US2013330297A1PendingUtilityA1

Modified 2' and 3'-nucleoside prodrugs for treating flaviviridae infections

72
Assignee: IDENIX PHARMACEUTICALS INCPriority: Jun 28, 2002Filed: Aug 2, 2013Published: Dec 12, 2013
Est. expiryJun 28, 2022(expired)· nominal 20-yr term from priority
Inventors:Richard StorerGilles GosselinJean-Pierre SommadossiPaolo Lacolla
A61K 31/7056A61K 38/21C07H 19/056C07H 19/00C07H 19/16A61K 38/212A61K 47/60A61K 45/06A61K 31/7068A61K 31/708A61K 9/20C07H 19/22A61K 31/7076A61K 31/7072C07H 19/06C07H 19/04A61K 31/675C07H 19/048A61P 31/14A61K 9/48
72
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Claims

Abstract

2′ and/or 3′ prodrugs of 1′, 2′, 3′ or 4′-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.

Claims

exact text as granted — not AI-modified
1 - 13 . (canceled) 
     
     
         14 . A method for the treatment of a host infected with a Flaviviridae virus, comprising administering to the host an effective treatment amount of a compound of Formula (IX): 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein:
 R 1  and R 2  are independently H; phosphate; straight chained, branched or cyclic alkyl; acyl; CO-alkyl; CO-aryl; CO-alkoxyalkyl; CO-aryloxyalkyl; CO-substituted aryl; sulfonate ester; benzyl, wherein the phenyl group is optionally substituted with one or more substituents; alkylsulfonyl; arylsulfonyl; aralkylsulfonyl; a lipid; an amino acid; a carbohydrate; a peptide; cholesterol; or a pharmaceutically acceptable leaving group which when administered in vivo is capable of providing a compound wherein R 1  and/or R 2  is independently H or phosphate; 
 X is O, S, SO 2  or CH 2 ; 
 Base* is a purine or pyrimidine base; 
 R 12  is C(Y 3 ) 3 ; 
 Y 3  is independently H, F, Cl, Br or I; and 
 R 13  is fluoro; 
 
         in combination or alternation with a second anti-viral agent. 
       
     
     
         15 . The method of  claim 14 , wherein X is O, and Y 3  is H. 
     
     
         16 . The method of  claim 15 , wherein R 1  and R 2  are H. 
     
     
         17 . The method of  claim 14 , wherein the Flaviviridae virus is hepatitis C virus. 
     
     
         18 . The method of  claim 17 , wherein the second anti-viral agent is an interferon, a ribavirin, or a combination thereof. 
     
     
         19 . The method of  claim 18 , wherein the second anti-viral agent is an interferon. 
     
     
         20 . The method of  claim 19 , wherein the second anti-viral agent is selected from the group consisting of pegylated interferon alpha 2a, interferon alphacon-1, natural interferon, albuferon, interferon beta-1a, omega interferon, interferon alpha, interferon gamma, interferon tau, interferon delta and interferon gamma-1b. 
     
     
         21 . The method of  claim 14 , wherein the second antiviral agent is ribavirin. 
     
     
         22 . The method of  claim 20 , wherein the second antiviral agent is pegylated interferon alpha 2a. 
     
     
         23 . The method of  claim 22 , further comprising administering ribavirin to the host. 
     
     
         24 . The method of  claim 15 , wherein R 1  is phosphate and R 2  is H. 
     
     
         25 . The method of  claim 15 , wherein R 1  is a pharmaceutically acceptable leaving group which when administered in vivo provides a compound wherein R 1  is H or phosphate; and R 2  is H. 
     
     
         26 . The method of  claim 15 , wherein Base* is a pyrimidine base. 
     
     
         27 . The method of  claim 26 , wherein Base* is uracil. 
     
     
         28 . The method of  claim 24 , wherein Base* is uracil. 
     
     
         29 . The method of  claim 25 , wherein Base* is uracil. 
     
     
         30 . The method of  claim 27 , wherein the second antiviral agent is an interferon, a ribavirin, or a combination thereof. 
     
     
         31 . The method of  claim 28 , wherein the second antiviral agent is an interferon, a ribavirin, or a combination thereof. 
     
     
         32 . The method of  claim 29 , wherein the second antiviral agent is an interferon, a ribavirin, or a combination thereof. 
     
     
         33 . The method of  claim 30 , wherein the second antiviral agent is ribavirin. 
     
     
         34 . The method of  claim 31 , wherein the second antiviral agent is ribavirin. 
     
     
         35 . The method of  claim 32 , wherein the second antiviral agent is ribavirin. 
     
     
         36 . The method of  claim 33 , further comprising administering pegylated interferon alpha 2a to the host. 
     
     
         37 . The method of  claim 34 , further comprising administering pegylated interferon alpha 2a to the host. 
     
     
         38 . The method of  claim 35 , further comprising administering pegylated interferon alpha 2a to the host.

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