公开(公告)号：US20110124870A1

公开(公告)日：2011-05-26

申请号：US13020079

申请日：2011-02-03

申请人： Jérôme Emile Georges GUILLEMONT ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

发明人： Jérôme Emile Georges GUILLEMONT ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

IPC分类号： C07D405/04 ,  C07D409/04 ,  C07D215/14

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 tautomeric 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 r 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）的新的取代喹啉衍生物，其药学上可接受的酸或碱加成盐，其季胺，其立体化学异构形式，其互变异构形式和 其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R1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R3的基团是任选取代的Ar或Het; q = 1，R4和R5各自独立地为烷基; R6是氢或式r的基团等于0或1，而R7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。

公开(公告)号：US20130030016A1

公开(公告)日：2013-01-31

申请号：US13568569

申请日：2012-08-07

申请人： Koenraad Jozef Lodewijk ANDRIES ,  Anil KOUL ,  David Francis Alain LANÇOIS ,  Magali Madeleine Simone MOTTE ,  Jérôme Emile Georges GUILLEMONT

发明人： Koenraad Jozef Lodewijk ANDRIES ,  Anil KOUL ,  David Francis Alain LANÇOIS ,  Magali Madeleine Simone MOTTE ,  Jérôme Emile Georges GUILLEMONT

IPC分类号： A61K31/47 ,  A61P31/04

CPC分类号： A61K31/4353 ,  A61K45/06 ,  C07D215/227 ,  C07D215/36 ,  Y02A50/473 ,  A61K2300/00

摘要： Method of treating a bacterial infection other than a Mycobacterial infection, using a compound of formula (Ia) or (Ib) a N-oxide, a tautomeric form or a stereochemically isomeric form thereof; A− is a counter ion; and the substituents R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined.

摘要翻译： 使用式（Ia）或（Ib）化合物的N-氧化物，互变异构形式或其立体化学异构体形式治疗除分枝杆菌感染之外的细菌感染的方法; A-是抗衡离子; 取代基R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10如上所定义。

公开(公告)号：US20110008434A1

公开(公告)日：2011-01-13

申请号：US12845463

申请日：2010-07-28

申请人： Jérôme Emile Georges GUILLEMONT ,  Paul Theodoor Agnes Stevens ,  Alex Herman Copmans ,  Jozef Peeters ,  Alfred Elisabeth Stappers ,  Roger Petrus Gerebern Vandecruys ,  Paul Stoffels

发明人： Jérôme Emile Georges GUILLEMONT ,  Paul Theodoor Agnes Stevens ,  Alex Herman Copmans ,  Jozef Peeters ,  Alfred Elisabeth Stappers ,  Roger Petrus Gerebern Vandecruys ,  Paul Stoffels

IPC分类号： A61K9/28 ,  A61K31/505 ,  A61P31/18

CPC分类号： A61K31/505 ,  A61K9/2018 ,  A61K9/2866 ,  C07D239/48

摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.

摘要翻译： 本发明涉及药物组合物，其包含4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基 - 苯基]氨基] -2-嘧啶基]氨基] 苄腈和其制备方法。