AMIDE COMPOUNDS AND THE USE THEREOF
    6.
    发明公开
    AMIDE COMPOUNDS AND THE USE THEREOF 审中-公开
    酰胺及其用途

    公开(公告)号:EP2164326A1

    公开(公告)日:2010-03-24

    申请号:EP08754805.3

    申请日:2008-05-30

    IPC分类号: A01N43/40 A61K31/445

    摘要: The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R1 and R2 are each independently hydrogen, halogen, cyano, optionally substituted lower alky, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl etc. R3 and R4 are hydrogen, each optionally substituted lower alkyl, cycloalkyl, aryl or heterocyclyl etc.; X is ═O, optionally substituted lower alkyl, halogen, cyano, nitro etc., n is 0-5, m is 1 or 2 and p is 0-2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

    NITROGEN-CONTAINING TRICYCLIC DERIVATIVE HAVING HIV REPLICATION INHIBITORY ACTIVITY
    7.
    发明公开
    NITROGEN-CONTAINING TRICYCLIC DERIVATIVE HAVING HIV REPLICATION INHIBITORY ACTIVITY 审中-公开
    含有HIV复制抑制活性的含氮三环衍生物

    公开(公告)号:EP3305789A1

    公开(公告)日:2018-04-11

    申请号:EP16803241.5

    申请日:2016-05-27

    摘要: The present invention provides a novel compound having antiviral activity, especially HIV replication inhibitory activity and a medicament containing the same. The compound represented by the formula:

    wherein A 3 is CR 3A , CR 3A R 3B , N or NR 3C ; R 3A , R 3B , R 4A and R 4B are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted non-aromatic carbocyclyl; R 3C is a hydrogen atom, substituted or unsubstituted alkyl, or substituted or unsubstituted non-aromatic carbocyclyl; ring T 1 is substituted or unsubstituted nitrogen-containing non-aromatic heterocycle; R 1 is a hydrogen atom, halogen, cyano, or substituted or unsubstituted alkyl; R 2 is each independently substituted or unsubstituted alkyl or the like: n is 1 or 2; R 3 is substituted or unsubstituted aromatic carbocyclyl or the like; R 4 is a hydrogen atom or a carboxy protecting group.

    摘要翻译: 本发明提供具有抗病毒活性,特别是HIV复制抑制活性的新型化合物和含有其的药物。 由下式表示的化合物:其中A3是CR3A,CR3A,R3B,N或NR3C; R3A,R3B,R4A和R4B各自独立地为氢原子,卤素,氰基,取代或未取代的烷基,取代或未取代的炔基或取代或未取代的非芳族碳环基; R3C是氢原子,取代或未取代的烷基或取代或未取代的非芳族碳环基; 环T1是取代或未取代的含氮非芳香杂环; R1是氢原子,卤素,氰基或取代或未取代的烷基; R2各自独立地为取代或未取代的烷基等:n为1或2; R3是取代或未取代的芳族碳环基等; R4是氢原子或羧基保护基。