专利号:US-10323010-B2 优先权日:2015-07-20 标题 :Methods of chemical synthesis of substituted 10H-phenothiazine-3,7-diamine compounds 发明人:STOREY JOHN MERVYN DAVID; LARCH CHRISTOPHER PAUL; KEMP STEVEN JOHN; CLUNAS SCOTT; NICOLL SARAH LOUISE; GIBBARD HELEN SARAH; SIMPSON MICHAEL; SINCLAIR JAMES PETER; MARSHALL COLIN 权利人:WISTA LAB LTD 摘要:The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.
专利号:US-5872244-A 优先权日:1994-09-02 标 题:3' protected nucleotides for enzyme catalyzed template-independent creation of phosphodiester bonds 发明人:HIATT ANDREW C; ROSE FLOYD 权利人:HIATT ANDREW C; ROSE FLOYD D 摘要:A method for the stepwise creation of phosphodiester bonds between desired nucleosides resulting in the synthesis of polynucleotides having a predetermined nucleotide sequence by preparing an initiation substrate containing a free and unmodified 3'-hydroxyl group; attaching a mononucleotide selected according to the order of the predetermined nucleotide sequence to the 3'-hydroxyl of the initiating substrate in a solution containing a catalytic amount of an enzyme capable of catalyzing the 5' to 3' phosphodiester linkage of the 5'-phosphate of the mononucleotide to the 3'-hydroxyl of the initiating substrate, wherein the mononucleotide contains a protected 3'-hydroxyl group, whereby the protected mononucleotide is covalently linked to the initiating substrate and further additions are hindered by the 3'-hydroxyl protecting group. Methods in which a mononucleotide immobilized on a solid support is added to a free polynucleotide chain are also disclosed.
专利号:US-5763594-A 优先权日:1994-09-02 标 题:3' protected nucleotides for enzyme catalyzed template-independent creation of phosphodiester bonds 发明人:HIATT ANDREW C; ROSE FLOYD 权利人:HIATT ANDREW C; ROSE FLOYD D 摘要:A method for the stepwise creation of phosphodiester bonds between desired nucleosides resulting in the synthesis of polynucleotides having a predetermined nucleotide sequence by preparing an initiation substrate containing a free and unmodified 3'-hydroxyl group; attaching a mononucleotide selected according to the order of the predetermined nucleotide sequence to the 3'-hydroxyl of the initiating substrate in a solution containing a catalytic amount of an enzyme capable of catalyzing the 5' to 3' phosphodiester linkage of the 5'-phosphate of the mononucleotide to the 3'-hydroxyl of the initiating substrate, wherein the mononucleotide contains a protected 3'-hydroxyl group, whereby the protected mononucleotide is covalently linked to the initiating substrate and further additions are hindered by the 3'-hydroxyl protecting group. Methods in which a mononucleotide immobilized on a solid support is added to a free polynucleotide chain are also disclosed.
专利号:US-5808045-A 优先权日:1994-09-02 标 题 :Compositions for enzyme catalyzed template-independent creation of phosphodiester bonds using protected nucleotides 发明人:HIATT ANDREW C; ROSE FLOYD 权利人:HIATT ANDREW C; ROSE FLOYD D 摘要:A method for the stepwise creation of phosphodiester bonds between desired nucleosides resulting in the synthesis of polynucleotides having a predetermined nucleotide sequence by preparing an initiation substrate containing a free and unmodified 3'-hydroxyl group; attaching a mononucleotide selected according to the order of the predetermined nucleotide sequence to the 3'-hydroxyl of the initiating substrate in a solution containing a catalytic amount of an enzyme capable of catalyzing the 5' to 3' phosphodiester linkage of the 5'-phosphate of the mononucleotide to the 3'-hydroxyl of the initiating substrate, wherein the mononucleotide contains a protected 3'-hydroxyl group, whereby the protected mononucleotide is covalently linked to the initiating substrate and further additions are hindered by the 3'-hydroxyl protecting group. Methods in which a mononucleotide immobilized on a solid support is added to a free polynucleotide chain are also disclosed.
专利号:WO-2017013174-A1 优先权日:2015-07-20 标 题 :Methods of chemical synthesis of substituted 10h-phenothiazine-3,7-diamine compounds
专利号:US-2018208565-A1 优先权日:2015-07-20 标题:Methods of chemical synthesis of substituted 10h-phenothiazine-3,7-diamine compounds
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合成参考文献
参考文献:10.1517/14656566.9.12.2175 摘要:Manenti L, Tansinda P, Vaglio A. Eprodisate in amyloid A amyloidosis: a novel therapeutic approach Expert Opin Pharmacother. 2008 Aug;9(12):2175–80. doi: 10.1517/14656566.9.12.2175. 参考文献:10.1080/13506129.2017.1284056 摘要:Dasgupta NR, Cummings OW, Phillips CL, Benson MD. AA cardiomyopathy. Amyloid. 2017 Mar;24(sup1):138–9. doi: 10.1080/13506129.2017.1284056. 参考文献:10.1007/s10934-025-01792-z 摘要:Hu A, Wang H. Synthesis and alcoholysis applications of zirconium imidazole propyl sulfonate. J Porous Mater. 2025 Apr 22;32(5):1741–50. doi: 10.1007/s10934-025-01792-z.