专利号:WO-2013034675-A1 优先权日:2011-09-09 标 题:Process for the synthesis of telavancin and its pharmaceutically acceptable salts as well as n-protected derivatives thereof 发明人:BENITO-GARAGORRI DAVID 权利人:SANDOZ AG; BENITO-GARAGORRI DAVID 摘要:The invention relates to a process for the preparation of telavancin, or a pharmaceutically acceptable salt thereof, wherein said process comprises a reductive alkylation of vancomycin which provides N-protected-decylaminoethylvancomycin, followed by aminomethyiation to obtain N-protected-telavancin, which is then deprotected to provide telavancin, or a pharmaceutically acceptable salt thereof. Another embodiment refers to N-protected-telavancin and pharmaceutically acceptable salts thereof, which are formed during the process of the invention.
专利号:WO-2013034676-A1 优先权日:2011-09-09 标 题 :Process for the synthesis of telavancin, its pharmaceutically acceptable salts as well as an n-protected imine-derivative of telavancin 发明人:BENITO-GARAGORRI DAVID 权利人:SANDOZ AG; BENITO-GARAGORRI DAVID 摘要:The invention relates to a process for the preparation of telavancin, or a pharmaceutically acceptable salt thereof, wherein said process comprises an alkylation of vancomycin which provides N-protected-decylaminoethylvancomycin-imine, followed by an aminomethylation to obtain N-protected-telavancin-imine, which is then reduced and deprotected to provide telavancin, or a pharmaceutically acceptable salt thereof. Another embodiment refers to N-protected-telavancin-imine which is formed during the process of the invention.
专利号:WO-0112817-A1 优先权日:1999-08-12 标题:Evolution and use of enzymes for combinathorial and medicinal chemistry 发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL 权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL 摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:EP-2753638-A1 优先权日:2011-09-09 标 题:Process for the synthesis of telavancin and its pharmaceutically acceptable salts as well as n-protected derivatives thereof