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26 条记录 (耗时 0.05 秒)

    FUSED QUINOLINE DERIVATIVE AND USE THEREOF
    8.
    发明申请
    FUSED QUINOLINE DERIVATIVE AND USE THEREOF 失效
    熔融喹啉衍生物及其用途

    公开(公告)号：US20090270625A1

    公开(公告)日：2009-10-29

    申请号：US12476619

    申请日：2009-06-02

    申请人： Masahiro Kajino ,  Nicholas William Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

    发明人： Masahiro Kajino ,  Nicholas William Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; — --- represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.

    摘要翻译： 本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数， ---表示未取代（即不存在）或单键; ＆lt; img id =“CUSTOM-CHARACTER-00001”he =“2.79mm”wi =“7.03mm”file =“US20090270625A1-20091029-P00001.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键，或其盐等。

    FUSED QUINOLINE DERIVATIVE AND USE THEREOF
    9.
    发明申请
    FUSED QUINOLINE DERIVATIVE AND USE THEREOF 失效
    熔融喹啉衍生物及其用途

    公开(公告)号：US20090258893A1

    公开(公告)日：2009-10-15

    申请号：US12476626

    申请日：2009-06-02

    申请人： Masahiro Kajino ,  Nicholas William Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

    发明人： Masahiro Kajino ,  Nicholas William Hird ,  Naoki Tarui ,  Hiroshi Banno ,  Yasuhiko Kawano ,  Nobuhiro Inatomi

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P1/00

    CPC分类号： C07D471/04

    摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.

    摘要翻译： 本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数， “img id =”CUSTOM-CHARACTER-00001“he =”0.68mm“wi =”3.13mm“file =”US20090258893A1-20091015-P00001.TIF“img-content =”character“img-format =”tif“/> 表示未取代的（即不存在）或单键; ＆lt; img id =“CUSTOM-CHARACTER-00002”he =“1.02mm”wi =“3.13mm”file =“US20090258893A1-20091015-P00002.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键，或其盐等。

    Method of Screening Transmembrane Enzyme Inhibitory Substance
    10.
    发明申请
    Method of Screening Transmembrane Enzyme Inhibitory Substance 审中-公开
    筛选跨膜酶抑制物质的方法

    公开(公告)号：US20080220445A1

    公开(公告)日：2008-09-11

    申请号：US11664086

    申请日：2005-09-30

    申请人： Naoki Tarui

    发明人： Naoki Tarui

    IPC分类号： G01N33/53 ,  C12N9/99

    CPC分类号： C12Q1/37 ,  C12N9/6478 ,  G01N33/573 ,  G01N2333/96472 ,  G01N2500/00

    摘要： The present invention provides a screening method for a compound inhibiting a transmembrane enzyme activity by binding to a transmembrane region of the enzyme, characterized by using (a) a protein having a part or all of an amino acid sequence of the enzyme, comprising a region comprising an active center and a part or all of a transmembrane region of the transmembrane enzyme, and optionally (b) a protein having a part of an amino acid sequence of the transmembrane enzyme, comprising the region comprising the active center and lacking the above-mentioned part or all of the transmembrane region, and measuring the binding of a test substance to each protein and the enzyme activity of each protein, as well as a kit for screening comprising the above-mentioned protein of (a) and (b). Also, the present invention provides a β-secretase selective inhibitor comprising a β-secretase inhibiting substance binding to a transmembrane region of the enzyme, and particularly an inhibitor for prophylaxis and/or treatment of Alzheimer's disease, Down syndrome or Age-Associated Memory Impairment.

    摘要翻译： 本发明提供了通过与酶的跨膜区结合来抑制跨膜酶活性的化合物的筛选方法，其特征在于使用（a）具有部分或全部所述酶的氨基酸序列的蛋白质，所述蛋白质包含区域 其包含所述跨膜酶的活性中心和部分或全部跨膜区，以及任选地（b）具有所述跨膜酶的氨基酸序列的一部分的蛋白质，所述蛋白质包含所述活性中心并且缺少所述跨膜酶的区域， 上述部分或全部的跨膜区，测定被检物质与各蛋白质的结合以及各蛋白质的酶活性，以及​​包含上述（a）和（b）的蛋白质的筛选试剂盒。 此外，本发明提供了一种β-分泌酶选择性抑制剂，其包含结合酶的跨膜区的β-分泌酶抑制物质，特别是用于预防和/或治疗阿尔茨海默氏病，唐氏综合征或年龄相关记忆障碍的抑制剂 。