NOVEL PYRROLE DERIVATIVE HAVING UREIDE GROUP AND AMINOCARBONYL GROUP AS SUBSTITUENTS
    7.
    发明公开

    公开(公告)号:EP2116530A1

    公开(公告)日:2009-11-11

    申请号:EP08720883.1

    申请日:2008-02-26

    摘要: Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R 1 represents a halogen atom, a hydrogen atom, a lower alkyl group or the like; R 2 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like.

    摘要翻译: 本发明的目的是研究具有脲基和氨基羰基作为取代基的新型吡咯衍生物或其盐的合成,以发现其衍生物或其盐的药理作用,并找到药物 其通过口服给药对视网膜疾病等具有预防和/或治疗作用。 由通式(1)表示的化合物或其盐对白介素-6的产生具有抑制活性和/或对脉络膜新生血管形成的抑制作用,因此可用作疾病的预防和/或治疗剂 与白细胞介素-6相关,眼炎和/或视网膜疾病。 在该式中,环A表示苯环等; R 1表示卤原子,氢原子,低级烷基等; R 2表示卤素原子,可以具有取代基的低级烷基,低级烯基,可具有取代基的低级炔基,低级环烷基,芳基,羟基,低级烷氧基, 可以具有取代基等; n表示0,1,2,3等。