Enzon Pharmaceuticals, Inc.

Enzon, Inc.

Belrose Pharma, Inc.

Hong Zhao

Richard B Greenwald

Annapurna Pendri

Dechun Wu

Puja Sapra

Belen Rubio

Maria Belen Rubio

Susan L Adler, Legal Representative

Jing Xia

Anthony J Martinez

Prasanna Reddy

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

The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Targeted polymeric prodrugs containing multifunctional linkers

A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as, is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.

Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers

The present invention provides polymeric delivery systems including hindered ester moieties. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Polyalkylene oxides having hindered ester-based biodegradable linkers

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

Methods for preparing substantially non-antigenic polymers having lone electron pair-containing moieties in high purity are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed. The resultant polymer-amines are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.

Methods of preparing activated polymers having alpha nitrogen groups

The invention provides hindered ester-based biodegradable linkers for the delivery of oligonucleotides in vivo, as well as method of making and using the same.

Hindered ester-based biodegradable linkers for oligonucleotide delivery

A new method of preparing a tertiary alkyl ester of a polyalkylene oxide is provided. The new method employs milder conditions that avoid the back reaction to the starting polyalkylene oxide. The tertiary alkyl ester of a polyalkylene oxide is then reacted with a suitable acid to produce a polyalkylene oxide acid.

Reacting polyalkylene oxide with base, tertiary alkyl haloacetate, then acid to prepare polyalkylene oxide carboxylic acid

A method of treating a resistant or refractory cancer in a mammal includes administering an effective amount of a compound of to the mammal. In preferred aspects, the cancer is resistant or refractory to CPT-11 or CPT therapy.

Treatment of resistant or refractory cancers with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin

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.

The present invention is directed to methods of preparing linear polymers such as polyalkylene oxides containing a terminal amine in high purity. One preferred method includes reacting a polyalkylene oxide such as polyethylene glycol containing a terminal azide with a phosphine-based reducing agent such as triphenylphosphine or an alkali metal borohydride reducing agent such as sodium borohydride in a solvent to reflux. The resultant polymer-amines are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.

Methods of preparing polymers having terminal amine groups

Improved posaconazole-based compositions and methods of treating and preventing fungal infections, cancer or metastatic diseases are disclosed. In preferred aspects, the conjugates are PEG-posaconazole conjugates in which the PEG has a molecular weight of about 20,000 daltons.

Posaconazole polymer conjugates and methods of treatment using posaconazole and polymer conjugates thereof

The present invention is directed to methods of preparing linear polymers such as polyalkylene oxides containing a terminal amine in high purity. One preferred method includes reacting a polyalkylene oxide such as polyethylene glycol containing a terminal tosylate with a protected amine salt to form a polymer containing a terminal protected amine and thereafter deprotecting the polymer containing the terminal protected amine to form the polymer having a terminal amine. The resultant polymer-amines are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.

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Edison, NJ, United States of America

Hong Zhao