CAS: 173089-81-1; Isoquinoline-6-Carbaldehyde

相似化合物

106778-43-2 106778-42-1 188861-59-8

上下游产品

6-bromo-isoquinoline carbon monoxide 6-vinylisoquinoline 6-Iodoisoquinoline isoquinoline-6-carboxylic acid methyl ester

📜6-异喹啉甲酸置于二异丁基氢化铝,(Benzotriazo-1-Yloxy)Tris(Dimethylamino)Phosphonium Hexafluorophosphate,三乙胺体系中,用 四氢呋喃,正己烷,二氯甲烷 用作溶剂,化学反应 4.0H,反应生成异喹啉-6-甲醛
参考文献:带有缺电子芳烃的烯烃连接双底物模拟物对烟酰胺 N-甲基转移酶的有效抑制
标题:带有缺电子芳烃的烯烃连接双底物模拟物对烟酰胺 N-甲基转移酶的有效抑制
摘要:烟酰胺n-甲基转移酶 (Nnmt) 将烟酰胺(维生素 B3)甲基化以反应生成1-甲基烟酰胺 (Mna).Nnmt 过表达与多种疾病有关,最突出的是人类癌症,表明其作为治疗靶点的潜力.近年来,小分子 Nnmt 抑制剂的开发引起了人们的兴趣,其中最有效的抑制剂具有基于烟酰胺底物和s-腺苷-L-甲硫氨酸 (Sam) 辅因子元素的结构特征.我们在这里报告了新的双底物抑制剂的开发,其中包括缺电子的芳族基团来模拟烟酰胺部分.此外,一个跨发现-烯烃接头最适合连接这些抑制剂中的底物和辅因子模拟物.鉴定出的最有效的 Nnmt 抑制剂的 Ic 50值为 3.7 Nm,使其成为迄今为止报道的最活跃的 Nnmt 抑制剂之一.补充分析技术,建模研究和基于细胞的检测提供了对这些抑制剂的结合模式,亲和力和选择性的深入了解.
Doi:10.1021/acs.Jmedchem.1C01094

专利信息

专利号:WO-2023072969-A1
优先权日:2021-10-26
标题 :Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4
发明人：DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC; ARCHAMBAUD SYLVIE
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) wherein A, B, C, D and E are selected from the group consisting of =CH- and -N=, R 2 is selected from a hydrogen atom, a (C 1 -C 4 )alkyl group and a (C 3 -C 6 )cycloalkyl group, R 1 represents a (C 4 -C 6 )alkyl group, a (C 3 -C 8 )cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R'-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome, Alzheimer's disease, dementia and/or tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; tendinopathy and osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia, infections and for regulating body temperature.