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US 6,552,170 B1Granted
PEGylation reagents and compounds formed therewith
AssigneeAmgen Inc.
InventorsRobert C. Thompson, Michael T. Brewer, Tadahiko Kohno
Life of this patent
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Abstract
Compounds are disclosed having the general formula R1-X-R2, wherein R1 and R2 are biologically active groups, at least one of which is polypeptidic. X is a non-peptidic polymeric group. R1 and R2 may be the same or different. Preferred R1 and R2 groups are TNF inhibitors.
Claims15
A compound of the formula R1-X-R2, wherein:
- R1 and R2 are each a tumor necrosis factor (TNF) inhibitor polypeptide selected from:
- (a) 30 kDa TNF inhibitor or 40 kDa TNF inhibitor,
- (b) 30 kDa TNF inhibitor or 40 kDa TNF inhibitor, modified to contain at least one non-native cysteine residue, and
- (c) a biologically active portion of (a) or (b), wherein R1 and R2 bind to TNF;
- and
- X is a non-peptidic polymer defined as -Y1-(Z)n-Y2-, wherein Y1 and Y2 represent residues of activating groups and (Z)n represents a base polymeric group wherein (Z)n is selected from polyethylene glycol, polypropylene glycol, polyoxyethylated glycerol, dextran, colonic acids, poly β-amino acids or carbohydrate polymers.
3 more elements
Dependencies are inferred from the claim text.