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-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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-5962515-A 优先权日:1997-05-29 标题 :Process for isolation and synthesis of 1-(3,4 methylenedioxy-phenyl)-1E-tetradecene and its analogues and their activities against tumors and infections 发明人:UPADHYAY SHAKTI N; VISHWAKARMA RAM A; GHOSAL SABARI; SHUKLA SUPRIYA; BOSE CHANDA; KAMRA ANITA 权利人:NAT INST IMMUNOLOGY 摘要:Process for isolation of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene from Piper longum. Processes for synthesis of 1-(3,4-methylenedioxy-phenyl)-1E-tetradecene; its stereoisomers and analogues are disclosed. The compounds isolated and synthesized according to this invention have immunomodulatory properties and can be used to treat tumors and infections.
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
1: Vaezi Z, Amini A. Cocaine- and Levamisole-Induced Vasculitis (CLIV). Cureus. 2025 Sep 19;17(9):e92701. doi: 10.7759/cureus.92701. 2: Amaral PEM, Beane SO, Albarouki A, Tan MJ, Schoenberger MJ, Yao Y, Liu L, Uljon SN, Zhu Y, Hall DC Jr, Qiu Y. Rising illicit drug Adulterants: Xylazine and levamisole. Clin Biochem. 2025 Jun;137:110912. doi: 10.1016/j.clinbiochem.2025.110912. Epub 2025 Mar 11. 13(17):5116. doi: 10.3390/jcm13175116. 4: Gholami MH, Rassouli A, Mirzaei S, Hashemi F. The potential immunomodulatory effect of levamisole in humans and farm animals. J Adv Vet Anim Res. 2023 Dec 31;10(4):620-629. doi: 10.5455/javar.2023.j717.
合成参考文献
参考文献:10.1309/ajcpopqnbp5thkp1 摘要:Czuchlewski DR, Brackney M, Ewers C, Manna J, Fekrazad MH, Martinez A, Nolte KB, Hjelle B, Rabinowitz I, Curtis BR, McFarland JG, Baumbach J, Foucar K. Clinicopathologic features of agranulocytosis in the setting of levamisole-tainted cocaine. Am J Clin Pathol. 2010 Mar;133(3):466–72. doi: 10.1309/ajcpopqnbp5thkp1. 参考文献:10.1007/s00436-010-1781-6 摘要:Paraud C, Pors I, Rehby L, Chartier C. Absence of ivermectin resistance in a survey on dairy goat nematodes in France. Parasitol Res. 2010 May;106(6):1475–9. doi: 10.1007/s00436-010-1781-6. 参考文献:10.2174/092986710790712174 摘要:Ulinski T, Aoun B. Pediatric idiopathic nephrotic syndrome: treatment strategies in steroid dependent and steroid resistant forms. Curr Med Chem. 2010;17(9):847–53. doi: 10.2174/092986710790712174. 参考文献:10.1186/1472-6750-10-12 摘要:Zhong L, Zhang W, Zer C, Ge K, Gao X, Kernstine KH. Protein microarray: sensitive and effective immunodetection for drug residues. BMC Biotechnol. 2010 Feb 16;10():12. 参考文献:10.3389/fphys.2011.00033 摘要:Alzamora R, O'Mahony F, Ko WH, Yip TW, Carter D, Irnaten M, Harvey BJ. Berberine Reduces cAMP-Induced Chloride Secretion in T84 Human Colonic Carcinoma Cells through Inhibition of Basolateral KCNQ1 Channels. Front Physiol. 2011;2():33.