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1. 发明授权

US08552192B2 Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same 有权
标题翻译：纯化的吡咯并喹啉基 - 吡咯烷-2,5-二酮组合物及其制备和使用方法
公开(公告)号：US08552192B2
公开(公告)日：2013-10-08
申请号：US12975644
申请日：2010-12-22
申请人： David P. Reed , Neil R. Barnes , John C. Kane , Christopher A. Lee , Jian-Xie Chen , Martin P. Redmon
发明人： David P. Reed , Neil R. Barnes , John C. Kane , Christopher A. Lee , Jian-Xie Chen , Martin P. Redmon
IPC分类号： C07D471/06
CPC分类号： C07D471/04 , C07D471/06
摘要： The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.
摘要翻译：本发明涉及（ - ） - 反式-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。本发明还涉及（ - ） - 反式-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-2,5-二酮化合物及其制备方法。本发明还涉及包含这些（ - ） - 反式-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-2,5-二酮化合物。本发明提供了通过向有需要的受试者施用治疗有效量的包含（ - ） - 反式-3-（5,6-二氢-4H-吡喃并[ 吡咯并[3,2,1-ij]喹啉-1-基）-4-（1H-吲哚-3-基）吡咯烷-2,5-二酮，手性纯度大于99％，形式1和形式2 （ - ） - 反式-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。

2. 发明申请

US20110160242A1 Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions And Methods For Preparing And Using Same 有权
标题翻译：纯化的吡咯并喹啉基 - 吡咯烷-2,5-二酮组合物及其制备和使用方法
公开(公告)号：US20110160242A1
公开(公告)日：2011-06-30
申请号：US12975644
申请日：2010-12-22
申请人： David P. Reed , Neil R. Barnes , John C. Kane , Christopher A. Lee , Jian-Xie Chen , Martin P. Redmon
发明人： David P. Reed , Neil R. Barnes , John C. Kane , Christopher A. Lee , Jian-Xie Chen , Martin P. Redmon
IPC分类号： A61K31/473 , C07D471/06 , A61P35/00
CPC分类号： C07D471/04 , C07D471/06
摘要： The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.
摘要翻译：本发明涉及（ - ） - 反式-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。本发明还涉及（ - ） - 反式-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-2,5-二酮化合物及其制备方法。本发明还涉及包含这些（ - ） - 反式-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-2,5-二酮化合物。本发明提供了通过向有需要的受试者施用治疗有效量的包含（ - ） - 反式-3-（5,6-二氢-4H-吡喃并[ 吡咯并[3,2,1-ij]喹啉-1-基）-4-（1H-吲哚-3-基）吡咯烷-2,5-二酮，手性纯度大于99％，形式1和形式2 （ - ） - 反式-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。

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