公开(公告)号：EP1125925A1

公开(公告)日：2001-08-22

申请号：EP00810128.9

申请日：2000-02-15

申请人： Applied Research Systems ARS Holding N.V.

发明人： Halazy, Serge ,  Schwarz, Matthias ,  Antonsson, Bruno ,  Bombrun, Agnès ,  Martinou, Jean-Claude ,  Church, Dennis

IPC分类号： C07D211/60 ,  A61K31/445 ,  C07D207/16 ,  A61K31/40 ,  A61P43/00 ,  C07D277/06 ,  A61K31/425 ,  A61K31/47 ,  C07D217/26 ,  C07C233/00 ,  C07C235/00

CPC分类号： C07D217/26 ,  C07B2200/07 ,  C07C237/22 ,  C07C2601/14 ,  C07D207/16 ,  C07D211/60 ,  C07D277/06

摘要： The present invention is related to substituted amine derivatives I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.
A 1 and A 2 are selected independently from each other from the group consisting of -C(O)- and -SO 2 -.
R a , R b , R 0 , R 1 and R 2 are as the application.

摘要翻译： 本发明涉及特别用作药物活性化合物的取代胺衍生物I以及含有咔唑类哌嗪衍生物的药物制剂。 所述取代的胺衍生物是Bax功能和/或活化的有效调节剂，特别是抑制剂。 本发明还涉及新型取代的胺衍生物及其制备方法。 A 1和A 2彼此独立地选自-C（O） - 和-SO 2 - 。 R a，R b，R o，R 1和R 2是应用。

公开(公告)号：EP1094063A1

公开(公告)日：2001-04-25

申请号：EP99810944.1

申请日：1999-10-18

申请人： Applied Research Systems ARS Holding N.V.

发明人： Halazy, Serge ,  Church, Dennis ,  Antonsson, Bruno ,  Bombrun, Agnès ,  Gerber, Patrick ,  Martinou Jean-Claude

IPC分类号： C07D403/06 ,  C07D407/14 ,  C07D417/14 ,  A61K31/495 ,  A61P25/28

CPC分类号： C07D209/88 ,  C07D209/86

摘要： The present invention is related to piperazine derivatives of carbazole notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.

摘要翻译： 本发明涉及咔唑的哌嗪衍生物，特别是用作药物活性化合物，以及含有咔唑类哌嗪衍生物的药物制剂。 所述咔唑的哌嗪衍生物是Bax功能和/或活化的有效调节剂，特别是抑制剂。 本发明还涉及咔唑的新型哌嗪衍生物及其制备方法。