FIELD: pharmaceutics.
SUBSTANCE: present invention relates to compounds of formula (I)
where R1 represents C1-6alkyl, haloC1-6alkyl, С3-7cycloalkyl-C1-6alkyl, C1-6alkoxy-C1-6alkyl or pyrrolidinylC1-6alkyl; R2 represents C1-6alkyl, phenylC1-6alkyl, pyridinylC1-6alkyl or pyrimidinylC1-6alkyl, where said phenylC1-6alkyl, pyridinylC1-6alkyl and pyrimidinylC1-6alkyl are unsubstituted or substituted by one or two alternates independently selected from the halogen atom, C1-6alkyl, C1-6alkoxy, cyano, carboxy, carbamoyl, haloC1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxycarbomyl, C1-6alkoxy-C1-6alkylaminecarbonyl, pyrrolidinylcarbonyl and piperidylcarbonyl; R3 represents Н. Disclosed is also a compound of formula (Ia) where R4 represents C1-6alkyl, haloC1-6alkyl, С3-7cycloalkyl-C1-6alkyl, C1-6alkoxy-C1-6alkyl or pyrrolidinylC1-6alkyl; R5 represents C1-6alkyl, phenylC1-6alkyl, pyridinylC1-6alkyl or pyrimidinylC1-6alkyl, where said phenylC1-6alkyl, pyridinylC1-6alkyl and pyrimidinylC1-6alkyl are unsubstituted or substituted by one or two alternates independently selected from the halogen atom, C1-6alkyl, C1-6alkoxy, cyano, carboxy, carbamoyl, haloC1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxycarbomyl, C1-6alkoxy-C1-6alkylaminecarbonyl, pyrrolidinylcarbonyl and piperidylcarbonyl; R6 represents Н or C1-6alkyl-С(O)O-C1-6alkyl-; R7 represents Н, C1-6alkyl, С3-7cycloalkyl or С1-10alkylcarbonyl; R8 represents Н, C1-6alkylcarbonyl, carboxy-C1-6alkylcarbonyl, C1-6alkyloxycarbonyl-C1-6alkylcarbonyl; in case R6, R7 and R8 do not represent Н simultaneously. In addition, a pharmaceutical composition based on these compounds and having the activity of the agonist of the TLR7 receptor was described, and the use of the above-mentioned compounds to produce a medicinal preparation for the treatment or prophylaxis of infection of the hepatitis B virus was described, as well as for inducing interferon-α production. The invention also relates to a method for treating or preventing a hepatitis B virus, which comprises introducing a therapeutically effective number of described compounds.
EFFECT: new compounds which are agonists of TLR7 and can be used in treatment of hepatitis B are obtained and described.
38 cl, 9 tbl, 81 ex
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Authors
Dates
2021-03-22—Published
2016-05-04—Filed