专利号:US-7301006-B2 优先权日:2002-07-16 标 题 :Methods and materials for the synthesis of modified peptides 发明人:YOUNG TRAVIS G; KIESSLING LAURA L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.
专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-5545568-A 优先权日:1992-09-14 标题:Solid phase and combinatorial synthesis of compounds on a solid support 发明人:ELLMAN JONATHAN A 权利人:UNIV CALIFORNIA 摘要:Methods, compositions, and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, β-turn mimetics and glycerol-derived drugs is described. In order to expediently synthesize such combinatorial libraries of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.
专利号:US-11447454-B2 优先权日:2015-08-07 标题:Synthesis of benzodiazepine derivatives 发明人:BOYCE MALCOLM JAMES; THOMSEN LIV; GILBERT DONALD ALAN; WOOD DAVID 权利人:TRIO MEDICINES LTD 摘要:The invention relates to processes for the synthesis of benzodiazepine derivatives of Formula I:
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-4769445-A 优先权日:1985-03-04 标 题:Process for the solid phase synthesis of peptides which contain sulfated tyrosine 发明人:COMSTOCK JEANNE; ROSAMOND JAMES D 权利人:PENNWALT CORP 摘要:Peptides and Peptide amides such as cholecystokinin (CCK-8) are synthesized in improved yields and purity by a solid phase process. The requisite protected peptide is elaborated and sulfated on a solid support, deprotected, and cleaved from the solid support to give the total synthesis of CCK-8 on a solid support. Thereafter, the peptide is purified in a single step by ion exchange chromatography to provide analytically pure CCK-8.
1: Covington MF, Krupinski E, Avery RJ, Kuo PH. Classification schema of symptomatic enterogastric reflux utilizing sincalide augmentation on hepatobiliary scintigraphy. J Nucl Med Technol. 2014 Sep;42(3):198-202. doi: 10.2967/jnmt.114.141168. Epub 2014 Jul 17. doi: 10.1053/j.semnuclmed.2011.10.002. doi: 10.2337/db15-0220. Epub 2015 Apr 16. doi: 10.1097/RLU.0b013e3182291c7a. doi: 10.1016/j.npep.2015.08.006. Epub 2015 Aug 19. doi: 10.1111/nmo.12633. Epub 2015 Jul 22. doi: 10.1097/RLU.0000000000000913. Review.
合成参考文献
参考文献:10.1016/j.peptides.2011.06.024 摘要:Brown TA, Washington MC, Metcalf SA, Sayegh AI. The feeding responses evoked by cholecystokinin are mediated by vagus and splanchnic nerves. Peptides. 2011 Aug;32(8):1581–6. doi: 10.1016/j.peptides.2011.06.024. 参考文献:10.1097/fjc.0b013e31822bf556 摘要:Bajza Á, Németh J, Peitl B, Szilvássy Z. Block by Nitrate Tolerance of Meal-Induced Insulin Sensitization in Conscious Rabbits. Journal of Cardiovascular Pharmacology. 2011 Nov;58(5):508–13. doi: 10.1097/fjc.0b013e31822bf556.