Multi-arm polymeric alkanoate conjugates

Patent metadata

Field	Value
Publication number	US-9504755-B2
Application number	US-201514948976-A
Country	US
Kind code	B2
Filing date	Nov 23, 2015
Priority date	Aug 11, 2008
Publication date	Nov 29, 2016
Grant date	Nov 29, 2016

Abstract

Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.

First claim

What is claimed is:

1. A method for synthesizing a conjugate, the method comprising the step of:
covalently attaching a multi-armed, active ester polymer bearing 4 arms to a functionalized drug;
wherein:
the multi-armed, active ester polymer bearing 4 arms has the structure:

n is an integer from about 40 to about 500;
the functionalized drug has the structure:

Drug is a residue of a hydroxyl-containing drug; and
the resulting conjugate has the structure:

2. The method of claim 1 , wherein the hydroxyl-containing drug is a taxane.

3. The method of claim 1 , wherein the hydroxyl-containing drug is a camptothecin.

4. The method of claim 1 , wherein the hydroxyl-containing drug is docetaxel.

5. The method of claim 1 , wherein the hydroxyl-containing drug is irinotecan.

6. The method of claim 1 , wherein the hydroxyl-containing drug is a vinca alkaloid.

7. The method of claim 6 , wherein the vinca alkaloid is selected from the group consisting of vincristine, vinorelbine and vinblastine.

Assignees

• Nektar Therapeutics

Inventors

• Kozlowski Antoni
• Mcmanus Samuel P
• Riggs-Sauthier Jennifer
• Shen Xiaoming
• Zhang Wen

Classifications

• A61K31/785

  Polymers containing nitrogen · CPC title

• A61K38/00

  Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) · CPC title

• A61K31/337 Primary

  having four-membered rings, e.g. taxol · CPC title

• A61K47/60

  the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol · CPC title

• A61K31/4745

  condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48) · CPC title