CAS: 63875-01-4; 2-Methylisonicotinaldehyde

相似化合物

105250-16-6 4021-11-8 65550-32-5

上下游产品

2,4-lutidine 2-methyl-4-cyanopyridine N,N-dimethyl-2-(2-methyl-4-pyridyl)ethenamine (2-methylpyridin-4-yl)methanol (2-methylpyridin-4-yl)methanol 4-chloro-N-{5-chloro-2-[hydroxy-(2-methyl-pyridin-4-yl)-methyl]-pyridin-3-yl}-N-methoxymethyl-3-trifluoromethyl benzenesulfonamide 1-(4,4-dimethyl-1-(2-methyl-pyridin-4-ylmethyl)-6-p-tolyl-1,2,3,4-tetrahydro-quinolin-7-yl)-ethanone

📜2,4-二甲基吡啶置于sodium Periodate,正丁基锂体系中,用 四氢呋喃,正己烷,二氯甲烷,水 作为反应溶剂,化学反应 4.34H,反应生成 2-甲基-4-吡啶甲醛
参考文献:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
标题:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
摘要:用于心力衰竭的一类新型治疗药物,高效和选择性的grk2抑制剂,在体外研究中表现出增强的β-肾上腺素信号传导能力.hts将衍生物5和1,2,4-三唑衍生物24A鉴定为命中化合物.新一代的脚手架和所有部分的sar研究都产生了带有n-苄基羧酰胺部分的4-甲基-1,2,4-三唑衍生物,对grk2的活性很高,对其他激酶的选择性更高.在亚型选择性方面,这些化合物对grk1,5,6和7表现出足够的选择性,并且对grk3具有几乎相同的抑制作用.我们的药物化学努力导致发现了115H(grk2 Ic 50= 18 Nm),获得了与人grk2和grk2抑制剂的共晶体结构,该抑制剂增强了β-肾上腺素能受体(βar)介导的camp积累,并防止了用异丙肾上腺素处理过的表达β2Ar的hek293细胞中βar的内在化.因此,115H似乎是心力衰竭治疗的一种新型疗法.
DOI:10.1021/acs.Jmedchem.7B00443

专利信息

专利号:WO-2023086801-A1
优先权日:2021-11-09
标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-2024309003-A1
优先权日:2021-05-04
标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-12319691-B2
优先权日:2020-05-04
标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI
权利人:AMGEN INC; VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-12428425-B2
优先权日:2020-05-04
标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; PANTELEEV JANE; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
权利人:AMGEN INC; VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:WO-2008119569-A1
优先权日:2007-03-30
标题 :Synthesis of anthranilamides

专利号:CN-118084861-A
优先权日:2017-10-04
标 题 :Synthesis of cantharidin