The United States Patent and Trademark Office (USPTO) has issued a Notice of Allowance for a key patent for a platform of Heat Shock Protein 90 (Hsp90) inhibitors based on derivatives of the naturally occurring pochonin family, Pochonia chlamydospora.

The new patent directly benefits NexGenix Pharmaceuticals Inc., a privately-held company developing treatments for cancer, neurodegenerative diseases, and orphan neurogenetic disorders.

The platform of fully synthetic small molecules covered by this composition of matter patent was developed in the laboratory of Dr. Nicolas Winssinger at the University of Strasbourg (UNISTRA) and is exclusively licensed to NexGenix.

The patent, entitled “Macrocyclic Compounds Useful as Inhibitors of Kinases and Hsp90”, provides an exclusivity period until August 2027. The patent specifically covers the proprietary “scaffold” and its composition along with a large library of compounds, including NexGenix’s lead Hsp90 inhibitors aimed at cancer and neurodegenerative indications. The pochonin scaffold represents an advancement in Hsp90 inhibition beyond several molecules developed over the last decade based on radicicol and geldanamycin derivative (17-AAG) which have been shown to exhibit highly potent anti-tumor activity in numerous pre-clinical and clinical studies.

Talking about the patent, Winssinger noted: “Through a research collaboration agreement with NexGenix in 2007, we have developed a library of hundreds of molecules based on the scaffold that is covered by the patent allowed by USPTO. These molecules have been developed through an iterative process based on extensive in vitro and in vivo studies conducted by NexGenix in the selection of a lead candidate. I am looking forward to continuing these collaborative development activities.”

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X-ray crystallography studies have demonstrated deeper binding of the propriatary molecules to the Hsp90 ATP binding pocket compared to other small-molecule Hsp90 inhibitor compounds for which crystallography has been published. This generally translates to interaction deep in the protein-binding pocket with the molecule remaining longer and thus inhibiting the protein for longer periods. Another major key differentiating point of the platform is that a subset of the library of over 500 molecules developed to date has the ability to cross the blood-brain barrier and the blood spinal cord barrier, making them particularly attractive candidate therapeutics for CNS indications, such as primary and secondary tumors of the CNS and neurodegenerative disorders.

Dr. Allan Rubenstein, NexGenix’s CEO, said, “The grant of this US patent is part of a broad platform of intellectual property rights. NexGenix now has seven patent families allowed or pending covering the Company’s compounds, various uses of these compounds, and other proprietary know-how. We believe that this matrix of intellectual property provides NexGenix with a unique position to benefit from the therapeutic applications of Hsp90 inhibitors.”

The Company is currently in late stage pre-clinical development for its lead Hsp90 inhibitor with its unique ability to cross the blood-brain-barrier as a treatment for primary and metastatic brain tumors. NexGenix plans to seek regulatory approval to conduct a Phase I clinical trial to evaluate the safety, tolerability, and pharmacokinetics of its lead Hsp90 inhibitor in advanced solid tumor malignancies.

For more information:
Macrocyclic Compounds Useful as Inhibitors of Kinases and Hsp90Patent serial number: US 11/891,652. Filed: August 10, 2007. Inventors: Nicolas Winssinger, et. al. Patent abstract: The invention relates to novel derivatives, analogs and intermediates of the naturally occurring pochonin family, Pochonia chlamydospora, and to their syntheses. The invention is further related to use of these compounds as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (Hsp90).

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