专利号:US-4301065-A 优先权日:1977-05-25 标 题 :Novel polypeptides having thymic activity or an antagonistic activity and processes for their synthesis 发明人:BACH JEAN-FRANCOIS; DARDENNE MIREILLE; PLEAU JEAN-MARIE; HAMBURGER JEAN; BRICAS EVANGHELOS; MARTINEZ JEAN; BLANOT DIDIER; AUGER GENEVIEVE 权利人:ANVAR 摘要:The invention is concerned with novel polypeptides and processes for the synthesis thereof. It is concerned with compounds having the sequence X-Gln-Gly-Gly-Y in which Y represents -Ser-Asn and X represents Ser-, Lys-Ser-, Ala-Lys-Ser-, Glx-Ala-Lys-Ser-; Glx representing Pyro-Glu or Gln; and when X represents Glx-Ala-Lys-Ser-, Y may in addition represent -Ser; as well as their derivatives comprising one or two modified amino acids, with the exception of the unmodified compound PyroGlu-Ala-Lys-Ser-Gln-Gly-Ser-Asn. These polypeptides are useful as medicines.
专利号:US-4696932-A 优先权日:1984-10-26 标题 :Biologically-active xanthine derivatives 发明人:JACOBSON KENNETH A; DALY JOHN W; KIRK KENNETH L 权利人:US HEALTH 摘要:Certain functionalized cogeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A 1 - and A 2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity. Some of these analogs, containing a distal amino- or carboxylic-functionalized chain, are suitable for synthesis of amino acid conjugates. The compounds of this invention are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.
专利号:US-3396157-A 优先权日:1964-12-01 标 题:Use of esters of nu, nu-dialkylhydroxylamines and 1-hydroxypiperidine for the synthesis of peptides and other amides 发明人:TYNDALE YOUNG GEOFFREY; ONSLOW HANDFORD BRIAN 权利人:NAT RES DEV
专利号:US-3137684-A 优先权日:1962-05-29 标 题 :Preparation of phenyl esters via alkoxyvinyl and alkoxyacetylene intermediates and use thereof in peptide synthesis 发明人:MIKLOS BODANSZKY 权利人:OLIN MATHIESON
参考标题:Use Of The 4-Methoxy-2,6-Dimethylbenzenesulfonyl (Mds) Group To Synthesize Dynorphin (1-13) And Related Peptides. 作者:Mitsuhiro Wakimasu,Chieko Kitada,Masahiko Fujino 摘要:The Syntheses Of A Tridecapeptide Corresponding To The Amino Acid Sequence Of Dynorphin [1-13], H-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Oh, And Related Truncated Peptides, [4-13], [8-11], And [8-13], Using The 4-Methoxy-2, 6-Dimethylbenzenesulfonyl (Mds) Group For The Protection Of The Guanidino Function Of Arginine, Are Described. To Synthesize Dynorphin [1-13], Three Fragments, 1-3, 4-10, And 11-13, Were Prepared And Used As Building Blocks For The Final Construction Of The Amino Acid Sequence Of This Peptide. Final Deprotection Of The Fully Protected Peptide Was Achieved By Treatment With Trifluoroacetic Acid-Thioanisole At 50°C For 2 H And The Purification Of This Synthetic Peptide Was Effected By Column Chromatography On Cm-Cellulose. Other Truncated Peptides, [4-13], [8-11], And [8-13], Were Synthesized In The Same Manner As Described For Dynorphin [1-13]. The Applicability Of The Mds Protecting Group For The Synthesis Of Arginine-Containing Peptides Was Confirmed.
合成参考文献
参考文献:10.1055/s-0031-1290414 摘要:Synthesis of GSK2137305. Synfacts. 2012 Jun 19;8(07):0702. doi: 10.1055/s-0031-1290414. 参考文献:10.1007/978-1-4613-0907-9_3 摘要:Sabongi GJ. Triggered Release of Acids, Bases, Radicals, Nitrenes, and Carbenes. 1987. In: Chemical Triggering.