Drug-Polymer Conjugates
AssigneePharmaEssentia Corp.
InventorsLaurence Wu, Bryan Wu, Kuo-Hsi Kao, Li-Ming Shen, Kelly Teng
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Abstract
This invention relates to a polypeptide-polymer conjugate that includes a polypeptide moiety, a polyalkylene oxide moiety, a linker connecting the polypeptide moiety with the polyalkylene oxide moiety, a first linkage between the polypeptide moiety and the linker, and a second linkage between the polyalkylene oxide moiety and the linker.
Claims37
A polypeptide-polymer conjugate comprising:
- a polypeptide moiety;
- a polyalkylene oxide moiety;
- a linker connecting the polypeptide moiety with the polyalkylene oxide moiety;
- a first linkage between the polypeptide moiety and the linker;
- and
- a second linkage between the polyalkylene oxide moiety and the linker;
- wherein the polypeptide moiety contains a human interferon-α moiety and 1-6 additional amino acid residues at the N-terminus of the human interferon-α moiety;
- the polyalkylene oxide moiety contains 1-20,000 C1-C8 alkylene oxide repeating units;
- the linker is C1-C8 alkylene, C1-C8 heteroalkylene, C3-C8 cycloalkylene, C3-C8 heterocycloalkylene, arylene, heteroarylene, aralkylene, or —Ar—X—(CH2)n—, in which Ar is arylene or heteroarylene, X is O, S, or N(R), R being H or C1-C10 alkyl, and n is 1-10;
- and each of the first and second linkages, independently, is a carboxylic ester, carbonyl, carbonate, amide, carbamate, urea, ether, thio, sulfonyl, sulfinyl, amino, imino, hydroxyamino, phosphonate, or phosphate group.
A polypeptide-polymer conjugate comprising:
- a polypeptide moiety;
- a polyalkylene oxide moiety;
- a linker connecting the polypeptide moiety with the polyalkylene oxide moiety;
- a first linkage between the polypeptide moiety and the linker;
- and
- a second linkage between the polyalkylene oxide moiety and the linker;
- wherein the polyalkylene oxide moiety contains 1-20,000 C1-C8 alkylene oxide repeating units;
- the linker is —Ar—X—(CH2)n—, in which Ar is arylene or heteroarylene, X is O, S, or N(R), R being H or C1-C10 alkyl, and n is 1-10;
- and each of the first and second linkages, independently, is a carboxylic ester, carbonyl, carbonate, amide, carbamate, urea, ether, thio, sulfonyl, sulfinyl, amino, imino, hydroxyamino, phosphonate, or phosphate group.
A compound of formula (I):
- wherein
- mPEG is a methoxy-capped polyethylene oxide moiety;
- one of R1, R2, R3, and R4 is C1-C10 alkyl substituted with CHO;
- and
- each of the other R1, R2, R3, and R4, independently, is H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl, C1-C20 heterocycloalkyl, C1-C20 heterocycloalkenyl, aryl, or heteroaryl.
A polypeptide comprising an interferon-α moiety and 1-6 additional amino acid residues at the N-terminus of the interferon-α moiety.
Dependencies are inferred from the claim text.