N-羟基丁二酰亚胺,异氰酸甲酯置于吡啶体系中,化学反应 24.0H,以80%的收率获得n-琥珀酰亚胺基 N-甲基氨基甲酸酯 参考文献:Activated N-Nitrosocarbamates For Regioselective Synthesis Of N-Nitrosoureas 标题:Activated N-Nitrosocarbamates For Regioselective Synthesis Of N-Nitrosoureas 摘要:A Practical And Convenient Method For Synthesizing Antitumor Compounds,N-Alkyl-N-Nitrosoureas,Regioselectively Nitrosated On The Nitrogen Atom Bearing The Alkyl Group Is Proposed. N-Alkyl-N-Nitrosocarbamates Are Interesting Intermediates In These Syntheses And Yield,By Reaction With Amino Compounds,The Regioselectively Nitrosated N-Alkyl-N-Nitrosoureas. As An Interesting Example,N,N'-Bis[(2-Chloroethyl)Nitrosocarbamoyl]Cystamine,A New Attractive Oncostatic Derivative,Has Been Prepared. The Cytotoxic Activity Of These Various Compounds Were Tested On L1210 Leukemia. Doi:10.1021/jm00344A017
专利号:US-9708317-B2 优先权日:2013-11-25 标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives 发明人:ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY 权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL 摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
专利号:US-12234240-B2 优先权日:2018-08-09 标 题:Substituted imidazo[5,1-d][1,2,3,5]tetrazines for the treatment of cancer 发明人:HERGENROTHER PAUL J; FAN TIMOTHY M; SVEC RILEY L 权利人:UNIV ILLINOIS 摘要:New synthetic methods to provide access to previously unexplored functionality at the C8 position of substituted imidazo[5,1-d][1,2,3,5]tetrazines of Formula I. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM.
专利号:WO-2025068371-A1 优先权日:2023-09-28 标 题:Inhibitors of the proprotein convertase furin, methods of production thereof and use 发明人:STEINMETZER TORSTEN; LANGE ROMAN WERNER; BOLLER CHARLOTTE; FRIEBERTSHÄUSER EVA; BLOCH KONSTANTIN 权利人:PHILIPPS UNIV MARBURG 摘要:The invention relates to novel inhibitors of the serine protease furin and to related furin-like proprotein convertases according to claim 1, and to methods of synthesis thereof and to use for production of medicaments for treatment of furin-dependent viral and bacterial infection diseases, and other disorders involving furin, such as cystic fibrosis, cancer, osteoarthritis, hypertension, and neurodegenerative disorders.
专利号:US-8178527-B2 优先权日:2006-10-02 标 题 :Tetra-substituted NDGA derivatives via ether bonds and carbamate bonds and their synthesis and pharmaceutical use 发明人:CHEN QINGQI; LOPEZ ROCIO ALEJANDRA; HELLER JONATHAN DANIEL; MORRIS AMANDA JEAN 权利人:CHEN QINGQI; LOPEZ ROCIO ALEJANDRA; HELLER JONATHAN DANIEL; MORRIS AMANDA JEAN; ERIMOS PHARMACEUTICALS LLC 摘要:Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
专利号:US-9067875-B2 优先权日:2006-10-02 标 题 :Tetra-substituted NDGA derivatives via ether bonds and carbamate bonds and their synthesis and pharmaceutical use 发明人:CHEN QINGQI; LOPEZ ROCIO ALEJANDRA; HELLER JONATHAN DANIEL; MORRIS AMANDA JEAN 权利人:CHEN QINGQI; LOPEZ ROCIO ALEJANDRA; HELLER JONATHAN DANIEL; MORRIS AMANDA JEAN; ERIMOS PHARMACEUTICALS LLC 摘要:Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
专利号:CA-2090860-C 优先权日:1990-11-21 标 题:Synthesis of equimolar multiple oligomer mixtures, especially of oligopeptide mixtures