📜8-(Trifluoromethyl)-3,4-Dihydro-1H-Benzo[b]Azepine-2,5-Dione置于吡啶,Tetraphosphorus Decasulfide,Potassium Carbonate体系中,用 四氢呋喃,乙醇 用作溶剂,化学反应生成Mln0905; 2-[[5-[3-(二甲基氨基)丙基]-2-甲基-3-吡啶基]氨基]-5,7-二氢-9-(三氟甲基)-6H-嘧啶并[5,4-D][1]苯并氮杂卓-6-硫酮 参考文献:Discovery Of A Potent And Orally Bioavailable Benzolactam-Derived Inhibitor Of Polo-Like Kinase 1 (Mln0905) 标题:Discovery Of A Potent And Orally Bioavailable Benzolactam-Derived Inhibitor Of Polo-Like Kinase 1 (Mln0905) 摘要:This Article Describes The Discovery Of A Series Of Potent Inhibitors Of Polo-Like Kinase 1 (Plk1). Optimization Of This Benzolactam-Derived Chemical Series Produced An Orally Bioavailable Inhibitor Of Plk1 (12C,Mln0905). In Vivo Pharmacokinetic-Pharmacodynamic Experiments Demonstrated Prolonged Mitotic Arrest After Oral Administration Of 12C To Tumor Bearing Nude Mice. A Subsequent Efficacy Study In Nude Mice Achieved Tumor Growth Inhibition Or Regression In A Human Colon Tumor (Ht29) Xenograft Model. Doi:10.1021/jm2011172
专利号:US-5139940-A 优先权日:1989-10-26 标题 :Activation compounds and methods of synthesis of activation compounds 发明人:ISAACS STEPHEN T; CIMINO GEORGE D; METCHETTE KENNETH C; TESSMAN JOHN W 权利人:ISAACS STEPHEN T; CIMINO GOERGE D; METCHETTE KENNETH C; TESSMAN JOHN W 摘要:The invention is directed to isopsoralen compound compositions that contain a variety of substitutions which yet permit their binding to nucleic acid polymers. Reaction conditions that activate these bound isopsoralens results in covalent crosslinking to the nucleic acid polymers. The resultant complex is inhibited from being a template for the template-directed enzymatic synthesis of a complementary nucleic acid polymer. Beside the isopsoralens compositions, the invention includes their synthesis, the nucleic acid complex production and detection, and the above inhibitory method of use of the isopsoralens.
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-9273023-B2 优先权日:2011-11-01 标 题:Modular synthesis of graphene nanoribbons and graphene substructures from oligo-alkynes 发明人:ALABUGIN IGOR; BYERS PHILIP M 权利人:UNIV FLORIDA STATE RES FOUND 摘要:A method for the synthesis of carbon-based structures, particularly graphene substructures and ribbons, from oligo- and poly-alkyne starting materials.
专利号:US-9969686-B2 优先权日:2014-08-05 标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.
专利号:US-2012095211-A1 优先权日:2010-09-22 标 题 :Substituted proline inhibitors of hepatitis c virus replication 发明人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D 权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC 摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.
专利号:US-7125986-B2 优先权日:1997-12-29 标题:Penicillanic acid derivative compounds and methods of making 发明人:BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA 权利人:UNIV SOUTHERN METHODIST 摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
1: Lin M, Pan Y, Han S, Zhu L, Ye P, Ye M, Fang Z. MLN0905 effectively kills gemcitabine-resistant pancreatic cancer cells by targeting PLK1. Eur J Med Res. 2025 Jul 3;30(1):567. doi: 10.1186/s40001-025-02825-8. 2: Piri R, Shahidi M, Pooraskari Z, Habibi S. MLN0905, a new inhibitor of Polo- like kinase 1 (PLK1), enhances the efficiency of lenalidomide in promoting the apoptosis of multiple myeloma cell lines. Invest New Drugs. 2025 Apr;43(2):348-356. doi: 10.1007/s10637-025-01531-w. Epub 2025 Apr 25. 165:115262. doi: 10.1016/j.biopha.2023.115262. Epub 2023 Aug 3. 37(3):1419-1429. doi: 10.3892/or.2017.5417. Epub 2017 Feb 2.
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.