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1.发明公开METHOD FOR AMPLIFICATION OF HEMATOPOIETIC STEM CELL USING HETEROCYCLIC COMPOUND 审中-公开用于扩增造血干细胞方法的杂环化合物的方法
公开(公告)号：EP2233561A1
公开(公告)日：2010-09-29
申请号：EP08856980.1
申请日：2008-12-05
发明人： NAKAMURA, Takanori , MIYAMURA, Atsushi , NISHINO, Taito , ISHIWATA, Norihisa , MIYAJI, Katsuaki
IPC分类号： C12M3/00 , A61K35/14 , A61P7/00 , A61P7/06 , A61P9/10 , A61P19/08 , A61P35/00 , A61P35/02 , A61P37/02 , C12N5/06
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, L 1 , L 2 , L 3 , L 4 , R 1 , R 2 , R 3 , X and Y are defined in the description), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.-
公开(公告)号：EP2955181A1
公开(公告)日：2015-12-16
申请号：EP14748793.8
申请日：2014-02-05
发明人： TAKAHASHI, Keiji , WATANABE, Tsuneo , HAYASHI, Keishi , KURIHARA, Kazunori , NAKAMURA, Takanori , YAMAMOTO, Akio , NISHIMURA, Takuya , KAMIYAMA, Toshihiko , HIDAKA, Yuuki
IPC分类号： C07D471/14 , A61K31/519 , A61P29/00 , A61P43/00
摘要： To provide a novel tricyclic pyrrolopyridine compound having a JAK inhibitory activity and useful for prevention, treatment and/or improvement of particularly autoimmune diseases, inflammatory diseases and allergic diseases.
A novel tricyclic pyrrolopyridine compound represented by the formula (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof:
wherein the respective substituents are defined in detail in the specification, and R 1 is a C 1-6 alkyl group or the like, R 2 is a hydrogen atom or the like, R 3 is a hydrogen atom or the like, the ring A is C 3-11 cycloalkane or the like, L 1 is a C 1-6 alkylene group or the like, and R 4 is NR a R b or the like.摘要翻译： 提供具有JAK抑制活性的新型三环吡咯并吡啶化合物，可用于预防，治疗和/或改善特别是自身免疫性疾病，炎性疾病和过敏性疾病。 由式（I）表示的新型三环吡咯并吡啶化合物，该化合物的互变异构体或药学上可接受的盐或其溶剂化物：其中各个取代基在说明书中详细定义，并且R 1是C 1-6烷基或 R 2为氢原子等，R 3为氢原子等，环A为C 3-11环烷烃等，L 1为C 1-6亚烷基等，R 4为NR a R b或 喜欢。
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公开(公告)号：EP3144309A1
公开(公告)日：2017-03-22
申请号：EP15791895.4
申请日：2015-05-11
发明人： WATANABE, Tsuneo , TAKAHASHI, Keiji , HAYASHI, Keishi , NAKAMURA, Takanori , MINAMI, Masataka , KURIHARA, Kazunori , YAMAMOTO, Akio , NISHIMURA, Takuya , UNI, Miyuki , KAMIYAMA, Toshihiko , IWAMOTO, Shunsuke
IPC分类号： C07D471/14 , A61K31/4375 , A61K31/519 , A61P29/00 , A61P43/00
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/519 , Y02P20/55
摘要： Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided.
Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein : each of A 1 , A 2 and A 3 is a cyclohexane-1,4-diyl group or the like; each of L 1 , L 2 and L 3 is a methylene group or the like; each of X 1 and X 3 is O or NH; each of R 1 and R 3 is a cyano C 1-6 haloalkyl group or the like; and R 2 is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.摘要翻译： 具有JAK抑制活性的新型三环化合物可用于预防，治疗或改善自身免疫疾病，炎性疾病和过敏性疾病。 由式（I），式（II）或式（III）表示的新型三环化合物（其中：A 1，A 2和A 3各自为环己烷-1,4-二基等; 的L 1，L 2和L 3是亚甲基等; X 1和X 3各自为O或NH; R 1和R 3各自为氰基C 1-6卤代烷基等;以及 R 2是芳族杂环基），化合物的互变异构体或药学上可接受的盐或其溶剂合物。
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4.发明授权FUSED HETEROCYCLIC COMPOUND AND THROMBOPOIETIN RECEPTOR ACTIVATOR 有权稠合杂环化合物及THROMBOPOETINREZEPTORAKTIVATOR
公开(公告)号：EP2492262B1
公开(公告)日：2016-04-20
申请号：EP10825062.2
申请日：2010-10-22
IPC分类号： C07D231/18 , A61K31/381 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/454 , A61P7/06 , A61P7/08 , A61P9/10 , A61P43/00 , C07D333/32 , C07D401/12 , C07D409/04 , C07D409/12 , C07D409/14
CPC分类号： C07D409/14 , C07D231/18 , C07D333/32 , C07D333/38 , C07D333/40 , C07D401/12 , C07D409/04 , C07D409/12
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5.发明公开METHOD FOR PRODUCING MEGAKARYOCYTES AND/OR PLATELETS FROM PLURIPOTENT STEM CELLS 审中-公开用于生产巨核细胞和/或血小板从多能干细胞
公开(公告)号：EP2765187A1
公开(公告)日：2014-08-13
申请号：EP12838198.5
申请日：2012-10-03
发明人： NISHINO, Taito , NAKAMURA, Takanori , IWAMOTO, Shunsuke , ETO, Koji , NAKAUCHI, Hiromitsu , TSUJI, Kayoko
IPC分类号： C12N5/0789 , A61K35/14 , A61P7/04 , C12N5/0735 , C12N5/078 , C12N5/10 , C07D333/38
CPC分类号： C12N5/0644 , A61K35/15 , A61K35/19 , A61K35/28 , C07D333/38 , C07D333/40 , C07D409/14 , C12N2501/145 , C12N2501/165 , C12N2501/734 , C12N2501/999 , C12N2502/13 , C12N2506/02 , C12N2506/45
摘要： An agent for inducing production of megakaryocytes and/or platelets from pluripotent stem cells which is useful for treatment of disease accompanied by a decrease in platelets is provided.
A method for producing megakaryocytes and/or platelets, comprising separating hematopoietic progenitor cells from the septal cells in sac-like structures produced by pluripotent stem cells, and culturing the hematopoietic progenitor cells ex vivo in the presence of a compound represented by the formula (I) (wherein R 1 to R 7 , W, X, Y, Z, Ar 1 and n are as defined in the description) to differentiate them into megakaryocytes and/or platelets.摘要翻译： 提供了一种用于诱导巨核细胞的生产和/或血小板的从多能干细胞的所有的试剂，其用于治疗疾病伴有的血小板减少的是有益的。 用于生产巨核细胞和/或血小板，其包含由多能干细胞产生网状结构分离室间隔细胞造血祖细胞，并培养所述造血祖细胞的离体中的化合物由下式表示的存在（A法予 ）（式中，R 1至R 7，W，X，Y，Z，Ar 1和n如说明书中所定义），以使它们分化成为巨核细胞和/或血小板。
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6.发明公开NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND THROMBOPOIETIN RECEPTOR ACTIVATOR 审中-公开血栓形成细胞激活剂的胶原蛋白
公开(公告)号：EP2025671A1
公开(公告)日：2009-02-18
申请号：EP07744900.7
申请日：2007-06-07
发明人： MIYAJI, Katsuaki , IWAMOTO, Shunsuke , SHIGETA, Yukihiro , HIROKAWA, Yutaka , OOWADA, Shingo , NAKAMURA, Takanori , ISHIWATA, Norihisa
IPC分类号： C07D231/22 , A61K31/454 , A61K31/496 , A61P7/00 , A61P7/04 , A61P9/00 , A61P9/10 , A61P43/00 , C07D401/12
CPC分类号： C07D231/22 , C07D401/12 , C07D403/12
摘要： Compounds effective for preventing, treatment or improving diseases against which activation of the thrombopoietin receptor is effective are provided.
