2-甲基-1H-吲哚-3-乙醇置于2-碘酰基苯甲酸体系中,用 甲醇,二氯甲烷,二甲基亚砜 作为反应溶剂,化学反应 18.08H,反应生成 帕比司他 参考文献: Process For The Preparation Of Panobinostat[fr] Procédé De Préparation De Panobinostat 标题: Process For The Preparation Of Panobinostat[fr] Procédé De Préparation De Panobinostat 摘要:本发明涉及一种用于制备帕诺比诺斯他及其中间体的新工艺.
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-11649285-B2 优先权日:2016-08-03 标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy 发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN 权利人:BIO TECHNE CORP 摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
专利号:US-2022118094-A1 优先权日:2019-02-21 标题:Synthesis of biomimetic cell wall structure 发明人:WANG YONG; SHI PENG 权利人:PENN STATE RES FOUND 摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
1: Zheng B, Cui D, Deng B, Long W, Ye G, Zhang S, Zeng J. Form-deprivation myopia promotes sclera M2-type macrophages polarization in mice. Biochem Biophys Res Commun. 2024 Aug 6;737:150490. doi: 10.1016/j.bbrc.2024.150490. Epub ahead of print. 16(15):2713. doi: 10.3390/cancers16152713. 4: Lopes N, Salta S, Flores BT, Miranda-Gonçalves V, Correia MP, Gigliano D, Guimarães R, Henrique R, Jerónimo C. Anti-tumour activity of Panobinostat in oesophageal adenocarcinoma and squamous cell carcinoma cell lines. Clin Epigenetics. 2024 Aug 3;16(1):102. doi: 10.1186/s13148-024-01700-3. 5: Yavari S, Naseroleslami M, Peymani M, Yekani F, Khayam Nekouei N. Investigation of SPOCD1 as A Suitable Diagnostic and Prognostic Biomarker in Various Common Cancer Types: Bioinformatics and Practical Analysis. Cell J. 2024 Jul 13;26(5):309-319. doi: 10.22074/cellj.2024.2022401.1506. 17(7):815. doi: 10.3390/ph17070815.
合成参考文献
参考文献:10.1007/s11912-011-0187-7 摘要:Schatz JH. Targeting the PI3K/AKT/mTOR pathway in non-Hodgkin's lymphoma: results, biology, and development strategies. Curr Oncol Rep. 2011 Oct;13(5):398–406. doi: 10.1007/s11912-011-0187-7. 参考文献:10.1182/blood-2011-02-336891 摘要:Kalac M, Scotto L, Marchi E, Amengual J, Seshan VE, Bhagat G, Ulahannan N, Leshchenko VV, Temkin AM, Parekh S, Tycko B, O'Connor OA. HDAC inhibitors and decitabine are highly synergistic and associated with unique gene-expression and epigenetic profiles in models of DLBCL. Blood. 2011 Nov 17;118(20):5506–16. 参考文献:10.1007/s10637-011-9718-1 摘要:Hwang JJ, Kim YS, Kim T, Kim MJ, Jeong IG, Lee JH, Choi J, Jang S, Ro S, Kim CS. A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL. Invest New Drugs. 2012 Aug;30(4):1434–42. doi: 10.1007/s10637-011-9718-1.