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    Substituted piperidines as kinase inhibitors
    3.
    发明授权
    Substituted piperidines as kinase inhibitors 有权

    公开(公告)号：US11407754B2

    公开(公告)日：2022-08-09

    申请号：US16770213

    申请日：2018-12-28

    申请人： Daewoong Pharmaceutical Co., Ltd.

    发明人： In Woo Kim ,  Nam Youn Kim ,  Seung Hwarn Jeong ,  Bo-Kyoung Kim ,  Jun Hee Lee

    IPC分类号： A61K31/519 ,  C07D487/04

    摘要： The present invention relates to a compound represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, and the compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions: wherein, X1 is —NR1—, —O—, or —S—, X2 is CH or N, R1 is C1-5 alkyl, C3-6 cycloalkyl, CH2CHF2, or CH2CF3, wherein the C1-5 alkyl is optionally substituted with one NHC(O)OC(CH3)3 substituent, R2 is H, C1-5 alkyl, or halogen, and R3 is H or C1-5 alkyl.

    PREPARATION FOR PERCUTANEOUS ABSORPTION COMPRISING HIGH DOSE OF DONEPEZIL OR SALT THEREOF
    4.
    发明申请
    PREPARATION FOR PERCUTANEOUS ABSORPTION COMPRISING HIGH DOSE OF DONEPEZIL OR SALT THEREOF 有权

    公开(公告)号：US20220226296A1

    公开(公告)日：2022-07-21

    申请号：US17610303

    申请日：2020-05-15

    申请人： Daewoong Pharmaceutical Co., Ltd.

    发明人： Seoyeo LEE ,  Gyoung Won KIM ,  Gwan Young KIM

    IPC分类号： A61K31/445 ,  A61K47/32 ,  A61K9/70 ,  A61K9/00

    摘要： A preparation for percutaneous absorption contains a drug-containing matrix layer having a single-layered structure, in which a high dose of donepezil or a pharmaceutically acceptable salt thereof is contained in an amount of 10 to 20 wt % with respect to the total weight of the drug-containing matrix layer, thereby reducing the size of a formulation. The single-layered structure of the preparation allows for easy preparation at a production site and reduced manufacturing costs compared to preparations for percutaneous absorption having multi-layered structures. In addition, despite the high dose of donepezil contained in the preparation, no crystallization of donepezil occurs even during long-term storage, and the preparation continuously exhibits high skin permeability for a long period of time. Above all, due to a high drug dose per unit area, the size of a formulation is reduced compared to that of conventional formulations, and thus patient medication compliance can be remarkably increased.

    Substituted piperidines as kinase inhibitors
    5.
    发明授权
    Substituted piperidines as kinase inhibitors 有权

    公开(公告)号：US11339167B2

    公开(公告)日：2022-05-24

    申请号：US16770638

    申请日：2018-12-28

    申请人： Daewoong Pharmaceutical Co., Ltd.

    发明人： In Woo Kim ,  Sun Ah Jun ,  Nam Youn Kim ,  Jun Hee Lee

    IPC分类号： A61K31/519 ,  C07D487/04

    摘要： The present invention relates to a compound represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, and the compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions: wherein: R1 is pyrazolyl, isooxazolyl, isothiazolyl, phenyl, or benzothiazolyl, wherein the pyrazolyl, isoxazolyl, isothiazolyl, phenyl, or benzothiazolyl is optionally substituted with one Ra substituent; R2 is H, halogen, CN, or C1-5 alkyl; and Ra is C1-5 alkyl, C1-5 haloalkyl, C1-5 hydroxyalkyl, C3-6 cycloalkyl, tetrahydropyranyl, piperidinyl, or morpholino.

    Substituted benzenesulfonamides as sodium channel blockers
    10.
    发明授权
    Substituted benzenesulfonamides as sodium channel blockers 有权

    公开(公告)号：US10227338B2

    公开(公告)日：2019-03-12

    申请号：US15771775

    申请日：2016-11-11

    申请人： Daewoong Pharmaceutical Co., Ltd.

    发明人： Hyung-Geun Lee ,  Il-Hwan Kim ,  Myunggi Jung ,  Hyo Shin Kim ,  Chun Ho Lee ,  Sun Ah Jun ,  Ji Sung Yoon ,  Sung-Young Kim

    IPC分类号： A61K31/18 ,  C07C311/21 ,  C07D417/12 ,  A61K31/427 ,  A61K31/497 ,  C07D417/14 ,  C07D277/52

    摘要： The invention relates to a compound represented by Chemical Formula 1, below, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound or salt. The compound of the invention or pharmaceutically acceptable salts thereof can be used for the prevention or treatment of sodium channel blocker-related diseases. in Chemical Formula 1, R1 is hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, halogen, or cyano, R2 and R3 are each independently hydrogen, or halogen, R4 is C5-10 heteroaryl containing one or two elements each independently selected from the group consisting of N, S and O, wherein the C5-10 heteroaryl is unsubstituted or substituted with C1-4 alkyl or halogen, R5 is —CH2CH2—N(R7)(R8), or —CH2CH2CH2—N(R7)(R8), R6 is hydrogen, or C1-4 alkyl; or R5 and R6 together form C3-5 alkylene, (C2-4 alkylene)-N(R9)—(C2-4 alkylene), or (C2-4 alkylene)-O—(C2-4 alkylene), wherein the C3-5 alkylene, or C2-4 alkylene is each independently unsubstituted or substituted with one or two R10, R7, R8, and R9 are each independently hydrogen, or C1-4 alkyl, R10 is C1-4 alkyl, C1-4 alkoxy, halogen, amino, NH(C1-4 alkyl), N(C1-4 alkyl)2, NHCO(C1-4 alkyl), or pyrrolidinyl, X1 is C—R′, or N, wherein R′ is hydrogen, or halogen, X2 is CH, or N, and X3 is N—R″, wherein R″ is hydrogen, or C1-4 alkyl.