Abstract: The present invention described the administration of halogenated flosequinan derivatives and the enantiomers of halogenated flosequinan derivatives for the treatment of sexual dysfunction (in males and females) and for the treatment of cardiovascular disease.
Abstract: Compositions of the present invention comprise chlorinated heterocyclic compounds, including racemic monochloroflosequinan, purified enantiomers of monochloroflosequinan and the sulfone derivative of monochloroflosequinan. The methods of the present invention comprise the synthesis of racemic monochloroflosequinan and derivatives thereof, including the sulfone derivative. Intermediates in the synthesis are also provided. The methods further comprise the synthesis of enantiomers of monochloroflosequinan.
Abstract: Compositions of the present invention comprise carboxylated heterocyclic compounds, including carboxyflosequinan. The methods of the present invention also comprise the synthesis of carboxyflosequinan.
Abstract: Compositions of the present invention comprise dichlorinated heterocyclic compounds, including dichloroflosequinan. The methods of the present invention also comprise the synthesis of dichloroflosequinan.
Abstract: Compositions of the present invention comprise fluorinated heterocyclic compounds, including monofluoroflosequinan and difluoroflosequinan. The methods of the present invention comprise the synthesis of monofluoroflosequinan and difluoroflosequinan.
Abstract: Methods and compositions for treating specific patient groups for Central Nervous System disorders, including but not limited to Tourette Syndrome, are provided. The methods of the present invention comprise the utilization of pharmaceutical compositions comprising quinolinones (and derivatives thereof) in patients with symptoms of a Central Nervous System Disorder who are otherwise free of cardiac disease and/or who have not been given organic nitrates.
Abstract: Methods for treating specific patient groups for sexual dysfunction are provided. The methods of the present invention comprise the utilization of pharmaceutical compositions in patients who are free of cardiac disease and/or who have not been given organic nitrates.
Abstract: Compositions that are selective PDE III inhibitors and that are effective to treat sexual dysfunction in males and females, including, but not limited to, erectile dysfunction in males. The compositions comprise halogenated quinolines, isoquinolines, quinolones, thioquinolones and 2-oxoquinolones, including derivatives thereof. The compounds can be taken orally or by a number of different routes or can be used to coat the interior of a condom to induce erection.
Abstract: Methods for treating specific patient groups for gastroparesis are provided. The methods of the present invention comprise the utilization of pharmaceutical compositions comprising quinolinones (and derivatives) in patients with symptoms of gastroparesis who are otherwise free of cardiac disease and/or who have not been given organic nitrates.
Abstract: A high-yield, 4-step synthesis for flosequinan
starting with 4-fluoroanthranilic acid comprising cyclization with phosgene to create an intermediate -A, followed by methylation to create an intermediate -B, then by reaction with dimsyl sodium to create an intermediate -C, then by reaction with triethyl orthoformate in the presence of piperdine and acetic acid to give flosequinan. The overall yield of the disclosed process is greater than about 16%.
Type:
Grant
Filed:
February 7, 2001
Date of Patent:
October 23, 2001
Assignee:
R. T. Alamo Venture I LLC
Inventors:
Stephan Kwiatkowski, Maya Siddidqui, Rodney Eisenberg, Sudarsan Mukhopadhyay, Lowell Jeffry Lawrence, Steven G. Mobley