专利号:US-8293930-B1 优先权日:2004-06-25 标题 :One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:NAIDU RAGINA; CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction of protecting the C-7 and C-10 positions and attaching a side chain at the C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and taxane intermediates.
专利号:US-7893283-B2 优先权日:2004-06-04 标题:Semi-synthesis of taxane intermediates and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediates.
专利号:WO-2008032104-A1 优先权日:2006-09-15 标题:One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:WALKER ROSS THOMSON; NAIDU RAGINA 权利人:CHATHAM BIOTEC LTD; WALKER ROSS THOMSON; NAIDU RAGINA 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction, of protecting the C-10 and attaching a side chain at C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and intermediates used therein.
专利号:US-7838694-B2 优先权日:2004-04-23 标题 :Semi-synthesis and isolation of taxane intermediates from a mixture of taxanes 发明人:NAIDU RAGINA; FOO SAMUEL SIANG KIANG 权利人:CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis and isolation of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis and isolation of 10-deacetylbaccatin III, the semi-synthesis of a mixture of 10-deacetylbaccatin III and baccatin III, and protected derivatives thereof, from a mixture of taxanes.
专利号:US-7906661-B2 优先权日:2004-06-29 标 题 :Semi-synthetic conversion of paclitaxel to docetaxel 发明人:NAIDU RAGINA; FOO SAMUEL SIANG KIANG; XUE BAOYU; FAN BO 权利人:CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2′, C-7 and C-10 positions and introducing a t-Boc group at the nitrogen of the amide group at the C-3′ position in paclitaxel and subsequently conversion to docetaxel, and derivatives used therein.
专利号:US-6869973-B2 优先权日:2000-06-22 标题:Nitrosated and nitrosylated taxanes, compositions and methods of use 发明人:GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; RICHARDSON STEWART K; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The present invention also provides novel compositions comprising at least one taxane and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.
1: Lataste H, Senilh V, Wright M, Guénard D, Potier P. Relationships between the structures of taxol and baccatine III derivatives and their in vitro action on the disassembly of mammalian brain and Physarum amoebal microtubules. Proc Natl Acad Sci U S A. 1984 Jul;81(13):4090-4. doi: 10.1073/pnas.81.13.4090.
合成参考文献
参考文献:10.1038/s42003-019-0744-4 摘要:Yang L, Chen T, Wang F, Li L, Yu W, Si Y, Chen J, Liu W, Zhu P, Gong W. Structures of β-glycosidase LXYL-P1-2 reveals the product binding state of GH3 family and a specific pocket for Taxol recognition. Communications Biology. 2020 Jan 10;3(1):22. doi: 10.1038/s42003-019-0744-4.