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    4' -C-substituted-2-haloadenosine derivative
    2.
    发明申请
    4' -C-substituted-2-haloadenosine derivative 有权
    4'-取代-2-卤代腺苷衍生物

    公开(公告)号：US20080153774A1

    公开(公告)日：2008-06-26

    申请号：US11984527

    申请日：2007-11-19

    申请人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    发明人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    IPC分类号： A61K31/7076 ,  C07H19/16 ,  A61P37/00

    CPC分类号： C07H19/16

    摘要： The present invention provides a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor.

    摘要翻译： 本发明提供由下式[I]，[II]或[III]表示的4'-C-取代-2-卤代腺嘌呤衍生物：其中X表示卤素原子，R 1 >表示乙炔基或氰基，R 2表示氢，磷酸酯残基或磷酸酯衍生物残基）。 本发明还提供含有该衍生物和药学上可接受的载体的药物组合物。

    MEDICINAL AGENT FOR DISEASE ASSOCIATED WITH EPSTEIN-BARR VIRUS, AND METHOD FOR SCREENING OF THE MEDICINAL AGENT
    3.
    发明申请
    MEDICINAL AGENT FOR DISEASE ASSOCIATED WITH EPSTEIN-BARR VIRUS, AND METHOD FOR SCREENING OF THE MEDICINAL AGENT 审中-公开
    与EPSTEIN-BARR病毒相关的疾病药物和药物代谢筛选方法

    公开(公告)号：US20120225837A1

    公开(公告)日：2012-09-06

    申请号：US13447727

    申请日：2012-04-16

    申请人： Eiichi KODAMA ,  Masao Matsuoka ,  Noriyuki Ashida

    发明人： Eiichi KODAMA ,  Masao Matsuoka ,  Noriyuki Ashida

    IPC分类号： A61K31/7072 ,  A61P31/20 ,  A61P35/00

    CPC分类号： C12Q1/18 ,  A61K31/7072 ,  G01N2333/05

    摘要： 1-(2-Fluoro-4-thio-β-D-arabinofuranosyl)-5-methyluracil exhibits an anti-EB virus activity, and is therefore effective as a prophylactic or therapeutic agent for a disease associated with an EB virus. Each of a plasmid capable of expressing EB virus-TK and a plasmid capable of expressing human-TK is introduced into a TK-defect cell, thereby producing two types of cells respectively having the plasmids introduced therein. By using the two types of cells, it is possible to screen a medicinal agent which has cytotoxicity against the cell having the plasmid capable of expressing EB virus-TK introduced therein but has no toxicity against the cell having the plasmid capable of expressing human-TK introduced therein. In this manner, it becomes possible to screen a medicinal agent which specifically exhibits an anti-EB virus activity.

    摘要翻译： 1-（2-氟-4-硫代-β-阿拉伯呋喃糖基）-5-甲基尿嘧啶具有抗EB病毒活性，因此作为与EB病毒相关疾病的预防或治疗剂是有效的。 将能够表达EB病毒-TG的质粒和能够表达人TK的质粒各自导入到TK缺陷细胞中，从而产生分别具有引入质粒的两种细胞。 通过使用两种类型的细胞，可以筛选对具有导入其中的能够表达EB病毒-TK的质粒的细胞具有细胞毒性的药剂，但对具有能够表达人TK的质粒的细胞没有毒性 在其中引入。 以这种方式，可以筛选特异性表现出抗EB病毒活性的药剂。

    4' -C-substituted-2-haloadenosine derivative
    4.
    发明授权
    4' -C-substituted-2-haloadenosine derivative 有权
    4'-取代-2-卤代腺苷衍生物

    公开(公告)号：US08039614B2

    公开(公告)日：2011-10-18

    申请号：US12453732

    申请日：2009-05-20

    申请人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    发明人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    IPC分类号： C07H19/173

    CPC分类号： C07H19/16

    摘要： The present invention provides a method for producing a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen or a phosphoryl group. The present invention also provides the derivative, and a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. The derivative is useful as a medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

    摘要翻译： 本发明提供由下式[I]，[II]或[III]表示的4'-C-取代-2-卤代腺苷衍生物的制造方法：其中，X表示卤素原子，R1表示乙炔基 或氰基，R 2表示氢或磷酰基。 本发明还提供了衍生物和含有该衍生物的药物组合物及其药学上可接受的载体。 该衍生物可用作治疗获得性免疫缺陷综合征（AIDS）的药物。

    MEDICINAL AGENT FOR DISEASE ASSOCIATED WITH EPSTEIN-BARR VIRUS, AND METHOD FOR SCREENING OF THE MEDICINAL AGENT
    5.
    发明申请
    MEDICINAL AGENT FOR DISEASE ASSOCIATED WITH EPSTEIN-BARR VIRUS, AND METHOD FOR SCREENING OF THE MEDICINAL AGENT 审中-公开
    与EPSTEIN-BARR病毒相关的疾病药物和药物代谢筛选方法

    公开(公告)号：US20100330563A1

    公开(公告)日：2010-12-30

    申请号：US12677116

    申请日：2008-09-08

    申请人： Eiichi Kodama ,  Masao Matsuoka ,  Noriyuki Ashida

    发明人： Eiichi Kodama ,  Masao Matsuoka ,  Noriyuki Ashida

    IPC分类号： C12Q1/68 ,  C07H19/00

    CPC分类号： C12Q1/18 ,  A61K31/7072 ,  G01N2333/05

    摘要： 1-(2-Fluoro-4-thio-β-D-arabinofuranosyl)-5-methyluracil exhibits an anti-EB virus activity, and is therefore effective as a prophylactic or therapeutic agent for a disease associated with an EB virus. Each of a plasmid capable of expressing EB virus-TK and a plasmid capable of expressing human-TK is introduced into a TK-defect cell, thereby producing two types of cells respectively having the plasmids introduced therein. By using the two types of cells, it is possible to screen a medicinal agent which has cytotoxicity against the cell having the plasmid capable of expressing EB virus-TK introduced therein but has no toxicity against the cell having the plasmid capable of expressing human-TK introduced therein. In this manner, it becomes possible to screen a medicinal agent which specifically exhibits an anti-EB virus activity.

