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    • 7. 发明授权
    • Pharmaceutically active pyrrolidine derivatives as Bax inhibitors
    • 作为Bax抑制剂的药物活性吡咯烷衍生物
    • US07018988B2
    • 2006-03-28
    • US10240000
    • 2001-03-20
    • Serge HalazyAnna QuattropaniAgnes BombrunMattias SchwarzRussel ThomasAnthony Baxter
    • Serge HalazyAnna QuattropaniAgnes BombrunMattias SchwarzRussel ThomasAnthony Baxter
    • A01N57/00A61K31/675
    • C07D401/12C07D207/22C07D403/04C07D403/06C07D403/14C07D405/06C07D405/12C07D405/14C07D409/12C07D417/12
    • 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 R , NOR , NNR R ; 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 R or represents a heterocyclic residue having the formula (II) wherein Q is NR , 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.
    • 本发明涉及式(I)的新的取代的吡咯烷衍生物。 所述化合物优选用作药物活性化合物。 具体地,式(I)的吡咯烷衍生物可用于治疗和/或预防神经退行性疾病,与多组胺胺束相关的疾病,癫痫,缺血,不育症,心血管疾病,肾脏缺氧,肝炎和艾滋病。 所述吡咯烷衍生物显示相对于细胞死亡激动剂Bax和/或导致Bax的活化途径的调节和最显着的下调至抑制活性,因此可以阻止细胞色素(c)的释放。 本发明还涉及新的药学活性取代的吡咯烷衍生物及其制备方法,其中X选自O,S,CR 6 R 7,NOR 6,NNR <6> R 7; A选自 - (CO) - , - (CO)-O - , - C(-NH) - , - (CO)-NH-, - (CS)-NH,-SO 2 - SO2NH-; -CH 2 - ; B是基团 - (C-O)-NR 8 R 9,或表示具有式(II)的杂环残基,其中Q是NR 10,O或S; n是选自0,1或2的整数; Y,Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。