📜3-Cyclopentylamino-2,2-Difluoro-Propanoic Acid Ethyl Ester置于盐酸,铁粉,碳酸氢钠,O-Benzotriazol-1-Yl-N,N,N',N'-Bis(Tetramethylene)Uronium Hexafluorophosphate,Caesium Carbonate,溶剂黄146,N,N-二异丙基乙胺体系中,用 乙醇,水,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 53.0H,反应生成Tak960抑制剂 参考文献:Identification Of Novel,Potent And Selective Inhibitors Of Polo-Like Kinase 1 标题:Identification Of Novel,Potent And Selective Inhibitors Of Polo-Like Kinase 1 摘要:A Series Of Pyrimidodiazepines Was Identified As Potent Polo-Like Kinase 1 (Plk1) Inhibitors. The Synthesis And Sar Are Discussed. The Lead Compound 7 (Ro3280) Has Potent Inhibitory Activity Against Plk1,Good Selectivity Against Other Kinases,And Excellent In Vitro Cellular Potency. It Showed Strong Antitumor Activity In Xenograft Mouse Models. (C) 2011 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2011.11.052
专利号:US-8003785-B2 优先权日:2008-06-18 标 题 :Halo-substituted pyrimidodiazepines 发明人:CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL 权利人:TAKEDA PHARMACEUTICAL 摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
专利号:EP-2878592-B1 优先权日:2013-11-27 标题 :Synthesis of amide derivatives of some nonsteroidal antiinflammatory drugs as potential pro-drugs 发明人:KÜCÜKGÜZEL ILKAY; KULABAS NECLA; SET IREM 权利人:KUECUEKGUEZEL ILKAY
专利号:EP-2878592-A1 优先权日:2013-11-27 标题 :Synthesis of amide derivatives of some nonsteroidal antiinflammatory drugs as potential pro-drugs
专利号:WO-2012100179-A1 优先权日:2011-01-21 标题:Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
专利号:US-2012009151-A1 优先权日:2007-12-21 标题 :Triazines And Related Compounds Having Antiviral Activity, Compositions And Methods Thereof 发明人:HAN AMY QI; COBURN GLEN A; PROVONCHA KATHLEEN P; ROTSHTEYN YAKOV 权利人:HAN AMY QI; COBURN GLEN A; PROVONCHA KATHLEEN P; ROTSHTEYN YAKOV; PROGENICS PHARM INC 摘要:Disclosed herein are novel triazines and related compounds, the synthesis thereof, and compositions, including pharmaceutical compositions, comprising the novel triazines and related compounds. Such novel triazines and related compounds function to inhibit or block entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.
专利号:US-2010160351-A1 优先权日:2008-12-19 标题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders 发明人:JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE 权利人:NUON THERAPEUTICS INC 摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II: n n n n n n n n n n n n or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.
This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message Sent On: Wed Nov 11 14:13:40 2020 Search: TAK-960 8 selected items Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734. 2: Klauck PJ, Bagby SM, Capasso A, Bradshaw-Pierce EL, Selby HM, Spreafico A, Tentler JJ, Tan AC, Kim J, Arcaroli JJ, Purkey A, Messersmith WA, Kuida K, Eckhardt SG, Pitts TM. Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer. BMC Cancer. 2018 Feb 5;18(1):136. doi: 10.1186/s12885-018-4036-z. 3: Talati C, Griffiths EA, Wetzler M, Wang ES. Polo-like kinase inhibitors in hematologic malignancies. Crit Rev Oncol Hematol. 2016 Feb;98:200-10. doi: 10.1016/j.critrevonc.2015.10.013. Epub 2015 Nov 4.
合成参考文献
参考文献:10.1124/mol.119.115964 摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.