CAS: 862723-42-0; 5-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-1H-Indazole

5-溴吲唑,联硼酸频那醇酯置于1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,Potassium Acetate体系中,用 二甲基亚砜 作为反应溶剂,化学反应 16.0H,以36%的收率获得产物1H-吲唑-5-硼酸频哪醇酯
参考文献:Gs-9973,脾酪氨酸激酶的选择性和口服有效抑制剂的发现
标题:Gs-9973,脾酪氨酸激酶的选择性和口服有效抑制剂的发现
摘要:脾酪氨酸激酶(syk)在自身免疫,炎症和肿瘤疾病适应症中是有吸引力的药物靶标.最先进的syk抑制剂,R406,1(或它的前药形式fostamatinib,2),已在多个治疗适应症中显示出功效,但其临床进展已经由已被归因,至少部分剂量限制性不利影响的阻碍,到的脱靶活性1.预期选择性更高的syk抑制剂将提供更大的治疗窗口.在本文中,我们报告了一系列新型咪唑并[1,2-A]吡嗪syk抑制剂的发现和优化.这项工作在gs-9973,鉴定高潮68是一种高度选择性和口服有效的syk抑制剂,目前正在针对自身免疫和肿瘤学适应症进行临床评估.
DOI:10.1021/jm500228A

专利信息

专利号:WO-2021038419-A1
优先权日:2019-08-23
标题 :Kinase inhibitors and methods of synthesis and treatment
发明人：ZAVORONKOVS ALEKSANDRS; IVANENKOV YAN; POLYKOVSKIY DANIIL; ALIPER ALEKSANDR
权利人:INSILICO MEDICINE IP LTD
摘要:Compounds that function as kinase inhibitors are provided. The kinase inhibitors can have any structure of the formulae provided herein, such as shown for Compounds 1-4. A pharmaceutical composition can include: the compound of one of the embodiments; and a pharmaceutically acceptable carrier having the compound. A method of inhibiting a kinase can include: providing the compound of one of the embodiments described herein to the kinase such that the kinase is inhibited. The methods can include inhibiting DDR1 and/or DDR2, and thereby providing a modulation or decrease in the activity of DDR1 and/or DDR2. This decrease in DDR1 and/or DDR2 activity can be used as therapy to treat conditions related to DDR1 and/or DDR2 activity, such as fibrosis, cancer, and others.