Back to results
US 8,618,124 B2Granted
Heterobifunctional polymeric bioconjugates
AssigneeBelrose Pharma, Inc.
InventorsRichard B. Greenwald, Hong Zhao
Life of this patent
Estimating the term…
Abstract
Heterobifunctional polymeric prodrug platforms for delivering biologically active compounds, including proteins, monoclonal antibodies and the like are disclosed. One preferred compound is Methods of making and using the compounds and conjugates described herein are also provided.
Claims5
A compound of the formula:
- wherein:
- X1-X6 are independently O, S or NR1;
- R44 and R44′ are independently selected polyalkylene oxides;
- R1 is selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, aralkyls, and C3-8 substituted cycloalkyls;
- R40-43 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy;
- y and y′ are independently zero or a positive integer;
- p and p′ are independently zero or one
- n and n′ are independently a positive integer;
- a and b are independently zero or a positive integer, provided that a+b is greater than or equal to 2;
- z is a positive integer;
- D10 and D11 are independently selected from the group consisting of OH, halogens, drugs, enzymes, proteins, therapeutically active compounds, dyes, chelating agents', isotope labeled compounds;
- Y7-9 are independently selected from the group consisting of O, S NR1″;
- R1″ is hydrogen or methyl;
- R9-18 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy;
- L3-4 are independently selected bifunctional linkers;
- Q is selected from the group consisting of -L5-C(═Y10)— wherein L5 is the same group that defines L3-4 and Y10 is the same group that defines Y7-9, hydrophobic moieties, bifunctional linking moieties and combinations thereof;
- l, k, m and o are independently positive integers;
- j and h are independently zero or a positive integer;
- g, i and q are independently zero or one;
- and
- B′ is selected from the group consisting of leaving groups, activating groups, OH, biologically active moieties and diagnostic agents.
18 more elements
Dependencies are inferred from the claim text.