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72 条记录 (耗时 0.035 秒)

    Method for producing cyclic diamine derivative
    1.
    发明授权
    Method for producing cyclic diamine derivative 失效
    环二胺衍生物的制备方法

    公开(公告)号：US07576203B2

    公开(公告)日：2009-08-18

    申请号：US11631397

    申请日：2005-06-30

    申请人： Kimiyuki Shibuya ,  Ayako Tosaka

    发明人： Kimiyuki Shibuya ,  Ayako Tosaka

    IPC分类号： C07D213/76 ,  C07D401/12

    CPC分类号： C07D213/75 ,  C07D401/12 ,  C07D413/12

    摘要： The present invention provides an industrially useful method for synthesizing a cyclic diamine derivative (4) or a salt thereof which serves as an ACAT inhibitor.A 2-hydroxyacetylaminopyridine compound represented by formula (1), and a method for producing a cyclic diamine derivative represented by formula (4) or a salt thereof from compound (1) through 1) Step A-1, 2) Steps B-1 and B-2, or 3) Steps B-1, B-3, and B-4.

    摘要翻译： 本发明提供用作合成作为ACAT抑制剂的环状二胺衍生物（4）或其盐的工业上有用的方法。 由式（1）表示的2-羟基乙酰基氨基吡啶化合物和由式（4）表示的环状二胺衍生物或其盐从化合物（1）至1）步骤A-1,2）步骤B-1 和B-2，或3）步骤B-1，B-3和B-4。

    Method for Producing Cyclic Diamine Derivative
    3.
    发明申请
    Method for Producing Cyclic Diamine Derivative 失效
    生产环状二胺衍生物的方法

    公开(公告)号：US20080045714A1

    公开(公告)日：2008-02-21

    申请号：US11631397

    申请日：2005-06-30

    申请人： Kimiyuki Shibuya ,  Ayako Tosaka

    发明人： Kimiyuki Shibuya ,  Ayako Tosaka

    IPC分类号： C07D405/14

    CPC分类号： C07D213/75 ,  C07D401/12 ,  C07D413/12

    摘要： The present invention provides an industrially useful method for synthesizing a cyclic diamine derivative (4) or a salt thereof which serves as an ACAT inhibitor. A 2-hydroxyacetylaminopyridine compound represented by formula (1), and a method for producing a cyclic diamine derivative represented by formula (4) or a salt thereof from compound (1) through 1) Step A-1, 2) Steps B-1 and B-2, or 3) Steps B-1, B-3, and B-4.

    摘要翻译： 本发明提供用作合成作为ACAT抑制剂的环状二胺衍生物（4）或其盐的工业上有用的方法。 由式（1）表示的2-羟基乙酰基氨基吡啶化合物和由式（4）表示的环状二胺衍生物或其盐从化合物（1）至1）步骤A-1,2）步骤B-1 和B-2，或3）步骤B-1，B-3和B-4。

    METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE
    7.
    发明申请
    METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE 审中-公开
    减少，稳定和防止破碎的富含PLAQUE的方法

    公开(公告)号：US20110207742A1

    公开(公告)日：2011-08-25

    申请号：US13096477

    申请日：2011-04-28

    申请人： Hideyuki Kobayashi ,  Yasunobu Yoshinaka ,  Kimiyuki Shibuya

    发明人： Hideyuki Kobayashi ,  Yasunobu Yoshinaka ,  Kimiyuki Shibuya

    IPC分类号： A61K31/497 ,  A61P9/10 ,  A61P7/02

    CPC分类号： A61K31/497 ,  A61K31/47 ,  A61K2300/00

    摘要： There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-p yridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof There is also to provide a method for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion, comprising simultaneously administering, or separately administering with interval of time an effective amount of the compound 1, its pharmaceutically acceptable salt or a hydrate thereof and an effective amount of Pitavastatin to a patient in need thereof.

