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    Amide compounds and medications containing the same technical field
    31.
    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：US06849647B1

    公开(公告)日：2005-02-01

    申请号：US09666152

    申请日：2000-09-20

    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 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04 ,  C07D513/04

    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 integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at one of these compounds.

    摘要翻译： 本发明涉及一种具有ACAT抑制活性的新型化合物。本发明涉及式（I）表示的化合物，其中表示任选取代的二价残基如苯，吡啶，环己烷或萘，或基团，Het表示 含有至少一个选自氮原子，氧原子和硫原子的杂原子的5-至8-元，取代或未取代的杂环基，例如单环基团，多环基团或稠合基团 环，X表示-NH-，氧原子或硫原子，Y表示-NR4-，氧原子，硫原子，亚砜或砜，Z表示单键或-NR5-，R4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，芳基或任选取代的甲硅烷基低级烷基，n为1至15的整数 ，要么 盐或溶剂合物，以及含有这些化合物之一的药物组合物。

    Process for preparation of 3,5-bisalkylphenols
    32.
    发明授权
    Process for preparation of 3,5-bisalkylphenols 失效
    3,5-二烷基苯酚的制备方法

    公开(公告)号：US06806395B2

    公开(公告)日：2004-10-19

    申请号：US10380169

    申请日：2003-03-18

    申请人： Kimiyuki Shibuya ,  Tadaaki Ohgiya ,  Toru Miura ,  Kazuhiro Onogi

    发明人： Kimiyuki Shibuya ,  Tadaaki Ohgiya ,  Toru Miura ,  Kazuhiro Onogi

    IPC分类号： C07C3906

    CPC分类号： C07C41/30 ,  C07C37/002 ,  C07C37/11 ,  C07C37/50 ,  C07C39/11 ,  C07C43/23 ,  Y02P20/55 ,  C07C39/06

    摘要： A process for producing a 3,5-bisalkylphenol (2) according to the following reaction scheme: (wherein R1 represents a hydrogen atom, an alkali metal atom, an alkaline earth metal atom, or a hydroxyl-protecting group (other than methyl group); R2 represents a C1 to C5 lower alkyl group or an optionally substituted phenyl group; and each of R3 and R4, which may be identical to or different from each other, represents a lower alkyl group, an aralkyl group, or an aryl group); a carbinol compound (1); and a process for producing the carbinol compound. The production process of the present invention enables efficient and safe production of a variety of 3,5-bisalkylphenols including 3,5-diisopropylphenol, which are important as synthesis intermediates for drugs and agricultural chemicals, in shorter steps at high purity in high yield, thus contributing to consistent supply of drugs and agricultural chemicals.

    摘要翻译： 根据以下反应方案制备3,5-双烷基苯酚（2）的方法：其中R 1表示氢原子，碱金属原子，碱土金属原子或羟基保护基（其他 比甲基）; R 2表示C1〜C5低级烷基或任选取代的苯基; R 3和R 4可以彼此相同或不同，表示 低级烷基，芳烷基或芳基）。 甲醇化合物（1）; 和甲醇化合物的制造方法。 本发明的制造方法能够高效安全地生产各种3,5-二异丙基苯酚，其中3,5-二异丙基苯酚作为药物和农用化学品的合成中间体是重要的，在高纯度，高收率的较短步骤中， 从而有助于持续供应毒品和农药。

    Anilide compounds, including use thereof in ACAT inhibitition
    33.
    发明授权
    Anilide compounds, including use thereof in ACAT inhibitition 失效
    酰苯胺化合物，包括其在ACAT抑制中的用途

    公开(公告)号：US06204278B1

    公开(公告)日：2001-03-20

    申请号：US08858244

    申请日：1997-05-19

    申请人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    发明人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    IPC分类号： A61K31423

    CPC分类号： C07D263/58 ,  C07D235/28 ,  C07D277/70

    摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

    摘要翻译： 本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基 ，或低级烷氧基; 并且R 4和R 5可以一起形成其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代的低级亚烷基; X是-NH-或氧或硫原子; Y是-NH-，氧 或硫原子，或亚砜或砜基; Z为单键或-NH6-; R6表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

    METHOD FOR PREPARING OPTICALLY ACTIVE 1-BROMO-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHANE
    34.
    发明申请
    METHOD FOR PREPARING OPTICALLY ACTIVE 1-BROMO-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHANE 有权
    制备光学活性1-溴-1- [3,5-BIS（三氟甲基）苯基]乙烯的方法

    公开(公告)号：US20130190540A1

    公开(公告)日：2013-07-25

    申请号：US13811651

    申请日：2011-07-21

    申请人： Taichi Kusakabe ,  Kennosuke Matsuda ,  Koichi Yamazaki ,  Tadaaki Ohgiya ,  Kimiyuki Shibuya

    发明人： Taichi Kusakabe ,  Kennosuke Matsuda ,  Koichi Yamazaki ,  Tadaaki Ohgiya ,  Kimiyuki Shibuya

    IPC分类号： C07C17/04

    CPC分类号： C07C17/04 ,  C07B53/00 ,  C07B2200/07 ,  C07C17/16 ,  C07C22/08

    摘要： A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R1)(R2)(R3) (in the formula, R1, R2, and R3 independently represent a C6-10 aryl group, a C6-10 aryloxy group, a C1-10 alkyl group, a C1-10 alkoxyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.

