US2013017171A1PendingUtilityA1

Methods and compositions for treating hepatitis c virus

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Assignee: UNIV CAGLIARIPriority: May 23, 2000Filed: Sep 20, 2012Published: Jan 17, 2013
Est. expiryMay 23, 2020(expired)· nominal 20-yr term from priority
Inventors:Jean-Pierre SommadossiIdenix Pharmaceuticals, Inc.
A61P 31/14A61P 43/00A61P 31/20A61P 31/12A61P 1/16A61K 38/21G03C 1/0051A61K 31/7056A61K 31/7076C07H 19/10A61K 45/06A61K 31/708A61K 31/7072A61K 31/7068C07H 19/04C07H 19/06C07H 19/16C07H 19/20C07H 19/167
63
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Claims

Abstract

A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Claims

exact text as granted — not AI-modified
1 . A β-D-2′-deoxy-2′-halo-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         2 . The deoxynucleoside of  claim 1 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         3 . The deoxynucleoside of  claim 1 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         4 . The deoxynucleoside of  claim 1 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         5 . The deoxynucleoside of  claim 3 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         6 . The deoxynucleoside of  claim 3 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         7 . The deoxynucleoside of  claim 3 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         8 . The deoxynucleoside of  claim 3 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         9 . The deoxynucleoside of  claim 1 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl-ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         10 . The deoxynucleoside of  claim 9 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         11 . The deoxynucleoside of  claim 10 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         12 . The deoxynucleoside of  claim 10 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         13 . A pharmaceutical composition comprising the deoxynucleoside of  claim 1  and a pharmaceutically acceptable excipient. 
     
     
         14 . The pharmaceutical composition of  claim 13 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         15 . The pharmaceutical composition of  claim 13 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         16 . The pharmaceutical composition of  claim 13 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         17 . The pharmaceutical composition of  claim 15 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         18 . The pharmaceutical composition of  claim 15 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         19 . The pharmaceutical composition of  claim 15 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         20 . The pharmaceutical composition of  claim 15 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         21 . The pharmaceutical composition of  claim 13 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl-ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         22 . The pharmaceutical composition of  claim 21 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         23 . The pharmaceutical composition of  claim 22 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         24 . The pharmaceutical composition of  claim 22 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         25 . The pharmaceutical composition of  claim 13 , wherein the composition is formulated as a dosage unit for single dose administration. 
     
     
         26 . The pharmaceutical composition of  claim 25 , wherein the dosage unit contains from about 50 to about 1000 mg of the deoxynucleoside. 
     
     
         27 . The pharmaceutical composition of  claim 25 , wherein the dosage unit is a tablet or capsule. 
     
     
         28 . A method for the treatment of a hepatitis C virus infection in a host, comprising administering to the host an antivirally effective amount of a deoxynucleoside, wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         29 . The method of  claim 28 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         30 . The method of  claim 28 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         31 . The method of  claim 28 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl pyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         32 . The method of  claim 31 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         33 . The method of  claim 31 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         34 . The method of  claim 31 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         35 . The method of  claim 31 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         36 . The method of  claim 35 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         37 . The method of  claim 31 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         38 . The method of  claim 31 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         39 . The method of  claim 38 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         40 . The method of  claim 28 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl-ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         41 . The method of  claim 40 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         42 . The method of  claim 41 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         43 . The method of  claim 41 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         44 . The method of  claim 28 , wherein the host is a human. 
     
     
         45 . The method of  claim 28 , wherein the antivirally effective amount is ranging from about 0.1 to about 100 mg/kg/day. 
     
     
         46 . The method of  claim 45 , wherein the antivirally effective amount is ranging from about 1 to about 50 mg/kg/day. 
     
     
         47 . The method of  claim 45 , wherein the antivirally effective amount is ranging from about 1 to about 20 mg/kg/day. 
     
     
         48 . The method of  claim 28 , wherein the deoxynucleoside is administered in combination or alternation with a second anti-hepatitis C agent. 
     
     
         49 . The method of  claim 48 , wherein the second agent is selected from the group consisting of an interferon, ribavirin, a protease inhibitor, a thiazolidine derivative, a polymerase inhibitor, and a helicase inhibitor. 
     
     
         50 . The method of  claim 48 , wherein the second agent is an interferon. 
     
     
         51 . The method of  claim 48 , wherein the second agent is ribavirin. 
     
     
         52 . 2′-C-Methyl-guanosine, or a pharmaceutically acceptable salt or prodrug thereof. 
     
     
         53 . 2′-C-Methyl-guanosine monophosphate, diphosphate, or triphosphate. 
     
     
         54 . A pharmaceutical composition comprising the 2′-C-methyl-guanosine of  claim 52  and a pharmaceutically acceptable excipient. 
     
     
         55 . A method for inhibiting replication of a hepatitis C virus in a host, comprising contacting the host with an antivirally effective amount of a deoxynucleoside, wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         56 . The method of  claim 55 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         57 . The method of  claim 55 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl-nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         58 . The method of  claim 55 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl pyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         59 . The method of  claim 55 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         60 . The method of  claim 59 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methylpyrimidine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         61 . The method of  claim 58 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         62 . The method of  claim 61 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         63 . The method of  claim 61 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl uracil nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         64 . The method of  claim 58 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         65 . The method of  claim 64 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         66 . The method of  claim 64 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-fluoro-2′-C-methyl cytosine nucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         67 . The method of  claim 56 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl-ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         68 . The method of  claim 67 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methylpyrimidine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         69 . The method of  claim 68 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl uracil ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         70 . The method of  claim 68 , wherein the deoxynucleoside is a β-D-2′-deoxy-2′-halo-2′-C-methyl cytosine ribonucleoside, or pharmaceutically acceptable salt or a prodrug thereof. 
     
     
         71 . The method of  claim 55 , wherein the host is a human cell.

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