CAS: 14160-93-1; 4-Amino-6-Chloropyrimidine-5-Carbaldehyde

相似化合物

60025-09-4 2091735-99-6 1446111-08-5

上下游产品

2,6-dichloro-pyrimidine carbaldehyde methyl 4-aminothieno[2,3-d]pyrimidine-6-carboxylate 4-amino-5-benzylmethylaminomethyl-6-chloropyrimidine 4-(6-amino-5-formyl-pyrimidin-4-yl)-piperazine-1-carboxylic acid (4-isopropoxy-phenyl)-amide

4,6-二氯-5-嘧啶甲醛置于氨体系中,用 甲苯 用作溶剂,以99%的收率获得4-氨基-6-氯-5-醛基嘧啶
参考文献:作为c-Met和vegfr-2双重抑制剂的4-氨基嘧啶-5-多聚甲醛肟的设计,合成和生物学评估
标题:作为c-Met和vegfr-2双重抑制剂的4-氨基嘧啶-5-多聚甲醛肟的设计,合成和生物学评估
摘要:C-Met / Hgf和vegfr-2 / Vegf的协同作用导致肿瘤血管生成的发展和各种人类癌症的进展.因此,同时抑制hgf / C-Met和vegf / Vegfr信号传导可能为治疗国外肿瘤患者提供一种新颖有效的治疗方法.为了实现这个目标,我们设计并合成了一系列带有4-氨基嘧啶-5-多聚甲醛肟支架的衍生物,它们是c-Met和vegfr-2的有效双重抑制剂.体外细胞增殖试验表明,大多数目标化合物对c-Met和vegfr-2均具有抑制作用,Ic 50值在纳摩尔范围内,尤其是化合物14I,18A和18B.根据进一步的体外酶分析,化合物18A被认为是最有效的化合物,其c-Met和vegfr-2的ic 50分别为210 Nm和170 Nm.之后,我们将化合物10和18A与c-Met和vegfr-2蛋白对接,并解释了这些类似物的sar.所有结果表明,18A是c-Met和vegfr-2的双重抑制剂,具有广阔的发展前景.
Doi:10.1016/j.Bmc.2016.03.061

专利信息

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:EP-4086245-A1
优先权日:2018-01-30
标 题 :Processes for preparing intermediates for the synthesis of a jak inhibitor

专利号:US-2009111810-A1
优先权日:2007-10-23
标题:Substituted pyrimidine-5-carboxamide and 5-carboxylic ester kinase inhibitors
发明人：CONNOLLY PETER J; HUGHES TERRY V; WETTER STEVEN K
权利人:CONNOLLY PETER J; HUGHES TERRY V; WETTER STEVEN K
摘要:The present invention is directed to substituted pyrimidine-5-carboxamide and 5-carboxylic ester compounds of Formula (I): n n n n n n n n n n and forms thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and L are as defined herein and their synthesis and use as kinase inhibitors for treating a chronic or acute protein kinase mediated disease.

专利号:US-8013153-B2
优先权日:2006-03-23
标 题:Substituted pyrimidine kinase inhibitors
发明人：BUTLER JEANNENE; CONNOLLY PETER J; FUENTES-PESQUERA ANGEL R; GREENBERGER LEE M; HUANG SHENLIN; LAMONTAGNE JR KENNETH R; LI RONGHUA; XU GUOZHANG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to substituted pyrimidine compounds of formula (I): n nand forms thereof, their synthesis and use for treating a chronic or acute protein kinase mediated disease, disorder or condition.

专利号:US-8367825-B2
优先权日:2005-12-21
标 题 :Substituted pyrimidinyl oxime kinase inhibitors
发明人：GUOZHANG XU; LEE LILY; HUGHES TERRY V; WETTER STEVEN K; CONNOLLY PETER J; ABAD MARTA C; EMANUEL STUART L; KAMACHI PRABHA S; MIDDLETON STEVEN A; BATTISTA KATHLEEN A; BIGNAN GILLES C
权利人:JANSSEN PHARMACEUTICA NV; GUOZHANG XU; LEE LILY; HUGHES TERRY V; WETTER STEVEN K; CONNOLLY PETER J; ABAD MARTA C; EMANUEL STUART L; KAMACHI PRABHA S; MIDDLETON STEVEN A; BATTISTA KATHLEEN A; BIGNAN GILLES C
摘要:The present invention is directed to substituted pyrimidine compounds of formula (I): n nand forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.