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    NOVEL INDOLE DERIVATIVE HAVING, CARBAMOYL GROUP, UREIDO GROUP AND SUBSTITUTED OXY GROUP
    1.
    发明申请
    NOVEL INDOLE DERIVATIVE HAVING, CARBAMOYL GROUP, UREIDO GROUP AND SUBSTITUTED OXY GROUP 失效
    新加坡衍生产品有限公司，卡巴集团，乌代组和替代氧化集团

    公开(公告)号：US20110124668A1

    公开(公告)日：2011-05-26

    申请号：US13054041

    申请日：2009-07-14

    申请人： Kenji Kawashima ,  Hiroshi Enomoto ,  Minoru Yamamoto ,  Masaaki Murai

    发明人： Kenji Kawashima ,  Hiroshi Enomoto ,  Minoru Yamamoto ,  Masaaki Murai

    IPC分类号： A61K31/404 ,  C07D209/42 ,  C07D403/12 ,  A61K31/506 ,  C07D401/12 ,  A61K31/4439 ,  C07D405/10 ,  A61P29/00 ,  A61P27/06 ,  A61P17/00 ,  A61P27/02 ,  A61P35/00 ,  A61P3/00 ,  A61P25/00 ,  A61P37/06 ,  A61P31/00 ,  A61P37/08

    CPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04

    摘要： The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKKβ inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKKβ. In the formula, R1 represents a hydrogen atom, a lower alkyl group which may have a substituent, a hydroxy group, or a lower alkoxy group which may have a substituent, or the like; R2 represents a hydrogen atom, a lower alkyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, an aryl group which may have a substituent, or a heterocyclic group which may have a substituent, or the like; R3 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group which may have a substituent, a lower alkynyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, or the like; m represents 0, 1, 2, or the like.

    摘要翻译： 本发明涉及具有氨基甲酰基，脲基和取代的氧基或其盐的新型吲哚衍生物的合成研究以及衍生物的药物作用。 由通式（1）表示的化合物及其盐具有IKK＆bgr; 抑制活性，并且可用作被认为与IKK＆bgr相关的疾病的预防和/或治疗剂。 式中，R 1表示氢原子，可以具有取代基的低级烷基，羟基或可具有取代基的低级烷氧基等。 R2表示氢原子，可以具有取代基的低级烷基，可以具有取代基的低级环烷基，可以具有取代基的芳基或可以具有取代基的杂环基等。 R3表示卤原子，可以具有取代基的低级烷基，可以具有取代基的低级烯基，可以具有取代基的低级炔基，可以具有取代基的低级环烷基，可以具有取代基的低级环烷基， 可以具有取代基，可以具有取代基的杂环基等; m表示0,1,2等。

    NOVEL PYRROLE DERIVATIVE HAVING UREIDO GROUP AND AMINOCARBONYL GROUP AS SUBSTITUENTS
    4.
    发明申请
    NOVEL PYRROLE DERIVATIVE HAVING UREIDO GROUP AND AMINOCARBONYL GROUP AS SUBSTITUENTS 失效
    具有尿素组和氨基羰基的新型衍生物作为替代物

    公开(公告)号：US20100099675A1

    公开(公告)日：2010-04-22

    申请号：US12449794

    申请日：2008-02-26

    申请人： Kenji Kawashima ,  Hiroshi Enomoto ,  Noriko Ishizaka ,  Minoru Yamamoto ,  Kazuhiro Kudou ,  Masaaki Murai ,  Takaaki Inaba ,  Kazuyoshi Okamoto

    发明人： Kenji Kawashima ,  Hiroshi Enomoto ,  Noriko Ishizaka ,  Minoru Yamamoto ,  Kazuhiro Kudou ,  Masaaki Murai ,  Takaaki Inaba ,  Kazuyoshi Okamoto

    IPC分类号： A61K31/5377 ,  C07D207/00 ,  A61K31/40 ,  C07D401/02 ,  A61K31/4439 ,  C07D401/12 ,  A61K31/445 ,  C07D403/12 ,  A61K31/497 ,  C07D413/12

    CPC分类号： C07D207/34 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/04 ,  C07D417/12

    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; R1 represents a halogen atom, a hydrogen atom, a lower alkyl group or the like; R2 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或其盐的新型吡咯衍生物的合成，以发现其衍生物或其盐的药理作用，并找到药剂 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; R1表示卤素原子，氢原子，低级烷基等; R 2表示卤原子，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，可以具有取代基的低级烷氧基 具有取代基等; n表示0,1,2,3等。

    Indole derivative having, carbamoyl group, ureido group and substituted oxy group
    5.
    发明授权
    Indole derivative having, carbamoyl group, ureido group and substituted oxy group 失效
    具有氨基甲酰基，脲基和取代氧基的吲哚衍生物

    公开(公告)号：US08445529B2

    公开(公告)日：2013-05-21

    申请号：US13054041

    申请日：2009-07-14

    申请人： Kenji Kawashima ,  Hiroshi Enomoto ,  Minoru Yamamoto ,  Masaaki Murai

    发明人： Kenji Kawashima ,  Hiroshi Enomoto ,  Minoru Yamamoto ,  Masaaki Murai

    IPC分类号： A61K31/404 ,  C07D209/40

    CPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04

    摘要： An indole compound having a carbamoyl group, a ureido group and a substituted oxy group having the following formula (1) or a salt thereof: In the formula (1), R1 represents a hydrogen atom, an alkyl group, a hydroxy group, or an alkoxy group; R2 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R3 represents a halogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group, a heterocyclic group an alkoxy group, an alkenyloxy group, an alkynyloxy group, a cycloalkyloxy group, an aryloxy group or a heterocyclic oxy group; m represents 0, 1, 2, or 3.

    摘要翻译： 具有氨基甲酰基，脲基和具有下式（1）的取代的氧基的吲哚化合物或其盐：在式（1）中，R 1表示氢原子，烷基，羟基或 烷氧基 R2表示氢原子，烷基，环烷基，芳基或杂环基; R3表示卤素原子，烷基，烯基，炔基，环烷基，芳基，杂环基，烷氧基，烯氧基，炔氧基，环烷氧基，芳氧基或 杂环氧基; m表示0,1,2或3。