HIGHLY PURE PYRROLOQUINOLINYL-PYRROLE-2,5-DIONE AND PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE AND METHODS OF PREPARING SAME
    1.
    发明申请
    HIGHLY PURE PYRROLOQUINOLINYL-PYRROLE-2,5-DIONE AND PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE AND METHODS OF PREPARING SAME 审中-公开
    高纯度吡咯烷醇溶液 - 吡咯烷-2,5-二酮和对羟基吡啶-2-基吡咯烷-2,5-二酮及其制备方法

    公开(公告)号:WO2013162714A1

    公开(公告)日:2013-10-31

    申请号:PCT/US2013/029572

    申请日:2013-03-07

    申请人: ARQULE, INC.

    IPC分类号: A61K31/473 A61P35/00

    CPC分类号: C07D471/06

    摘要: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,l-ij]quinolin-l- yl)-4-(lH-indol-3-yl)-lH-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,l-ij]quinolin-l-yl)-4-(lH- indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl- pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H- pyrrolo[3,2,l-ij]quinolin-l-yl)-4-(lH-indol-3-yl)-lH-pyrrole-2,5-dione, 3-(5,6-dihydro-4H- pyrrolo[3,2,l-ij]quinolin-l-yl)-4-(lH-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.

    摘要翻译: 本发明涉及高纯度的吡咯并喹啉基 - 吡咯-2,5-二酮和吡咯并喹啉基 - 吡咯烷-2,5-二酮,例如3-(5,6-二氢-4H-吡咯并[3,2,1- ij]喹啉-1-基)-4-(1H-吲哚-3-基)-1H-吡咯-2,5-二酮,3-(5,6-二氢-4H-吡咯并[3,2,1- ij]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2,5-二酮及其药学上可接受的盐,溶剂化物和非对映异构体。 本发明还涉及制备高纯度的吡咯并喹啉基 - 吡咯-2,5-二酮和吡咯并喹啉基 - 吡咯烷-2,5-二酮的方法,例如3-(5,6-二氢-4H-吡咯并[ 1,2-ij]喹啉-1-基)-4-(1H-吲哚-3-基)-1H-吡咯-2,5-二酮,3-(5,6-二氢-4H-吡咯并[3,3- 1,2-ij]喹啉-1-基)-4-(1H-吲哚-3-基)吡咯烷-2,5-二酮及其药学上可接受的盐,溶剂化物和非对映异构体。