    摘要翻译： 1-（2-氟-4-硫代-β-阿拉伯呋喃糖基）-5-甲基尿嘧啶具有抗EB病毒活性，因此作为与EB病毒相关疾病的预防或治疗剂是有效的。 将能够表达EB病毒-TG的质粒和能够表达人TK的质粒各自导入到TK缺陷细胞中，从而产生分别具有引入质粒的两种细胞。 通过使用两种类型的细胞，可以筛选对具有导入其中的能够表达EB病毒-TK的质粒的细胞具有细胞毒性的药剂，但对具有能够表达人TK的质粒的细胞没有毒性 在其中引入。 以这种方式，可以筛选特异性表现出抗EB病毒活性的药剂。

    4' -C-substituted-2-haloadenosine derivative
    6.
    发明申请
    4' -C-substituted-2-haloadenosine derivative 有权
    4'-取代-2-卤代腺苷衍生物

    公开(公告)号：US20090234110A1

    公开(公告)日：2009-09-17

    申请号：US12453732

    申请日：2009-05-20

    申请人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    发明人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    IPC分类号： C07H19/167

    CPC分类号： C07H19/16

    摘要： The present invention provides a method for producing a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen or a phosphoryl group. The present invention also provides the derivative, and a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. The derivative is useful as a medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

    摘要翻译： 本发明提供由下式[I]，[II]或[III]表示的4'-C-取代-2-卤代腺苷衍生物的制造方法：其中，X表示卤素原子，R1表示乙炔基 基团或氰基，R2表示氢或磷酰基，本发明还提供该衍生物和含有该衍生物的药物组合物及其药学上可接受的载体，该衍生物可用作治疗获得性免疫的药物 缺血综合征（AIDS）。

    4′-C-ethynyl purine nucleoside compounds
    8.
    发明授权
    4′-C-ethynyl purine nucleoside compounds 有权
    4'-C-乙炔嘌呤核苷化合物

    公开(公告)号：US06333315B1

    公开(公告)日：2001-12-25

    申请号：US09570042

    申请日：2000-05-12

    申请人： Hiroshi Ohrui ,  Eiichi Kodama ,  Satoru Kohgo ,  Hiroaki Mitsuya ,  Masao Matsuoka ,  Kenji Kitano

    发明人： Hiroshi Ohrui ,  Eiichi Kodama ,  Satoru Kohgo ,  Hiroaki Mitsuya ,  Masao Matsuoka ,  Kenji Kitano

    IPC分类号： A61K3170

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： The invention provides 4′-C-ethynyl purine nucleosides represented by formula [I]: wherein B represents a base selected from the group consisting of purine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.

    摘要翻译： 本发明提供由式[I]表示的4'-C-乙炔嘌呤核苷：其中B表示选自嘌呤及其衍生物的碱; X表示氢原子或羟基; R表示氢原子或磷酸酯残基; 以及含有上述化合物和药学上可接受的载体的药物组合物。 优选地，组合物用作抗HIV剂或用于治疗AIDS的药物。

    4′-c-substituted-2-haloadenosine derivative
    9.
    发明授权
    4′-c-substituted-2-haloadenosine derivative 有权
    4'-c-取代-2-卤代腺苷衍生物

    公开(公告)号：US07625877B2

    公开(公告)日：2009-12-01

    申请号：US11984527

    申请日：2007-11-19

    申请人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    发明人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    IPC分类号： A61K31/70 ,  C07H19/173 ,  C07H19/20

    CPC分类号： C07H19/16

    摘要： The present invention provides a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue. The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. The derivative is useful as a medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

    摘要翻译： 本发明提供由下式[I]，[II]或[III]表示的4'-C-取代-2-卤代腺嘌呤衍生物：其中X表示卤素原子，R1表示乙炔基或氰基 ，R2代表氢，磷酸酯残基或磷酸酯衍生物残基。 本发明还提供含有该衍生物和药学上可接受的载体的药物组合物。 该衍生物可用作治疗获得性免疫缺陷综合征（AIDS）的药物。

    4′-C-substituted-2-haloadenosine derivative
    10.
    发明授权
    4′-C-substituted-2-haloadenosine derivative 有权
    4'-C-取代-2-卤代腺苷衍生物

    公开(公告)号：US07339053B2

    公开(公告)日：2008-03-04

    申请号：US11087588

    申请日：2005-03-24

    申请人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    发明人： Satoru Kohgo ,  Hiroshi Ohrui ,  Eiichi Kodama ,  Masao Matsuoka ,  Hiroaki Mitsuya

    IPC分类号： C07H19/173 ,  C07H19/20 ,  A61K31/70

    CPC分类号： C07H19/16

    摘要： The present invention provides a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. Such derivative is useful as medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

    摘要翻译： 本发明提供由下式[I]，[II]或[III]表示的4'-C-取代-2-卤代腺嘌呤衍生物：其中X表示卤素原子，R 1 >表示乙炔基或氰基，R 2表示氢，磷酸酯残基或磷酸酯衍生物残基）。 本发明还提供含有该衍生物和药学上可接受的载体的药物组合物。 该衍生物可用作治疗获得性免疫缺陷综合征（AIDS）的药物。