Novel CCR5 antagonists for the treatment of HIV infection: a review of compounds patented in 2006 - 2008.
BACKGROUND
The HIV/AIDS epidemic and the resultant therapeutic efforts have continued to evolve over the last several years. The continued challenges in vaccine development, the growing longevity of the patient population and the emergence of resistant strains to current highly active antiretroviral therapy necessitate the development of new, effective therapeutics which target novel mechanism of actions. CCR5, a member of the GPCR superfamily, plays a key role as a co-receptor during the HIV viral entry process. The utility of CCR5 antagonists in the clinical setting has been validated, culminating in the launch of maraviroc (Selzentry by Pfizer (New York, NY, USA) in 2007.


METHODS
This review covers patent applications for small-molecule CCR5 selective antagonists published between 2006 and 2008 and related literature, with a focus on the treatment of HIV infection.


RESULTS
The reader will gain information on patent literature from 2006 to 2008 on CCR5 antagonists for the treatment of HIV infection.


CONCLUSIONS
A variety of new chemotypes have emerged over this period. These efforts support the potential to develop the next generation of CCR5 antagonists for the treatment of HIV with improved potency, tolerability and convenience.
Yang
Hanbiao
H
Department of Medicinal Chemistry, Roche Palo Alto LLC, 3431 Hillview Ave., Palo Alto, CA 94304, USA. hanbiaoyang@gmail.com
Rotstein
David M
DM
D016915:AIDS Vaccines / Q000627:therapeutic use; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D016503:Drug Delivery Systems; D024882:Drug Resistance, Viral; D023581:HIV Fusion Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D015658:HIV Infections / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D000077592:Maraviroc; D010330:Patents as Topic; D014230:Triazoles / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use
D016915:AIDS Vaccines; D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes; D023581:HIV Fusion Inhibitors; D014230:Triazoles; D000077592:Maraviroc