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2-氨基-5-溴三氟甲苯置于盐酸,硫酸,硝酸体系中,化学反应 12.0H,反应生成2-氨基-5-溴-3-硝基三氟甲苯
参考文献:取代的1,4-二氢喹喔啉-2,3-二酮的合成与构效关系:N-甲基-D-天冬氨酸(nmda)受体甘氨酸位点和非nmda谷氨酸受体的拮抗剂.
标题:取代的1,4-二氢喹喔啉-2,3-二酮的合成与构效关系:N-甲基-D-天冬氨酸(nmda)受体甘氨酸位点和非nmda谷氨酸受体的拮抗剂.
摘要:合成了一系列的单,二,三和四取代的1,4-二氢喹喔啉-2,3-二酮(qxs),并在n-甲基-D-天冬氨酸(nmda)/甘氨酸位点和α位作为拮抗剂进行了评估-氨基-3-羟基-5-甲基异恶唑-4-丙酸优先的非nmda受体.通过电测定在表达大鼠全脑poly(a)+ Rna的非洲爪蟾卵母细胞中测量拮抗剂的效力.三取代qx 17A(acea 1021),17B(acea 1031),24A和27,在5位含硝基,在6和7位含卤素,在甘氨酸上显示出高效价(kb约为6-8 Nm)位点,对非nmda受体的药效中等(kb = 0.9-1.5 Microm),与非nmda受体相比,甘氨酸位点拮抗作用的选择性最高(120-250倍).四取代的qx 17D E是比相应的三取代qx弱100倍的弱甘氨酸位点拮抗剂,在8位上f作为取代基比cl具有更好的耐受性.与三取代类似物相比,二取代和单取代的qx显示出越来越弱的拮抗作
Doi:10.1021/jm00022A003

专利信息

专利号:US-2017369470-A1
优先权日:2014-12-16
标 题:Cyclic Compounds and Uses Thereof
发明人：BALOGLU ERKAN; SENAPEDIS WILLIAM; SHACHAM SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted benzothiophenyl, substituted benzothiazolyl, substituted indolyl and substituted benzoimidazolyl compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, inflammatory diseases or an autoimmune system disease (e.g., a T-Cell mediated autoimmune disesase).