CAS: 57381-26-7; 6-(2,5-Dichlorophenyl)-1,3,5-Triazine-2,4-Diamine

上下游产品

irsogladine maleate 2,5-dichlorobenzonitrile N-Cyanoguanidine dicyandiamide2-Amino-4-(2,5-dichlorophenyl)-6-methylamino-1,3,5-triazine irsogladine maleate

马来酸伊索拉定置于碳酸氢钠体系中,用 乙酸乙酯 作为反应溶剂,化学反应 1.0H,以70%的收率获得产物伊索拉定
参考文献:将厄索拉定重新定位为hsp90抑制剂
标题:将厄索拉定重新定位为hsp90抑制剂
摘要:|热休克蛋白90(hsp90)是一种普遍存在的依赖于三磷酸腺苷(atp)的分子伴侣,由于其在维持许多致癌蛋白的正确折叠和稳定性方面的作用,因此是有吸引力的癌症治疗靶标.为了将现有药物改用于hsp90抑制剂,我们根据化学结构相似性筛选了美国食品与药物管理局(fda)批准的药物,并发现粘膜保护药irsogladine抑制了hsp90折叠机制.体外荧光偏振分析和基于细胞的机制研究表明,伊索拉定与hsp90 N末端结构域中的atp结合口袋结合,并损害了hsp90伴侣功能.因此,伊索拉定可诱导hsp90客户蛋白(包括her2,Akt和cdk4)的下调,以及伴侣伴侣hsp70的上调.
DOI:10.1002/bkcs.10291

专利信息

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-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-9220714-B2
优先权日:2006-03-16
标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
发明人：SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.