Other

Genzyme Corporation

Genzyne Corporation

Barbara Y Wan

James R Rasmussen

Marianne Borowski

Jeffrey T Davis

Shirish Hirani

Marcelo Colon

Alan E Walts

Mark M Staveski

This invention relates to a method of producing peracetyloxazolines from peracetyl saccharides. The method involves reacting the starting material, a peracetyl saccharide, with a reagent combination, to directly produce the peracetyl oxazoline. This method may be used for the activation of oligosaccharides, wherein an oligosaccharide containing a reducing GlcNAc terminus is activated by the formation of an oxazolide at the terminal GlcNAc, and then coupled with a bifunctional spacer to provide an oligosaccharide-spacer conjugate. The activated oligosaccharide-spacer conjugate is then coupled to a protein, such as granulocyte colony stimulating factor or .gamma.-interferon, providing a neoglycoprotein conjugate. The invention provides a method for forming neoglycoprotein conjugates which may improve biological and physiochemical properties of the protein. For example, serum lifetime or efficiency of drug delivery of the peptide to a target organ or cell may be improved.

Oligosaccharide oxazolines, oligosaccharide conjugates and methods of

A process is described for generating conjugates of lipids and biologically active agents to produce compositions having therapeutic utility, such as drug delivery vehicles. The process involves mixing the reactive lipid with an appropriate amount of diketene to form an acetoacetylated lipid which is then isolated, dissolved in a suitable medium, and mixed with a nucleophilic-containing biologically active agent to form a biologically active agent-lipid conjugate. Alternatively, the acetoacetylated lipid can be mixed with a polyamine to form a cationic lipid.

Process for making lipid conjugates

Novel phospholipid-saccharide conjugates are produced by the reaction of a phospholipid derivative and an activated saccharide. The resulting conjugates can be used to make liposomes which are target-specific or resistant to degradation in vivo.

Phospholipid-saccharide conjugates

An efficient, technically straightforward and inexpensive process for generating conjugates of phospholipids with biologically important molecules is described.

Phosphatidylalkanolamine derivatives and their use in generating

This invention relates to a method of producing peracetyloxazolines from peracetyl saccharides. The method involves reacting the starting material, a peracetyl saccharide, with a reagent combination, to directly produce the peracetyl oxazoline. This method may be used for the activation of oligosaccharides, wherein an oligosaccharide containing a reducing GlcNAc terminus is activated by the formation of an orazoline at the terminal GlcNAc, and then coupled with a bifunctional spacer to provide an oligosaccharide-spacer conjugate. The activated oligosaccharide-spacer conjugate is then coupled to a protein, such as granulocyte colony stimulating factor or .gamma.-interferon, providing a neoglycoprotein conjugate. The invention provides a method for forming neoglycoprotein conjugates which may improve biological and physiochemical properties of the protein. For example, serum lifetime or efficiency of drug delivery of the peptide to a target organ or cell may be improved.

Growing community of inventors

Tewksbury, MA, United States of America

Barbara Y Wan