SUBSTITUTED POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVE PRODRUG

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),Prepresents a group selected from -C(=O)-P, -C(=O)-P, -C(=O)-L-P, -C(=O)-L-O-P, -C(=O)-L-O-L-O...

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Hauptverfasser: MIKAMIYAMA Khidenori, TOMITA Kendzi, TAODA Esiuki, TAKAKHASI Tika, ANAN Kosuke, KAVAI Makoto, MIYAGAVA Masaesi, AKIYAMA Tosiyuki, SUDZUKI Naoyuki
Format: Patent
Sprache:eng ; rus
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Zusammenfassung: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),Prepresents a group selected from -C(=O)-P, -C(=O)-P, -C(=O)-L-P, -C(=O)-L-O-P, -C(=O)-L-O-L-O-P, -C(=O)-O-P, -C(=O)-N(P), -C(=O)-O-L-O-P, -CH-O-P, -CH-O-L-O-P, -CH-O-C(=O)-P, -CH-O-C(=O)-O-P, -CH(-CH)-O-C(=O)-O-P, -CH-O-C(=O)-N(-K)-P, -CH-O-C(=O)-O-L-O-P, -CH-O-C(=O)-O-L-N(P), -CH-O-C(=O)-N(-K)-L-O-P, -CH-O-C(=O)-N(-K)-L-N(P), -CH-O-C(=O)-O-L-O-L-O-P, -CH-O-C(=O)-O-L-N(-K)-C(=O)-P, -CH-O-P(=O)(-OH), -CH-O-P(=O)(-OBn), -CH-P, -C(=NP)(-NP); R- hydrogen, halogen, carboxy, lower alkyl, possibly containing substituent C, lower alkyl carbonyl, possibly containing substituent C, or -Z-N(R)(R), R- hydrogen or lower alkyl, possibly containing substituent C; R- 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 B, or Brepresents a CRR, and the other represents a NR, or Brepresents a CRRand Brepresents a CRR. 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 Изобретение относится к соединениям формулы (I) и их фармацевтически приемлемым солям, которые обладают ингибирующей активностью в отношении кэп-зависимой эндонуклеазы. В формуле (I),Pпредставляет собой группу, выбранную из -C(=O)-P, -C(=O)-P, -C(=O)-L-P, -C(=O)-L-O-P, -C(=O)-L-O-L-O-P, -С(=O)-О-P, -C(=O)-N(P), -С(=O)-O-L-O-P, -CH-O-P, -CH-O-L-O-P, -CH-O-C(=O)-P, -CH-O-C(=O)-O-P, -CH(-CH)-O-C(=O)-O-P, -CH-O-C(=O)-N(-K)-P, -CH-O-C(=O)-O-L-O-P, -CH-O-C(=O)-O-L-N(P), -CH-O-C(=O)-N(-K)-L-O-P, -CH-O-C(=O)-N(-K)-L-N(P), -CH-O-C(=O)-O-L-O-L-O-P, -CH-O-C(=O)-O-L-N(-K)-C(=O)-P, -CH-O-P(=O)(-OH), -СН-O-Р(=O)(-OBn), -СН-P, -C(=NP)(-NP); R- водород, галоген, карбокси, низший алкил, возможно содержащий заместитель С, низший алкилкарбонил, возможно содержащий заместитель С, или -Z-N(R)(R), R- водород или низший алкил, возможно содержащий заместитель С; R- водород, низший алкил, в