    摘要翻译： 提供的是减少富含脂质的斑块，稳定富含脂质的斑块和/或预防动脉粥样硬化病变中脂质丰富斑块破裂的药剂，其包含有效量的2- [4- [2-（ 苯并咪唑-2-基硫基）乙基]哌嗪-1-基] -N- [2,4-双（甲硫基）-6-甲基-3-吡啶基]乙酰胺（以下称为化合物1），其药学上可接受的 盐或其水合物和匹伐他汀，以及药学上可接受的载体，其中所述试剂旨在同时施用或分开施用于有需要的患者的时间间隔。还提供降低富含脂质的方法 斑块，富含脂质的斑块的稳定化和/或预防动脉粥样硬化病变中富含脂质的斑块的破裂，其包括同时施用或分开施用有效量的化合物1，其药学上可接受的盐或水合物 并且对有需要的患者有效量的匹伐他汀。

    Pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same
    8.
    发明授权
    Pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same 失效
    具有苄基（吡啶基甲基）胺结构的嘧啶化合物及其组合物

    公开(公告)号：US07750019B2

    公开(公告)日：2010-07-06

    申请号：US11835127

    申请日：2007-08-07

    申请人： Tadaaki Ohgiya ,  Toru Miura ,  Ayumu Okuda ,  Toshiharu Arai ,  Koichi Yamazaki ,  Taro Aoki ,  Katsutoshi Miyosawa ,  Haruki Shibata ,  Kimiyuki Shibuya

    发明人： Tadaaki Ohgiya ,  Toru Miura ,  Ayumu Okuda ,  Toshiharu Arai ,  Koichi Yamazaki ,  Taro Aoki ,  Katsutoshi Miyosawa ,  Haruki Shibata ,  Kimiyuki Shibuya

    IPC分类号： C07D239/42 ,  A61K31/505

    CPC分类号： C07D401/12

    摘要： A compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: (wherein R1, R2, R3, R4 and R5 are the same or different, and represent hydrogen atom, a halogen atom, a lower alkyl group etc., R6, R7 and R8 are the same or different, and represent hydrogen atom, a halogen atom, a lower alkyl group etc., R9 and R10 are the same or different, and represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group etc., and R11 represents hydrogen atom, a halogen atom, a lower alkoxy group, a (lower alkyl)thio(lower alkoxy) group, a (lower alkyl)sulfinyl(lower alkoxy) group, a (lower alkyl)sulfonyl(lower alkoxy) group etc.), which has potent inhibitory activity on CETP.

    摘要翻译： 由下列通式（I）表示的化合物或其盐或其溶剂化物：（其中R1，R2，R3，R4和R5相同或不同，表示氢原子，卤素原子，低级烷基 基团等，R6，R7和R8相同或不同，表示氢原子，卤素原子，低级烷基等，R9和R10相同或不同，表示氢原子，低级烷基， （低级环烷基）（低级烷基）等，R11表示氢原子，卤素原子，低级烷氧基，（低级烷基）硫代（低级烷氧基），（低级烷基）亚磺酰基（低级烷氧基） 基团，（低级烷基）磺酰基（低级烷氧基）等），其对CETP具有有效的抑制活性。

    Process for producing optically active ester
    10.
    发明授权
    Process for producing optically active ester 失效
    光学活性酯的制备方法

    公开(公告)号：US07582791B2

    公开(公告)日：2009-09-01

    申请号：US12063440

    申请日：2006-08-24

    申请人： Takaaki Araki ,  Yukiyoshi Yamazaki ,  Kimiyuki Shibuya

    发明人： Takaaki Araki ,  Yukiyoshi Yamazaki ,  Kimiyuki Shibuya

    IPC分类号： C07C69/66

    CPC分类号： C07C319/14 ,  C07B53/00 ,  C07B2200/07 ,  C07C67/317 ,  C07C69/675 ,  C07C323/52

    摘要： A process for producing an optically active 2-hydroxybutyric ester (1), characterized by including reacting an optically active 2,3-epoxybutyric ester (2) with a thiol in the presence of scandium trifluoromethanesulfonate or ytterbium trifluoromethanesulfonate, to thereby produce Compound (3), and subjecting Compound (3) to desulfurization reaction: (wherein R represents a C1 to C6 alkyl group or a C7 or C8 aralkyl group; R1 represents a C1 to C12 alkyl group or a phenyl group; and * represents S- or R-absolute configuration). The present invention provides a process for producing an optically active 2-hydroxybutyric ester at high yield and high optical purity.

    摘要翻译： 一种光学活性2-羟基丁酸酯（1）的制造方法，其特征在于，在三氟甲磺酸钪或三氟甲磺酸镱的存在下，使光学活性的2,3-环氧丁酸酯（2）与硫醇反应，由此制备化合物 ）和化合物（3）进行脱硫反应：（其中R表示C1至C6烷基或C7或C8芳烷基; R1表示C1至C12烷基或苯基; *表示S-或R - 绝对配置）。 本发明提供以高产率和高光学纯度制备光学活性2-羟基丁酸酯的方法。