公开(公告)号：US20140038989A1

公开(公告)日：2014-02-06

申请号：US14112564

申请日：2012-04-20

申请人： Emilio Alvarez-Ruiz ,  Luis Ballell-Pages ,  Julia Castro Pichel ,  Lourdes Encinas ,  Jorge Esquivias ,  Franscisco Gamo-Benito ,  Maria Cruz Garcia-Palancar ,  Modesto Jesus Remuinan-Blanco

发明人： Emilio Alvarez-Ruiz ,  Luis Ballell-Pages ,  Julia Castro Pichel ,  Lourdes Encinas ,  Jorge Esquivias ,  Franscisco Gamo-Benito ,  Maria Cruz Garcia-Palancar ,  Modesto Jesus Remuinan-Blanco

IPC分类号： C07D487/04 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

摘要： A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: R1 represents a group selected from: i) phenyl optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; furanyl, thiophenyl, pyrrolyl, pyridyl, cyclohexyl or naphthyl, each of which is optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; and iii) benzo[1,3]dioxo5-yl or 2,3-dihydrobenzo[1,4]dioxin-6-yl; R2 represents CF3, C1-4alkyl, or CHF2; when R1 represents optionally substituted furanyl, thiophenyl, pyrrolyl, pyridyl or naphthyl, R3 represents Et; when R1 represents optionally substituted cyclohexyl, R3 represents Et or Me; otherwise R3 represents Et, Me, Br or OMe, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided, together with certain novel compounds.

摘要翻译： 式（I）化合物或其药学上可接受的盐：其中：R1表示选自以下的基团：i）任选被一个或两个独立地选自Me，OMe，CF 3，F，Cl和NMe 2的取代基取代的苯基; 呋喃基，噻吩基，吡咯基，吡啶基，环己基或萘基，其各自任选被一个或两个独立地选自Me，OMe，CF 3，F，Cl和NMe 2的取代基取代; 和iii）苯并[1,3]二氧代-5-基或2,3-二氢苯并[1,4]二恶英-6-基; R 2表示CF 3，C 1-4烷基或CHF 2; 当R 1表示任选取代的呋喃基，噻吩基，吡咯基，吡啶基或萘基时，R 3表示Et; 当R 1表示任选取代的环己基时，R 3表示Et或Me; 否则R3表示Et，Me，Br或OMe，含有它们的组合物，它们在治疗中的用途，例如治疗结核病以及制备这些化合物的方法，以及某些新型化合物。