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    Crystalline forms of thiazolidinedione compound and its manufacturing method
    4.
    发明申请
    Crystalline forms of thiazolidinedione compound and its manufacturing method 失效
    噻唑烷二酮化合物的结晶形式及其制备方法

    公开(公告)号：US20110046388A1

    公开(公告)日：2011-02-24

    申请号：US12311610

    申请日：2008-02-08

    申请人： Hisaki Kajino ,  Yutaka Ikeuchi ,  Hiroshi Miyamoto ,  Eiji Numagami ,  Satoru Nihei

    发明人： Hisaki Kajino ,  Yutaka Ikeuchi ,  Hiroshi Miyamoto ,  Eiji Numagami ,  Satoru Nihei

    IPC分类号： C07D417/12

    CPC分类号： C07D417/12

    摘要： It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I). [Formula 1]

    摘要翻译： 本发明的目的是提供作为制备过氧化物酶体增殖物激活受体（PPAR）活化剂和抗癌药物组合物的药物成分的噻唑烷二酮化合物的结晶形式。 本发明涉及5-（4 - {[6-（4-氨基-3,5-二甲基苯氧基）-1-甲基-1H苯并咪唑-2-基]甲氧基}苄基） -1,3-噻唑烷-2,4-二酮盐酸盐，由下式（I）表示。 [公式1]

    METHOD FOR MANUFACTURING A 6-SUBSTITUTED 1-METHYL-1H-BENZIMIDAZOLE DERIVATIVE AND AN INTERMEDIATE OF SAID METHOD
    5.
    发明申请
    METHOD FOR MANUFACTURING A 6-SUBSTITUTED 1-METHYL-1H-BENZIMIDAZOLE DERIVATIVE AND AN INTERMEDIATE OF SAID METHOD 审中-公开
    制备6-取代的1-甲基-1H-苯并咪唑衍生物的方法和所述方法的中间体

    公开(公告)号：US20120238759A1

    公开(公告)日：2012-09-20

    申请号：US13511190

    申请日：2010-11-25

    申请人： Yutaka Ikeuchi ,  Chiharu Satoh ,  Eiji Numagami ,  Satoru Nihei ,  Hisaki Kajino

    发明人： Yutaka Ikeuchi ,  Chiharu Satoh ,  Eiji Numagami ,  Satoru Nihei ,  Hisaki Kajino

    IPC分类号： C07D417/12 ,  C07C217/90 ,  C07C213/02 ,  C07D277/34

    CPC分类号： C07C213/02 ,  A61K31/427 ,  C07C217/90 ,  C07D277/34 ,  C07D417/12 ,  Y02P20/55

    摘要： A method for manufacturing a 6-substituted 1-methyl-1H-benzimidazole derivative represented by the formula (IV) wherein R3 represents a hydrogen atom or a C1-C4 alkyl group. A 4-substituted N2-methylbenzene-1,2-diamine derivative is prepared from a particular 5-substituted N-methyl-2-nitroaniline derivative, subsequently reacting the resulting compound with {4-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]phenoxy}acetic acid or an acid chloride or a mixed acid anhydride thereof, and subsequently subjecting the resulting compound to intramolecular dehydration condensation. A compound of the formula (II) wherein R1 represents a hydrogen atom, a C1-C4 alkyl group, or a protective group for the nitrogen atom, and R2 represents a hydrogen atom or a protective group for the nitrogen atom is prepared and used as an intermediate.

    摘要翻译： 制备由式（IV）表示的6-取代的1-甲基-1H-苯并咪唑衍生物的方法，其中R 3表示氢原子或C 1 -C 4烷基。 4-取代的N-甲基苯-1,2-二胺衍生物由特定的5-取代的N-甲基-2-硝基苯胺衍生物制备，随后将得到的化合物与{4 - [（2,4-二氧代-1,2-二氢 - 3-噻唑烷-5-基）甲基]苯氧基}乙酸或其酰氯或其混合酸酐，然后将所得化合物进行分子内脱水缩合。 制备式（II）化合物，其中R1表示氢原子，C1-C4烷基或氮原子的保护基，R2表示氢原子或氮原子的保护基，并用作 一个中间人

    Crystalline forms of thiazolidinedione compound and its manufacturing method
    7.
    发明授权
    Crystalline forms of thiazolidinedione compound and its manufacturing method 失效
    噻唑烷二酮化合物的结晶形式及其制备方法

    公开(公告)号：US08236834B2

    公开(公告)日：2012-08-07

    申请号：US12311610

    申请日：2008-02-08

    申请人： Hisaki Kajino ,  Yutaka Ikeuchi ,  Eiji Numagami

    发明人： Hisaki Kajino ,  Yutaka Ikeuchi ,  Eiji Numagami

    IPC分类号： A61K31/427 ,  C07D277/34

    CPC分类号： C07D417/12

    摘要： It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I). [Formula 1]

    摘要翻译： 本发明的目的是提供作为制备过氧化物酶体增殖物激活受体（PPAR）活化剂和抗癌药物组合物的药物成分的噻唑烷二酮化合物的结晶形式。 本发明涉及5-（4 - {[6-（4-氨基-3,5-二甲基苯氧基）-1-甲基-1H-苯并咪唑-2-基]甲氧基}苄基 ）-1,3-噻唑烷-2,4-二酮盐酸盐，由下式（I）表示。 [公式1]

    Preparation of intermediates useful in the synthesis of 2′-cyano-2′-deoxy-N4-palmi-toyl-1-β-D-arabinofuranosylcytosine
    8.
    发明授权
    Preparation of intermediates useful in the synthesis of 2′-cyano-2′-deoxy-N4-palmi-toyl-1-β-D-arabinofuranosylcytosine 有权
    制备可用于合成2'-氰基-2'-脱氧-N4-棕榈酰-1-基 - D-阿拉伯呋喃糖基胞嘧啶的中间体

    公开(公告)号：US08884001B2

    公开(公告)日：2014-11-11

    申请号：US12991582

    申请日：2009-05-08

    申请人： Gavin Wood ,  Robert Westwood ,  Tsuyoshi Murofushi ,  Eiji Numagami ,  Takashi Takita

    发明人： Gavin Wood ,  Robert Westwood ,  Tsuyoshi Murofushi ,  Eiji Numagami ,  Takashi Takita

    IPC分类号： C07H19/06 ,  C07F7/08

    CPC分类号： C07F7/0838

    摘要： The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2′ into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2′-cyano-2′-deoxy-N4-palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.

    摘要翻译： 本发明涉及一种制备式682-4化合物的方法，所述方法包括以下步骤：（i）将式682-1化合物转化为式682-2化合物; （ii）将所述式682-2'化合物转化为式682-3化合物; 和（iii）将所述式682-3化合物转化为式682-4化合物。 本发明的其它方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-基 - D-阿糖呋喃糖基胞嘧啶的用途，嘧啶核苷在治疗中是有用的 和/或预防癌症。