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)
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