公开(公告)号：US07498343B2

公开(公告)日：2009-03-03

申请号：US11007026

申请日：2004-12-08

申请人： Jozef Frans Elisabetha Van Gestel ,  Jérôme Emile Georges Guillemont ,  Marc Gaston Venet ,  Hervé Jean Joseph Poignet ,  Laurence Françoise Bernadette Decrane ,  Daniel F. J. Vernier ,  Frank Christopher Odds

发明人： Jozef Frans Elisabetha Van Gestel ,  Jérôme Emile Georges Guillemont ,  Marc Gaston Venet ,  Hervé Jean Joseph Poignet ,  Laurence Françoise Bernadette Decrane ,  Daniel F. J. Vernier ,  Frank Christopher Odds

IPC分类号： A61K31/44 ,  C07D215/38

CPC分类号： C07D215/227 ,  C07D215/36 ,  C07D215/48 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D471/04

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 stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. 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）的药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式和N-氧化物形式的新的取代喹啉衍生物 其中。 所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌和马氏海马。 特别是要求保护的化合物，其中R 1为溴，p = 1，R 2为烷氧基，R 3为任选取代的萘基或苯基，q为1，R 4和R 5各自独立地为氢，甲基或乙基， R6是氢，r等于0或1，而R7是氢。 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。