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    Substituted 3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione, pharmaceutical composition, method for the production and use thereof
    1.
    发明授权
    Substituted 3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione, pharmaceutical composition, method for the production and use thereof 有权

    公开(公告)号：US12091423B2

    公开(公告)日：2024-09-17

    申请号：US16768892

    申请日：2020-03-27

    申请人： VIRIOM, INC.

    发明人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Oleg Dmitrievich Mitkin

    IPC分类号： C07D498/14 ,  A61K31/5383 ,  A61P31/16

    CPC分类号： C07D498/14 ,  A61K31/5383 ,  A61P31/16

    摘要： Influenza is an acute infectious respiratory disease caused by the influenza virus. It is part of the group of Acute Respiratory Viral Infections (ARVI). It occasionally spreads in the form of epidemics and pandemics. Currently, more than 2000 variants of the influenza virus differing in the antigen spectrum have been identified. Given that influenza is a serious threat to public health (worldwide, these annual epidemics lead to 3-5 million cases of severe illness, millions of hospitalizations, and up to 650,000 deaths), it seems appropriate to search for new anti-influenza drugs with improved characteristics.
    The inventors surprisingly found out that the previously unknown substituted 3,4,12,12a-tetrahydro-1H-[1,4] oxazino[3,4-c]pyrido[2,1-f] [1,2,4]triazine-6,8-dione of general formula 1, its stereoisomer, their prodrug, pharmaceutically acceptable salt, solvate, hydrate, and a crystalline or polycrystalline form thereof are effective agents for prophylaxis and treatment of viral diseases, including influenza




    where

    R1 is (6,7-difluoro-5,10-dihydrothieno[3,2-c][2]benzothiepin-10-yl, (7,8-difluoro-4,9-dihydrothieno[2,23-c][2]benzothiepin-4-yl, (3,4-difluorophenyl)(phenyl)methyl, (3,4-difluorophenyl)(2-methylsulfanylphenyl)methyl, diphenylmethyl, bis(4-fluorophenyl)-methyl; R2 is hydrogen or a protective group selected from a series comprising (C1-C3 alkyl) oxycarbonyloxy, {[(C1-C3 alkyl)oxycarbonyl]-oxy}methoxy, {[2-(C1-C3 alkyl) oxyethoxy]carbonyl}oxy, ({[(1R)-2-[(C1-C3alkyl)oxy]-1-methylethoxy} carbonyl)oxy, {[(3S)-ethoxyfuran-3-yloxy]-carbonyl}oxy, [(ethoxy-2H-pyran-4-yloxy) carbonyl]oxy, {[(1-acetylazetidine)-3-yloxy]carbonyl}oxy, {[(C1-C3alkyl) oxycarbonyl]-oxy}methoxy, ({[2-(C1-C3 alkyl)oxyethoxy]carbonyl}oxy) methoxy.

    PYRIDONE DERIVATIVE CRYSTAL FORM AND PREPARATION METHOD AND APPLICATION THEREFOR
    9.
    发明公开
    PYRIDONE DERIVATIVE CRYSTAL FORM AND PREPARATION METHOD AND APPLICATION THEREFOR 审中-公开

    公开(公告)号：US20230144122A1

    公开(公告)日：2023-05-11

    申请号：US17595013

    申请日：2019-11-05

    申请人： Jiangxi Caishi Pharmaceutical Technology Co., Ltd.

    发明人： Qing SHAO ,  Libin GAN ,  Li CHEN

    IPC分类号： C07D498/14

    CPC分类号： C07D498/14 ,  C07B2200/13

    摘要： Provided are crystals of (((R)-12′-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-6′,8′-dioxo-6′,8′,12′,12a′-tetrahydro-1′H,4′H-spiro[cyclopropane-1,3′-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin]-7′-yl)oxy)methyl methyl carbonate, i.e. compound of Formula (1) or a solvate thereof and a preparation method therefor, the crystals comprising crystal form A, crystal form B, crystal form C, crystal form D, crystal form E, crystal form F, and single crystal. The crystal of the compound of Formula (1) or a solvate thereof can be individually used for clinical treatment or in combination with other anti-influenza drugs such as neuraminidase inhibitors, nucleoside drugs, or PB2 inhibitors, being capable of clinically curing influenza patients quickly, and having very good activity and good bioavailability compared to existing pyridone derivatives. In addition, the stability, hygroscopicity, and storability of the crystals meet the requirements for pharmaceutical use.