CAS: 149947-19-3; 3-(4-Bromo-2-Fluorophenyl)-2-Propenoic Acid

相似化合物

149947-09-1 202865-71-2 744240-66-2

上下游产品

4-bromo-2-fluoroaniline aminosulfonic acid acrylic acid maleic anhydride trans 3-(2-fluoro-4-bromophenyl)-2-propenoic acid chloride (E)-ethyl 3-(4-bromo-2-fluorophenyl)acrylate 3-(4-Bromo-2-fluorophenyl)-2-propen-1-ol

丙二酸,4-溴-2-氟苯甲醛置于4-二甲氨基吡啶体系中,用 N,N-二甲基甲酰胺 用作溶剂,以85%的收率获得2-溴4-氟肉桂酸
参考文献:类组蛋白组去乙酰化酶抑制剂的药代动力学优化和肝癌肿瘤反应相关候选预测生物标志物的鉴定
标题:类组蛋白组去乙酰化酶抑制剂的药代动力学优化和肝癌肿瘤反应相关候选预测生物标志物的鉴定
摘要:在这里,我们描述了一系列的类选择性组蛋白去乙酰化酶(hdac)抑制剂的药代动力学优化,以及随后使用患者来源的hcc肿瘤异种移植模型为我们的临床线索鉴定了肝细胞癌(hcc)肿瘤反应的候选预测性生物标志物.通过构象约束和支架跳跃的结合,我们降低了我们的hdac抑制剂的体内清除率(cl),并显着提高了其hdac抑制剂的生物利用度(f)和暴露(auc),同时保持了对i类hdac系列的选择性以及对hdac1的特殊效力,导致产生临床铅5(hdac1 Ic 50 = 60 Nm,小鼠cl = 39 Ml / Min / Kg,小鼠f= 100%,单次口服剂量10 Mg / Kg后的小鼠auc = 6316 H.ng / Ml).然后,我们在生物标记物发现先导研究中使用患者衍生的肿瘤异种移植模型评估了5个,其中三个模型中的两个对治疗有反应.通过比较这三种模型在不同时间点的肿瘤反应状态与复合肿瘤暴露,乙酰化
Doi:10.1021/jm3011838

专利信息

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-6562844-B2
优先权日:1998-01-23
标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-7002020-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.