CAS: 507475-17-4; 5-(4-Fluorophenyl)-2-Ureidothiophene-3-Carboxamide

上下游产品

2-amino-5-(4-fluorophenyl)-3-thiophenecarboxamide is°Cyanate de chlorosulfonyle 4-fluorophenylacetaldehyde 2-(4-fluorophenyl)cyclopropane-1,1-dicarboxylic acid dimethyl ester

📜对氟苯乙醛置于sulfur,三乙胺体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 5-(4-氟苯基)-2-脲基噻吩-3-甲酰胺
参考文献:Attenuation Of Murine Collagen-Induced Arthritis By A Novel,Potent,Selective Small Molecule Inhibitor Of IKb Kinase 2,Tpca-1 (2-[(Aminocarbonyl)Amino]-5-(4-Fluorophenyl)-3-Thiophenecarboxamide),occurs Via Reduction Of Proinflammatory Cytokines And Antigen-Induced T Cell Proliferation
标题:Attenuation Of Murine Collagen-Induced Arthritis By A Novel,Potent,Selective Small Molecule Inhibitor Of IKb Kinase 2,Tpca-1 (2-[(Aminocarbonyl)Amino]-5-(4-Fluorophenyl)-3-Thiophenecarboxamide),occurs Via Reduction Of Proinflammatory Cytokines And Antigen-Induced T Cell Proliferation
摘要:IKb 激酶 2(ikk-2)在肿瘤坏死因子(tnf)-α 和白细胞介素(il)-1 等刺激核因子-Kb 调节的促炎分子反应生成过程中起着关键作用,这表明抑制 Ikk-2 可能有益于类风湿性关节炎的治疗.在本研究中,我们证明了一种新型,强效(ic50 = 17.9 Nm),选择性的人 Ikk-2 抑制剂 2-[(氨基羰基)氨基]-5-(4-氟苯基)-3-噻吩甲酰胺(tpca-1)可抑制脂多糖诱导的人单核细胞产生 Tnf-α,Il-6 和 Il-8,Ic50 = 170 至 320 Nm.预防性服用 3,10 或 20 毫克/千克的 Tpca-1 后,小鼠胶原诱导的关节炎(cia)的严重程度会出现剂量依赖性下降.以每公斤 10 毫克,每次口服,每天两次的剂量服用 Tpca-1 后,疾病严重程度明显减轻,发病时间也有所推迟,这与每隔一天以每公斤 4 毫克,每次口服的剂量预防性服用抗风湿药物依那西普(etanercept)的效果相当.在 Tpca-1 和依那西普治疗的小鼠爪组织中,P65 的核定位以及 Il-1β,Il-6,Tnf-α 和干扰素-γ 的水平均显著降低.此外,体内服用 Tpca-1 还能显著减少胶原蛋白诱导的体内 T 细胞增殖.治疗性服用 20 毫克/千克(3 或 10 毫克/千克)tpca-1(i.P.,B.I.D.)可显著减轻 Cia 的严重程度,而服用 12.5 毫克/千克(i.P.,隔日一次)依那西普(etanercept)则无效.这些结果表明,减少促炎介质和抑制抗原诱导的 T 细胞增殖是 Ikk-2 抑制剂 Tpca-1 减轻 Cia 的基本机制.
DOI:10.1124/jpet.104.074484

专利信息

专利号:US-2024336679-A1
优先权日:2021-08-06
标题 :Methods for the treatment of cancer
发明人：LINARES LÆTITIA; FIRMIN NELLY; MANTEAUX GABRIELLE
权利人:INST REGIONAL CANCER MONTPELLIER; INST NAT SANTE RECH MED; UNIV MONTPELLIER
摘要:The present disclosure relates to an Interleukin-6 (IL-6) signaling inhibitor selected from an IL-6 inhibitor, an IL-6 receptor inhibitor, an IL-6/IL-6 receptor complex inhibitor, a gp130 inhibitor and a STAT3 inhibitor or a pharmaceutical composition comprising such an IL-6 signaling inhibitor. for use in a method for treating and/or preventing cancer in a subject in need thereof. wherein the subject has been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin. The inventors have observed that cancers exhibiting recruitment of MDM2 to chromatin have been shown to secrete IL-6 that in turn acts on myoblast cells to activate serine synthesis. Following these surprising and unexpected observations. the inventors set up methods of treatment that are able to induce cancer cells death in subjects that have been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin.