CAS: 206873-63-4; N-(2-((4-(2-(6,7-Dimethoxy-3,4-Dihydroisoquinolin-2(1H)-yl)Ethyl)Phenyl)Carbamoyl)-4,5-Dimethoxyphenyl)Quinoline-3-Carboxamide

上下游产品

2-amino-N-{4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-phenyl}-4,5-dimethoxybenzamide quinoline-3-carbonyl chloride 4,5-dimethoxy-2-nitro-benzoic acid quinoline-3-carboxylic acid

📜6-硝基藜芦酸置于氯化亚砜,Palladium 10% On Activated Carbon,氢气,甲酸铵,碳酸氢钠体系中,用 甲醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 35.0H,反应生成2-醛基-4-甲氧基苯硼酸
参考文献:Reversal Of P-Gp And Bcrp-Mediated Mdr By Tariquidar Derivatives
标题:Reversal Of P-Gp And Bcrp-Mediated Mdr By Tariquidar Derivatives
摘要:With An Aim To Generate Non-Toxic,Specific And Highly Potent Multidrug Resistance (Mdr) Modulators,A Novel Series Of Anthranilic Acid Amide-Substituted Tariquidar Derivatives Were Synthesized. The New Compounds Were Evaluated For Their Cytotoxicity Toward Normal Human Colon Fibroblasts (Ccd18-Co),Human Gastric Epithelial Cell Line (Hfe) And Primary Rat Liver Cells,And For Their Ability To Inhibit P-Gp/bcrp-Mediated Drug Efflux And Reversal Of P-Gp And Bcrp-Mediated Mdr In Parental And Drug-Resistant Cancer Cell Lines (Lcc6 Mdr1,Mcf-7 Flv1000,R-Hepg2,Sw620-Ad300). While Tariquidar Is Highly Toxic To Normal Cells,The New Derivatives Exhibited Much Lower Or Negligible Cytotoxicity. Some Of The New Tariquidar Derivatives Inhibited Both P-Gp And Bcrp-Mediated Drug Efflux Whereas A Few Of Them Bearing A Sulfonamide Functional Group (1,5,And 16) Are Specific To P-Gp. The New Compounds Were Also Found To Potentiate The Anticancer Activity Of The Transporter Substrate Anticancer Drugs In The Corresponding Transporter-Overexpressing Cell Lines. The Extent Of Resistance Reversal Was Found To Be Consistent With The Transporter Inhibitory Effect Of The New Derivatives. To Further Understand The Mechanism Of P-Gp And Bcrp Inhibition,The Tariquidar Derivatives Were Found To Interact With The Transporters Using An Antibody-Based Uic2 Or 5D3 Shift Assay. Moreover,The Transporters-Inhibiting Derivatives Were Found To Modulate The Atpase Activities Of The Two Mdr Transporters. Our Data Thus Advocate Further Development Of The New Compounds For The Circumvention Of Mdr. (C) 2015 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2015.06.049

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-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

专利号:US-2025241876-A1
优先权日:2023-07-19
标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof
发明人：QUAY STEVEN CARL
权利人:ATOSSA THERAPEUTICS INC
摘要:Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

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