Branched polymers
DCFirst Claim
1. A biologically active conjugate comprising a branched polymer covalently attached to a biologically active molecule, wherein the conjugate has the structure:
-
D-L1-(X)p—
RX′
-POLY)q wherein;
D is the biologically active molecule;
R is an aliphatic hydrocarbon having a length of at least three carbon atoms;
L1 is a linkage resulting from the reaction of a functional group on the linker (X), when present, or on the aliphatic hydrocarbon having a length of at least three carbon atoms (R) of the branched polymer and a functional group of the biologically active molecule;
each POLY is a water soluble and non-peptidic polymer that terminates with a hydroxyl or methoxy group;
X′
is —
O—
, —
NH—
, or —
S—
;
X is a linker of 1 to 10 atoms in length;
p is 0 or 1; and
q is 2,and further wherein the branched polymer has a molecular weight of about 12,000 Da to about 100,000 Da.
4 Assignments
Litigations
1 Petition
Reexamination
Accused Products
Abstract
The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.
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Citations
18 Claims
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1. A biologically active conjugate comprising a branched polymer covalently attached to a biologically active molecule, wherein the conjugate has the structure:
-
D-L1-(X)p—
RX′
-POLY)qwherein; D is the biologically active molecule; R is an aliphatic hydrocarbon having a length of at least three carbon atoms; L1 is a linkage resulting from the reaction of a functional group on the linker (X), when present, or on the aliphatic hydrocarbon having a length of at least three carbon atoms (R) of the branched polymer and a functional group of the biologically active molecule; each POLY is a water soluble and non-peptidic polymer that terminates with a hydroxyl or methoxy group; X′
is —
O—
, —
NH—
, or —
S—
;X is a linker of 1 to 10 atoms in length; p is 0 or 1; and q is 2, and further wherein the branched polymer has a molecular weight of about 12,000 Da to about 100,000 Da. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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Specification