US 7,803,777 B2 · Branched water-soluble polymers and their conjugates

Abstract

The present invention provides branched water-soluble polymers that allow two or more water-soluble polymers to be conjugated to another species. The branched polymers provide access to therapeutic agents that are conjugated at a single site to two or more water-soluble polymers. The branched polymers are based upon branch points that are simple branched alkyl structures, reactive side-chain amino acids and small peptides of reactive side-chain amino acids, and saccharides. Also provided is a method for preparing mono-disperse poly(ethylene glycol) of a well-defined and determinable molecular weight, and a method for the rational end-functionalization of poly(ethylene glycol). Conjugates of the branched water-soluble polymers with diverse species, e.g., peptides, lipids, glycolipids and small molecules are also provided.

Claims20

Dependent claims

An amino acid having the formula:

wherein
A is a member selected from O, NH, and S;
R11, R11′, R12 are independently selected from H, substituted or unsubstituted alkyl and water-soluble polymers, with the proviso that at least two of R11, R11′, R12 are water-soluble polymer moieties;
and
R14 is a nucleotide sugar or comprises a saccharide moiety conjugated to a member selected from a peptide and a lipid;
and
s is an integer selected from between 1 and 5.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

10/549,445Filed 15 Mar 2004 · us provisional application

Priority

14 Mar 2003

Published

US 2007/0032405 A18 Feb 2007

Granted

28 Sep 2010

Term ends

Not estimatedThe source records don’t support an estimate.

Classification14 codes

C07H 19/20
Purine radicals: with the saccharide radical esterified by phosphoric or polyphosphoric acids
A61K 47/60
Obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes: the organic…
C07C 237/12
The carbon skeleton being acyclic and saturated: having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon…
C07C 271/22
With the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms: to carbon atoms of hydrocarbon radicals…

Family

Application60/454,993Us provisional application · filed 14 Mar 2003

Application60/474,094Us provisional application · filed 29 May 2003

Application60/509,752Us provisional application · filed 7 Oct 2003

US 2007/0032405 A1Pre-grant publication · published 8 Feb 2007

US 7,803,777 B2This patent

From the US filing history. Foreign family members aren’t listed.

Branched water-soluble polymers and their conjugates

Life of this patent

Branched water-soluble polymers and their conjugates

Life of this patent

Abstract

Claims20