Novel Bicyclic CCR5 Antagonists for Treatment of HIV/AIDS

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Track Code	65342
Categories	Medical/Health Pharmaceuticals
Keywords	Darunavir Drug Resistance HIV/AIDS Medical/Health Pharmaceuticals Protease Inhibitors
Public Abstract	Advances in the treatment of HIV-AIDS with HIV-1 protease inhibitors in combination with reverse transcriptase inhibitors, known as highly active antiretroviral therapy (HAART), has resulted in improved life expectancy and significantly reduced HIV/AIDS-related mortality in the developed world. Unfortunately, HAART suffers from adverse drug side effects, poor oral bioavailability, and drug interactions. In addition, drug-resistant HIV-1 variants have begun to emerge. Development of antiretroviral therapy with broad-spectrum activity and minimal side effects is needed for current and future HIV/AIDS treatment. Purdue University researchers developed Darunavir, brand name Prezista, a drug used to treat HIV infection. Prezista was developed by the pharmaceutical company Tibotec and is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents. It is also used in patients with drug-resistant HIV. They have also developed a new generation of protease inhibitors that are exceedingly potent and maintain potency against multidrug resistant HIV-1 variants. Dr. Ghosh's laboratory has designed, synthesized, and evaluated several different series of compounds. These novel protease inhibitors show potent enzyme inhibitory, antiviral activity, and exceptional broad-spectrum activity against highly cross-resistant mutant. Advantages: -Decreased adverse side effects -Effective against multidrug resistant HIV-1 variants -Improved bioavailability -Superior pharmacokinetic properties Potential Applications: -Medical/Healthcare -Pharmaceuticals -Drug Development -HIV/AIDS Treatment
People	Ghosh, Arun K (Project leader) Kalapala, Venkateswara Rao Mitsuya, Hiroaki
Intellectual Property	Application Date Sep 18, 2012 Type NATL-Patent Country of Filing United States Patent Number 9,062,057 Issue Date Jun 23, 2015 Application Date Mar 18, 2011 Type PCT-Patent Country of Filing WO Patent Number (None) Issue Date (None) Application Date Mar 18, 2011 Type NATL-Patent Country of Filing European Patent Patent Number (None) Issue Date (None) Application Date Mar 18, 2011 Type NATL-Patent Country of Filing Japan Patent Number (None) Issue Date (None) Application Date Mar 19, 2010 Type Provisional-Patent Country of Filing United States Patent Number (None) Issue Date (None)
Contact OTC	Purdue Office of Technology Commercialization The Convergence Center 101 Foundry Drive, Suite 2500 West Lafayette, IN 47906 Phone: (765) 588-3475 Fax: (765) 463-3486 Email: otcip@prf.org