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US 2003/0147844 A1Published application
Polymeric thiol-linked prodrugs
AssigneeEnzon Pharmaceuticals, Inc.
InventorsYun H. Choe, Richard B. Greenwald
Life of this patent
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Abstract
Thiol-linked polymeric prodrugs and methods of making and using the same are disclosed. The use of a sulfhydryl bond as the basic link for linking the polymer to the drug allows a prodrug to be formed which takes advantage of plasma enzymes in vivo. A preferred conjugate is 1 Methods of preparing and treatment are also disclosed.
Claims17
A compound comprising the formula:
- R1—E (I)
- wherein:
- R1 is a straight or branched residue of a water soluble polymer;
- 16
- wherein:
- D1 is residue of a —SH containing moiety;
- (AA) is an amino acid residue;
- 17
- E2 and E3 are independently H,
- 18
- Y1, Y2 and Y3 are independently O, S or NR7;
- X1 and X2 are independently OH or E;
- R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are independently selected from the group consisting of H, 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;
- n is zero or a positive integer;
- and
- p is zero or a positive integer.
13 more elements
Dependencies are inferred from the claim text.