专利号:WO-2020128469-A1 优先权日:2018-12-19 标 题 :Synthesis of 8-chloroadenosine derivatives including nuc-9701 发明人:GARLAPATI RAMESH; KOTALA MANI BUSHAN; EVANS JAMES; KENNOVIN GORDON 权利人:NuCana plc 摘要:The present invention generally relates to a novel process for the preparation of 8-chloroadenosine derivatives, and particularly NUC-9701(8-chloroadenosine-5'-O- [naphthyl(benzyloxy-L-alaninyl)] phosphate) an anticancer ProTide of 8-chloroadenosine.
专利号:US-9738679-B2 优先权日:2013-03-15 标 题:Methods of synthesizing substituted purine compounds 发明人:OLHAVA EDWARD JAMES 权利人:EPIZYME INC 摘要:The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure.
专利号:WO-2022189846-A1 优先权日:2021-03-10 标 题:NOVEL ADENOSYLMERCAPTANE DERIVATIVES AS VIRAL mRNA CAP METHYLTRANSFERASE INHIBITORS 发明人:BOBILEVA OLGA; BOBROVS RAITIS; KANEPE IVETA; KALNINS GINTS; SISOVS MIHAILS; BULA ANNA LINA; JIRGENSONS AIGARS; TARS KASPARS; JAUDZEMS KRISTAPS 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:The present invention relates to medicine, and in particular to the treatment of viral infections, more particularly to inhibitors of viral mRNA cap methyltransf erases (MTases). Even more particularly, the invention relates to adenosylmercaptane derivatives and pharmaceutical compositions thereof and their use as inhibitors for viral mRNA cap methyltransferases.
专利号:US-2004181078-A1 优先权日:1997-10-10 标 题 :Tetraphosphonate bicyclic trisanhydrides 发明人:PANKIEWICZ KRZYSZTOF W; LESIAK KRYSTYNA; WATANABE KYOICHI A 权利人:PHARMASSET LTD 摘要:Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.
专利号:US-7371852-B2 优先权日:2003-01-22 标 题 :Alkyl-linked nucleotide compositions 发明人:HARDEMAN KLASS P; HALL STEVEN E; WARE ROY W; HINKLEY LINDSAY A; JENKS MATTHEW G 权利人:SERENEX INC 摘要:Alkyl-linked nucleotide non-homogeneous solid supports and nucleotide affinity media comprising an alkyl-linked nucleotide are provided. The linker is generally a hydrophobic linker that can be a 3, 4, 5, 6, 7, 8, 9, 10, or a longer carbon chain. Also included in the invention are methods for synthesis of an alkyl-linked nucleotide, nucleotide affinity media and methods of use thereof for affinity chromatography and screening methods.
专利号:US-6713623-B2 优先权日:1996-10-09 标 题:Tetraphosphonate bicyclic trisanhydrides 发明人:PANKIEWICZ KRZYSZTOF W; LESIAK KRYSTYNA; WATANABE KYOICHI A 权利人:PHARMASSET LTD 摘要:Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.
参考标题:One-Pot Synthesis Of Nucleoside 5′-Triphosphates From Nucleoside 5′-H-Phosphonates 作者:Qi Sun,Jocelyn P. Edathil,Runzhi Wu,Eric D. Smidansky,Craig E. Cameron,Blake R. Peterson |发布日期:2008.5.1 摘要:Nucleoside 5'-Triphosphates (Ntps) Play Key Roles In Biology And Medicine. However, These Compounds Are Notoriously Difficult To Synthesize. We Describe A One-Pot Method To Prepare Ntps From Nucleoside 5'-H-Phosphonate Monoesters Via Pyridinium Phosphoramidates, And We Used This Approach To Synthesize Atp, Utp, Gtp, Ctp, Ribavirin-Tp, And 6-Methylpurine Ribonucleoside-Tp (6Meptp). Poliovirus Rna-Dependent
合成参考文献
参考文献:10.1080/14756366.2022.2070909 摘要:Kaur S, Nieto NS, McDonald P, Beck JR, Honzatko RB, Roy A, Nelson SW. Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase. Journal of Enzyme Inhibition and Medicinal Chemistry. 2022 May 05;37(1):1320–6. doi: 10.1080/14756366.2022.2070909.