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    Process for production of optically active PPAR-activating compound and intermediate of the same
    1.
    发明授权
    Process for production of optically active PPAR-activating compound and intermediate of the same 有权
    光学活性PPAR活化化合物及其中间体的制备方法

    公开(公告)号：US07790903B2

    公开(公告)日：2010-09-07

    申请号：US11816472

    申请日：2006-02-23

    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： C07D263/58

    摘要： A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided.A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.

    摘要翻译： 提供了以高产率和高光学收率获得化合物（1）及其中间体的方法。 一种制备化合物（4）的方法，该方法包括在碱的存在下使化合物（2）与化合物（3）反应; 和化合物（1）的制造方法，其特征在于，在碱的存在下使化合物（2）与化合物（3）反应，得到化合物（4），然后使化合物（4）脱酯化。 其中R表示碳原子数1〜6的烷基或碳原子数7〜8的芳烷基。

    PROCESSES FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUNDS AND INTERMEDIATES FOR PRODUCTION THEREOF
    3.
    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。

    Process For Production of Optically Active Ppar-Activating Compound and Intermediate of the Same
    4.
    发明申请
    Process For Production of Optically Active Ppar-Activating Compound and Intermediate of the Same 有权
    光活性活性化合物及其中间体的制备方法

    公开(公告)号：US20080194833A1

    公开(公告)日：2008-08-14

    申请号：US11816472

    申请日：2006-02-23

    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： C07D263/58

    摘要： A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided.A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.

    摘要翻译： 提供了以高产率和高光学收率获得化合物（1）及其中间体的方法。 一种制备化合物（4）的方法，该方法包括在碱的存在下使化合物（2）与化合物（3）反应; 和化合物（1）的制造方法，其特征在于，在碱的存在下使化合物（2）与化合物（3）反应，得到化合物（4），然后使化合物（4）脱酯化。 其中R表示碳原子数1〜6的烷基或碳原子数7〜8的芳烷基。

    Processes for production of optically active PPAR-activating compounds and intermediates for production thereof
    5.
    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。

    Process for producing optically active ester
    6.
    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
    8.
    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。

    PPAR-activating compound and pharmaceutical composition comprising the compound
    10.
    发明授权
    PPAR-activating compound and pharmaceutical composition comprising the compound 有权
    PPAR活化化合物和包含该化合物的药物组合物

    公开(公告)号：US07183295B2

    公开(公告)日：2007-02-27

    申请号：US11407076

    申请日：2006-04-20

    申请人： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    发明人： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    IPC分类号： A61K31/4439 ,  C07D413/12 ,  C07D411/12 ,  C07D401/12

    CPC分类号： C07D413/12 ,  C07D263/58

    摘要： A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosulfonyl group; Z represents CH or N; n is a number of 1 to 6; and m is a number of 2 to 6) or a salt thereof; and therapeutic drugs containing any of such a compound or salt.

    摘要翻译： 由下式（1）表示的化合物：其中R 1和R 2各自可以相同或不同，表示氢原子 ，甲基或乙基; R 3a，R 3b，R 4a和R 4b中的每一个， 它们可以相同或不同，表示氢原子，卤素原子，硝基，羟基，C 1-4烷基，三氟甲基， C 1-4烷氧基，C 1-4烷基羰基氧基，二-C 1-4烷基氨基，C 1 -C 4烷基氨基， C 1-4烷基磺酰氧基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基或C 1〜 4个烷硫基或R 3a和R 3b，或R 4a和R 4b可以是 连接在一起形成亚烷基二氧基; X表示氧原子，硫原子或NR 5（R 5）表示氢原子，C