CAS: 1082041-85-7; 5-Bromo-4-Fluoro-1H-Indazole

相似化合物

105391-70-6 1427377-75-0 885520-23-0

上下游产品

3-fluoro-2-methylaniline 4-bromo-3-fluoro-2-methylbenzenamine 4-fluoro-5-(2-trifluoromethylphenyl)-1H-indazole 5-bromo-4-fluoro-3-iodo-1H-indazole

3-氟-2-甲基苯胺置于n-溴代丁二酰亚胺(Nbs),溶剂黄146,Sodium Nitrite体系中,用 乙腈 用作溶剂,化学反应 6.0H,反应生成5-溴-4-氟 (1H)吲唑
参考文献:发现用于治疗 2 型糖尿病的新型基于吡啶酮的 Ep3 拮抗剂系列
标题:发现用于治疗 2 型糖尿病的新型基于吡啶酮的 Ep3 拮抗剂系列
摘要:发现了一系列新的吡啶酮作为有效的 Ep3 拮抗剂.由 Ep3 结合和功能测定以及 Eadme 和 Pk 分析指导的优化导致多种化合物具有非常好的物理特性,出色的口服生物利用度和干净的体外安全性.化合物13被鉴定为先导化合物,这可以通过在体外 Ins 1E β 细胞和体内大鼠 Ivgtt 模型中逆转磺胺前列酮诱导的葡萄糖刺激的胰岛素分泌抑制来证明.通过用结构43的吲唑环代替结构13的萘,消除了谷胱甘肽加合倾向.
Doi:10.1021/acsmedchemlett.0C00667

专利信息

专利号:US-12365682-B2
优先权日:2022-12-19
标 题 :Process to make GLP1 RA and intermediates therefor
发明人：ALLIAN AYMAN D; BERGLUND KENNETH DEREK; COLE KEVIN PAUL; DAVIS ASHLEE JEANETTE; HESS MOLLY; JEMISON ADRIANA; KERR MARK STEVEN; MACK AUDREY GRACE; ORTIZ-MEDINA XAVIER A; REMICK DAVID MICHAEL; STARKEY DEREK ROBERT; VAID RADHE KRISHAN; YANG QIANG; KAWAGISHI FUMIKI; EMURA TAKASHI; TSUCHIYA SATOSHI; WADAMOTO MANABU; YAMAWAKI MINORU
权利人:LILLY CO ELI; CHUGAI PHARMACEUTICAL CO LTD
摘要:The present invention relates to the synthesis of 3-[(1S,2S)-1-[5-[(4S)-2,2-dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl ]-4-methyl-6,7-dihydro-4H-pyrazolo [4,3-c] pyridine-5-carbonyl] indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one, or a salt thereof, and related synthetic intermediate compounds.

专利号:WO-2024068976-A1
优先权日:2022-09-29
标 题 :Azole derivatives as shp2 inhibitors
发明人：PETROCCHI ALESSIA; MONTALBETTI CHRISTIAN; DI FABIO ROMANO; CIAMMAICHELLA ALINA; ROSSETTI ILARIA
权利人:IRBM S P A; C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING
摘要:The present invention relates to new compounds capable of inhibiting the activity of SHP2 phosphatase. Compounds of the invention can be used for the treatment of disorders associated with SHP2 deregulation. The present invention also relates to pharmaceutical compositions containing said compounds and to their method of synthesis.