SUBSTITUTED POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVE PRODRUG Russian patent published in 2017 - IPC C07D471/04 C07D253/10 A61K31/53 A61P31/16 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (I) and their pharmaceutically acceptable salts thereof, which have inhibitory effect on cep-dependent endonuclease. In formula (I)

,

P^R represents a group selected from -C(=O)-P^R0, -C(=O)-P^R1, -C(=O)-L-P^R1, -C(=O)-L-O-P^R1, -C(=O)-L-O-L-O-P^R1, -C(=O)-O-P^R2, -C(=O)-N(P^R2)₂, -C(=O)-O-L-O-P^R2, -CH₂-O-P^R3, -CH₂-O-L-O-P^R3, -CH₂-O-C(=O)-P^R3, -CH₂-O-C(=O)-O-P^R3, -CH(-CH₃)-O-C(=O)-O-P^R3, -CH₂-O-C(=O)-N(-K)-P^R3, -CH₂-O-C(=O)-O-L-O-P^R3, -CH₂-O-C(=O)-O-L-N(P^R3)₂, -CH₂-O-C(=O)-N(-K)-L-O-P^R3, -CH₂-O-C(=O)-N(-K)-L-N(P^R3)₂, -CH₂-O-C(=O)-O-L-O-L-O-P^R3, -CH₂-O-C(=O)-O-L-N(-K)-C(=O)-P^R3, -CH₂-O-P(=O)(-OH)₂, -CH₂-O-P(=O)(-OBn)₂, -CH₂-P^R4, -C(=N⁺P^R5₂)(-NP^R5₂); R^1a – hydrogen, halogen, carboxy, lower alkyl, possibly containing substituent C, lower alkyl carbonyl, possibly containing substituent C, or -Z-N(R^A1)(R^A2), R^2a – hydrogen or lower alkyl, possibly containing substituent C; R^3a – hydrogen, lower alkyl, possibly containing substituent C, a carboxylic group, possibly containing substituent C, carbocycle-lower alkyl, possibly containing substituent C, carbocycloksi-lower alkyl, possibly containing substituent C, heterocyclic group, possibly containing substituent C, or heterocycle-lower alkyl, possibly containing substituent C, or B¹, or B² represents a CR^5aR^6a, and the other represents a NR^7a, or B¹ represents a CR^8aR^9a and B² represents a CR^10aR^11a. Values of other radicals are given in the patent claim. Invention also refers to pharmaceutical compositions.

EFFECT: obtained new compounds of formula (I) possessing inhibitory activity against the cep-dependent endonuclease and which can be useful in treating influenza.

10 cl, 4 dwg, 35 tbl, 1035 ex