Piscataway, NJ, United States
Piscataway, NJ, United States

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Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2013-04-30

The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers.


Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2012-06-22

The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment.


Patent
Enzon Pharmaceuticals and Santaris Pharma | Date: 2011-04-04

The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5-(T_(x))G_(x)G_(x)c_(s)a_(s)a_(s)g_(s)c_(s)a_(s)t_(s)c_(s)c_(s)T_(x)G_(x)T-3 and 5-(G_(x))T_(x)a_(s)c_(s)t_(s)g_(s)c_(s)c_(s)t_(s)t_(s)c_(s)T_(x)T_(x)A-3, wherein capital letters designate a beta-D-oxy-LNA nucleotide analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript s designates a phosphorothioate link between neighbouring nucleotides/LNA nucleotide analogues, and subscript x designates either a phosphorothioate link or a phosphorodiester link between neighbouring nucleotides/LNA nucleotide analogues, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.


Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2012-12-21

Oligonucleotides directed against the hypoxia-inducible factor-1 (HIF-1) gene are provided for modulating the expression of HIF-1. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1. Methods of using these compounds for modulation of HIF-1 expression and for the treatment of diseases associated with the hypoxia-inducible factor-1 are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof.


Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2011-05-31

The invention relates to oligonucleotide compounds (oligomers), which target androgen receptor mRNA in a cell, leading to reduced expression of the androgen receptor. Reduction of the androgen receptor expression is beneficial for the treatment of certain disorders, such as a hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of androgen receptor using said oligomers, including methods of treatment.


Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2011-09-14

The invention relates to oligomer compounds (oligomers), which target beta-catening mRNA in a cell, leading to reduced expression of beta-catenin. Reduction of beta-catenin expression is beneficial for a range of medical disorders, such as hyperproliferative disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of beta-catenin using said oligomers, including methods of treatment.


Patent
Santaris Pharma and Enzon Pharmaceuticals | Date: 2012-05-22

Oligonucleotides directed against the hypoxia-inducible factor-1 (HIF-1) gene are provided for modulating the expression of HIF-1. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1. Methods of using these compounds for modulation of HIF-1 expression and for the treatment of diseases associated with the hypoxia-inducible factor-1 are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof.


Patent
Enzon Pharmaceuticals and Dana-Farber Cancer Institute | Date: 2013-02-15

The disclosure relates to oligonucleotide compounds (oligomers) that target Myc mRNA in a cell, leading to reduced expression of Myc. Reduction of Myc expression is beneficial for the treatment of certain disorders, such as hyperproliferative disorders (e.g., cancer). The disclosure provides therapeutic compositions comprising oligomers and methods for modulating the expression of Myc using said oligomers, including methods of treatment.


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.


Patent
Enzon Pharmaceuticals | Date: 2011-04-15

The present invention relates to polymeric conjugates of adenine nucleoside analogs. In particular, the invention relates to multi-arm polyethylene glycol conjugates of adenine nucleoside analogs and use thereof. The present invention, more specifically, provides polymeric conjugates of toyocamycin and its derivatives. Furthermore, the present invention provides a method for preparing the polymeric conjugates of adenine nucleoside analogs and a method of using the same for treating a cancer, inhibiting the growth or proliferation of cancer cells, treating a viral infection, treating a disease or condition associated with abnormal expression of VEGF. Most polymeric conjugates of toyocamycin was stable in PBS but released toyocamycin in vivo to provided inhibition of cancer cell growth.

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