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US 12,673,104 B2Granted
Cleavable polymer drug conjugates
AssigneeRs Arastirma Egitim Danismanlik Ilac Sanayi Ticaret Anonim Sirketi
InventorsRana Sanyal, Amitav Sanyal, Mehmet Arslan, Burcu Sumer Bolu, Ozgul Gok, Merve Karacivi, Sadik Kaga
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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.
Claims11
A polymer-drug conjugate having a formula I
- wherein
- R1 and R2 are independently selected from —CH3;
- R3 is selected from —H or —CH3;
- 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 C1-C10 substituted or hetero substituted hydrocarbon comprising two or more functional groups selected from the group consisting of disulfide, carbonate, carbamate, or a combination thereof.
12 more elements
Dependencies are inferred from the claim text.