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    Pyrazole compounds having therapeutic effect on multiple myeloma
    4.
    发明授权
    Pyrazole compounds having therapeutic effect on multiple myeloma 有权
    对多发性骨髓瘤具有治疗作用的吡唑类化合物

    公开(公告)号：US08658686B2

    公开(公告)日：2014-02-25

    申请号：US13991024

    申请日：2011-12-01

    申请人： Taito Nishino ,  Katsuaki Miyaji ,  Shunsuke Iwamoto ,  Takumi Mikashima ,  Koichiro Saruhashi ,  Yo Kishikawa

    发明人： Taito Nishino ,  Katsuaki Miyaji ,  Shunsuke Iwamoto ,  Takumi Mikashima ,  Koichiro Saruhashi ,  Yo Kishikawa

    IPC分类号： A61K31/415 ,  C07D231/10

    CPC分类号： C07D231/20 ,  C07D401/06 ,  C07D403/06

    摘要： Novel therapeutic agents for myeloma are provided.A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.

    摘要翻译： 提供了新型骨髓瘤治疗剂。 一种含有由式（1）表示的吡唑化合物的多发性骨髓瘤治疗剂：其中R1是C1-C6烷基，被R17取代的C1-C6烷基，C1-C6卤代烷基，苯基，被R11等取代的苯基， R 2是氢原子，C 1 -C 6烷基，苯基或任选被e R 21等取代的苯基，R 3是氢原子等，X是单键或 - （CR 6 R 7）n - 各自为R 4和R 5 独立地为C 1 -C 6烷基等，R 6和R 7为氢原子或C 1 -C 6烷基，R 8为苯基，任选被k R 81等取代的苯基，化合物的互变异构体或其药学上可接受的盐或溶剂合物， 作为活性成分。

    PYRAZOLE COMPOUNDS HAVING THERAPEUTIC EFFECT ON MULTIPLE MYELOMA
    5.
    发明申请
    PYRAZOLE COMPOUNDS HAVING THERAPEUTIC EFFECT ON MULTIPLE MYELOMA 有权
    具有多种MYELOMA治疗效果的吡唑化合物

    公开(公告)号：US20130253204A1

    公开(公告)日：2013-09-26

    申请号：US13991024

    申请日：2011-12-01

    申请人： Taito Nishino ,  Katsuaki Miyaji ,  Shunsuke Iwamoto ,  Takumi Mikashima ,  Koichiro Saruhashi ,  Yo Kishikawa

    发明人： Taito Nishino ,  Katsuaki Miyaji ,  Shunsuke Iwamoto ,  Takumi Mikashima ,  Koichiro Saruhashi ,  Yo Kishikawa

    IPC分类号： C07D231/20

    CPC分类号： C07D231/20 ,  C07D401/06 ,  C07D403/06

    摘要： Novel therapeutic agents for myeloma are provided.A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6, R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.

    摘要翻译： 提供了新型骨髓瘤治疗剂。 一种含有由式（1）表示的吡唑化合物的多发性骨髓瘤治疗剂：其中R1是C1-C6烷基，被R17取代的C1-C6烷基，C1-C6卤代烷基，苯基，被R11等取代的苯基， R 2是氢原子，C 1 -C 6烷基，苯基或任选被e R 21等取代的苯基，R 3是氢原子等，X是单键或 - （CR 6，R 7）n - ，每个R 4 并且R 5独立地为C 1 -C 6烷基等，R 6和R 7为氢原子或C 1 -C 6烷基，R 8为苯基，任选被k R 81等取代的苯基，化合物的互变异构体或其药学上可接受的盐或溶剂合物 作为活性成分。

    Thrombopoetin receptor activator and process for producing the same
    9.
    发明授权
    Thrombopoetin receptor activator and process for producing the same 失效
    血小板生成素受体激活剂及其制备方法

    公开(公告)号：US07851503B2

    公开(公告)日：2010-12-14

    申请号：US10524666

    申请日：2003-08-14

    申请人： Katsuaki Miyaji ,  Norihisa Ishiwata ,  Takanori Nakamura ,  Taito Nishino ,  Hisao Kamiya ,  Masao Yamamoto

