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-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-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
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.
专利号:US-10577387-B1 优先权日:2018-08-09 标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment 发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng 权利人:UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Pt(II) 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 Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
1: Mallaredy V, Roy R, Cheng Z, Thej C, Benedict C, Truongcao M, Joladarashi D, Magadum A, Ibetti J, Cimini M, Gonzalez C, Garikipati VNS, Koch WJ, Kishore R. Tipifarnib Reduces Extracellular Vesicles and Protects From Heart Failure. Circ Res. 2024 Jul 5;135(2):280-297. doi: 10.1161/CIRCRESAHA.123.324110. Epub 2024 Jun 7. 2: Norman P. Tipifarnib (Janssen Pharmaceutica). Curr Opin Investig Drugs. 2002 Feb;3(2):313-9. 6(3):313-9. doi: 10.1586/14737140.6.3.313. 39(17):1856-1864. doi: 10.1200/JCO.20.02903. Epub 2021 Mar 22. Erratum in: J Clin Oncol. 2021 Oct 1;39(28):3192. doi: 10.1200/JCO.21.02057. 5: Untch BR, Dos Anjos V, Garcia-Rendueles MER, Knauf JA, Krishnamoorthy GP, Saqcena M, Bhanot UK, Socci ND, Ho AL, Ghossein R, Fagin JA. Tipifarnib Inhibits HRAS-Driven Dedifferentiated Thyroid Cancers. Cancer Res. 2018 Aug 15;78(16):4642-4657. doi: 10.1158/0008-5472.CAN-17-1925. Epub 2018 May 14.
合成参考文献
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