号:US-2025171493-A1 优先权日:2022-03-05 标题 :Processes for synthesis of withanolides and withaferins and analogs thereof 发明人:LOPCHUK JUSTIN MATTHEW 权利人:H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure provides processes for the synthesis of withanolides such as Withanolide A and Withanolide D.
专利号:WO-2024105420-A3 优先权日:2022-11-15 标 题 :Cyclic designer scaffolds for the covalent targeting of proteins via michael addition 发明人:REMÉNYI ATTILA; SOÓS Tibor; PÓTI Ã?DÃ?M LEVENTE; BÃ?LINT DÃ?NIEL; ALEXA ANITA; SOK PÉTER DÃ?NIEL; TORDA LILI; VARGA SZILÃ?RD; OZSVÃ?TH KRISTÓF; ALBERT KRISZTIÃ?N; PALKÓ ROBERTA; EMBER ORSOLYA; KÃ?LLAINÉ SZARKA ESZTER; IMRE TÃ?MEA 权利人:HUN REN TERMESZETTUDOMANYI KUTATOKOEZPONT 摘要:Many biologically active natural products contain electrophilic Michael acceptor fragments. For example, curcumin and 4-hydroxyderricin contain an acyclic α,β-unsaturated ketone that alkylates cysteines. Other antitumor or anti-inflammatory herbal compounds such as Withaferin A or zerumbone contain cyclic α,β-unsaturated ketones and react with nucleophilic residues of proteins. These observations contributed to a paradigm shift in drug design and development in the last two decades: various drugs with covalent warhead have been developed and approved. Despite the apparent importance and success of covalent warheads in current drug design and developments, the applied warheads display a rather limited structural variance and complexity which automatically limits the attainable chemical space. Furthermore, to minimize possible side-reactions during the synthesis of drugs, the applied warheads are added appendages in the late-stage of the synthetic route, thus a warhead scaffold that can be synthetically easily varied using orthogonal chemistry and used as a tunable covalent warhead is still missing. Such a structurally more complex scaffold would be much more like the warheads of the natural products and is expected to be more selective in targeting nucleophiles found on the proteins. Moreover, owing to a larger contact surface, it might be more suitable for targeting shallow protein surfaces involved in protein-protein interactions.
专利号:US-2014274978-A1 优先权日:2013-03-15 标题 :Phytosterol spirostane and spirostene derivatives having a wide variety of utilities in humans and other animals 发明人:FASCIOLA ANDRE ARMEL 权利人:FASCIOLA ANDRE ARMEL 摘要:The present invention utilizes phytosterol, phytoecdysteroid, sapogenin, triterpene, terpene, spirostane, spirostene and androstene derivative compounds to provide a wide variety of utilities to humans and other animals. The compounds and methods provide numerous and wide-ranging benefits including biochemical and constructive metabolic benefits including increases in protein synthesis and synthesis efficiency, ergogenic, adaptogenic, cosmetic and medicinal skin agents and veterinary utilities. The compounds provide agents that increase physical endurance and work output, act as a general tonic for increasing health and vigor, increase sleep time and sleep efficiency and act as rejuvenating agents to reverse the effects of fatigue and stress. Novel utilities for pet, farm, zoo and companion animals are also provided.
专利号:US-12187735-B2 优先权日:2018-09-17 标 题:Matter of composition, synthesis, formulation and application of FL118 platform positions 7 and 9-derived analogues for treatment of human disease 发明人:LING XIANG; LI QINGYONG; LI FENGZHI 权利人:CANGET BIOTEKPHARMA LLC 摘要:Described herein, are the chemical synthesis, matter of compositions, formulation, function, methods and uses of the FL118 platform Positions 7 and/or 9-derived analogues for treating cancer or other human diseases. Compounds derived from chemical modifications of the FL118 platform are employed alone or in combination with other anti-cancer agents to preclude, eliminate or reverse cancer phenotypes. This invention intends to realize unique personalized cancer treatment (personalized precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogues, which target multiple cellular human disease-relevant proteins and their signaling pathways.
专利号:US-2025092058-A1 优先权日:2018-09-17 标 题 :Matter of composition, synthesis, formulation and application of fl 118 platform positions 7 and 9-derived analogues for treatment of human disease 发明人:LING XIANG; LI QINGYONG; LI FENGZHI 权利人:CANGET BIOTEKPHARMA LLC 摘要:Described herein, are the chemical synthesis, compounds, methods and uses of the fluoroaryl-substituted derivatives at the FL118 position 7, which target multiple cellular human disease-relevant proteins and their signaling pathways.
专利号:WO-2011011384-A9 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates
1: Nie HJ, Fu YJ, Long S, Wang JY, Zhao WS, Zhai LH, Yang YL, Tan MJ, Hu H, Chen XH. Chemoproteomics reveals proteome-wide covalent and non-covalent targets of withaferin A. Acta Pharmacol Sin. 2025 Feb 3. doi: 10.1038/s41401-024-01468-5. Epub ahead of print. 132:108844. doi: 10.1016/j.reprotox.2025.108844. Epub ahead of print. 26(2):493. doi: 10.3390/ijms26020493. 5: Sharma KB, Subramani C, Ganesh K, Sharma A, Basu B, Balyan S, Sharma G, Ka S, Deb A, Srivastava M, Chugh S, Sehrawat S, Bharadwaj K, Rout A, Sahoo PK, Saurav S, Motiani RK, Singh R, Jain D, Asthana S, Wadhwa R, Vrati S. Withaferin A inhibits Chikungunya virus nsP2 protease and shows antiviral activity in the cell culture and mouse model of virus infection. PLoS Pathog. 2024 Dec 30;20(12):e1012816. doi: 10.1371/journal.ppat.1012816.
合成参考文献
参考文献:10.1007/s12156-010-0071-y 摘要:Patel SA, Dave MA, Murthy RG, Helmy KY, Rameshwar P. Metastatic breast cancer cells in the bone marrow microenvironment: novel insights into oncoprotection. Oncology Reviews. 2010 Dec 29;5(2):93–102. doi: 10.1007/s12156-010-0071-y.