阿巴卡韦置于硫酸体系中,用 乙腈 用作溶剂,化学反应 2.0H,反应生成硫酸阿巴卡韦 参考文献: Novel Crystalline Forms Of Abacavir Sulfate[fr] Nouvelles Formes Cristallines De Sulfate D'Abacavir 标题: Novel Crystalline Forms Of Abacavir Sulfate[fr] Nouvelles Formes Cristallines De Sulfate D'Abacavir 摘要:本发明涉及阿巴卡韦硫酸盐的新型晶体形式,以及其制备方法和含有它们的药物组合物.
专利信息
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-11845970-B2 优先权日:2016-01-15 标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins 发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN 权利人:UNIV MARYLAND 摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.
专利号:WO-2005105153-A1 优先权日:2004-04-30 标 题 :Hydroxyalkyl derivatives of biologically active compounds 发明人:DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL 权利人:KOPRAN RES LAB LTD; DESHPANDE JAYANT VENKATESH; KADAM VAISHALI MADHUKAR; GUPTE VANDANA SANDEEP; RANBHAN KAMLESH JAYANTILAL 摘要:Hydroxyalkyl derivatives of biologically active compounds represented by the formula VII wherein R2 = H, CI-12 alkyl, C6-12 aryl, or -OH and D = Biologically active agent having functional groups such as Formula (a) epoxy or aziridine and Z' = Formula (b) L= spacer comprising (un)substituted alkyl, hydroxyalkyl or alkoxy alkyl with the condition that the carbon chain length contains 2 to 6 carbon atoms when Z' = Formula (c) and pharmaceutically acceptable acid addition salts and enantiomers thereof Also process for the synthesis of compounds of the Formula VII and pharmaceutically acceptable acid addition salts and enantiomers thereof comprising condensation of the biologically active agents having functional groups such as Formula (d) epoxy or azifidine with substituted alkyl derivatives under alkaline conditions, at 20 - 80°C, in an organic solvent.
专利号:US-2010204463-A1 优先权日:2007-08-07 标题 :Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation 发明人:LIOTTA DENNIS C; LI YONGFENG 权利人:LIOTTA DENNIS C; LI YONGFENG 摘要:This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.
专利号:US-9994550-B2 优先权日:2014-01-07 标题 :Heterocyclic modulators of lipid synthesis for use against cancer and viral infections 发明人:WAGMAN ALLAN S; JOHNSON RUSSELL J; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREG; OHOL-GUPTA YAMINI; HEUER TIMOTHY; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds.
专利号:US-2024400552-A1 优先权日:2016-11-11 标题 :Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
1: Dean L. Abacavir Therapy and HLA-B*57:01 Genotype. 2015 Sep 1 [updated 2018 Apr 18]. In: Pratt V, McLeod H, Dean L, Malheiro A, Rubinstein W, editors. Medical Genetics Summaries [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK315783/ doi: 10.7573/dic.212519. eCollection 2018. Review. 3: Gerogianni K, Tsezou A, Dimas K. Drug-Induced Skin Adverse Reactions: The Role of Pharmacogenomics in Their Prevention. Mol Diagn Ther. 2018 Mar 21. doi: 10.1007/s40291-018-0330-3. [Epub ahead of print] Review. doi: 10.1155/2017/3186328. Epub 2017 Nov 23. Review. 5: Redwood AJ, Pavlos RK, White KD, Phillips EJ. HLAs: Key regulators of T-cell-mediated drug hypersensitivity. HLA. 2018 Jan;91(1):3-16. doi: 10.1111/tan.13183. Review.
合成参考文献
摘要:McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 621 参考文献:10.1128/aac.00434-08 摘要:Saitoh A, Haas RH, Naviaux RK, Salva NG, Wong JK, Spector SA. Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. Antimicrob Agents Chemother. 2008 Aug;52(8):2825–30.