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    METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE
    4.
    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
    5.
    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
    7.
    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。

    PROCESS FOR PRODUCING OPTICALLY ACTIVE ESTER
    9.
    发明申请
    PROCESS FOR PRODUCING OPTICALLY ACTIVE ESTER 失效
    生产光学活性酯的方法

    公开(公告)号：US20090118535A1

    公开(公告)日：2009-05-07

    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。

    Amide compounds and medications containing the same technical field
    10.
    发明授权
    Amide compounds and medications containing the same technical field 失效
    酰胺化合物和含有相同技术领域的药物

    公开(公告)号：US07414066B2

    公开(公告)日：2008-08-19

    申请号：US10985915

    申请日：2004-11-09

    申请人： Kimiyuki Shibuya ,  Toru Miura ,  Katsumi Kawamine ,  Yukihiro Sato ,  Tadaaki Ohgiya ,  Takahiro Kitamura ,  Chiyoka Ozaki ,  Toshiyuki Edano ,  Mitsuteru Hirata

    发明人： Kimiyuki Shibuya ,  Toru Miura ,  Katsumi Kawamine ,  Yukihiro Sato ,  Tadaaki Ohgiya ,  Takahiro Kitamura ,  Chiyoka Ozaki ,  Toshiyuki Edano ,  Mitsuteru Hirata

    IPC分类号： A61K31/4439 ,  C07D401/12

    CPC分类号： C07D403/12 ,  A61K31/4439 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

    摘要： The present invention provides to a novel compound having an ACAT inhibiting activity.The present invention relates to compounds represented by formula (I) wherein represents an optionally substituted divalent residue such as benzene, pyridine, cyclohexane or naphthalene, or a group, Het represents a 5- to 8-membered, substituted or unsubstituted heterocyclic group containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, such as a monocyclic group, a polycyclic group or a group of a fused ring, X represents —NH—, an oxygen atom or a sulfur atom, Y represents —NR4—, an oxygen atom, a sulfur atom, a sulfoxide or a sulfone, Z represents a single bond or —NR5—, R4 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds.

    摘要翻译： 本发明提供具有ACAT抑制活性的新型化合物。 本发明涉及由式（I）表示的化合物，其中表示任选取代的二价残基例如苯，吡啶，环己烷或萘，或者基团，Het表示5至8元，取代或未取代的杂环基， 至少一个选自氮原子，氧原子和硫原子的杂原子，如单环基团，多环基团或稠环基团，X表示-NH-，氧原子或硫原子 原子，Y表示-NR 4 - ，氧原子，硫原子，亚砜或砜，Z表示单键或-NR 5 - ， - R 4表示氢原子，低级烷基，芳基或任选取代的甲硅烷基低级烷基，R 5表示氢原子，低级烷基，芳基 基团或任选取代的甲硅烷基低级烷基，n为1至15的整数，或其盐或溶剂化物， d含有这些化合物中的至少一种的药物组合物。