Boc-甘氨酸置于diborane(6)体系中,化学反应生成N-(叔丁氧羰基)乙醇胺 参考文献:"Inverse" Type Of Synthetic Inhibitors Of Trypsin,S-.Omega.-Aminoalkyl Thioesters. 标题:"Inverse" Type Of Synthetic Inhibitors Of Trypsin,S-.Omega.-Aminoalkyl Thioesters. 摘要:一系列ω-氨基烷基硫代苯甲酸酯对胰蛋白酶的抑制作用与ω-氨基烷基苯甲酸酯进行了比较.在评估的硫代酯类中,S-4-氨基丁基和s-5-氨基戊基硫代苯甲酸酯是新型"逆向"类型的最具前景的可逆抑制剂,其抑制顺序可与苯甲脒相媲美. Doi:10.1248/cpb.31.3360
专利号:US-2007122841-A1 优先权日:2005-11-30 标题:Massively parallel synthesis of proteinaceous biomolecules 发明人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 权利人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 摘要:Methods for fabricating dense arrays of polymeric molecules in a highly multiplexed manner are provided using semiconductor-processing-derived lithographic methods. Advantageously, the methods are adaptable to the synthesis of a variety of polymeric compounds. For example, arrays of peptides and polymers joined by peptide bonds may be fabricated in a highly multiplexed manner.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
专利号:US-2006009642-A1 优先权日:2001-10-12 标题 :Methods for the synthesis of substituted purines 发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G 权利人:IRM LLC 摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.
专利号:US-7339065-B2 优先权日:2003-07-21 标题 :Design and synthesis of optimized ligands for PPAR 发明人:AVERY MITCHELL A; PERSHADSINGH HARRIHAR A 权利人:BETHESDA PHARMACEUTICALS INC; UNIV MISSISSIPPI 摘要:This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.
专利号:US-10221132-B2 优先权日:2016-10-24 标题:Process for the preparation of a sulfur-amine 发明人:BARATELLA MARCO; GABOARDI MAURO; CASTALDI GRAZIANO; OLDANI ERMINIO 权利人:CHEMELECTIVA SRL 摘要:The present invention relates to a process for the synthesis of cysteamine or a salt thereof.
[参考文献]: An S, Et Al. Small-Molecule Protacs: An Emerging And Promising Approach For The Development Of Targeted Therapy Drugs. Ebiomedicine. 2018 Oct;36:553-562
合成参考文献
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