Cornell Research Foundation Inc.

Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Chee-Youb Won

Chih-Chang Chu

Yeli Zhang

Pascal Sebastian Bailon

A new class of activated polyalkylene glycol acids and their active ester reagents for conjugation to biopharmaceuticals such as polypeptides, sugars, proteins and therapeutically active small molecules to produce biologically active conjugates of these pharmaceuticals and methods for producing these conjugates.

Polyalkylene glycol acid additives

Polyethylene glycol aldehyde compounds are provided. Methods of making and using such compounds, as well as chemical intermediates are also provided.

Polyethylene glycol aldehydes

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Agent can be entrapped in the polymer network, e.g., drugs, macromolecules or synthetic or natural polymers, for controlled release therefrom. In one embodiment, a vascular stent is coated with hydrogel with therapeutic agent entrapped therein.

Hydrogel entrapping therapeutic agent and stent with coating comprising this

Pegylated T1249 polypeptide compounds are provided. Also provided are pharmaceutical compositions containing pegylated T1249 polypeptide compounds, and methods of making. Further provided are methods of inhibiting HIV infection using such compounds and compositions.

Pegylated T1249 polypeptide

Pegylated T20 polypeptide compounds are provided. Also provided are pharmaceutical compositions containing pegylated T20 polypeptide compounds, and methods of making and using such compounds and compositions.

Pegylated T20 polypeptide

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide (e.g. dextran) containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Agent can be entrapped in the polymer network, e.g., drugs, macromolecules or synthetic or natural polymers, for controlled release therefrom.

Hydrogel-forming system with hydrophobic and hydrophilic components

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide (e.g., dextran) containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Agent can be entrapped in the polymer network, e.g., drugs, macromolecules or synthetic or natural polymers, for controlled release therefrom.

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Preferably, the hydrophobic polymer is prepared by reacting the hydroxyls of a diol obtained by converting hydroxy of terminal carboxylic acid group of poly(lactic acid) to aminoethanol group, with an unsaturated group introducing compound which is acryloyl chloride or isocyanate having an unsaturated group at one end of the molecule. Preferably, the hydrophilic polymer is dextran wherein one or more hydroxyls in a glucose unit of the dextran is (are) reacted with an unsaturated group introducing compound which is acryloyl chloride or isocyanate having an unsaturated group at one end of a molecule. Agent can be entrapped in the polymer network, e.g., drugs, water-soluble macromolecules or synthetic or natural polymers, for controlled release therefrom.

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Livingston, NJ, United States of America

Chee-Youb Won