Segmented polymers and their conjugates
First Claim
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1. A water soluble polymer comprising:
- (i) a first water soluble polymer segment having at least 4 and at most about 2000 monomeric units (POLYA);
(ii) a second water soluble segment comprising 1 to about 120 monomeric units (POLYB), which has a lower molecular weight than that of POLYA and is covalently attached to POLYA through a linkage X; and
(iii) a functional group, Y, attached to POLYA or POLYB;
wherein each of POLYA and POLYB independently comprises one monomer or up to three different monomers selected from the group consisting of alkylene glycol, olefinic alcohol, vinylpyrrolidone, hydroxyalkylmethacrylamide, hydroxyalkylmethacrylate, saccharide, α
-hydroxy acid, phosphazene, oxazoline, and N-acryloylmorpholine.
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Abstract
Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.
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Citations
48 Claims
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1. A water soluble polymer comprising:
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(i) a first water soluble polymer segment having at least 4 and at most about 2000 monomeric units (POLYA); (ii) a second water soluble segment comprising 1 to about 120 monomeric units (POLYB), which has a lower molecular weight than that of POLYA and is covalently attached to POLYA through a linkage X; and (iii) a functional group, Y, attached to POLYA or POLYB; wherein each of POLYA and POLYB independently comprises one monomer or up to three different monomers selected from the group consisting of alkylene glycol, olefinic alcohol, vinylpyrrolidone, hydroxyalkylmethacrylamide, hydroxyalkylmethacrylate, saccharide, α
-hydroxy acid, phosphazene, oxazoline, and N-acryloylmorpholine. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 46, 47, 48)
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39. A method of forming a water soluble polymer comprising two or more segments, said method comprising the steps of:
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reacting a first water soluble polymer segment, having at least 4 and at most about 2000 monomeric units and having at least one first functional group Z, with a second water soluble segment, having from 1 to about 120 monomeric units and having at least one second functional group Y′
, thereby forming a covalent linkage between said first and second segments by reaction of said first and second functional groups;
wherein;said second segment has a lower molecular weight than said first segment; either said first or said second segment further comprises an additional functional group Y that is not readily reactive with either said first or said second functional group, and each of said first and second segments independently comprises one monomer or up to three different monomers which are selected from the group consisting of alkylene glycol, olefinic alcohol, vinylpyrrolidone, hydroxyalkylmethacrylamide, hydroxyalkylmethacrylate, saccharides, α
-hydroxy acid, vinyl alcohol, polyphosphazene, polyoxazoline, and N-acryloylmorpholine. - View Dependent Claims (40, 41, 42, 43, 44, 45)
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Specification