6-(4-Bromo-2-Fluorophenylamino)-7-Fluoro-3-Methyl-3H-Benzoimidazole-5-Carboxylic Acid Ethyl Ester置于盐酸,乙醇,水,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,Sodium Hydroxide体系中,用 四氢呋喃,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 24.0H,反应生成 比尼替尼 参考文献: Process Of Preparation Of Benzimidazole Compounds[fr] Procédé De Préparation De Composés De Benzimidazole 标题: Process Of Preparation Of Benzimidazole Compounds[fr] Procédé De Préparation De Composés De Benzimidazole 摘要:该应用程序提供苯并咪唑化合物的制备过程,例如binimetinib和selumetinib.此外,该申请还提供了binimetinib和selumetinib制备过程的中间体.
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-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-2024400519-A1 优先权日:2023-06-01 标 题 :Crystal forms a, b, c, d, e, f and g of selumetinib sulfate and preparation methods thereof 发明人:HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han 权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD 摘要:The present invention relates to crystal forms of A, B, C, D, E, F and G of selumetinib sulfate and the preparation method thereof. The crystal forms A, B and F of selumetinib sulfate are obtained by adding 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-vinyloxy-ethoxy)-amide (SEL-3) into an organic solvent; further, crystal form A of selumetinib sulfate can be as a raw material to prepare crystal forms C, D and E of selumetinib sulfate, and crystal form C of selumetinib sulfate can be as a raw material to prepare crystal form G of selumetinib sulfate.
专利号:US-11612610-B2 优先权日:2018-12-14 标题:Mito-magnolol compounds and methods of synthesis and use thereof 发明人:KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER 权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC 摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.