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    Cycloalkene derivatives, process for producing the same, and use
    1.
    发明授权
    Cycloalkene derivatives, process for producing the same, and use 有权
    环烯烃衍生物，生产方法和使用

    公开(公告)号：US06495604B1

    公开(公告)日：2002-12-17

    申请号：US09622392

    申请日：2000-08-14

    申请人： Yuzo Ichimori ,  Masayuki Ii ,  Katsumi Itoh ,  Tomoyuki Kitazaki ,  Junji Yamada

    发明人： Yuzo Ichimori ,  Masayuki Ii ,  Katsumi Itoh ,  Tomoyuki Kitazaki ,  Junji Yamada

    IPC分类号： A61K3118

    CPC分类号： C07D249/08 ,  C07C311/14 ,  C07C2601/10 ,  C07C2601/16 ,  C07C2601/18 ,  C07D249/06 ,  C07D257/04 ,  C07D275/06

    摘要： The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseases such as cardiac disease, autoimmune disease, septick shock, etc.

    摘要翻译： 本发明提供由下式表示的化合物：其中R表示任选具有取代基的脂族烃基，任选具有取代基的芳族烃基，任选具有取代基的杂环基，由式OR1表示的基团（其中R1表示 氢原子或任选具有取代基的脂族烃基）或由下式表示的基团：其中R 1b表示氢原子或任选具有取代基的脂族烃基，R 1c与R 1b相同或不同，为氢原子或脂族 任选具有取代基的烃基，R 0表示氢原子或脂族烃基，或R和R 0表示彼此的键，Ar表示任选具有取代基的芳香族烃基，n表示1〜4的整数，或者 其盐，其是用于预防或治疗诸如心脏病的疾病的药剂 麻疹，败血性休克等

    Screening method for a substance that binds to an intracellular region of TLR4
    5.
    发明授权
    Screening method for a substance that binds to an intracellular region of TLR4 失效
    结合TLR4细胞内区域的物质的筛选方法

    公开(公告)号：US08329420B2

    公开(公告)日：2012-12-11

    申请号：US12225721

    申请日：2007-03-29

    申请人： Osamu Hazeki ,  Kaoru Hazeki ,  Masayuki Ii ,  Naoko Matsunaga

    发明人： Osamu Hazeki ,  Kaoru Hazeki ,  Masayuki Ii ,  Naoko Matsunaga

    IPC分类号： G01N33/567 ,  C12N1/21 ,  C12N1/19 ,  C12N5/10 ,  C12N5/16 ,  C12N5/18 ,  C12N5/22 ,  C07K14/705

    CPC分类号： G01N33/566 ,  G01N2333/70596 ,  G01N2500/04 ,  G01N2500/10

    摘要： The present invention provides a method of screening for a drug for the prophylaxis or treatment of at least one disease selected from the group consisting of cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, severe sepsis and septic shock, which includes selecting a substance that binds to an intracellular region of TLR4, and inhibits signal transduction from said molecule, and a kit for this method, which contains (1) a cell that expresses wild-type TLR4 and (2) a cell that expresses a mutant TLR4, and which can detect a signal from TLR4 with expression of a reporter gene as an index.

    摘要翻译： 本发明提供了一种筛选用于预防或治疗选自心脏病，自身免疫疾病，炎性疾病，中枢神经系统疾病，感染性疾病，败血症，严重败血症和败血症的至少一种疾病的药物的方法 其包括选择与TLR4的细胞内区域结合的物质，并抑制所述分子的信号转导，以及用于该方法的试剂盒，其包含（1）表达野生型TLR4的细胞和（2）细胞 其表达突变体TLR4，并且可以以报告基因的表达作为指标检测来自TLR4的信号。

    Substituted aromatic-ring compounds, process for producing the same, and use
    6.
    发明授权
    Substituted aromatic-ring compounds, process for producing the same, and use 失效

