专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-2006246505-A1 优先权日:2003-09-02 标题:Modulation of the synthesis of insulin 发明人:WALTHER REINHARD 权利人:WALTHER REINHARD 摘要:The invention particularly relates to the use of substances, which modulate the activity of the proteins casein kinase II (CK II) and 14-3-3 epsilon and/or of the PcG protein EED or which influence the binding of the proteins casein kinase II (CK II) and 14-3-3 epsilon, of the PcG protein EED and/or of a fragment thereof with the protein pancreatic duodenal homeobox-1 (PDX-1) that plays a decisive roll in the glucose-induced biosynthesis of insulin, for influencing the synthesis of insulin or the provision of insulin.
专利号:EP-1546732-B1 优先权日:2002-09-03 标 题:Modulation of the synthesis of insulin 发明人:WALTHER REINHARD 权利人:UNIV ERNST MORITZ ARNDT 摘要:The invention particularly relates to the use of substances, which modulate the activity of the proteins casein kinase II (CK II) and 14-3-3 epsilon and/or of the PcG protein EED or which influence the binding of the proteins casein kinase II (CK II) and 14-3-3 epsilon, of the PcG protein EED and/or of a fragment thereof with the protein pancreatic duodenal homeobox-1 (PDX-1) that plays a decisive roll in the glucose-induced biosynthesis of insulin, for influencing the synthesis of insulin or the provision of insulin.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-10905769-B2 优先权日:2015-11-13 标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI 权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
1: Pérez-Castro MÁ, Hernández-Rasco F, Alonso-Bellido IM, Letrán-Sánchez MS, Pérez-Villegas EM, Vitallé J, Real LM, Ruiz-Mateos E, Venero JL, Tabares L, Carrión ÁM, Armengol JÁ, Bachiller S, Ruiz R. HERC1 E3 Ubiquitin Ligase Is Necessary for Autophagy Processes and for the Maintenance and Homeostasis of Vesicles in Motor Nerve Terminals, but Not for Proteasomal Activity. Int J Mol Sci. 2025 Jan 18;26(2):793. doi: 10.3390/ijms26020793. 2: Zhang W, Sunami K, Liu S, Triana D, Tachrim ZP, Kikuchi R, Taniguchi T, Monde K, Takehara T, Zhou DY, Suzuki T, Hashidoko Y, Hashimoto M, Murai Y. Scalable preparation of furanosteroidal viridin, β-viridin and viridiol from Trichoderma virens. Sci Rep. 2025 Jan 24;15(1):3110. doi: 10.1038/s41598-025-87070-z. 3: Meng NN, Xia LZ, Gong YQ, Lu PR. Autophagy serves as a protective effect against inflammatory injury of oxidative stress in ARPE-19 cell. Int J Ophthalmol. 2025 Jan 18;18(1):28-38. doi: 10.18240/ijo.2025.01.04.
合成参考文献
参考文献:10.4049/jimmunol.0903170 摘要:Antignano F, Ibaraki M, Kim C, Ruschmann J, Zhang A, Helgason CD, Krystal G. SHIP is required for dendritic cell maturation. J Immunol. 2010 Mar 15;184(6):2805–13. doi: 10.4049/jimmunol.0903170. 参考文献:10.1152/ajpheart.01330.2008 摘要:Tsubokawa T, Yagi K, Nakanishi C, Zuka M, Nohara A, Ino H, Fujino N, Konno T, Kawashiri M, Ishibashi-Ueda H, Nagaya N, Yamagishi M. Impact of anti-apoptotic and anti-oxidative effects of bone marrow mesenchymal stem cells with transient overexpression of heme oxygenase-1 on myocardial ischemia. American Journal of Physiology-Heart and Circulatory Physiology. 2010 May;298(5):H1320–9. doi: 10.1152/ajpheart.01330.2008. 参考文献:10.1093/eurjhf/hfq011 摘要:Shyu KG, Wang BW, Chen WJ, Kuan P, Hung CR. Mechanism of the inhibitory effect of atorvastatin on endoglin expression induced by transforming growth factor-beta1 in cultured cardiac fibroblasts. Eur J Heart Fail. 2010 Mar;12(3):219–26. doi: 10.1093/eurjhf/hfq011. 参考文献:10.4196/kjpp.2008.12.2.37 摘要:Kong PJ, Byun JS, Lim SY, Lee JJ, Hong SJ, Kwon KJ, Kim SS. Melatonin Induces Akt Phosphorylation through Melatonin Receptor- and PI3K-Dependent Pathways in Primary Astrocytes. Korean J Physiol Pharmacol. 2008 Apr;12(2):37–41. 参考文献:10.18632/aging.100045 摘要:Currais A, Hortobágyi T, Soriano S. The neuronal cell cycle as a mechanism of pathogenesis in Alzheimer's disease. Aging (Albany NY). 2009 Apr 28;1(4):363–71.