CAS: 263349-73-1; 4-Bromo-3-Fluorobenzenesulphonamide

上下游产品

4-bromo-3-fluorobenzene-1-sulfonyl chloride 4-ethynyl-3-fluorobenzenesulfonamide 4-(4-(4-chlorophenyl)-2-(piperidine-1-carbonyl)thiazol-5-yl)-3-fluorobenzenesulfonamide

3-氟-4-溴苯磺酰氯置于氨体系中,用 乙腈 用作溶剂,化学反应 0.17H,以82%的收率获得4-溴-3-氟苯磺酰胺
参考文献:靶向丝裂原活化蛋白激酶激酶 4 (Mkk4) 的 1H-吡唑并[3,4-B]吡啶的设计和合成--肝再生的一个有希望的靶点
标题:靶向丝裂原活化蛋白激酶激酶 4 (Mkk4) 的 1H-吡唑并[3,4-B]吡啶的设计和合成--肝再生的一个有希望的靶点
摘要:目前,治疗肝功能衰竭的治疗选择非常有限.由于最近通过体内rnai 实验发现丝裂原活化蛋白激酶激酶 4 (Mkk4)是肝细胞再生的主要调节因子,因此我们致力于开发一种针对该蛋白激酶的小分子.从已获批的 Braf V600E抑制剂 Vemurafenib ( 8 )开始,该抑制剂在初始筛选中显示出对 Mkk4 的高脱靶亲和力,我们采用了支架跳跃方法,将核心杂环从 1 H-吡咯 [2,3-B ]吡啶到 1 H-吡唑并[2,3-B ]吡啶(10).对 Mkk4 的亲和力可以得到保留,而对脱靶蛋白激酶的选择性略有提高.进一步的修改导致58和59在低纳摩尔范围内显示出对 Mkk4 的高亲和力,以及来自必需抗靶点(mkk7,Jnk1)和脱靶点(braf,Map4K5,Zak)的强制性多参数优化的优异选择性. Mkk4 通路.在此我们报告了此类中的第一个选择性 Mkk4 抑制剂.
Doi:10.1016/j.Ejmech.2021.113371

专利信息

专利号:US-2007275968-A1
优先权日:2004-09-07
标 题 :Substituted Biphenyl Derivative
发明人：KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI
权利人:KURATA HITOSHI; NISHIMATA TOYOKI; WATANABE YUKIKO; EBISAWA MASAYUKI; FUJIMOTO TEPPEI; KOBAYASHI HIDEKI
摘要:The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: n nwherein n R 1 represents a C 6 -C 10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C 1 -C 6 alkyl)amino group, a di-(C 1 -C 6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C 1 -C 6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R 2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R 3 represents a C 1 -C 6 alkyl group, and so on; and R 4 represents a C 1 -C 6 alkyl group, and so on.