CAS: 5305-59-9; 6-Chloropyrimidin-4-Amine

相似化合物

1849595-31-8 10132-07-7 1749-68-4

4,6-二氯嘧啶置于ammonium Hydroxide体系中,用 异丙醇 作为反应溶剂,化学反应 16.0H,以77%的收率获得产物4-氨基-6-氯嘧啶
参考文献:Wt Ret和v804M Ret抑制剂的发现:从命中到领先.
标题:Wt Ret和v804M Ret抑制剂的发现:从命中到领先.
摘要:Ret激酶的致癌激活已在多种肿瘤疾病中发现,如甲状腺髓样癌,多发性内分泌肿瘤,甲状腺乳头状癌和非小细胞肺癌.目前批准的ret抑制剂最初并未设计为ret抑制剂,而且它们对ret激酶的效能尚未优化.因此,需要能够抑制野生型ret(wt Ret)及其突变体(例如v804M Ret)的新型化合物.本文中,我们介绍了新型亚微摩尔wt Ret / V804M Ret抑制剂n-(2-氟-5-三氟甲基苯基)-N'-{4'-[(2''-苯甲酰胺基)吡啶的开发和初步评估从我们先前鉴定的4-苯胺基嘧啶命中化合物开始,具有4-苯胺基吡啶结构的-4"-基氨基]苯基}脲(69).
DOI:10.1002/cmdc.201700243

专利信息

专利号:WO-2025052163-A1
优先权日:2023-09-07
标 题:2-amino-n-(benzo[d]thiazol-2-ylsulfonyl)-3-hydroxybutanamide derivatives acting as a threonyl-t-rna synthetase inhbitors for the treatment of malaria
发明人：JIRGENSONS AIGARS; BOLSAKOVA JEKATERINA; BOBROVS RAITIS; VARACEVA LARISA
权利人:LATVIAN INST ORGANIC SYNTHESIS
摘要:Representatives of 2-amino-N-(benzo[d]thiazol-2-ylsulfonyl)-3-hydroxybutanamide with general formula (I) show potency to inhibit malarial threonyl-tRNA synthetase (ThrRS) in low micromolar to nanomolar concentrations. As such they can be applied as compounds for prevention or treatment of malaria.

专利号:US-9751851-B2
优先权日:2013-09-20
标 题:Molecules and compositions that inhibit gram negative bacteria and their uses
发明人：BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; CONRAD-MILLER LAURA C; O'LOUGHLIN COLLEEN T
权利人:UNIV PRINCETON; BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; MILLER LAURA C; O'LOUGHLIN COLLEEN T
摘要:Antivirulence strategies to combat Pseudomonas aeruginosa , are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.

专利号:US-2007042401-A1
优先权日:2003-12-17
标题 :Methods for synthesis of encoded libraries

专利号:US-10112955-B2
优先权日:2015-10-29
标题 :Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
发明人：SPRENGELER PAUL A; REICH SIEGFRIED H; ERNST JUSTIN T; WEBBER STEPHEN E; SHAGHAFI MIKE; MURPHY DOUGLAS; TRAN CHINH
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n nFor Formula I compounds A 1 , A 2 , A 3 , A 4 , A 5 , W 1 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 , R 8 , R 8a , R 8b , R 9 , R 9a , R 9b , and R 10 and subscript “nâ€? are as defined in the specification. The inventive Formula I 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:US-12304912-B2
优先权日:2020-07-28
标 题 :Fused bicyclic RAF inhibitors and methods for use thereof
发明人：BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA
权利人:JAZZ PHARMACEUTICALS IRELAND LTD
摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.

专利号:US-7972994-B2
优先权日:2003-12-17
标 题 :Methods for synthesis of encoded libraries