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    3-(6-ALKOXY-5-CHLOROBENZO[D]ISOXAZOL-3-YL)PROPANOIC ACID USEFUL AS KYNURENINE MONOOXYGENASE INHIBITORS
    1.
    发明申请
    3-(6-ALKOXY-5-CHLOROBENZO[D]ISOXAZOL-3-YL)PROPANOIC ACID USEFUL AS KYNURENINE MONOOXYGENASE INHIBITORS 有权

    公开(公告)号：US20170349577A1

    公开(公告)日：2017-12-07

    申请号：US15537805

    申请日：2015-12-17

    Applicant: GlaxoSmithKline Intellectual Property Development Limited

    Inventor： Anne Marie Jeanne BOUILLOT ,  Alexis DENIS ,  Ann Louise WALKER ,  John LIDDLE

    IPC: C07D413/12

    CPC classification number: C07D413/12

    Abstract: Compound of formula (I) wherein: R1 is heteroaryl either unsubstituted or substituted by methyl, ethyl, halo or ═O; and R2 is H, methyl or ethyl; and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

    COMPOUNDS
    4.
    发明申请
    COMPOUNDS 审中-公开

    公开(公告)号：US20180127405A1

    公开(公告)日：2018-05-10

    申请号：US15574506

    申请日：2016-05-19

    Applicant: GlaxoSmithKline Intellectual Property Development Limited

    Inventor： Anne Marie Jeanne BOUILLOT ,  Alexis DENIS ,  John LIDDLE ,  Ann Louise WALKER

    IPC: C07D417/12

    CPC classification number: C07D417/12

    Abstract: Compounds of formula (I) wherein: R1 is heteroaryl optionally substituted by methyl, ethyl, halo or =0; and R2 is H, methyl or ethyl. and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel disease, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

    PRODRUG OF 1,1'-(1,6-DIOXO-1,6-HEXANEDIYL)BIS-D-PROLINE
    6.
    发明申请
    PRODRUG OF 1,1'-(1,6-DIOXO-1,6-HEXANEDIYL)BIS-D-PROLINE 有权
    1,1' - （1,6-二氧代-1,6-庚二酰）双 - 二苯酚的制备

    公开(公告)号：US20160081983A1

    公开(公告)日：2016-03-24

    申请号：US14925350

    申请日：2015-10-28

    Applicant: GlaxoSmithKline Intellectual Property Development Limited

    Inventor： Alexis DENIS ,  Olivier Mirguet ,  Jérôme Toum

    IPC: A61K31/4025 ,  C07K16/18 ,  A61K39/395

    CPC classification number: A61K31/4025 ,  A61K39/3955 ,  A61K45/06 ,  C07D405/14 ,  A61K2300/00

    Abstract: The present invention relates to the compound (2R,2′R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.

    Abstract translation: 本发明涉及化合物（2R，2'R） - 双（（（（（四氢-2H-吡喃-4-基）氧基）羰基）氧基）甲基）1,1'-己二酰双（（吡咯烷-2-基） 羧酸盐），包含其的药物组合物及其用于治疗其中血清淀粉样蛋白P组分（SAP）的消耗将是有益的疾病或病症的用途，其包括淀粉样变性病，阿尔茨海默氏病，2型糖尿病和骨关节炎。

    A PRODRUG OF 1,1'-(1,6-DIOXO-1,6-HEXANEDIYL)BIS-D-PROLINE
    7.
    发明申请
    A PRODRUG OF 1,1'-(1,6-DIOXO-1,6-HEXANEDIYL)BIS-D-PROLINE 有权
    1,1' - （1,6-二氧代-1,6-庚二酰）双 - 对 - 苯酚的制剂

    公开(公告)号：US20160075694A1

    公开(公告)日：2016-03-17

    申请号：US14787608

    申请日：2015-04-27

    Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

    Inventor： Alexis DENIS ,  Olivier MIRGUET ,  Jérôme TOUM

    IPC: C07D405/14 ,  A61K9/00 ,  A61K39/395 ,  A61K31/4025

    CPC classification number: C07D405/14 ,  A61K9/0053 ,  A61K31/4025 ,  A61K39/3955 ,  A61K2039/505

    Abstract: The present invention relates to the compound (2R,2′R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1′-adipoylbis(pyrrolidine-2-carboxylate) of formula (I), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.

    Abstract translation: 本发明涉及化合物（2R，2'R） - 双（（（（（四氢-2H-吡喃-4-基）氧基）羰基）氧基）甲基）1,1'-己二酰双（（吡咯烷-2-基） 羧酸酯），包含其的药物组合物及其用于治疗其中血清淀粉样蛋白P组分（SAP）的消耗将是有益的疾病或病症的用途，包括淀粉样变性病，阿尔茨海默病，2型糖尿病和 骨关节炎。

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