氯乙醛,2-氨基-5-溴吡啶置于碳酸氢钠体系中,用 异丙醇 作为反应溶剂,以44 %的收率获得产物6-溴-咪唑并[1,2-A]吡啶 参考文献:表型筛选鉴定出可诱导多种 Aml 细胞系分化的三取代咪唑并[1,2-A]吡啶系列 标题:表型筛选鉴定出可诱导多种 Aml 细胞系分化的三取代咪唑并[1,2-A]吡啶系列 摘要:急性髓系白血病 (Aml) 是一种侵袭性白血病,长期生存率较低.虽然当前的护理标准基于细胞毒性化疗,但一种有前途的新兴方法是分化疗法.然而,目前大多数分化剂针对特定突变,并且仅对某些患者亚型有效.为了确定可能对更广泛人群有效的药物,我们使用骨髓标记物 Cd11B 进行了表型筛选,并鉴定了一系列化合物,能够在体外区分 Aml 细胞系,无论其突变状态如何.构效关系研究表明,用磺酰胺和吲唑取代甲酰胺和儿茶酚甲基醚基团分别改善了该系列的体外代谢特征,同时保持了多个细胞系中的分化特征.这种优化工作使得先导化合物能够进入体内功效测试.我们的工作支持表型筛选的前景,以鉴定诱导多种 Aml 亚型分化的新型小分子. DOI:10.1016/j.Ejmech.2023.115509
专利号:US-10226449-B2 优先权日:2013-12-20 标 题:Heterocyclic modulators of lipid synthesis and combinations thereof 发明人:HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
专利号:US-2012077802-A1 优先权日:2009-06-10 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:US-2012172350-A1 优先权日:2009-09-11 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:EP-1600451-A2 优先权日:1999-11-12 标题 :Synthesis of 2'-deoxy-l-nucleosides
专利号:EP-1600452-A2 优先权日:1999-11-12 标题 :Synthesis of 2'-deoxy-L-nucleosides
专利号:EP-1634888-A2 优先权日:1999-11-12 标题 :Synthesis of 2'-deoxy-L-nucleosides