专利号:WO-2023207921-A1 优先权日:2022-04-25 标题 :Taxamairin analogs and methods of preparation and use thereof 发明人:LEE CHI SING; GE SIYUAN; ZHUANG ANDREW-GO 权利人:UNIV HONG KONG BAPTIST UNIV 摘要:Taxamairin analogs useful in the treatment of cancer, pharmaceutical compositions including the same, methods of use thereof, and methods of preparation are provided. An efficient and scalable semi-synthesis of taxamairin compounds and analogs thereof from readily available commercial starting materials is provided. The synthesis involves low cost and relatively non-toxic reagents and is capable of synthesizing taxamairin A and taxamairin B and analogs thereof on multi-gram scale in yields up 12%and 21%, respectively.
专利号:US-11512075-B2 优先权日:2017-06-14 标 题:Synthesis of 20-nor-salvinorin A 发明人:SHENVI RYAN; ROACH JEREMY; SASANO YUSUKE; BOHN LAURA; SCHMID CULLEN 权利人:SCRIPPS RESEARCH INST 摘要:The invention provides 20-nor-salvinorin A, an analog of the kappa-opioid agonist salvinorin A. The 20-nor-salvinorin A is an active kappa-opioid modulator and can be used for treatment of medical conditions wherein modulation of the kappa-opioid receptor is medically indicated, such as pain, pruritis, depression, or inflammation, or conditions implicating perception and consciousness. 20-nor-salvinorin A can be less additive when used in treatment compared to a mu-opioid receptor agonist, and 20-nor-salvinorin A is more stable in vivo than is parent compound salvinorin A. The invention further provides synthetic intermediates and procedures for preparation of 20-nor-salvinorin A.
专利号:US-11767302-B2 优先权日:2020-10-01 标题 :Reagents and methods for tetrazine synthesis 发明人:FOX JOSEPH M; LAMBERT WILLIAM; FANG YINZHI; AM ENDE CHRISTOPHER WILLIAM; MAHAPATRA SUBHAM; XIE YIXIN; WANG CHUANQI 权利人:UNIV DELAWARE 摘要:Disclosed herein are mono- and di-substituted tetrazines and methods of their preparation and converting an oxetanyl ester to a thio-substituted tetrazine, which is then converted to a mono-substituted tetrazine, a di-substituted tetrazine, or a vinylether disubstituted tetrazine.
专利号:US-8338451-B2 优先权日:2008-03-21 标 题 :Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof 发明人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO 权利人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO; SANOFI SA 摘要:Compounds of formula (I): n nwherein R, R 1 , R 2 , R 3 , R 4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
专利号:US-8221719-B2 优先权日:2007-09-05 标 题:Luminescent lanthanide (III) chelates, chelating agents and conjugates derived thereof 发明人:PEURALAHTI JARI; HOVINEN JARI; KETOLA JANNE; JAAKKOLA LASSI; MUKKALA VELI-MATTI; LIITTI PAEIVI 权利人:PEURALAHTI JARI; HOVINEN JARI; KETOLA JANNE; JAAKKOLA LASSI; MUKKALA VELI-MATTI; LIITTI PAEIVI; WALLAC OY 摘要:This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid supports conjugated with said chelates, chelating agents or labeled biomolecules. Especially the invention relates to novel chelating agents useful in solid phase synthesis of oligonucleotides or oligopeptides and the oligonucleotides and oligopeptides so obtained.
专利号:US-2020131162-A1 优先权日:2017-06-14 标题:Synthesis of 20-nor-salvinorin a
摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 351. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 268. 摘要:Wang, K.; Wang, J., Science of Synthesis, (2022) , 15. 摘要:Sloane, S. E.; Behlow, K. T.; Mills, M. D.; Clark, J. R., Science of Synthesis Knowledge Updates, (2022) 2, 404. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 210.