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    Carbinol derivatives having heterocyclic linker
    8.
    发明授权
    Carbinol derivatives having heterocyclic linker 有权
    具有杂环连接体的甲醇衍生物

    公开(公告)号：US08551985B2

    公开(公告)日：2013-10-08

    申请号：US12769104

    申请日：2010-04-28

    申请人： Minoru Koura ,  Hisashi Sumida ,  Takayuki Matsuda ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya ,  Sumiko Kurobuchi

    发明人： Minoru Koura ,  Hisashi Sumida ,  Sayaka Kurobuchi ,  Takayuki Matsuda ,  Yuichiro Watanabe ,  Takashi Enomoto ,  Kimiyuki Shibuya

    IPC分类号： A61K31/496 ,  A61K31/551 ,  C07D233/72 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D491/048 ,  C07D491/056

    CPC分类号： C07D233/78 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D491/04

    摘要： [Object]It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease.[Solving Means]A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)

    摘要翻译： 本发明提供可用作动脉粥样硬化的预防和/或治疗剂的新型LXRbeta激动剂; 动脉硬化，如糖尿病引起的; 血脂异常 高胆固醇血症 脂质相关疾病; 由炎性细胞因子引起的炎性疾病; 皮肤病如过敏性皮肤病; 糖尿病; 或阿尔茨海默病。 [解决方案]由以下通式（I）表示的甲醇化合物或其盐或其溶剂化物：（其中，V和W各自独立地表示N或C-R7; X和Y各自独立地表示CH 2，C = O ，SO2等; Z表示CH或N;每个R1，R2和R7独立地表示氢原子，C1-8烷基等; R3表示C1-8烷基; R4表示任选取代的C6-10芳基 或任选取代的5至11元杂环基; R 5和R 6表示氢原子等; L表示任选被氧代基等取代的C 1-8烷基链; n表示0〜 2.）

    Processes for production of optically active PPAR-activating compounds and intermediates for production thereof
    10.
    发明授权
    Processes for production of optically active PPAR-activating compounds and intermediates for production thereof 失效
    用于制备光学活性PPAR活化化合物的方法及其生产用中间体

    公开(公告)号：US07714141B2

    公开(公告)日：2010-05-11

    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 ,  C07D277/82 ,  C07D235/30

    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 therefore 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： 本发明提供了一种以高产率和高纯度生产光学活性丁酸化合物和生产中间体的方法。 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。