CAS: 1229208-44-9; 6-(1H-Indazol-6-yl)-N-(4-Morpholinophenyl)Imidazo[1,2-A]Pyrazin-8-Amine

上下游产品

6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indazole 6-bromo-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazine-8-amine

1H-吲唑-6-硼酸频哪醇酯,6-溴-N-[4-(4-吗啉基)苯基]咪唑并[1,2-A]吡嗪-8-胺置于四(三苯基膦)钯,Sodium Carbonate体系中,用 1,4-二氧六环,水 用作溶剂,化学反应 0.58H,反应生成脾脏酪氨酸激酶(Syk)抑制剂
参考文献:Gs-9973,脾酪氨酸激酶的选择性和口服有效抑制剂的发现
标题:Gs-9973,脾酪氨酸激酶的选择性和口服有效抑制剂的发现
摘要:脾酪氨酸激酶(syk)在自身免疫,炎症和肿瘤疾病适应症中是有吸引力的药物靶标.最先进的syk抑制剂,R406,1(或它的前药形式fostamatinib,2),已在多个治疗适应症中显示出功效,但其临床进展已经由已被归因,至少部分剂量限制性不利影响的阻碍,到的脱靶活性1.预期选择性更高的syk抑制剂将提供更大的治疗窗口.在本文中,我们报告了一系列新型咪唑并[1,2-A ]吡嗪syk抑制剂的发现和优化.这项工作在gs-9973,鉴定高潮68是一种高度选择性和口服有效的syk抑制剂,目前正在针对自身免疫和肿瘤学适应症进行临床评估.
Doi:10.1021/jm500228A

专利信息

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.