    公开(公告)号：US07078540B1

    公开(公告)日：2006-07-18

    申请号：US10048938

    申请日：2000-08-03

    申请人： Norikazu Tamura ,  Takashi Ichikawa ,  Masayuki Ii

    发明人： Norikazu Tamura ,  Takashi Ichikawa ,  Masayuki Ii

    IPC分类号： C07D315/00 ,  C07D321/00

    CPC分类号： C07C317/44 ,  C07C2601/10

    摘要： A compound of the formula: wherein R1 is an aliphatic hydrocarbon group optionally having substituent(s), an aromatic hydrocarbon group optionally having substituent(s), a heterocyclic group optionally having substituent(s), a group of the formula: OR1a wherein R1a is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), or a group of the formula: wherein R1b and R1c are the same or different and each is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), X is a methylene group, a nitrogen atom, a sulfur atom or an oxygen atom, Y is an optionally substituted methylene group or an optionally substituted nitrogen atom, ring A is a 5 to 8-membered ring optionally substituted further by 1 to 4 substituent(s) selected from (1) an aliphatic hydrocarbon group optionally having substituent(s), (2) an aromatic hydrocarbon group optionally having substituent(s), (3) a group of the formula: OR2 wherein R2 is a hydrogen atom, or an aliphatic hydrocarbon group optionally having substituent(s) and (4) a halogen atom, Ar is an aromatic hydrocarbon group optionally having substituent(s), a group of the formula: is a group of the formula: or the formula: m is an integer of 0 to 2, n is an integer of 1 to 3, and the sum of m and n is not more than 4, provided that when X is a methylene group, Y is an optionally substituted methylene group, and a salt thereof have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases, such as cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, septic shock and the like.

    Screening Method
    7.
    发明申请
    Screening Method 失效
    筛选方法

    公开(公告)号：US20090317833A1

    公开(公告)日：2009-12-24

    申请号：US12225721

    申请日：2007-03-29

    申请人： Osamu Hazeki ,  Kaoru Hazeki ,  Masayuki Ii ,  Naoko Matsunaga

    发明人： Osamu Hazeki ,  Kaoru Hazeki ,  Masayuki Ii ,  Naoko Matsunaga

    IPC分类号： G01N33/53

    CPC分类号： G01N33/566 ,  G01N2333/70596 ,  G01N2500/04 ,  G01N2500/10

    摘要： The present invention provides a method of screening for a drug for the prophylaxis or treatment of at least one disease selected from the group consisting of cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, severe sepsis and septic shock, which includes selecting a substance that binds to an intracellular region of TLR4, and inhibits signal transduction from said molecule, and a kit for this method, which contains (1) a cell that expresses wild-type TLR4 and (2) a cell that expresses a mutant TLR4, and which can detect a signal from TLR4 with expression of a reporter gene as an index.

    摘要翻译： 本发明提供了一种筛选用于预防或治疗选自心脏病，自身免疫疾病，炎性疾病，中枢神经系统疾病，感染性疾病，败血症，严重败血症和败血症的至少一种疾病的药物的方法 其包括选择与TLR4的细胞内区域结合的物质，并抑制所述分子的信号转导，以及用于该方法的试剂盒，其包含（1）表达野生型TLR4的细胞和（2）细胞 其表达突变体TLR4，并且可以以报告基因的表达作为指标检测来自TLR4的信号。

    Pharmaceutical Agent
    8.
    发明申请
    Pharmaceutical Agent 审中-公开
    药剂

    公开(公告)号：US20090105314A1

    公开(公告)日：2009-04-23

    申请号：US12227359

    申请日：2007-05-14

    申请人： Masayuki Ii ,  Hideyasu Matsuda ,  Kouji Mouri

    发明人： Masayuki Ii ,  Hideyasu Matsuda ,  Kouji Mouri

    IPC分类号： A61K31/24 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/428 ,  A61P9/00

    CPC分类号： A61K31/215

    摘要： The present invention provides an agent for the prophylaxis or treatment of complications after coronary-artery bypass surgery or cardiac diseases, autoimmune diseases, central nervous system diseases, inflammatory diseases, sepsis, severe sepsis or septic shock in a patient who undergoes coronary-artery bypass surgery, which comprises a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof, and an agent for the prophylaxis or treatment of sepsis and the like, as well as complications after coronary-artery bypass surgery, which is prepared for administration of ethyl (6R)-6-[(2-chloro-4-fluoroanilino)sulfonyl]-1-cyclohexene-1-carboxylate or a salt thereof or a prodrug thereof in a specific dose at a specific administration time.

    摘要翻译： 本发明提供了用于预防或治疗冠状动脉旁路手术后并发症的药物或心脏疾病，自身免疫性疾病，中枢神经系统疾病，炎性疾病，败血症，严重脓毒症或败血症休克的患者。 手术，其包含由式（I）表示的化合物：其中每个符号如说明书中所定义，或由式（II）表示的化合物：其中每个符号如说明书中所定义，或其盐或 其前药，以及用于预防或治疗败血症等的试剂以及冠状动脉搭桥手术后的并发症，其制备用于给予（6R）-6 - [（2-氯-4- 氟苯胺基）磺酰基] -1-环己烯-1-羧酸酯或其盐或其前药在特定给药时间内以特定剂量。