Anagrelide Hemiformate置于水体系中,用 乙醇 作为反应溶剂,化学反应 3.0H,以99%的收率获得产物氯喳味唑酮 参考文献: Process For Making Anagrelide[fr] Procédé De Préparation D'Anagrélide 标题: Process For Making Anagrelide[fr] Procédé De Préparation D'Anagrélide 摘要:该发明涉及一种制备和纯化药用活性化合物阿格雷利特(分子式为(1))的方法.该方法基于将阿格雷利特或其酸盐转化为阿格雷利特的甲酸盐,特别是阿格雷利特半甲酸盐.
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-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-8828984-B2 优先权日:2012-11-19 标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection 发明人:CHE CHI MING; ZOU TAOTAO 权利人:UNIV HONG KONG; UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.
1: Buxhofer-Ausch V, Steurer M, Sormann S, Schloegl E, Schimetta W, Gisslinger B, Schalling M, Krauth MT, Thiele J, Ruckser R, Gastl G, Gisslinger H. Impact of white blood cells on thrombotic risk in patients with optimised platelet count in essential thrombocythemia. Eur J Haematol. 2018 Mar 30. doi: 10.1111/ejh.13070. [Epub ahead of print] pii: bcr-2017-220723. doi: 10.1136/bcr-2017-220723. doi: 10.1097/MD.0000000000008735. Review. 4: Birgegård G, Besses C, Griesshammer M, Gugliotta L, Harrison CN, Hamdani M, Wu J, Achenbach H, Kiladjian JJ. Treatment of essential thrombocythemia in Europe: a prospective long-term observational study of 3649 high-risk patients in the Evaluation of Anagrelide Efficacy and Long-term Safety study. Haematologica. 2018 Jan;103(1):51-60. doi: 10.3324/haematol.2017.174672. Epub 2017 Oct 27. 5: Speirs C, Williams JJL, Riches K, Salt IP, Palmer TM. Linking energy sensing to suppression of JAK-STAT signalling: A potential route for repurposing AMPK activators? Pharmacol Res. 2018 Feb;128:88-100. doi: 10.1016/j.phrs.2017.10.001. Epub 2017 Oct 13. Review. doi: 10.1016/j.jogoh.2017.08.005. Epub 2017 Sep 1. doi: 10.1038/leu.2017.230. Epub 2017 Jul 24.
合成参考文献
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355