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Title:
4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/053216
Kind Code:
A3
Abstract:
The present invention is directed to 4'-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4'-substituted nucleoside derivatives of Formula (I) and derivatives thereof.

Inventors:
GIRIJAVALLABHAN, Vinay, M. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MCLAUGHLIN, Mark (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
CLEATOR, Edward (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
KONG, Jongrock (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
GIBSON, Andrew William (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
LIEBERMAN, David, R. (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
DIEGUEZ VAZQUEZ, Alejandro (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
KEEN, Stephen Philip (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
WILLIAMS, Michael, J. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MOORE, Jeffrey, C. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MILCZEK, Erika, M. (107 Thompson Street, Apt. 2, New York New York, 10012, US)
PENG, Feng (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
BELYK, Kevin, M. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
SONG, Zhiguo Jake (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
Application Number:
US2016/052409
Publication Date:
March 30, 2017
Filing Date:
September 19, 2016
Export Citation:
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Assignee:
MERCK SHARP & DOHME CORP. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MERCK SHARP & DOHME LIMITED (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
GIRIJAVALLABHAN, Vinay, M. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MCLAUGHLIN, Mark (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
CLEATOR, Edward (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
KONG, Jongrock (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
GIBSON, Andrew William (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
LIEBERMAN, David, R. (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
DIEGUEZ VAZQUEZ, Alejandro (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
KEEN, Stephen Philip (Hertford Road, Hoddesdon Hertfordshire EN11 9BU, 9BU, GB)
WILLIAMS, Michael, J. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MOORE, Jeffrey, C. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
MILCZEK, Erika, M. (107 Thompson Street, Apt. 2, New York New York, 10012, US)
PENG, Feng (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
BELYK, Kevin, M. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
SONG, Zhiguo Jake (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
International Classes:
A61K38/44; C12N1/20
Foreign References:
US20140309412A12014-10-16
US20150133395A12015-05-14
Other References:
KAGEYAMA ET AL.: "Concise Synthesis of the Anti-HIV Nucleoside EFdA", BIOSCIENCE, BIOTECHNOLOGY, AND BIOCHEMISTRY, vol. 76, no. 6, 2012, pages 1219 - 1225, XP055381618
OHRUI: "Development of modified nucleosides that have supremely high anti-HIV activity and low toxicity and prevent the emergence of resistant HIV mutants", PROCEEDINGS OF THE JAPAN ACADEMY, SERIES B PHYSICAL AND BIOLOGICAL SCIENCES., vol. 87, no. 3, 11 March 2011 (2011-03-11), pages 53 - 65, XP055381625
Attorney, Agent or Firm:
MERCK SHARP & DOHME CORP. (126 East Lincoln Avenue, Rahway, New Jersey, 07065-0907, US)
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