Title:
MUTAGENIC NUCLEOSIDE ANALOGS AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2016/123397
Kind Code:
A3
Abstract:
The present disclosure provides nucleoside analogs of Formula (I) or (II). The nucleoside analogs may show multiple tautomerism and may increase the mutation of an RNA and/or DNA (be mutagenic) of a virus or cancer cell. The multiple tautomerism and mutagenesis of the nucleoside analogs may be adjusted by substituting the nucleoside analogs with one or more electron-donating groups and/or electron-withdrawing groups to increase or decrease the pK
a
(e.g., to a pK
a
between 5.5 or 8.5). The present disclosure also provides pharmaceutical compositions and kits including the nucleoside analogs and methods of treating a viral infection (e.g., influenza, HIV infection, or hepatitis) or cancer using the nucleoside analogs, pharmaceutical compositions, or kits.
Inventors:
ESSIGMANN JOHN M (US)
TOKMAKOFF ANDREI (US)
FEDELES BOGDAN I (US)
SINGH VIPENDER (US)
PENG CHUNTE (CN)
TOKMAKOFF ANDREI (US)
FEDELES BOGDAN I (US)
SINGH VIPENDER (US)
PENG CHUNTE (CN)
Application Number:
PCT/US2016/015456
Publication Date:
November 03, 2016
Filing Date:
January 28, 2016
Export Citation:
Assignee:
MASSACHUSETTS INST TECHNOLOGY (US)
International Classes:
C07H19/173; A61K31/7052; A61K31/706; A61K31/7076; A61K31/708; A61P31/12; A61P31/18; A61P31/20; A61P35/00; C07H19/04; C07H19/23
Domestic Patent References:
| WO2003018030A1 | 2003-03-06 |
Foreign References:
| US20140206639A1 | 2014-07-24 | |||
| GB2415431A | 2005-12-28 |
Other References:
D. LI ET AL: "Tautomerism provides a molecular explanation for the mutagenic properties of the anti-HIV nucleoside 5-aza-5,6-dihydro-2'-deoxycytidine", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 111, no. 32, 12 August 2014 (2014-08-12), US, pages E3252 - E3259, XP055270208, ISSN: 0027-8424, DOI: 10.1073/pnas.1405635111
Attorney, Agent or Firm:
ZHANG, Wei (Greenfield & Sacks P.C.,600 Atlantic Avenu, Boston MA, US)
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