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    4H-3,1-BENZOXAZIN-4-ONE DERIVATIVES AND ANALOGS AS ANTIVIRAL AGENTS
    5.
    发明申请
    4H-3,1-BENZOXAZIN-4-ONE DERIVATIVES AND ANALOGS AS ANTIVIRAL AGENTS 审中-公开
    4H-3,1-BENZOXAZIN-4-ONE衍生物和类似物作为抗病毒剂

    公开(公告)号：WO1997048707A1

    公开(公告)日：1997-12-24

    申请号：PCT/EP1997003158

    申请日：1997-06-16

    Applicant: SMITHKLINE BEECHAM PLC ,  McNAIR, David, Jonathan ,  SHAW, Antony, Nicholas ,  GRIBBLE, Andrew, Derrick ,  JENNINGS, Leslie, John, Arthur ,  PARRATT, Martin, John ,  JARVEST, Richard, Lewis

    Inventor： SMITHKLINE BEECHAM PLC

    IPC: C07D498/04

    CPC classification number: C07D265/22

    Abstract: Herpesvirus protease inhibitor 4H-3,1-benzoxazin-4-one, 4H-thieno[3,2-d][1,3]oxazin-4-one, or 4H-thieno[2,3-d][1,3]oxazin-4-one; derivatives which are 2-substituted by C(XY)-R1, C(XY)-CH2-R1, C(XY)-C2H4-R1, or CX=CY-R1 wherein one of X and Y is hydrogen or halo or an alkyl substituent and the other is hydrogen or an alkyl substituent, and R1 is aryl or heteroaryl substituted by ZR4 wherein Z is CO, NRxCO, NRxCOCO, NRxCOCH2, or NRxSO2 wherein Rx is hydrogen or alkyl and R4 is aryl or heteroaryl.

    Abstract translation: 疱疹病毒蛋白酶抑制剂4H-3,1-苯并恶嗪-4-酮，4H-噻吩并[3,2-d] [1,3]恶嗪-4-酮或4H-噻吩并[2,3-d] 3]恶嗪-4-酮; 由C（XY）-R1，C（XY）-CH2-R1，C（XY）-C2H4-R1或CX = CY-R1 2-取代的衍生物，其中X和Y中的一个是氢或卤素或 烷基取代基，另一个是氢或烷基取代基，并且R 1是被ZR 4取代的芳基或杂芳基，其中Z是CO，NR x CO，NR x COCO，NR x COCH 2或NR x SO 2，其中R x是氢或烷基，且R 4是芳基或杂芳基。

    CHEMICAL COMPOUNDS
    6.
    发明申请
    CHEMICAL COMPOUNDS 审中-公开
    化学化合物

    公开(公告)号：WO2013096153A1

    公开(公告)日：2013-06-27

    申请号：PCT/US2012/070000

    申请日：2012-12-17

    Applicant: GLAXOSMITHKLINE LLC ,  BROWN, Kristin, K. ,  CHAI, Deping ,  DODSON, Christopher, S. ,  DUFFY, Kevin, J. ,  SHAW, Antony, Nicholas

    Inventor： BROWN, Kristin, K. ,  CHAI, Deping ,  DODSON, Christopher, S. ,  DUFFY, Kevin, J. ,  SHAW, Antony, Nicholas

    IPC: A01N55/02

    CPC classification number: A61K45/06 ,  A61K9/0019 ,  A61K9/2009 ,  A61K9/4858 ,  A61K31/475 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  A61K2300/00

    Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R, R 1 , R 2 , R 3 and R 4 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    Abstract translation: 本发明涉及取代的喹啉衍生物。 具体地，本发明涉及式I化合物：其中R，R 1，R 2，R 3和R 4在本文中定义。 本发明的化合物是乳酸脱氢酶A的抑制剂，并且可用于治疗与肿瘤细胞代谢相关的癌症和疾病，例如癌症，更具体地说，涉及乳腺癌，结肠癌，前列腺癌和肺癌。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制乳酸脱氢酶A活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的疾病。

    CHEMICAL COMPOUNDS
    7.
    发明申请
    CHEMICAL COMPOUNDS 审中-公开
    化学化合物

    公开(公告)号：WO2013096151A1

    公开(公告)日：2013-06-27

    申请号：PCT/US2012/069997

    申请日：2012-12-17

    Applicant: GLAXOSMITHKLINE LLC ,  BROWN, Kristin, K. ,  CHAI, Deping ,  DODSON, Christopher, S. ,  DUFFY, Kevin, J. ,  SHAW, Antony, Nicholas

    Inventor： BROWN, Kristin, K. ,  CHAI, Deping ,  DODSON, Christopher, S. ,  DUFFY, Kevin, J. ,  SHAW, Antony, Nicholas

    IPC: A01N55/02

    CPC classification number: A61K31/47 ,  A61K31/4706 ,  C07D215/54 ,  C07D401/04 ,  C07D401/14 ,  C07D417/06

    Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R 1 , R 2 , R 3 ; R 4 ; and R 5 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    Abstract translation: 本发明涉及取代的喹啉衍生物。 具体地，本发明涉及根据式（I）的化合物：其中R1，R2，R3; R4; 和R5在本文中定义。 本发明的化合物是乳酸脱氢酶A的抑制剂，并且可用于治疗与肿瘤细胞代谢相关的癌症和疾病，例如癌症，更具体地说，涉及乳腺癌，结肠癌，前列腺癌和肺癌。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制乳酸脱氢酶A活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的疾病。

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