Chromeno[4,3,2-de]isoquinolines as Potent Dopamine Receptor Ligands

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Track Code	99031
Categories	Pharmaceuticals
Keywords	Compounds Dopamine Drug Development Medical/Health Pharmaceuticals
Public Abstract	According to the Parkinson's Disease Foundation, as many as one million people in the U.S. have Parkinson's disease, with approximately 60,000 new diagnoses annually. Worldwide, there are an estimated 7 to 10 million people living with this disease. Reduced dopamine transmission is known to be a cause of Parkinson's disease. While a dopamine precursor, levodopa, can be used to alleviate dopamine depletion, it has a very short pharmacokinetic life and increased doses are required over time to achieve desired therapeutic results. Dopamine agonist drugs have been used to activate post synaptic dopamine receptors and allow the available dopamine in the brain to bind efficiently to these receptors. These agonists can be used in monotherapy applications or in conjunction with the standard levodopa therapy. A compound developed by Purdue University researchers, dinoxyline(8,9-dihydroxy-1,2,3,11b- tetragydrichromeno[4,3,2-de]isoquinoline), provides a novel class of therapeutic agents for any disorder that can be treated by drugs affecting dopamine receptors. Where dihydrexidine is ten-fold D1:D2 selective and dinapsoline is five-fold D1:D2 selective, dinoxyline has an equally high affinity for both D1 and D2 receptors. This is surprising considering the structure of this new compound in comparison to related work with other dopamine agonists. The unexpected result suggests that dinoxyline may bind to the D2 receptor in another way, which could translate into unanticipated therapeutic benefits. Advantages: -Useful in treating certain cognitive disorders and dementia -Potent anti-hypertensive effects -Provides novel strategies to treat schizophrenia and drug addiction Potential Applications: -Pharmaceutical industry
People	Nichols, David E (Project leader) Grubbs, Russell A Mailman, Richard B
Intellectual Property	Application Date Jul 2, 2002 Type CON-Patent Country of Filing United States Patent Number 6,916,832 Issue Date Jul 12, 2005 Application Date Jun 20, 2000 Type NATL-Patent Country of Filing Mexico Patent Number 228804 Issue Date Jun 30, 2005 Application Date Jun 20, 2000 Type NATL-Patent Country of Filing Australia Patent Number 777522 Issue Date Feb 10, 2005 Application Date Jun 20, 2000 Type NATL-Patent Country of Filing New Zealand Patent Number 515613 Issue Date Jul 5, 2004 Application Date Jun 20, 2000 Type NATL-Patent Country of Filing European Patent Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Austria Patent Number E 240 959 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Belgium Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Cyprus Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Switzerland Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Germany Patent Number 60002867.4 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Denmark Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Spain Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Finland Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing France Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing United Kingdom Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Greece Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Ireland Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Italy Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Luxembourg Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Monaco Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Netherlands Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Portugal Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Sweden Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 20, 2000 Type RE Country of Filing Slovenia Patent Number 1192161 Issue Date May 21, 2003 Application Date Jun 21, 2000 Type Utility Patent Country of Filing United States Patent Number 6,413,977 Issue Date Jul 2, 2002 Application Date Jun 20, 2000 Type PCT-Patent Country of Filing WO Patent Number (None) Issue Date (None) Application Date Jun 20, 2000 Type NATL-Patent Country of Filing Canada Patent Number (None) Issue Date (None) Application Date Jun 20, 2000 Type NATL-Patent Country of Filing Japan Patent Number (None) Issue Date (None) Application Date Jun 20, 2000 Type NATL-Patent Country of Filing Norway Patent Number (None) Issue Date (None) Application Date Jun 20, 2000 Type NATL-Patent Country of Filing South Korea Patent Number (None) Issue Date (None) Application Date Jun 20, 2000 Type NATL-Patent Country of Filing Brazil Patent Number (None) Issue Date (None) Application Date Jun 21, 1999 Type Provisional-Patent Country of Filing United States Patent Number (None) Issue Date (None)
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