相似化合物
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CAS号5469-69-2 3-氨基-6-氯哒嗪 | CAS号19967-57-8 2-溴丙醛📜3-氨基-6-氯哒嗪,2-溴丙醛 以 乙醇 用作溶剂,化学反应 2.0H,以83%的收率获得6-氯-3-甲基咪唑并[1,2-B]哒嗪
参考文献:缩合唑衍生物的合成研究.Iv.ω-氨磺酰基烷基氧基咪唑并[1,2-B]哒嗪的合成及抗哮喘活性.
标题:缩合唑衍生物的合成研究.Iv.ω-氨磺酰基烷基氧基咪唑并[1,2-B]哒嗪的合成及抗哮喘活性.
摘要:合成了一系列新颖的(咪唑并[1,2-B]哒嗪-6-基)氧基烷基磺酰胺,并评估了其抑制血小板活化因子(paf)诱导的豚鼠支气管收缩的能力.发现在侧链的氨磺酰基丙氧基的2位上带有宝石二烷基或亚环烷基的化合物具有有效的活性.其中,3-(咪唑并[1,2-B]哒嗪-6-基)氧基-2,2-二甲基丙烷磺酰胺(6)具有非常好的抗哮喘活性,且作用时间最长.发现在咪唑并[1,2-B]哒嗪环的7或8位带有甲基的化合物具有增强的活性.其中,3-(7-甲基咪唑并[1,2-B]哒嗪-6-基)氧基-2,2-二甲基丙烷磺酰胺(25)表现出最强的抑制作用,在过敏性哮喘实验模型中的抗哮喘作用优于茶碱.讨论了这一系列化合物中的构效关系.
Doi:10.1248/cpb.44.122
专利信息
专利号:US-10000487-B2
优先权日:2015-11-20
标 题 :Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers
发明人:SPRENGELER PAUL A; REICH SEIGFRIED H; WEBBER STEPHEN E; ERNST JUSTIN T
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. n nFor Formula IA and Formula IB compounds A 1 , A 2 , A 3 , A 4 , W 1 , W 2 , Y, X, R 1 , R 2 , R 3 , R 4a , R 4b , R 5a , R 5b , R 6 , R 7 , R 8 , R 9 , R 9a , R 9b , R 10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:RU-2036924-C1
优先权日:1989-01-31
标题:Method of synthesis of imidazo-(1,2-b)-pyridazine or their salts and imidazo-(1,2-b)-pyridazine derivatives or their salts