124737-24-2Relevant articles and documents
Discovery of ANA975: An oral prodrug of the TLR-7 agonist isatoribine
Xiang, Alan X.,Webber, Stephen E.,Kerr, Bradley M.,Rueden, Erik J.,Lennox, Joseph R.,Haley, Gregory J.,Wang, Tingmin,Ng, John S.,Herbert, Mark R.,Clark, David L.,Banh, Virginia N.,Li, Wei,Fletcher, Simon P.,Steffy, Kevin R.,Bartkowski, Darian M.,Kirkovsky, Leonid I.,Bauman, Lisa A.,Averett, Devron R.
, p. 635 - 640 (2007)
ANA975, a 5-amino-3-β-D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2- one derivative, was synthesized in the search of an oral prodrug of isatoribine, a small molecule toll-like receptor 7 (TLR-7) agonist. Several strategies were studied to enable the kilogram-scale synthesis of ANA975. Three general total syntheses are described. In the phase I clinical study of ANA975 against hepatitis C virus (HCV), conversion to isatoribine in plasma was rapid and effective, delivering levels of isatoribine that have been shown to be clinically relevant. Copyright Taylor & Francis Group, LLC.
3-β-D-RIBOFURANOSYLTHIAZOLO[4,5-d]PYRIDIMINE NUCLEOSIDES AND USES THEREOF
-
Page/Page column 79; 80, (2010/02/15)
The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
Immune system enhancing 3-β-d-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and nucleotides
-
, (2008/06/13)
Compounds of the structure: STR1 wherein R4, R5, R6 and R7 individually are H, OH or C1 -C18 O-acyl and R3 is H, C1 -C18 acyl or STR2 or R5 and R7 are H or OH, R6 is H and together R3 and R4 are STR3 and X is =O or =S; Y is --OH, --SH, --Nh2 or halogen; and Z is H , --Nh2, --OH or halogen; wherein halogen is Cl or Br; or pharmaceutically acceptable salt thereof are useful as antivirals, antitumors, antimetastatics and as immune system enhancers.
