Out-licensing

A series of novel soluble adamantyl-oligoethyleneglycol-fullerene hybrids was prepared via Bingel-Hirsch functionalization of C60 fullerene with various adamantyl-oligoethyleneglycol malonates. As NMDA-targeted antioxidants, these compounds have...

A series of novel soluble adamantyl-oligoethyleneglycol-fullerene hybrids was prepared via Bingel-Hirsch functionalization of C60 fullerene with various adamantyl-oligoethyleneglycol malonates. As NMDA-targeted antioxidants, these compounds have potential as therapeutic agents for the treatment of neurological disorders.

Potential Applications

Novel treatment for neurological diseases:

• Multiple Sclerosis liver cancer
• Parkinson's disease
• Alzheimer’s diseases
• Similar concept deploying fullerene-based compounds with tumors targeting moieties could be developed for anticancer Photodynamic Therapy treatment.

The Need

NMDA receptor contributes importantly to the etiology and progression of many neurological diseases such as Multiple Sclerosis, Parkinson's and Alzheimer’s diseases.
The market for drugs for the treatment of neurological diseases and disorders is large, growing, and characterized by significant unmet needs that offer great opportunity. Approximately 8% of the population, worldwide, suffers from neurological diseases and disorders. Many of the approved drugs are not effective in large numbers of patients or cause significant side effects.

Advantages

• Novel and selective fullerene-based neuroprotectants.
• Water Soluble
• Specific mechanism of action via binding to NMDA receptor.
• Results in animal model for MS demonstrate both efficacy and blood brain barrier   penetration.

Stage of Development

A  new adamantyl-oligoethyleneglycol-fullerene hybrids were prepared,  in which adamantyl groups were connected to a carboxyfullerene moiety through various lengths oligoethyleneglycol (OEG) bridges.
The demonstrated solubility of the novel compounds in aqueous solution, exhibiting a substantial improvement over previously described fullerene compounds.

In vivo preclinical studies conducted at Harvard Medical School, used NOD mice model for experimental autoimmune encephalomyelitis (EAE).  This model provides an excellent platform for investigating mechanisms involved in MS pathogenesis.

The results demonstrate that the novel fullerene hybrid:
 

• Is a potent inhibitor of both clinical disease score and disease progression. 
• Is able to reduce axonal loss and demyelination.

Links

Patent

Pending ID: 2004086