CAS: 663619-89-4; 7-Methyl-2-Morpholino-9-(1-(Phenylamino)Ethyl)-4H-Pyrido[1,2-A]Pyrimidin-4-One

上下游产品

aniline 3-bromo-5-methylpyridin-2-amine 9-bromo-2-hydroxy-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 066TGX066 1TGX-D1 2-SL-TGXNH2-SL-TGX

2-氨基-3-溴-5-甲基吡啶置于(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,Sodium Tetrahydroborate,甲基磺酰氯,三乙胺,N,N-二异丙基乙胺体系中,用 甲醇,二氯甲烷,甲苯 作为反应溶剂,化学反应 5.0H,反应生成 7-甲基-2-(吗啉-4-基)-9-[1-(苯氨基)乙基]吡啶并[1,2-A]嘧啶-4-酮
参考文献:Development Of A Peptide-drug Conjugate For Prostate Cancer Therapy
标题:Development Of A Peptide-drug Conjugate For Prostate Cancer Therapy
摘要:Tgx-221 Is A Highly Potent Phosphoinositide 3-Kinase Beta (Pi3K Beta) Inhibitor That Holds Great Promise As A Novel Chemotherapeutic Agent To Treat Prostate Cancer. However,Poor Solubility And Lack Of Targetability Limit Its Therapeutic Applications. The Objective Of This Present Study Is To Develop A Peptide-Drug Conjugate To Specifically Deliver Tgx-221 To Her2 Overexpressing Prostate Cancer Cells. Four Tgx-221 Derivatives With Added Hydroxyl Groups Were Synthesized For Peptide Conjugation. Among Them,Tgx-D1 Exhibited A Similar Bioactivity To Tgx-221,And It Was Selected For Conjugation With A Peptide Promoiety Containing A Her2-Targeting Ligand And A Prostate Specific Antigen (Psa) Substrate Linkage. From This Selection,The Peptide-Drug Conjugate Was Proven To Be Gradually Cleaved By Psa To Release Tgx-D1. Cellular Uptake Of The Peptide-Drug Conjugate Was Significantly Higher In Prostate Cancer Cells Compared To The Parent Drug. Moreover,Both The Peptide-Drug Conjugate And Its Cleaved Products Demonstrated Comparable Activities As The Parent Drug Tgx-D1. Our Results Suggest That This Peptide-Drug Conjugate May Provide A Promising Chemotherapy For Prostate Cancer Patients.
DOI:10.1021/mp200007B

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-2023192682-A1
优先权日:2019-11-14
标题:Improved synthesis of kras g12c inhibitor compound

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:WO-2020102730-A1
优先权日:2018-11-16
标 题:Improved synthesis of key intermediate of kras g12c inhibitor compound