Therapeutic nucleosides-uses
AssigneeBurroughs Wellcome Co.
InventorSusan M. Daluge
Life of this patent
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Abstract
Antiviral nucleoside analogues containing a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue, particularly those in which the 2-, 5- and 6-positions of the benzimidazole base are substituted by halogen, have activity against hepatitis B virus infections.
Claims20
A method of treating a host having an HBV infection which comprises administering to said host a therapeutically effective amount of a compound of formula (I) or (I-1) ##STR7## wherein R.sup.1 is H, CH.sub.3 or CH.sub.2 OH;
- R.sup.2 is H or OH;
- R.sup.3 is H or OH;
- or R.sup.2 and R.sup.3 together form a bond;
- R.sup.4 is H, Cl, Br, I, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, C.sub.1-4 perfluoroalkyl, NH.sub.2, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, C.sub.3-7 cycloalkylamino, diC.sub.3-7 cycloalkylamino, N-C.sub.1-4 alkyl-N-C.sub.3-7 cycloalkylamino, N-C.sub.1-4 alkyl-N-C.sub.3-7 cycloalkylC.sub.1-4 alkylamino, diC.sub.3-7 cycloalkylC.sub.1-4 alkylamino, C.sub.3-7 cycloalkylC.sub.1-4 alkylamino, N-C.sub.3-7 cycloalkyl-N-C.sub.3-7 cycloalkylC.sub.1-4 alkylamino, SH, C.sub.1-4 alkylthio, C.sub.6-10 arylC.sub.1-4 alkylthio, OH, C.sub.1-4 alkoxy, C.sub.6-10 arylC.sub.1-4 alkoxy or C.sub.6-10 arylC.sub.1-4 alkyl;
- and R.sup.5, R.sup.6 and R.sup.7 are independently selected from H, F, Cl, Br, I, CF.sub.3 and CH.sub.3, provided that at least one of R.sup.1, R.sup.2 and R.sup.3 is or contains OH;
- or a pharmaceutically acceptable derivative thereof.
A method of treating a host having an HBV infection which comprises administering to said host a therapeutically effective amount of a compound of formula (IA) or (lA-1) ##STR8## wherein R.sup.2 is H or OH;
- R.sup.4 is H, Cl, Br, I, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, C.sub.1-4 perfluoroalkyl, NH.sub.2, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, C.sub.3-7 cycloalkylamino, diC.sub.3-7 cycloalkylamino, N-C.sub.1-4 alkyl-N-C.sub.3-7 cycloalkylamino, N-C.sub.1-4 alkyl-N-C.sub.3-7 cycloalkylC.sub.1-4 alkylamino, diC.sub.3-7 cycloalkylC.sub.1-4 alkylamino, C.sub.3-7 cycloalkylC.sub.1-4 alkylamino, N-C.sub.3-7 cycloalkyl-N-C.sub.3-7 cycloalkylC.sub.1-4 alkylamino, SH, C.sub.1-4 alkylthio, C.sub.6-10 arylC.sub.1-4 alkylthio, OH, C.sub.1-4 alkoxy, C.sub.6-10 arylC.sub.1-4 alkoxy or C.sub.6-10 arylC.sub.1-4 alkyl;
- and
- R.sup.5, R.sup.6 and R.sup.7 are independently selected from H, F, Cl, Br, I, CF.sub.3 and CH.sub.3 ;
- or a pharmaceutically acceptable derivative thereof.
A method according to claim I wherein said compound is administered in an effective HBV infection treatment amount.
Dependencies are inferred from the claim text.