公开(公告)号：US20070093478A1

公开(公告)日：2007-04-26

申请号：US10596270

申请日：2005-01-21

申请人： Jerome Guillemont ,  Elisabeth Pasquier ,  David Lancois

发明人： Jerome Guillemont ,  Elisabeth Pasquier ,  David Lancois

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D215/14 ,  C07D215/227 ,  C07D215/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof the tautomers forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R1 is halo; p=1; R2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R3 is optionally substituted Ar or Het; q=1, R4 and R5 each independently are alkyl; R6 is hydrogen or a radical of formula is equal to 0 or 1 and R7 is hydrogen or Ar. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.

摘要翻译： 本发明涉及根据通式（Ia）或通式（Ib）的其取代的喹啉衍生物，其药学上可接受的酸或碱加成盐，其季胺，其互变异构体形式的立体化学异构形式和 N-氧化物形式。 所要求保护的化合物可用于治疗分枝杆菌病。 特别地，要求保护的化合物，其中R 1彼此独立地为卤素; p = 1; R 2是任选取代的烷氧基，烷基，Ar，Het或式R 3的基团是任选取代的Ar或Het; q = 1，R 4和R 5各自独立地为烷基; R 6是氢或式的基团等于0或1，R 7是氢或Ar。 还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗分枝杆菌疾病的药物中的用途以及制备方法 要求保护的化合物。