公开(公告)号：EP1399465A2

公开(公告)日：2004-03-24

申请号：EP01935432.3

申请日：2001-05-11

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： RAINES, Ronald, T. ,  KIESSLING, Laura, L. ,  NILSSON, Bradley, L.

IPC分类号： C07K1/00

CPC分类号： C07K1/082 ,  C07F9/4866 ,  C07F9/5004 ,  C07F9/5022 ,  C07F9/5054 ,  C07K1/1072 ,  C07K1/1077

摘要： Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.

公开(公告)号：EP1200484B1

公开(公告)日：2011-10-05

申请号：EP00954149.1

申请日：2000-06-19

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： KIESSLING, Laura, L. ,  GORDON, Eva, J. ,  STRONG, Laura, E.

IPC分类号： C08G61/08 ,  B01J19/00 ,  B01J31/22 ,  C07F15/00 ,  C08F10/00 ,  C08F2/38 ,  C08F4/80 ,  B01J31/16

CPC分类号： B01J31/2265 ,  B01J19/0046 ,  B01J31/1666 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/00596 ,  B01J2219/00603 ,  B01J2219/00605 ,  B01J2219/0061 ,  B01J2219/00626 ,  B01J2219/00722 ,  B01J2219/00738 ,  B01J2231/14 ,  B01J2531/821 ,  B01J2531/825 ,  C07B2200/11 ,  C07F15/002 ,  C07F15/0046 ,  C08F10/00 ,  C40B40/14 ,  C08F2/38 ,  C08F4/80

摘要： Methods of preparing libraries of multivalent arrays and libraries made by the methods. Component multivalent arrays of a library have defined length, defined terminal functionality and defined pendant functional groups. Methods include the preparation of a multivalent array having the steps of polymerizing at least one monomer comprising at least one polymerizable group and at least one latent reactive group in the presence of a metal carbene catalyst to form a polymer template comprising at least one latent reactive group; and combining the polymer template with at least one functionalizing reagent comprising at least one reactive group under conditions effective to react the latent reactive group of the polymer template with the reactive group of the functionalizing reagent to form a multivalent array. Methods further include preparation of a telechelic polymer (mono- or bi-telechelic) that use a ruthenium or osmium carbene catalyst and a capping agent, at least one of which is functionalized.

公开(公告)号：EP1399465B1

公开(公告)日：2005-04-13

申请号：EP01935432.3

申请日：2001-05-11

申请人： Wisconsin Alumni Research Foundation

发明人： RAINES, Ronald, T. ,  KIESSLING, Laura, L. ,  NILSSON, Bradley, L.

IPC分类号： C07K1/00

CPC分类号： C07K1/082 ,  C07F9/4866 ,  C07F9/5004 ,  C07F9/5022 ,  C07F9/5054 ,  C07K1/1072 ,  C07K1/1077

公开(公告)号：EP1334118A2

公开(公告)日：2003-08-13

申请号：EP01959934.9

申请日：2001-03-21

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： KIESSLING, Laura, L. ,  STRONG, Laura, E. ,  GESTWICKI, Jason, E.

IPC分类号： C07K14/00

CPC分类号： A61K31/74 ,  A61K31/70 ,  A61K31/785 ,  A61K38/178 ,  A61K39/385 ,  B82Y30/00 ,  G01N33/5005 ,  A61K2300/00

摘要： This invention provides multivalent ligands which carry or display at least one recognition element (RE), and preferably a plurality of recognition elements, for binding directly or indirectly to cells or other biological particles or more generally by binding to any biological molecule. The multivalent ligands provided can most generally function for binding or targeting to any biological particle or molecule and particularly to targeting of cells or cell types or viruses, for cell aggregation and generally for macromolecular assembly of biological macromoleculares. The multivalent ligands of this invention are generally applicable for creating scaffolds (assemblies) of chemical or biological species, including without limitation, antigens, epitopes, ligand binding groups, ligands for cell receptors (cell surface receptors, transmembrane receptors and cytoplasmic receptors), various macromolecules (nucleic acids, carbohydrates, saccharides, proteins, peptides, etc.). In these scaffolds, the number, spacing, relative positioning and relative orientation of recognition elements can be controlled. Multivalent ligands of this invention can carry or display at least one signal recognition element (SRE), and preferably a plurality of signal recognition elements, and modulate biological responses in biological systems. The invention also relates to methods for aggregating biological particles and macromolecules and for modulating biological response employing the multivalent ligands provided.

公开(公告)号：EP1534718A1

公开(公告)日：2005-06-01

申请号：EP03757381.3

申请日：2003-06-06

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： RAINES, Ronald, T. ,  KIESSLING, Laura, L. ,  NILSSON, Bradley, L. ,  HE, Yi ,  SOELLNER, Matthew, B. ,  HINKLIN, Roland, J.

IPC分类号： C07F5/02 ,  C07K2/00 ,  C07K17/00 ,  C07K14/00

CPC分类号： C07F9/5004 ,  C07F9/5045 ,  C07K1/006 ,  C07K5/06026

摘要： The present invention provides improved methods for synthesis of phosphinothiol reagents, as well as novel protected reagents, for use in formation of amide bonds, and particularly for peptide ligation. The invention provides phosphineborane complexes useful as reagents in the formation of amide bonds, particularly for the formation of an amide bond between any two of an amino acid, a peptide, or a protein.

公开(公告)号：EP1200484A1

公开(公告)日：2002-05-02

申请号：EP00954149.1

申请日：2000-06-19

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： KIESSLING, Laura, L. ,  GORDON, Eva, J. ,  STRONG, Laura, E.

IPC分类号： C08F4/80

CPC分类号： B01J31/2265 ,  B01J19/0046 ,  B01J31/1666 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/00596 ,  B01J2219/00603 ,  B01J2219/00605 ,  B01J2219/0061 ,  B01J2219/00626 ,  B01J2219/00722 ,  B01J2219/00738 ,  B01J2231/14 ,  B01J2531/821 ,  B01J2531/825 ,  C07B2200/11 ,  C07F15/002 ,  C07F15/0046 ,  C08F10/00 ,  C40B40/14 ,  C08F2/38 ,  C08F4/80

摘要： Methods of preparing libraries of multivalent arrays and libraries made by the methods. Component multivalent arrays of a library have defined length, defined terminal functionality and defined pendant functional groups. Methods include the preparation of a multivalent array having the steps of polymerizing at least one monomer comprising at least one polymerizable group and at least one latent reactive group in the presence of a metal carbene catalyst to form a polymer template comprising at least one latent reactive group; and combining the polymer template with at least one functionalizing reagent comprising at least one reactive group under conditions effective to react the latent reactive group of the polymer template with the reactive group of the functionalizing reagent to form a multivalent array. Methods further include preparation of a telechelic polymer (mono- or bi-telechelic) that use a ruthenium or osmium carbene catalyst and a capping agent, at least one of which is functionalized.