EP 1179011 A1 20020213 - GLYCOPEPTIDE ANTIBIOTICS, COMBINATORIAL LIBRARIES OF GLYCOPEPTIDE ANTIBIOTICS AND METHODS OF PRODUCING SAME
Title (en)
GLYCOPEPTIDE ANTIBIOTICS, COMBINATORIAL LIBRARIES OF GLYCOPEPTIDE ANTIBIOTICS AND METHODS OF PRODUCING SAME
Title (de)
KOMBINATORISCHE BIBLIOTHEKEN VON GLYCOPEPTID-ANTIBIOTIKA UND VERFAHREN ZU DEREN HERSTELLUNG
Title (fr)
ANTIBIOTIQUES DE GLYCOPEPTIDE, BIBLIOTHEQUES DE COMBINAISONS D'ANTIBIOTIQUES DE GLYCOPEPTIDES ET PROCEDES DE PRODUCTION DE CES DERNIERS
Publication
Application
Priority
- US 0013679 W 20000519
- US 13483999 P 19990519
Abstract (en)
[origin: WO0069892A1] A glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified alpha -amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified alpha -amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N<+>(R1)=CR2R3, N=PR1R2R3, N<+>R1R2R3 or P<+>R1R2R3 in which Y is a single bond, O, NR1 or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention. A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic. A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.
IPC 1-7
IPC 8 full level
C07K 1/04 (2006.01); C07K 9/00 (2006.01); A61K 38/00 (2006.01)
CPC (source: EP)
C07K 1/047 (2013.01); C07K 9/008 (2013.01); A61K 38/00 (2013.01)
Citation (search report)
See references of WO 0069892A1
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 0069892 A1 20001123; AU 5141900 A 20001205; CA 2372392 A1 20001123; EP 1179011 A1 20020213; ZA 200109187 B 20030129
DOCDB simple family (application)
US 0013679 W 20000519; AU 5141900 A 20000519; CA 2372392 A 20000519; EP 00936050 A 20000519; ZA 200109187 A 20011107