CAS: 371935-74-9; 3-(4-Morpholinopyrido[3',2':4,5]Furo[3,2-D]Pyrimidin-2-yl)Phenol

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CAS号371945-16-3 2-(3-甲氧基苯基)吡啶并[... | CAS号371945-06-1 3-氨基呋喃并[2,3-b]吡... | CAS号371943-84-9 3-(3-methoxyben... | CAS号371944-46-6 3-(3-甲氧基苯酰胺)呋喃并... | CAS号6602-54-6 2-氯烟腈 | CAS号371945-23-2 3-(4-氧代-3,4-二氢吡...

3-氨基-呋喃并[2,3-B]嘧啶-2-甲酸乙酯置于氨,氢溴酸,Sodium Acetate,溶剂黄146,三乙胺,Sodium Hydroxide,三氯氧磷体系中,用 甲醇,二氯甲烷,水 作为反应溶剂,化学反应 70.5H,反应生成 N,N,N-三甲基-2-[(二甲氨基)甲酰氧基]苯铵甲磺酸盐
参考文献:开发生物可利用的含硼 Pi-103 生物电子等排体 Pi-103Be.
标题:开发生物可利用的含硼 Pi-103 生物电子等排体 Pi-103Be.
摘要:Pi-103 是一种有效的双磷脂酰肌醇 3-激酶 (Pi3K)/mtor 抑制剂,但其快速的体内代谢阻碍了其进一步的临床开发.为了提高 Pi-103 的生物利用度,我们设计并合成了 Pi-103 生物电子等排体 Pi-103Be (9),其中 Pi-103 的酚羟基被硼酸酯取代,这是一种已知可提高分子生物利用度的结构修饰含有酚羟基部分.在细胞培养中,Pi-103Be 部分转化为其相应的硼酸 (10),并在较小程度上转化为活性成分 Pi-103.这种混合物有助于9 的体外活性与母体化合物相比,这表明效力降低.当通过口服管饲法对小鼠给药时,与 Pi-103 相比,9显示出显着改善的药代动力学特征,Pi-103 在相同剂量下没有显示口服生物利用度.通过曲线下面积 (Auc) 值测量的9 的药物暴露对于7为 88.2 Ng/ml*h,对于10为 8879.9 Ng/ml*h .当通过腹膜内注射
DOI:10.1016/j.Bmcl.2020.127258

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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.

专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:US-2009227575-A1
优先权日:2008-03-04
标 题 :7H-PYRROLO[2,3-H]QUINAZOLINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS
发明人：VENKATESAN ARANAPAKAM MUDUMBAI; CHEN ZECHENG; DOS SANTOS OSVALDO; BROOIJMANS NATASJA; GOPALSAMY ARIAMALA
权利人:WYETH CORP
摘要:A 7H-pyrrolo[2,3-h]quinazoline compound of the formula I n n n n n n n n n n wherein Ar, R 1 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and n are as defined in the specification, and methods for making same.

专利号:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.