IP Library Granted Patent US 10,894,087
Granted Patent B2
US 10,894,087 · App. 13/995,902 · Granted Jan 19, 2021

Multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds

Inventor: Antoni Kozlowski (Huntsville, AL)
Assignee: Nektar Therapeutics
A61K47/60
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Quick Facts
Patent No.
US 10,894,087
App. No.
13/995,902
Granted
Jan 19, 2021
Kind
B2
Abstract

Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the cabazitaxel-based compound is achieved.

Claims (20)

1. A conjugate of formula:

wherein:

each R 1 is methyl;

each R 2 is methyl;

each X is —(CH 2 ) m — or —CH 2 C(O)NHCH(R 3 )—;

each m is a positive integer from 1 to about 12;

R 3 is —H; and

each n is a positive integer from 10 to about 400;

or pharmaceutically acceptable salts and solvates thereof;

wherein the conjugate has an increased tumor growth delay compared to cabazitaxel.

2. The conjugate of claim 1 of formula:

or pharmaceutically acceptable salts and solvates thereof.

3. The conjugate of claim 1 of formula:

or pharmaceutically acceptable salts and solvates thereof.

4. The conjugate of claim 1 selected from the group consisting of:

or pharmaceutically acceptable salts of each of the foregoing.

5. A composition comprising a plurality of conjugates, wherein at least 80% of the conjugates in the composition have a structure encompassed by claim 1 .

6. The composition of claim 5 , further comprising a pharmaceutical excipient.

7. The composition of claim 5 , wherein at least 85% of the conjugates in the composition have a structure encompassed by claim 1 .

8. The composition of claim 5 , wherein at least 95% of the conjugates in the composition have a structure encompassed by claim 1 .

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Apr 17, 2020
From: TC LENDING, LLC, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 053180/0009 →
RELEASE OF SECURITY INTEREST RECORDED AT REEL 31217, FRAME 0776 Recorded Oct 14, 2015
From: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 036876/0130 →
GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Oct 6, 2015
From: NEKTAR THERAPEUTICS
To: TC LENDING, LLC, AS COLLATERAL AGENT
Reel/Frame 036796/0562 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 11, 2014
From: KOZLOWSKI, ANTONI
To: NEKTAR THERAPEUTICS
Reel/Frame 033724/0316 →
SECURITY AGREEMENT Recorded Sep 16, 2013
From: NEKTAR THERAPEUTICS
To: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 031217/0776 →