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1. 发明公开

EP3209642A1 SEMI-SYNTHESIS PROCEDURES 无效
标题翻译：半合成程序
公开(公告)号：EP3209642A1
公开(公告)日：2017-08-30
申请号：EP15791440.9
申请日：2015-10-23
申请人： Tetraphase Pharmaceuticals, Inc.
发明人： ZHANG, Wu-Yan , LAFRANCE, Danny , RONN, Magnus, P.
IPC分类号： C07D207/06 , C07C231/12 , C07C245/20 , C07C237/26
CPC分类号： C07D295/15 , C07C231/12 , C07C237/26 , C07C245/20 , C07C2603/46 , C07D207/06
摘要： Provided herein are improved processes for convening C7-amino-substituted tetracylines to C7-fluoro-substituted tetracyclines as well as intermediates produced by or used in these processes. In one embodiment, a thermal fluorination method is provided in which a suspension comprising a non-polar organic solvent and a C7-diazo-substituted tetracycline hexafluorophosphate, hexafluoarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof is healed to provide a C7-fluoro-substituted tetracyline, or salt, solvate or combination thereof. In another embodiment, a photolytic fluorination is provided in which a solution comprising an ionic liquid and a C-7diazo-substituted tetracyline tetrafluoroborate, hexafluorophosphate, hexafluoroarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof is irradiated to provide a C7-fluoro-substituted tetracyline, or salt, solvate or combination thereof.
摘要翻译：本文提供了将C7-氨基取代的四环素转化为C7-氟取代的四环素以及由这些方法产生或在这些过程中使用的中间体的改进方法。在一个实施方案中，提供了热氟化方法，其中包含非极性有机溶剂和C7-重氮 - 取代的六氟磷酸四环素，六氟砷酸盐或六氟硅酸盐或其盐，溶剂化物或其组合的悬浮液被治愈以提供 C7-氟取代的四环素或其盐，溶剂合物或其组合。在另一个实施方案中，提供光解氟化，其中辐照包含离子液体和C-7重氮 - 取代的四氟硼酸四氟硼酸盐，六氟磷酸盐，六氟砷酸盐或六氟硅酸盐或其盐，溶剂化物或其组合的溶液以提供C7- 氟取代的四环素或其盐，溶剂化物或其组合。

2. 发明公开

EP3461809A1 TETRACYCLINE COMPOUNDS 审中-实审转让
公开(公告)号：EP3461809A1
公开(公告)日：2019-04-03
申请号：EP18192684.1
申请日：2013-08-30
申请人： Tetraphase Pharmaceuticals, Inc.
发明人： XIAO, Xiao-Yi , CLARK, Roger B. , HUNT, Diana Katharine , SUN, Cuixiang , RONN, Magnus , ZHANG, Wu-Yan , HE, Minsheng
IPC分类号： C07C237/26 , C07D221/18 , C07D471/04 , C07D207/08 , C07D295/155 , A61K31/437 , A61P31/04
摘要： The present invention is directed to a compound represented by Structural Formula (I):

or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I), or a pharmaceutically acceptable salt thereof, and its therapeutic use.

3. 发明授权

EP2890673B1 TETRACYCLINE COMPOUNDS 有权
公开(公告)号：EP2890673B1
公开(公告)日：2018-11-14
申请号：EP13762660.2
申请日：2013-08-30
申请人： Tetraphase Pharmaceuticals, Inc.
发明人： XIAO, Xiao-Yi , CLARK, Roger, B. , HUNT, Diana, Katharine , SUN, Cuixiang , RONN, Magnus , ZHANG, Wu-Yan , HE, Minsheng
IPC分类号： C07C237/26 , C07D221/18 , C07D471/04 , C07D207/08 , C07D295/155 , A61K31/437 , A61P31/04
CPC分类号： C07D207/09 , C07C237/26 , C07D207/08 , C07D221/18 , C07D295/155 , C07D471/04
摘要： The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I), or a pharmaceutically acceptable salt thereof, and its therapeutic use.

4. 发明公开

EP2890673A2 TETRACYCLINE COMPOUNDS 有权
标题翻译： TETRACYCLINVERBINDUNGEN
公开(公告)号：EP2890673A2
公开(公告)日：2015-07-08
申请号：EP13762660.2
申请日：2013-08-30
申请人： Tetraphase Pharmaceuticals, Inc.
发明人： XIAO, Xiao-Yi , CLARK, Roger, B. , HUNT, Diana, Katharine , SUN, Cuixiang , RONN, Magnus , ZHANG, Wu-Yan , HE, Minsheng
IPC分类号： C07C237/26 , C07D221/18 , C07D471/04 , C07D207/08 , C07D295/155 , A61K31/437 , A61P31/04
CPC分类号： C07D207/09 , C07C237/26 , C07D207/08 , C07D221/18 , C07D295/155 , C07D471/04
摘要： The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I), or a pharmaceutically acceptable salt thereof, and its therapeutic use.
摘要翻译：本发明涉及由结构式（I）表示的化合物或其药学上可接受的盐。结构式（I）的变量在本文中定义。还描述了包含结构式（I）的化合物或其药学上可接受的盐及其治疗用途的药物组合物。

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