Protein-polymer-drug conjugates
AssigneeMersana Therapeutics, Inc.
InventorsAleksandr V. Yurkovetskiy, Mao Yin, Timothy B. Lowinger, Joshua D. Thomas, Cheri A. Stevenson, Venu R. Gurijala
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Abstract
A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.
Claims19
A polymeric scaffold of Formula (Id) useful to conjugate with a protein based recognition-molecule (PBRM):
- wherein:
- the scaffold comprises poly(1-hydroxymethylethylene hydroxymethyl-formal) (PHF) having a molecular weight ranging from about 2 kDa to about 40 kDa, and wherein the disconnection between the monomeric units indicates that the units are randomly arranged;
- each occurrence of D independently is a therapeutic agent having a molecular weight of ≦5 kDa, and the
- between D and the carbonyl group denotes direct or indirect attachment of D to the carbonyl group,
- X is CH2, O, or NH;
- m is an integer from 1 to about 300,
- m1 is an integer from 1 to about 140,
- m7 is an integer from 1 to about 40,
- m3 is an integer from 1 to about 18, and
- the sum of m, m1, m3, and m7 ranges from about 15 to about 300.
A polymeric scaffold of Formula (Ic):
- wherein:
- the scaffold comprises PHF having a molecular weight ranging from about 2 kDa to about 40 kDa, and wherein the disconnection between the monomeric units indicates that the units are randomly arranged;
- X is CH2, O, or NH;
- m is an integer from 1 to about 300,
- m6 is an integer from 2 to about 180,
- m3 is an integer from 1 to about 18, and
- the sum of m, m6, and m3 ranges from about 15 to about 300.
Dependencies are inferred from the claim text.