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    Novel carboxylate derivatives exhibiting phospholipase A2 inhibitory activity
    3.
    发明公开
    Novel carboxylate derivatives exhibiting phospholipase A2 inhibitory activity 失效
    磷脂酶A2 hemmendenAktivität。

    公开(公告)号：EP0646569A1

    公开(公告)日：1995-04-05

    申请号：EP94307136.5

    申请日：1994-09-29

    申请人： SHIONOGI & CO., LTD.

    发明人： Ohtani, Mitsuaki ,  Kato, Toshiyuki ,  Hori, Yozo

    IPC分类号： C07C69/92 ,  C07C323/19 ,  C07C317/22 ,  C07C65/01 ,  C07C217/22 ,  C07C311/17 ,  C07C233/18 ,  C07D209/48 ,  C07D275/06 ,  C07D211/70 ,  C07D295/084

    CPC分类号： C07D209/48 ,  C07C69/92 ,  C07C217/22 ,  C07C233/69 ,  C07C233/92 ,  C07C235/46 ,  C07C235/60 ,  C07C311/17 ,  C07C311/48 ,  C07C317/18 ,  C07C323/03 ,  C07D211/70 ,  C07D275/06 ,  C07D295/088

    摘要： Novel carboxylate derivatives exhibiting phospholipase A₂ inhibitory activity are disclosed. Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed:

    wherein A is hydroxy, amino, or lower alkylamino; R¹ to R¹² are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R¹ to R¹² are not hydrogen; G¹ is a single bond, or a group of -(CH₂) x O(CH₂) y - wherein x and y are independently 0-5; G² is a single bond, oxygen, sulfur, carbonyl, etc.; G³ is alkyl, aryl, or a group of the formula:

    wherein R¹³ and R¹⁴ are independently hydrogen, alkyl, aryl, etc.; or R¹³ and R¹⁴ may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula:

    wherein Z is a carbon atom or a nitrogen atom,
       J, K ,and L are independently hydrogen or aryl, etc.; p and q are independently 0, 1, or 2; and n is an integer of 1 to 8.

    摘要翻译： 公开了显示磷脂酶A2抑制活性的新型羧酸衍生物。 具体地，公开了下列式及其药学上可接受的盐的化合物：其中A是羟基，氨基或低级烷基氨基; R 1至R 1独立地为氢，甲基，甲氧基或羟基，条件是R 1至R 12全部不为氢; G 1是单键或 - （CH 2）x O（CH 2）y - ，其中x和y独立地为0-5; G 2是单键，氧，硫，羰基等; G 3是烷基，芳基或下式的基团：其中R 1，3和R 4独立地是氢，烷基，芳基等; 或R 1'和R 1'可以与相邻的氮原子一起形成杂环基团或下式的基团：其中Z是碳原子或氮原子 ，J，K和L独立地为氢或芳基等; p和q独立地为0,1或2; n为1〜8的整数。