Enzon, Inc.

Enzon Pharmaceuticals, Inc.

Belrose Pharma, Inc.

Richard B Greenwald

Annapurna Pendri

Hong Zhao

Anthony J Martinez

Yun Hwang Choe

Robert G Shorr

Carl W Gilbert

Mike A Clark

Alahari Arunakumari

Durgadas Bolikal

Dechun Wu

Susan L Adler, Legal Representative

Yun H Choc

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.

Heterobifunctional polymeric bioconjugates

Activated polymeric bicine derivatives such as, as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Releasable polymeric conjugates based on aliphatic biodegradable linkers

Polymer conjugates containing nucleotides and/or oligonucleotides are disclosed.

Polymeric oligonucleotide prodrugs

Activated polymeric bicine derivatives such as as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Vancomycin-polymer conjugates are disclosed. In preferred aspects, polymer residues which are hydrolysis resistant in vitro, are selectively attached to the sugar amino and/or N-methyl amino groups of vancomycin and related compounds. Vancomycin-polymer conjugates made by the methods and methods of treatment using the conjugates are also disclosed.

Prodrugs of vancomycin with hydrolysis resistant polymer linkages

Polymeric derivatives of indoles such as are disclosed. Methods of making and using the same as well as related polymeric conjugates are also disclosed.

Polymeric acyl derivatives of indoles

Methods of preparing vancomycin-polymer conjugates are disclosed. In preferred aspects, polymer residues which are preferably releasable, are selectively attached to the sugar amino and/or N-methyl amino groups of vancomycin and related compounds. Vancomycin-polymer conjugates made by the methods and methods of treatment using the conjugates are also disclosed.

Polymeric prodrugs of vancomycin

Thiol-linked polymeric prodrugs, methods of making and using the same are disclosed. The use of a sulfhydryl bond in combination with a benzyl elimination system results in the formation of prodrugs which can take advantage of plasma enzymes in vivo for regeneration of the parent molecule. A preferred prodrug in accordance with the invention is: where S-MP is 6-mercaptopurine.

Polymeric thiol-linked prodrugs employing benzyl elimination systems

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 isMethods of preparing and treatment are also disclosed.

Polymeric thiol-linked prodrugs

Polymeric prodrugs of the formula:wherein

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Somerset, NJ, United States of America

Richard B Greenwald