Substituted triazolo[1,5-A]pyrimidines as antiviral agents
A pharmaceutical composition comprising an effective amount of a compound of formulas (I-III) and a pharmaceutically acceptable carrier. Methods for treating a hepatitis virus in a patient comprising administering an effective amount of the compound of formulas (I-III) are also presented.
1. A method for treating a hepatitis B virus in a patient comprising administering an effective amount of a composition to a patient in need thereof comprising:
(a) an effective amount of a compound selected from the group consisting of Formulas I, II, III, and mixtures thereof;
wherein
R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 each independently represent a phenyl or Het, wherein each phenyl or Het is optionally substituted with at least one substitutuent independently selected from the group consisting of alkyl, cycloalkyl, acyl, aryl, halo, OR a , trifluoromethoxy, trifluoromethyl, NO 2 , NR a R b , cyano, CONR a R b , and CO 2 R a ;
X 1 , X 2 , X 3 , X 4 , X 5 , and X 6 are selected from the group consisting of a bond, a saturated alkylenegroup and an unsaturated alkylenegroup;
R a and R b are each independently H, alkyl, cycloalkyl, alkanoyl, alkanoyloxy,or aryl, or R a and R b together with a nitrogen to which they are attached form a Het; and
(b) a pharmaceutically acceptable carrier.
2. A method for treating a hepatitis B virus in a patient in need thereof comprising administering to said patient an effective amount of a compound selected from the group consisting of formula I, II, III, and mixtures thereof that reduce the serum level of hepatitis B surface antigen (HBsAg) in said patient, said formula I, II, and III defined as follows:
wherein
R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 each independently represent a phenyl or Het, wherein each phenyl or Het is optionally substituted with at least one substitutuent independently selected from the group consisting of alkyl, cycloalkyl, acyl, aryl, halo, OR a , trifluoromethoxy, trifluoromethyl, NO 2 , NR a R b , cyano, CONR a R b , and CO 2 R a ;
X 1 , X 2 , X 3 , X 4 , X 5 , and X 6 are selected from the group consisting of a bond a saturated alkylenegroup and an unsaturated alkylenegroup;
R a and R b are each independently H, alkyl, cycloalkyl, alkanoyl, alkanoyloxy, or aryl, or R a and R b together with a nitrogen to which they are attached form a Het.