发明名称 Pharmaceutically active pyrrolidine derivatives as bax inhibitors
摘要 The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c). The present invention is furthermore related to novel pharmaceutically activity substituted pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of O, S, CR<6>R<7>, NOR<6>, NNR<6>R<7>; A is selected from the group consisting of -(C-O)-, -(C-O)-O-, -C(-NH)-, -(C-O)-NH-, -(C-S)-NH, -SO2-, -SO2NH-; -CH2-; B is either a group -(C-O)-NR<8>R<9> or represents a heterocyclic residue having the formula (II) wherein Q is NR<10>, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
申请公布号 AU5222201(A) 申请公布日期 2001.10.15
申请号 AU20010052222 申请日期 2001.03.20
申请人 APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. 发明人 SERGE HALAZY;MATTHIAS SCHWARZ;ANNA QUATTROPANI;RUSSEL THOMAS;ANTHONY BAXTER;AGNES BOMBRUN
分类号 C07D401/04;A61K31/40;A61K31/401;A61K31/4025;A61K31/403;A61K31/4184;A61K31/433;A61K31/454;A61K31/4545;A61K31/4709;A61K31/4725;A61K31/496;A61K31/506;A61K31/517;A61K31/5377;A61P1/04;A61P1/16;A61P9/02;A61P9/04;A61P9/10;A61P11/06;A61P15/08;A61P15/12;A61P21/04;A61P25/00;A61P25/08;A61P25/16;A61P25/28;A61P27/02;A61P29/00;A61P31/04;A61P31/18;A61P37/06;C07D207/22;C07D207/24;C07D207/325;C07D401/10;C07D401/12;C07D403/04;C07D403/06;C07D403/12;C07D403/14;C07D405/06;C07D405/12;C07D405/14;C07D409/12;C07D417/12 主分类号 C07D401/04
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