CAS: 96187-53-0; 6-Fluoro-2-(2'-Fluoro-[1,1'-Biphenyl]-4-yl)-3-Methylquinoline-4-Carboxylic Acid

📜4'-溴苯丙酮置于dipotassium Hydrogenphosphate,四(三苯基膦)钯,Potassium Hydroxide体系中,用 1,4-二氧六环,乙醇,水 作为反应溶剂,化学反应 13.75H,反应生成 布喹那
参考文献:Brequinar缀合物的设计,合成和表征,作为研究dhodh抑制作用的探针
标题:Brequinar缀合物的设计,合成和表征,作为研究dhodh抑制作用的探针
摘要:Brequinar是一种有效的二氢乳清酸脱氢酶(dhodh)抑制剂,已在多项临床试验中评估为潜在的癌症治疗方法.为了进一步了解基于臀肌的dhodh抑制作用和dhodh在癌症中的治疗意义,我们开发了新型的基于臀肌的探针.我们公开了第一个brequinar-Protac的16个步骤的收敛合成,以及第一个线粒体定向的brequinar探针的四个步骤的方法.在菌落形成试验中,布雷塔那的protac和线粒体定向探针均具有比布雷库那更好的细胞毒性.
DOI:10.1002/chem.201702999

专利信息

专利号:WO-2022226312-A1
优先权日:2021-04-22
标 题:Combination nucleotide pool depletion for treatment of viral infections and cancers
发明人：KUMAR VIKRAM; HESSON DAVID; DEMAREST JAMES
权利人:CLEAR CREEK BIO INC
摘要:The invention provides methods of treating cancers and viral infections by providing a combination of agents that inhibit both nucleotide synthesis and nucleotide salvage in the cells of a subject to prevent cancer proliferation and viral replication. The invention provides methods of depleting nucleotide pools by using both inhibitors of dihydroorotate dehydrogenase (DHODH), such as brequinar, which block synthesis of pyrimidine-based nucleotides, in combination of one or more nucleotide salvage inhibitors, for example deoxycytidine kinase (dCK) inhibitors, Equilibrative nucleoside transporter (ENT) inhibitors, and Uridine-cytidine kinase (UCK) inhibitors, which inhibit salvage of purine and/or pyrimidine-based nucleotides or nucleosides

专利号:US-8461298-B2
优先权日:2004-11-01
标 题:Compositions and methods for modification of biomolecules
发明人：BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL
权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA
摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

专利号:US-9260371-B2
优先权日:2004-11-01
标题:Compositions and methods for modification of biomolecules
发明人：BERTOZZI CAROLYN RUTH; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; SLETTEN ELLEN MAY
权利人:UNIV CALIFORNIA
摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

专利号:US-9650407-B2
优先权日:2011-11-02
标 题 :Reprogramming of cellular adhesion
发明人：GARTNER ZEV JORDAN; SELDEN NICHOLAS SCOTT; TODHUNTER MICHAEL E; LIANG SAMANTHA ISABEL; WEBER ROBERT JOSEPH; JEE NOEL YOUNGHO; LIU JENNIFER S
权利人:UNIV CALIFORNIA
摘要:Disclosed are membrane-anchored polynucleotides, and compositions comprising the membrane-anchored polynucleotides. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds and compositions in research and therapeutic applications.

专利号:US-2005255071-A1
优先权日:1998-12-10
标 题 :Preparation having improved therapeutic breadth comprising nucleotide synthesis inhibitors
发明人：LINDNER JURGEN; HAASE BURKHARD
权利人:AVENTIS PHARMA GMBH
摘要:A preparation comprising a compound which essentially prevents the enterohepatic circulation of nucleotide synthesis inhibitors or antagonizes the action of the nucleotide synthesis inhibitors with a displacement in time, and a nucleotide synthesis inhibitor such as brequinar, mycophenolatemofetil (2-morpholinoethyl (E)-6-(1,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxoisobenzofuran-5-yl)-4-methyl-4-hexenoate), methotrexate, mizoribine and compounds of formulae (I) and (II) n nis suitable for the treatment of immunological disorders, cancer, or in transplantations.

专利号:US-2023390297-A1
优先权日:2022-06-02
标 题:Use of nucleotide synthesis inhibitors for targeted therapy in mll3/4 compass mutant cancer
发明人：SHILATIFARD ALI; ZHAO ZIBO
权利人:UNIV NORTHWESTERN
摘要:Disclosed herein are methods and compositions for treating a subject comprising the administration of an effective amount of a nucleotide synthesis inhibitor to a subject in need of treatment for a MLL3/4 COMPASS deficient cancer or a MLL3/4 loss of function mutation.