A compound represented by the formula (I) (wherein R 1 , R 2 , R 3 , L 1 , L 2 , L 3 , X and Y are defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.摘要翻译： 提供了有效预防，治疗或改善血小板生成素受体活化有效的疾病的化合物。 由式（I）表示的化合物（其中R 1，R 2，R 3，L 1，L 2，L 3，X和Y在说明书中定义），化合物的互变异构体，前药或药学上可接受的盐 或其溶剂合物。
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公开(公告)号：EP2228434A1
公开(公告)日：2010-09-15
申请号：EP08857879.4
申请日：2008-12-05
发明人： NAKAMURA, Takanori , MIYAMURA, Atsushi , NISHINO, Taito , ISHIWATA, Norihisa , MIYAJI, Katsuaki
IPC分类号： C12M3/00 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K35/14 , A61P3/00 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/10 , A61P35/00 , A61P37/04 , A61P37/06 , C12N5/06
CPC分类号： C12N5/0647 , A61K2035/124 , C07D231/12 , C07D333/22 , C07D409/12 , C07D409/14 , C07D417/14 , 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, L 1 , L 2 , L 3 , L 4 , R 1 , R 2 , R 3 , 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。 一种扩增CD34 +细胞的方法，其包括在式（I）表示的化合物的存在下离体培养CD34 +细胞（其中A，B，L 1，L 2，L 3，L 4，R 1， R 2，R 3，X和Y在说明书中定义），化合物的互变异构体或药学上可接受的盐或其溶剂合物。
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公开(公告)号：EP1549618A1
公开(公告)日：2005-07-06
申请号：EP03751429.6
申请日：2003-10-09
IPC分类号： C07D231/22 , C07D401/04 , C07D403/12 , C07D403/04 , C07D409/12 , A61K31/4152 , A61P35/00 , A61P1/16
CPC分类号： C07D231/26
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 A is a C?2-14#191 aryl group, B is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, D is a hydrogen atom, a C?1-6#191 alkyl group, a C?1-3#191 alkyl group substituted with one or more fluorine atoms or a C?2-14#191 aryl group, and E is a C?2-14#191 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the activator or a solvate thereof, as an active ingredient.
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公开(公告)号：EP2765187B1
公开(公告)日：2018-08-08
申请号：EP12838198.5
申请日：2012-10-03
发明人： NISHINO, Taito , NAKAMURA, Takanori , IWAMOTO, Shunsuke , ETO, Koji , NAKAUCHI, Hiromitsu , TSUJI, Kayoko
IPC分类号： C12N5/0789 , A61K35/14 , A61P7/04 , C12N5/0735 , C12N5/078 , C12N5/10 , C07D333/38 , A61K35/15 , A61K35/19 , A61K35/28 , C07D333/40 , C07D409/14
CPC分类号： C12N5/0644 , A61K35/15 , A61K35/19 , A61K35/28 , C07D333/38 , C07D333/40 , C07D409/14 , C12N2501/145 , C12N2501/165 , C12N2501/734 , C12N2501/999 , C12N2502/13 , C12N2506/02 , C12N2506/45
摘要： An agent for inducing production of megakaryocytes and/or platelets from pluripotent stem cells which is useful for treatment of disease accompanied by a decrease in platelets is provided. A method for producing megakaryocytes and/or platelets, comprising separating hematopoietic progenitor cells from the septal cells in sac-like structures produced by pluripotent stem cells, and culturing the hematopoietic progenitor cells ex vivo in the presence of a compound represented by the formula (I) (wherein R 1 to R 7 , W, X, Y, Z, Ar 1 and n are as defined in the description) to differentiate them into megakaryocytes and/or platelets.
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公开(公告)号：EP2492262A1
公开(公告)日：2012-08-29
申请号：EP10825062.2
申请日：2010-10-22
IPC分类号： C07D231/18 , A61K31/381 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/454 , A61P7/06 , A61P7/08 , A61P9/10 , A61P43/00 , C07D333/32 , C07D401/12 , C07D409/04 , C07D409/12 , C07D409/14
CPC分类号： C07D409/14 , C07D231/18 , C07D333/32 , C07D333/38 , C07D333/40 , C07D401/12 , C07D409/04 , C07D409/12
摘要： Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided.
A compound represented by the formula (I) (wherein R 1 is an aryl group fused to a saturated ring or the like, A, B, L 1 , R 2 , L 2 , L 3 , Y, L 4 , R 3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.摘要翻译： 提供了可用于预防，治疗或改善血小板生成素受体活化有效的疾病的融合杂环化合物。 由式（I）表示的化合物（其中R 1是与饱和环等稠合的芳基，A，B，L 1，R 2，L 2，L 3，Y，L 4，R 3和 X在说明书中定义），化合物的互变异构体，前药或药学上可接受的盐或其溶剂合物。
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