专利号:US-8546533-B2 优先权日:2008-08-29 标 题:Pipecolic linker and its use for chemistry on solid support 发明人:MARTINEZ JEAN; ZAJDEL PAWEL; PAWLOWSKI MACIEJ; SUBRA GILLES 权利人:MARTINEZ JEAN; ZAJDEL PAWEL; PAWLOWSKI MACIEJ; SUBRA GILLES; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER 1; UNIV JAGELLONE; UNIV MONTPELLIER II 摘要:The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
专利号:US-7943775-B2 优先权日:2006-06-21 标 题:Small molecules for imaging protein-protein interactions 发明人:LI KING C; DANTHI S NARASIMHAN 权利人:US HEALTH 摘要:A tissue is imaged to detect the presence of amyloid deposits or other target proteins prior to their aggregation into plaques, with the assistance of the administration of a labeled bifunctional compound of which one functionality binds to the target protein and the second functionality binds to a chaperone protein that is present in the tissue of interest. The two functionalities have different binding affinities, the target-binding functionality having the greater binding affinity, with the result that the bifunctional compound preferentially remains in the tissue when bound to the chaperone and then the target protein while bifunctional compound that is not bound to the target protein will leave the tissue. The inclusion of the chaperone allows the imaging process to detect the non-aggregated proteins by way of the label and the difference in kinetics of the binding to the chaperone and the target protein permits one to distinguish between binding of the bifunctional molecule to the chaperone only and binding to the chaperone and then to the target protein. Certain intermediates toward the synthesis of these bifunctional compounds are novel by themselves, and labeled bifunctional molecules in general that utilize a lysine linker are also disclosed as a novel class of compounds.
专利号:CA-2831987-C 优先权日:2011-04-04 标 题 :Method for the preparation of process intermediates for the synthesis of argatroban monohydrate
专利号:CA-2960667-A1 优先权日:2011-04-04 标题:Method for the preparation of process intermediates for the synthesis of argatroban monohydrate
专利号:CA-2960667-C 优先权日:2011-04-04 标 题:Method for the preparation of process intermediates for the synthesis of argatroban monohydrate
专利号:CA-2831987-A1 优先权日:2011-04-04 标 题:Method for the preparation of process intermediates for the synthesis of argatroban monohydrate
摘要:Rodríguez-Mata, M.; Gotor-Fernández, V., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 211. 参考文献:10.1007/bf01388169 摘要:Miyazawa T. Enzymatic resolution of amino acids via ester hydrolysis. Amino Acids. 1999;16(3-4):191–213. doi: 10.1007/bf01388169.