摘要 |
A 3-oxo-3,4-dihydro-2-pyrazine-formamide derivative, a pharmaceutical composition of same, a method for preparing same, and a use thereof. Specifically, a compound as represented by formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, where R1 is either hydrogen or a halogen, where R2 and R3 are independently selected from: hydrogen, (C1-6 alkyl acyloxy)-C1-6 alkyl, 1-(C1-6 alkyl acyloxy)-C1-6 alkyl, tetrahydrofuranyl, tetrahydropyranyl, and hydroxy- or halogen-substituted C1-6 alkyl, and where the halogen is selected from fluorine, chlorine, bromine, and iodine, also, when R2 and R3 simultaneously are hydrogen, R1 can neither be hydrogen nor fluorine. The compound as represented by formula (I) can be in vivo converted into the corresponding 6-R1-3-oxo-3,4-dihydro-2-pyrazine-formamide and thus exerting antiviral efficacy. Compared with 6-R1-3-oxo-3,4-dihydro-2-pyrazine-formamide, the parent medicament, the compound as represented by formula (I) has increased bioavailability and extended period of in vivo efficacy. |
申请人 |
INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A. CHINA |
发明人 |
LI, SONG;LI, XINGZHOU;ZHONG, WU;ZHANG, ZHENQING;ZHANG, TIANHONG;XIAO, JUNHAI;WANG, LILI;ZHENG, ZHIBING;ZHOU, XINBO;ZHAO, GUOMING;WANG, XIAOKUI |