📜4-氨基吡唑并[3,4-D]嘧啶置于n-溴代丁二酰亚胺(Nbs),四(三苯基膦)钯,Sodium Carbonate,Caesium Carbonate体系中,用 1,4-二氧六环,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 21.75H,反应生成3-(2-氨基-5-苯并恶唑基)-1-(1-甲基乙基)-1H-吡唑并[3,4-D]嘧啶-4-胺 参考文献:Impact Of Minor Structural Modifications On Properties Of A Series Of Mtor Inhibitors 标题:Impact Of Minor Structural Modifications On Properties Of A Series Of Mtor Inhibitors 摘要:Minor Structural Modifications-Sometimes Single Atom Changes-Can Have A Dramatic Impact On The Properties Of Compounds. This Is Illustrated Here On Structures Related To Known Mtor Inhibitor Sapanisertib. Subtle Changes In The Hinge Binder Lead To Strikingly Different Overall Profiles With Changes In Physical Properties,Metabolism,And Kinase Selectivity. Doi:10.1021/acsmedchemlett.9B00401
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-2025268920-A1 优先权日:2022-04-20 标 题:Use of androgen receptor-mediated mechanisms in the treatment of acute myeloid leukemia 发明人:QIAN FENGHUA; PRABHU KUMBLE SANDEEP; PAULSON ROBERT F 权利人:PENN STATE RES FOUND 摘要:Provided is a method for treating a blood cancer in an individual in need thereof by administrating to the individual an agent that inhibits activity or expression of one or more enzymes that participate in synthesis of either or both dihydrotestosterone (DHT) or androgen receptor (AR), or an antagonist AR, or a combination of an agent and the antagonist. The methods are shown in connection with acute myeloid leukemia (AML).
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-10272065-B2 优先权日:2013-01-14 标题 :Gem-difluorinated C-glycoside compounds as anti-cancer agents 发明人:SLILATY STEVE N 权利人:ADVANOMICS CORP; BENOIT & COTE 摘要:The present document describes a synthesis of a class of gem-difluorinated C-glycoside compounds derived from podophyllotoxin, which may be used, but not exclusively, in oncology for the treatment of cancer. More particularly, the podophyllotoxin gem-difluorinated C-glycoconjugated derivatives display improved conformational and chemical stability, and improved cytotoxicity exhibited against drug-resistant cancer cell lines.
1: Sehgal K, Serritella A, Liu M, ONeill A, Nangia C, Pappa T, Demeure MJ, Worden FP, Haddad R, Lorch J. A phase I/II trial of sapanisertib in advanced anaplastic and radioiodine refractory differentiated thyroid carcinoma. J Clin Endocrinol Metab. 2024 Jun 29:dgae443. doi: 10.1210/clinem/dgae443. Epub ahead of print. 22(5):102123. doi: 10.1016/j.clgc.2024.102123. Epub 2024 May 23. 16(8):1456. doi: 10.3390/cancers16081456. 4: Kadiyala GN, Telwatte S, Wedrychowski A, Janssens J, Kim SJ, Kim P, Deeks S, Wong JK, Yukl SA. Differential susceptibility of cells infected with defective and intact HIV proviruses to killing by obatoclax and other small molecules. AIDS. 2024 Jul 15;38(9):1281-1291. doi: 10.1097/QAD.0000000000003908. Epub 2024 Apr 20.
合成参考文献
参考文献:10.3324/haematol.2015.130351 摘要:Rahmani M, Aust MM, Hawkins E, Parker RE, Ross M, Kmieciak M, Reshko LB, Rizzo KA, Dumur CI, Ferreira-Gonzalez A, Grant S. Co-administration of the mTORC1/TORC2 inhibitor INK128 and the Bcl-2/Bcl-xL antagonist ABT-737 kills human myeloid leukemia cells through Mcl-1 down-regulation and AKT inactivation. Haematologica. 2015 Oct 09;100(12):1553–63. doi: 10.3324/haematol.2015.130351. 参考文献:10.1186/s12885-019-5861-4 摘要:Skaga E, Kulesskiy E, Fayzullin A, Sandberg CJ, Potdar S, Kyttälä A, Langmoen IA, Laakso A, Gaál-Paavola E, Perola M, Wennerberg K, Vik-Mo EO. Intertumoral heterogeneity in patient-specific drug sensitivities in treatment-naïve glioblastoma. BMC Cancer. 2019 Jun 25;19(1):628.