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    (AZA)INDOLIZINE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
    2.
    发明申请
    (AZA)INDOLIZINE DERIVATIVE AND PHARMACEUTICAL USE THEREOF 有权
    （AZA）吲哚衍生物及其药物用途

    公开(公告)号：US20130217878A1

    公开(公告)日：2013-08-22

    申请号：US13824147

    申请日：2011-09-28

    申请人： Masato Iizuka ,  Kazuo Shimizu

    发明人： Masato Iizuka ,  Kazuo Shimizu

    IPC分类号： C07D487/04 ,  C07D471/04

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： (Aza)indolizine derivatives represented by Formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In Formula (I), 0 to 2 of X1, X2, X3 and X4 are a nitrogen atom and the others are CR1; one of T1 and T2 represents cyano and the other represents a group represented by Formula (A), with the proviso that when T1 is cyano, at least one of X1 to X4 is a nitrogen atom; R1 independently represents a hydrogen atom, a halogen atom, a hydroxy group, C1-6 alkyl, C1-6 alkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; R2 independently represents a fluorine atom, a hydroxy group or the like.

    摘要翻译： 具有黄嘌呤氧化酶抑制活性的式（I）表示的（Aza）中氮茚衍生物，可用作预防或治疗与血清尿酸水平异常相关的疾病，其前药，其盐等的药剂。 在式（I）中，X 1，X 2，X 3和X 4的0〜2为氮原子，其余为CR 1; T1和T2之一表示氰基，另一个表示由式（A）表示的基团，条件是当T1为氰基时，X 1至X 4中的至少一个为氮原子; R1独立地表示氢原子，卤素原子，羟基，C1-6烷基，C1-6烷氧基等; 环U表示苯环等; m表示0〜2的整数; R2独立地表示氟原子，羟基等。

    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    3.
    发明申请
    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 审中-公开
    熔融杂环衍生物及其用于医疗用途的方法

    公开(公告)号：US20110201815A1

    公开(公告)日：2011-08-18

    申请号：US13124336

    申请日：2009-10-14

    申请人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

    发明人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

    IPC分类号： C07D401/10 ,  C07D417/10

    CPC分类号： C07D401/04 ,  A61K31/427 ,  A61K31/443 ,  A61K31/4439 ,  C07D405/04 ,  C07D417/04

    摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

    摘要翻译： 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠合杂环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前体药物，其盐或类似物 。 在式（I）中，T代表三氟甲基，硝基或氰基; 环Q表示杂芳基; X1和X2独立地表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

    (aza)indolizine derivative and pharmaceutical use thereof
    6.
    发明授权
    (aza)indolizine derivative and pharmaceutical use thereof 有权

    公开(公告)号：US09643969B2

    公开(公告)日：2017-05-09

    申请号：US13824147

    申请日：2011-09-28

    申请人： Masato Iizuka ,  Kazuo Shimizu

    发明人： Masato Iizuka ,  Kazuo Shimizu

    IPC分类号： C07D487/04 ,  C07D471/04

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： (Aza)indolizine derivatives represented by Formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In Formula (I), 0 to 2 of X1, X2, X3 and X4 are a nitrogen atom and the others are CR1; one of T1 and T2 represents cyano and the other represents a group represented by Formula (A), with the proviso that when T1 is cyano, at least one of X1 to X4 is a nitrogen atom; R1 independently represents a hydrogen atom, a halogen atom, a hydroxy group, C1-6 alkyl, C1-6 alkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; R2 independently represents a fluorine atom, a hydroxy group or the like.

    INDOLIZINE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    10.
    发明申请
    INDOLIZINE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
    用于医疗用途的衍生衍生物及其用途

    公开(公告)号：US20120015972A1

    公开(公告)日：2012-01-19

    申请号：US13259621

    申请日：2010-03-30

    申请人： Kazuo Shimizu ,  Masato Iizuka ,  Yasushi Takigawa

    发明人： Kazuo Shimizu ,  Masato Iizuka ,  Yasushi Takigawa

    IPC分类号： A61K31/437 ,  A61P13/12 ,  A61P19/02 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.

    摘要翻译： 本发明提供了可用作预防或治疗与血清尿酸水平异常等有关的疾病的药剂的化合物。 也就是说，本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的中氮茚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药，其盐或 类似。 在该式中，环U表示芳基或杂芳基; R1表示卤素，羟基等; R 2表示卤素，羟基，烷基，烷氧基，被氟取代的烷基，被氟取代的烷氧基等; m表示0〜2的数; n表示0〜3的数; R 3表示氢，氟等。