IP Library › Granted Patent US 12673104
Granted Patent B2
US 12673104 · App. 16/314,328 · Granted Jul 7, 2026

Cleavable polymer drug conjugates

Inventors: Rana Sanyal (Istanbul, TR); Amitav Sanyal (Istanbul, TR); Mehmet Arslan (Istanbul, TR); Burcu Sumer Bolu (Istanbul, TR); Ozgul Gok (Istanbul, TR); Merve Karacivi (Istanbul, TR); Sadik Kaga (Istanbul, TR)
Assignee: RS ARASTIRMA EGITIM DANISMANLIK ILAC SANAYI TICARET ANONIM SIRKETI
A61K47/32A61K47/10A61K47/183A61K47/58A61K47/60A61K47/65C08F220/286A61K31/09A61K31/337A61K31/35A61K31/4706A61K31/506A61K31/519A61K45/06C08F220/603C08F222/1063
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Quick Facts
Patent No.
US 12673104
App. No.
16/314,328
Granted
Jul 7, 2026
Kind
B2
Abstract

This invention relates to polymer drug conjugates comprising a (meth)acrylate based polymer backbone with at least two types of side chains wherein one of the side chains is a PEG chain and the other side chain comprises at least one therapeutic agent covalently bonded to a cleavable linker, methods of preparing said polymer-drug conjugates and their use for treatment of diseases such as cancer.

Claims (22)

1 . A polymer-drug conjugate having a formula I

wherein

R 1 and R 2 are independently selected from —CH 3 ; R 3 is selected from —H or —CH 3 ;

n is a natural number between 1-200;

L is a cleavable linker;

D is at least one anticancer agent selected from the group consisting of docetaxel, gemcitabine, or combretastatin;

Z is selected from —O;

A is an end group that is optionally a polymerization initiator or a fragment thereof;

B is an end group that is optionally a polymerization initiator or a fragment thereof; and

Formula I is a random copolymer,

x and y are each independently a natural number such that the polymer-drug conjugate has a molecular weight between 20 kDa to 300 kDa,

wherein the linker is selected from the group consisting of: Gly-Phe-Leu-Gly (SEQ ID NO: 1), and a C 1 -C 10 substituted or hetero substituted hydrocarbon comprising two or more functional groups selected from the group consisting of disulfide, carbonate, carbamate, or a combination thereof.

2 . The polymer drug conjugate of claim 1 wherein the linker is Gly-Phe-Leu-Gly (SEQ ID NO: 1).

3 . The polymer drug conjugate of claim 1 having the formula VI:

4 . The polymer drug conjugate of claim 1 , wherein one or both of the end groups is a polymerization initiator or a fragment thereof.

5 . The polymer-drug conjugate of claim 1 , wherein the anti-cancer agent is gemcitabine and the linker comprises disulfide.

6 . The polymer-drug conjugate of claim 1 , wherein the anti-cancer agent is gemcitabine and the linker comprises carbamate.

7 . The polymer-drug conjugate of claim 1 , wherein the anti-cancer agent is docetaxel and the linker comprises GFLG.

8 . The polymer-drug conjugate according to claim 1 , wherein the polymer conjugate comprises a first anti-cancer agent and a second-cancer agent.

9 . The polymer-drug conjugate of claim 8 , wherein the first anti-cancer agent comprises docetaxel, and the second anti-cancer agent comprises combretastatin.

10 . The polymer-drug conjugate of claim 8 , wherein the first anti-cancer agent comprises docetaxel and the second anti-cancer agent comprises gemcitabine.

11 . The polymer-drug conjugate of claim 1 for use as a medicament for therapeutic therapy of cancer.