Polyoxazoline antibody-drug conjugates and methods of use
AssigneeSerina Therapeutics (AL), Inc.
InventorsJoshua D. Thomas, Randall Moreadith, Zhihao Fang
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Abstract
Polymer antibody drug conjugates including peptide linkers and methods of using such conjugates are disclosed. Polymer drug linker moieties useful to conjugate with a recognition moiety (i.e. antibody) and drug linker moieties useful to conjugate with a recognition moiety and a polymer moiety to produce the polymer antibody drug conjugates are also disclosed.
Claims25
A polymer antibody drug conjugate of Formula (I), or a pharmaceutically acceptable salt or solvate thereof:
- wherein:
- M is a recognition moiety;
- and
- S is a scaffold of Formula (II):
- wherein:
- F has Formula (III):
- wherein:
- A is A1 after conjugation to M and A2 prior to conjugation to M, wherein A1 is a divalent linker moiety connecting M to LC;
- LC is a linker moiety connecting A1 to D;
- and
- D is a drug moiety;
- and
- B1 is a polymer moiety;
- and
- p is an integer ranging from about 1 to about 8.
A scaffold of Formula (IIa), or a pharmaceutically acceptable salt or solvate thereof:
- wherein F is a drug linker moiety having Formula (IIIa), or a pharmaceutically acceptable salt or solvate thereof:
- wherein:
- A2 is a monovalent linker moiety comprising a functional group capable of forming a covalent bond with a functional group of the recognition moiety.
- LC is a linker moiety connecting A2 to D;
- and
- D is a drug moiety;
- and
- B1 is a polymer moiety.
A polymer antibody-drug conjugate having one of the following formulas:
- wherein:
- R24 is
- R25 is:
- S is the sulfur atom of an antibody (mAb) cysteine residue;
- m is an integer from about 10, 20 or 50;
- n ranges from 1 to 3;
- k indicates that the polymer units m and n and polymer units m and (n−1) are connected to each other in a random order;
- and
- p is 6 or 8.
Dependencies are inferred from the claim text.