📜2-(3-硝基苯胺基)苯甲酸置于三氯氧磷体系中,用 Various Solvent(S) 作为反应溶剂,化学反应 1.08H,反应生成 尼曲吖啶 参考文献:Acheson,R. Morrin; Constable,Edwin C.; Wright,R. Gordon Mcr.,Journal Of Chemical Research,Miniprint,1983,# 1,P. 101-132 标题:Acheson,R. Morrin; Constable,Edwin C.; Wright,R. Gordon Mcr.,Journal Of Chemical Research,Miniprint,1983,# 1,P. 101-132
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-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-2022118123-A1 优先权日:2019-02-22 标 题 :Combination of ar antagonists and targeted thorium conjugates 发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY 权利人:BAYER AG; BAYER AS 摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
专利号:US-2023192682-A1 优先权日:2019-11-14 标题:Improved synthesis of kras g12c inhibitor compound
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合成参考文献
参考文献:10.1007/bf03190006 摘要:Degterev IA, Nogueira PCL, Marsaioli AJ, Verces AE. Microsomal metabolism of quinifuryl — a nitrofurylethenyl-quinolone antiseptic possessing antitumor activityin vitro. European Journal of Drug Metabolism and Pharmacokinetics. 1999 Mar;24(1):15–22. doi: 10.1007/bf03190006. 参考文献:10.1016/s1734-1140(11)70499-6 摘要:Cholewiński G, Dzierzbicka K, Kołodziejczyk AM. Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis. Pharmacol Rep. 2011;63(2):305–36. doi: 10.1016/s1734-1140(11)70499-6. 参考文献:10.1023/a:1006242321596 摘要:Adjei AA. Current status of pyrazoloacridine as an anticancer agent. Invest New Drugs. 1999;17(1):43–8. doi: 10.1023/a:1006242321596.