191162-39-7 + 915019-50-0 = 915019-65-7 反应条件:1.1 Reagents: Potassium Bicarbonate Catalysts: Triphenylphosphine,Dichlorobis(Triphenylphosphine)Palladium Solvents: Dimethylformamide,Water; 60 °C; 60 °C -> 100 °C; 95 - 100 °C; 1.5 H,> 95 °C; 2 - 6 H,> 95 °C1.2 Reagents: L-(+)-Cysteine Solvents: Water; 20 Min,> 95 °C; 0.5 - 1 H,> 95 °C; 9 H,95 °C -> 0 °C; 4 H,0 °C 标题:Development Of A Robust Synthesis Of Dactolisib On A Commercial Manufacturing Scale 作者:Baenziger,Markus; Pachinger,Werner; Stauffer,Frederic; Zaugg,Werner 参考文献:Organic Process Research & Development 日期:2019 卷标:23(9) 页码:1908-1917]
= 915019-65-7 [标题:Reaction Conditions 标题:A Drug Targeting Only P110α Can Block Phosphoinositide 3-Kinase Signalling And Tumour Growth In Certain Cell Types 作者:Jamieson,Stephen; Flanagan,Jack U.; Kolekar,Sharada; Buchanan,Christina; Kendall,Jackie D.; Et Al 参考文献:Biochemical Journal 日期:2011 卷标:438(1) 页码:53-62
喹啉-3-硼酸,2-(4-(8-溴-3-甲基-2-氧代-2,3-二氢咪唑并[4,5-C]喹啉-1-基)苯基)-2-甲基丙腈置于喹啉-3-硼酸体系中,化学反应生成 苯乙氰,4-[2,3-二氢-3-甲基-2-氧代-8-(3-喹啉基)-1H-咪唑并[4,5-C]喹啉-1-基]-.Alpha.,.Alpha.-二甲基- 参考文献:Salts And Crystall Forms Of 2-Methyl-2-[4-(3-Methyl-2-Oxo-8-Quinolin-3-Yl-2,3-Dihydro-Imidazo[4,5-C]Quinolin-1-yl)-Phenyl]-Propionitrile 标题:Salts And Crystall Forms Of 2-Methyl-2-[4-(3-Methyl-2-Oxo-8-Quinolin-3-Yl-2,3-Dihydro-Imidazo[4,5-C]Quinolin-1-yl)-Phenyl]-Propionitrile 摘要:本发明涉及2-甲基-2-[4-(3-甲基-2-氧代-8-喹啉-3-基-2,3-二氢咪唑[4,5-C]喹啉-1-基)-苯基]-丙腈的特定晶体形式,其水合物和溶剂化合物,其盐及其盐的水合物和溶剂化合物,以及其制备的某些过程,含有这些晶体形式的制药组合物,并且它们在诊断方法中的使用或更好地用于治疗恒温动物,特别是人类,以及它们用作中间体或用于制备用于诊断方法或更好地用于治疗恒温动物,特别是人类的制药制剂.
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-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
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.
1: Witteck L, Jaster R. Trametinib and dactolisib but not regorafenib exert antiproliferative effects on rat pancreatic stellate cells. Hepatobiliary Pancreat Dis Int. 2015 Dec;14(6):642-50. doi: 10.1186/s12885-016-2712-4. 3: Choudhary GS, Al-Harbi S, Mazumder S, Hill BT, Smith MR, Bodo J, Hsi ED, Almasan A. MCL-1 and BCL-xL-dependent resistance to the BCL-2 inhibitor ABT-199 can be overcome by preventing PI3K/AKT/mTOR activation in lymphoid malignancies. Cell Death Dis. 2015 Jan 15;6:e1593. doi: 10.1038/cddis.2014.525. 4: Bellozi PM, Lima IV, Dória JG, Vieira ÉL, Campos AC, Candelario-Jalil E, Reis HJ, Teixeira AL, Ribeiro FM, de Oliveira AC. Neuroprotective effects of the anticancer drug NVP-BEZ235 (dactolisib) on amyloid-β 1-42 induced neurotoxicity and memory impairment. Sci Rep. 2016 May 4;6:25226. doi: 10.1038/srep25226.
合成参考文献
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