CAS: 120022-63-1; 2,5-Difluorobenzenesulfonamide

相似化合物

30058-40-3 778-36-9 60230-37-7

上下游产品

2,5-二氟苯磺酰氯 2,5-Difluorobenzenesulfonyl Chloride 26120-86-5

2,5-二氟苯胺置于盐酸,Ammonium Hydroxide,溶剂黄146,Sodium Nitrite体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 0.75H,反应生成2,5-二氟苯磺酰胺
参考文献:结合谷氨酸受体 A2 配体结合域的新型正变构调节剂的热力学表征:结合实验和计算方法揭示驱动力的差异
标题:结合谷氨酸受体 A2 配体结合域的新型正变构调节剂的热力学表征:结合实验和计算方法揭示驱动力的差异
摘要:离子型谷氨酸受体 Glua2 的正变构调节为认知障碍(例如阿尔茨海默病)提供了潜在的治疗方法.在本研究中,我们描述了一系列单氟取代的 3,4-二氢-2 H-1,2,4-苯并噻二嗪 1,1-二氧化物的合成,药理学和热力学研究.通过等温滴定量热法 (Itc) 对配体结合的测量表明,Glua2 Lbd 处的调节剂系列具有相似的结合亲和力,但热力学驱动力存在差异.结合图5C(7-F)和6(无-F)是焓驱动的,图5A(5-F)和图5B(6-F)的熵驱动.对于5D(8-F),两个数量的大小相等.热力学积分 (Ti) 和一步扰动 (Osp) 用于计算调节剂的相对结合亲和力.Osp 计算具有比 Ti 更高的预测能力,并且结合较短的总仿真时间,我们发现 Osp 方法对于此设置更有效.此外,从分子动力学模拟中,我们提取了焓和熵,以及 Itc 数据,这表明结合自由能的差异在很大程度上是由直接配体周围的焓解释的.此外,
Doi:10.1021/ci500559B

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.

专利号:US-9701686-B2
优先权日:2009-12-04
标题:Tricyclopyrazole derivatives
发明人：DISINGRINI TERESA; MANTEGANI SERGIO; VARASI MARIO
权利人:NERVIANO MEDICAL SCIENCES SRL
摘要:Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

专利号:WO-2024115549-A1
优先权日:2022-11-30
标题:Aryl- and heteroaryl-sulfonamide derivatives as ccr8 modulators
发明人：AISSAOUI HAMED; CORMINBOEUF OLIVIER; DIETHELM STEFAN; REMEN LUBOS; RICHARD-BILDSTEIN SYLVIA
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR8 receptor modulators in medicine.