CAS: 303162-79-0; N-(4-(2-Ethyl-4-(M-Tolyl)Thiazol-5-yl)Pyridin-2-yl)Benzamide

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CAS号303162-39-2 4-[2-ethyl-4-(3... | CAS号303162-37-0 tert-butyl 3-am... | CAS号21384-43-0 (2-methylazirid... | CAS号90101-20-5 (4-甲基吡啶-2-基)氨基甲酸叔丁酯 | CAS号98-88-4 苯甲酰氯

📜4-[2-Ethyl-4-(3-Methylphenyl)-1,3-Thiazol-5-Yl]-Pyridin-2-Ylamine置于盐酸,三乙胺体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 17.0H,反应生成 N-(4-(2-乙基-4-(3-甲基苯基)噻唑-5-基)吡啶-2-基)苯甲酰胺
参考文献:作为抗tnf-α药物的新型p38 Map激酶抑制剂:N-[4-[2-乙基-4-(3-甲基苯基)-1,3-噻唑-5-基]-2-吡啶基]的发现苯甲酰胺(tak-715)作为有效的口服活性抗类风湿关节炎药.
标题:作为抗tnf-α药物的新型p38 Map激酶抑制剂:N-[4-[2-乙基-4-(3-甲基苯基)-1,3-噻唑-5-基]-2-吡啶基]的发现苯甲酰胺(tak-715)作为有效的口服活性抗类风湿关节炎药.
摘要:P38促分裂原活化蛋白(map)激酶与促炎细胞因子信号通路有关,其抑制剂可能对治疗慢性炎性疾病(如类风湿性关节炎(ra)和炎性肠病)有用.为开发用于ra的新药,我们合成了一系列新的4-苯基-5-吡啶基-1,3-噻唑,并评估了它们对p38 Map激酶,脂多糖(lps)刺激的肿瘤坏死因子-α释放的抑制作用(从人单核细胞thp-1细胞体外提取tnf-α,在小鼠体内从lps诱导的tnf-α产生.在研究过程中,我们发现这些化合物可能会通过4-吡啶基氮与血红素铁的配位而具有抑制细胞色素p450(cyp)同工型的风险.因此,我们更详细地研究了吡啶基环2位上的取代对p38 Map激酶和cyps抑制活性的影响.结果,N-[4-[2-乙基-4-(3-甲基苯基)-1,3-噻唑-5-基]-2-吡啶基]苯甲酰胺(8H,Tak-715)在小鼠体内表现出有效的抑制活性.这些测定法(抑制p38Alpha,Ic50 =
DOI:10.1021/jm050165O

专利信息

专利号:EP-1971603-B1
优先权日:2005-12-13
标题:SULFOXIMINE DERIVATIVES AS p38 MAP KINASE INHIBITORS
发明人：SHETTY SHANKAR JAYRAM; PATEL GAUTAM D; LOHRAY BRAJ BHUSHAN; LOHRAY VIDYA BHUSHAN; CHAKRABARTI GANES; CHATTERJEE ABHIJIT; JAIN MUKUL R; PATEL PANKAJ RAMANBHAI
权利人:CADILA HEALTHCARE LTD
摘要:The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.