📜6-溴-4-碘-喹啉置于1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,Potassium Acetate,Sodium Carbonate体系中,用 1,4-二氧六环 用作溶剂,化学反应生成芸香苷 参考文献:[11C]Gsk2126458 And [18F]Gsk2126458,The First Radiosynthesis Of New Potential Pet Agents For Imaging Of Pi3K And Mtor In Cancers 标题:[11C]Gsk2126458 And [18F]Gsk2126458,The First Radiosynthesis Of New Potential Pet Agents For Imaging Of Pi3K And Mtor In Cancers 摘要:Gsk2126458 Is A Highly Potent Inhibitor Of Phosphoinositide 3-Kinase (Pi3K) And Mammalian Target Of Rapamycin (Mtor) With Low Picomolar To Subnanomolar Activity. [c-11]Gsk2126458 And [f-18]Gsk212 6458,New Potential Pet Agents For Imaging Of Pi3K And Mtor In Cancer,Were First Designed And Synthesized In 40-50% And 20-30% Decay Corrected Radiochemical Yield,And 370-740 And 37-222 Gbq/lmol Specific Activity At End Of Bombardment (Eob),Respectively. (C) 2012 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2011.12.136
专利信息
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-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.
专利号:US-2024342244-A1 优先权日:2021-07-28 标 题:Isthmin Protein Therapeutics for the Treatment of Non-Alcoholic Fatty Liver Disease 发明人:SVENSSON KATRIN JENNIFER; VOILQUIN LAETITIA 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Compositions and methods are provided for the treatment of one or both of type 2 diabetes and fatty liver disease, e.g. non-alcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH). The adipokine Isthmin-1 (ISM1) protein increases adipose glucose uptake while suppressing hepatic lipid synthesis.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2022047711-A1 优先权日:2018-12-10 标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins 发明人:SADOWSKY JACK; ZACHARIAS NEELIE TYANA 权利人:GENENTECH INC 摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.
参考文献:10.1021/ml900028r 摘要:Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett. 2010 Apr 08;1(1):39–43. 参考文献:10.1186/s13045-019-0754-1 摘要:Hua H, Kong Q, Zhang H, Wang J, Luo T, Jiang Y. Targeting mTOR for cancer therapy. Journal of Hematology & Oncology. 2019 Jul 05;12(1):71. doi: 10.1186/s13045-019-0754-1. 参考文献:10.12659/msm.927106 摘要:Zhu DS, Dong JY, Xu YY, Zhang XT, Fu SB, Liu W. Omipalisib Inhibits Esophageal Squamous Cell Carcinoma Growth Through Inactivation of Phosphoinositide 3-Kinase (PI3K)/AKT/Mammalian Target of Rapamycin (mTOR) and ERK Signaling. Med Sci Monit. 2020 Aug 17;26():e927106. 摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749