    发明人： Katsuaki Miyaji ,  Norihisa Ishiwata ,  Takanori Nakamura ,  Taito Nishino ,  Hisao Kamiya ,  Masao Yamamoto

    IPC分类号： A61K31/275

    CPC分类号： A61K31/4409 ,  A61K31/277 ,  A61K31/4402 ,  A61K31/4453 ,  C07C255/37

    摘要： A preventive, therapeutic or improving agent for diseases against which activation of the thrombopoietin receptor is effective or a platelet increasing agent, which contains a thrombopoietin receptor activator represented by the formula (1): [wherein each of R1 and R3 is independently a hydrogen atom, SO3H, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-18 arylcarbonyl group (the C1-6 alkyl group, the C1-6 alkylcarbonyl group and the C6-18 arylcarbonyl group may be optionally substituted with a halogen atom, a hydroxyl group, a C2-6 alkenyl group, a C1-6 alkoxy group, a C1-6 alkoxycarbonyl group, a C6-18 aryl group, a 2-pyridyl group, a 3-pyridyl group, a 4-pyridyl group, a 2-furanyl group, a 3-furanyl group, a 2-thienyl group, a 3-thienyl group or NR9R10) , and each of R2, R4 and Ra is independently a hydrogen atom, a hydroxyl group or a C1-6 alkoxy group].

    摘要翻译： 含有血小板生成素受体活化剂的式（1）表示的血小板生成素受体活化有效的疾病或血小板增多剂的预防，治疗或改善剂：其中R 1和R 3各自独立地为氢原子 ，SO 3 H，C 1-6烷基，C 1-6烷基羰基或C 6-18芳基羰基（C 1-6烷基，C 1-6烷基羰基和C 6-18芳基羰基可以任选地被 卤素原子，羟基，C 2-6烯基，C 1-6烷氧基，C 1-6烷氧基羰基，C 6-18芳基，2-吡啶基，3-吡啶基， 吡啶基，2-呋喃基，3-呋喃基，2-噻吩基，3-噻吩基或NR9R10），R2，R4和Ra各自独立地为氢原子，羟基或C1 -6烷氧基]。

    Method for expanding hematopoietic stem cells using heterocyclic compound
    10.
    发明授权
    Method for expanding hematopoietic stem cells using heterocyclic compound 有权
    使用杂环化合物扩增造血干细胞的方法

    公开(公告)号：US09115341B2

    公开(公告)日：2015-08-25

    申请号：US12746507

    申请日：2008-12-05

    申请人： Takanori Nakamura ,  Atsushi Miyamura ,  Taito Nishino ,  Norihisa Ishiwata ,  Katsuaki Miyaji

    发明人： Takanori Nakamura ,  Atsushi Miyamura ,  Taito Nishino ,  Norihisa Ishiwata ,  Katsuaki Miyaji

    IPC分类号： C12N5/00 ,  C12N5/0789 ,  C07D333/02 ,  C07D207/00 ,  A61K35/12

    CPC分类号： C12N5/0647 ,  A61K35/12 ,  C12N2501/125 ,  C12N2501/145 ,  C12N2501/999

    摘要： An object of the present invention is to expand CD34+ cells ex vivo efficiently in a short term using a biologically safe and inexpensively obtainable low molecular weight compound. A still another object of the present invention is to provide an expansion agent for CD34+ cells useful for treatment of various hematopoietic disorders caused by dysfunctional hematopoietic stem cells and/or hematopoietic progenitor cells.A method for expanding CD34+ cells, which comprises culturing CD34+ cells ex vivo in the presence of a compound represented by the formula (I) (wherein A, B, L1, L2, L3, L4, R1, R2, R3, X and Y are defined in the description), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.

    摘要翻译： 本发明的目的是使用生物安全且廉价的低分子量化合物在短期内有效地扩增CD34 +细胞。 本发明的另一个目的是提供用于治疗由功能异常的造血干细胞和/或造血祖细胞引起的各种造血障碍的CD34 +细胞的扩张剂。 一种用于扩增CD34 +细胞的方法，其包括在式（I）表示的化合物（其中A，B，L1，L2，L3，L4，R1，R2，R3，X和Y）存在下离体培养CD34 +细胞 在描述中定义），化合物的互变异构体或药学上可接受的盐或其溶剂合物。