Lipid-Polymer-Conjugates
AssigneeAstellas Pharma Europe Ltd.
InventorsJosbert Maarten Metselaar, Wilhelmus Everardus Hennick, Tom De Vringer, Leonardus Wilhelmus Theodorus De Boer, Christien Oussoren, Gerrit Storm, Peter Bruin
Life of this patent
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Abstract
Lipid conjugates of a poly-(amino acid), a poly-(amino acid derivative) or a poly-(amino acid analogue), such as poly-[N-(2-hydroxyethyl)-glutamine](PHEG), are provided.
Claims10
1-13. (canceled)
A lipid-polymer conjugate consisting of (a) an amphiphilic liquid having at least one hydrophobic apolar moiety and a hydrophilic polar head group and (b) a polymer or a monomeric precursor thereof,
- wherein the polymer is selected from the group consisting of poly[N-(2-hydroxyethyl)-L-glutamine];
- poly[N-(2-hydroxypropyl)-L-glutamine];
- poly[(2-hydroxyethyl)-L-asparagine];
- poly(DL-glutamine);
- poly(DL-asparagine);
- copolypeptide of β-alanine and hydroxyethyl-L-glutamine;
- poly[N-(2-hydroxyethyl)-L-glutamine-co-dimethylaminoethylglutamine];
- and poly(D,L-methionine sulfoxide), and
- wherein the amphiphilic lipid contains at least two hydrophobic apolar moieties and is selected from the group consisting of 1-heptadecyloctadecylamine;
- N-succinyldioctadecylamine;
- and distearylphosphatidylethanolamine.
Use of a polymer selected from the group consisting of poly[N-(2-hydroxyethyl)-L-glutamine];
- poly[N-(2-hydroxypropyl)-L-glutamine];
- poly[(2-hydroxyethyl)-L-asparagine];
- poly(DL-glutamine);
- poly(DL-asparagine);
- copolypeptide of β-alanine and hydroxyethyl-L-glutamine;
- poly[N-(2-hydroxyethyl)-L-glutamine-co-dimethylaminoethylglutamine];
- and poly(D,L-methionine sulfoxide) for preparing a lipid-polymer conjugate,
- wherein the lipid is an amphiphilic lipid containing at least two hydrophobic apolar moieties and is selected from the group consisting of 1-heptadecyloctadecylamine;
- N-succinyldioctadecylamine and distearylphosphatidylethanolamine, and
- wherein the lipid-polymer conjugate, when present at a sufficient molar concentration in a colloidal carrier composition, extends the blood circulation time of said colloidal carrier composition as compared to a colloidal carrier composition containing the amphiphilic lipid only.
Dependencies are inferred from the claim text.