    摘要翻译： 一种具有高光学纯度的光学活性1-溴-1- [3,5-双（三氟甲基） - 苯基]乙烷的制备方法，其包括将光学活性的1- [3,5-双（三氟甲基） 苯基]乙醇通过使用溴化剂，（a）卤化磷和溴化氢的组合，（b）1,2-二溴-1,1,2,2-四氯乙烷与有机磷化合物的组合 由通式（I）表示：P（R1）（R2）（R3）（在式中，R1，R2和R3独立地表示C6-10芳基，C6-10芳氧基，C1-10 烷基，C1-10烷氧基，C3-6环烷基或C3-6环烷氧基），或（c）N-溴代琥珀酰亚胺与二烷基硫醚的组合。

    Method of stabilizing lipid-rich plaque and method of preventing rupture thereof
    37.
    发明授权
    Method of stabilizing lipid-rich plaque and method of preventing rupture thereof 失效
    稳定富含脂质的斑块的方法和防止其破裂的方法

    公开(公告)号：US07884106B2

    公开(公告)日：2011-02-08

    申请号：US10569642

    申请日：2004-08-19

    申请人： Kimiyuki Shibuya ,  Hideyuki Kobayashi ,  Yasunobu Yoshinaka

    发明人： Kimiyuki Shibuya ,  Hideyuki Kobayashi ,  Yasunobu Yoshinaka

    IPC分类号： A61K31/497

    CPC分类号： A61K31/496 ,  A61K31/4439 ,  C07D401/12

    摘要： A method of stabilizing lipid-rich plaques and method of preventing the rupture thereof, characterized in that an effective amount of 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, its acid adduct salt or a hydrate thereof is administered to patients with lipid-rich plaques. Prevention of plaque rupture and stabilization of plaques can be attained by reducing the occupancy of macrophages in lipid-rich plaques being unstable and tending to rupture among plaques being a lesion from a seat of atherosclerosis and simultaneously increasing the occupancy of collagen therein.

    摘要翻译： 一种稳定富含脂质斑块的方法和防止其破裂的方法，其特征在于有效量的2- [4- [2-（苯并咪唑-2-基硫基）乙基]哌嗪-1-基] -N- [ 将2,4-二（甲硫基）-6-甲基-3-吡啶基]乙酰胺，其酸加成盐或其水合物给予富含脂质斑块的患者。 防止斑块破裂和斑块稳定可以通过减少富含脂质的斑块中的巨噬细胞的占有而变得不稳定并且趋于在来自动脉粥样硬化部位的病变的斑块之间破裂并同时增加其中的胶原占有量来实现。

    METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE
    38.
    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：US20090275595A1

    公开(公告)日：2009-11-05

    申请号：US11721402

    申请日：2005-12-09

    申请人： Hideyuki Kobayashi ,  Yasunobu Yoshinaka ,  Kimiyuki Shibuya

    发明人： Hideyuki Kobayashi ,  Yasunobu Yoshinaka ,  Kimiyuki Shibuya

    IPC分类号： A61K31/497

    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-pyridyl]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。 还提供减少富含脂质的斑块，稳定富含脂质的斑块和/或防止动脉粥样硬化病变中富含脂质斑块的破裂的方法，其包括同时施用或分开施用一段时间间隔的有效 化合物1的量，其药学上可接受的盐或其水合物和有效量的匹伐他汀给有需要的患者。

    PROCESSES FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUNDS AND INTERMEDIATES FOR PRODUCTION THEREOF
    40.
    发明申请
    PROCESSES FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUNDS AND INTERMEDIATES FOR PRODUCTION THEREOF 失效
    生产光活性PPAR活化化合物的方法及其生产中间体

    公开(公告)号：US20090076280A1

    公开(公告)日：2009-03-19

    申请号：US11912811

    申请日：2006-05-30

    申请人： Yukiyoshi Yamazaki ,  Takaaki Araki ,  Minoru Koura ,  Kimiyuki Shibuya

    发明人： Yukiyoshi Yamazaki ,  Takaaki Araki ,  Minoru Koura ,  Kimiyuki Shibuya

    IPC分类号： C07D263/58

    CPC分类号： C07D413/12 ,  C07D263/58

    摘要： The invention provides a process for producing an optically active butyric acid compound and a production intermediate therefor at high yield and high purity.The present invention provides a process for producing Compound (6), including reacting Compound (1) with optically active 2-trifluoromethanesulfonyloxybutyrolactone (2a) in the presence of a base or reacting optically active 2-hydroxybutyrolactone (2b) under Mitsunobu reaction conditions, to thereby form Compound (3); reacting Compound (3) with an alcohol and a halogenating agent, to thereby form Compound (4); dehalogenating Compound (4), to thereby form Compound (5); and de-esterifying Compound (5).

    摘要翻译： 本发明提供一种以高产率和高纯度生产光学活性丁酸化合物及其制备中间体的方法。 本发明提供化合物（6）的制造方法，其包括使光学活性2-三氟甲磺酰氧基丁内酯（2a）在光学活性2-羟基丁内酯（2b）的存在下，在Mitsunobu反应条件下，使化合物（1）与光活性2-三氟甲磺酰氧基丁内酯 从而形成化合物（3）; 使化合物（3）与醇和卤化剂反应，从而形成化合物（4）; 脱卤化合物（4），从而形成化合物（5）; 并使化合物（5）脱酯化。