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1. 发明授权

US6090937A Methods for producing nucleoside derivatives and intermediates therefor 失效
标题翻译：制备核苷衍生物的方法及其中间体
公开(公告)号：US6090937A
公开(公告)日：2000-07-18
申请号：US267789
申请日：1999-03-15
申请人： Satoshi Takamatsu , Satoshi Katayama , Naoko Hirose , Kunisuke Izawa , Tokumi Maruyama
发明人： Satoshi Takamatsu , Satoshi Katayama , Naoko Hirose , Kunisuke Izawa , Tokumi Maruyama
IPC分类号： C07D473/00 , C07H19/16 , C07H19/167 , C07H19/19
CPC分类号： C07D473/00 , C07H19/16
摘要： Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even substrates, of which the 3'-position of the saccharide moiety is deoxylated, can be substituted at the 2'-position at an extremely high yield. Specifically, by subjecting a 3'-deoxy derivative of inosine to 6-halogenation to give a 6-halide of the derivative, and then subjecting it to 2'-deoxylation/substitution with a fluorine atom or the like, followed by further subjecting it to substitution with an amino group, a hydroxyl group or any other intended substituent at the 6-positioned halogen atom, nucleoside derivatives are produced at a high yield.Methods for producing nucleoside derivatives including 9-(2,3-dideoxy-2-fluoro-.beta.-D-threo-pentofuranosyl)adenine (FddA) and their related compounds, in a simplified manner, at a high yield and at low costs, and especially Economical methods for substituting substrates, of which the 3'-position of the saccharide moiety is deoxylated, at the 2'-position to produce those nucleoside derivatives on an industrial scale are also provided.
摘要翻译：产生其核酸碱基部分的6位被卤素原子取代的核苷衍生物的新型中间体。使用这些新型中间体，其中糖基部分的3'-位脱氧的偶联底物可以在2'-位以非常高的收率被取代。具体来说，通过使肌苷的3'-脱氧衍生物进行6-卤化，得到该衍生物的6-卤化物，然后用氟原子等进行2'-脱氧/取代，然后进一步对其进行以6-取代的卤素原子被氨基，羟基或任何其它目的取代基取代，以高产率生产核苷衍生物。以简单的方式以高产率和低成本生产包括9-（2,3-二脱氧-2-氟-β-D-苏氨酸 - 呋喃鸟糖基）腺嘌呤（FddA）及其相关化合物的核苷衍生物的方法，并且还提供了用于将2'-位上的糖部分的3'-位脱氧的底物替代为工业规模生产这些核苷衍生物的经济方法。

2. 发明授权

US06500946B1 Methods for producing nucleoside derivatives and intermediates therefor 失效
标题翻译：制备核苷衍生物的方法及其中间体
公开(公告)号：US06500946B1
公开(公告)日：2002-12-31
申请号：US09567980
申请日：2000-05-10
申请人： Satoshi Takamatsu , Satoshi Katayama , Naoko Hirose , Kunisuke Izawa , Tokumi Maruyama
发明人： Satoshi Takamatsu , Satoshi Katayama , Naoko Hirose , Kunisuke Izawa , Tokumi Maruyama
IPC分类号： C07H1919
CPC分类号： C07D473/00 , C07H19/16
摘要： Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even substrates, of which the 3′-position of the saccharide moiety is deoxylated, can be substituted at the 2′-position at an extremely high yield. Specifically, by subjecting a 3′-deoxy derivative of inosine to 6-halogenation to give a 6-halide of the derivative, and then subjecting it to 2′-deoxylation/substitution with a fluorine atom or the like, followed by further subjecting it to substitution with an amino group, a hydroxyl group or any other intended substituent at the 6-positioned halogen atom, nucleoside derivatives are produced at a high yield. Methods for producing nucleoside derivatives including 9-(2,3-dideoxy-2-fluoro-&bgr;-D-threo-pentofuranosyl)adenine (FddA) and their related compounds, in a simplified manner, at a high yield and at low costs, and especially Economical methods for substituting substrates, of which the 3′-position of the saccharide moiety is deoxylated, at the 2′-position to produce those nucleoside derivatives on an industrial scale are also provided.
摘要翻译：产生其核酸碱基部分的6位被卤素原子取代的核苷衍生物的新型中间体。使用这些新型中间体，其中糖基部分的3'-位脱氧的偶联底物可以在2'-位以非常高的收率被取代。具体来说，通过使肌苷的3'-脱氧衍生物进行6-卤化，得到该衍生物的6-卤化物，然后用氟原子等进行2'-脱氧/取代，然后进一步对其进行以6-取代的卤素原子被氨基，羟基或任何其它目的取代基取代，以高产率生产核苷衍生物。以简单的方式以高产率和低成本制备包括9-（2,3-二脱氧-2-氟-β-D-苏 - 呋喃鸟糖基）腺嘌呤（FddA）及其相关化合物的核苷衍生物的方法，并且还提供了用于将2'-位上的糖部分的3'-位脱氧的底物替代为工业规模生产这些核苷衍生物的经济方法。

3. 发明申请

US20110230659A1 CYCLOBUTYL PURINE DERIVATIVE, ANGIOGENESIS PROMOTING AGENT, LUMEN FORMATION PROMOTING AGENT, NEUROCYTE GROWTH PROMOTING AGENT, AND DRUG 有权
标题翻译：环磷酰胺衍生物，促血管发生剂，促红细胞生成促进剂，神经生长促进剂和药物
公开(公告)号：US20110230659A1
公开(公告)日：2011-09-22
申请号：US13130952
申请日：2009-11-27
申请人： Ikuko Tsukamoto , Ryoji Konishi , Masaaki Tokuda , Yasuo Kubota , Tokumi Maruyama , Hiroaki Kosaka , Junsuke Igarashi
发明人： Ikuko Tsukamoto , Ryoji Konishi , Masaaki Tokuda , Yasuo Kubota , Tokumi Maruyama , Hiroaki Kosaka , Junsuke Igarashi
IPC分类号： C07D473/24 , C07D473/40 , C07D473/18
CPC分类号： C07D473/18 , C07D473/24 , C07D473/34 , C07D473/40
摘要： Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight. A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.
摘要翻译：本发明提供一种化学稳定的低分子量物质，其具有选自细胞生长促进活性，血管生成促进活性，管腔形成促进活性，细胞迁移促进活性和神经细胞生长促进活性的至少一种化合物具有高吸收性，由于其低分子量，可以以低成本稳定地供给。根据本发明的环丁基嘌呤衍生物，其互变异构体或立体异构体或其盐，溶剂化物或水合物是由以下通式（1）表示的环丁基嘌呤衍生物，其互变异构体或立体异构体，或其盐，溶剂合物或水合物。

4. 发明授权

US09273050B2 Cyclobutyl purine derivative, angiogenesis promoting agent, lumen formation promoting agent, neurocyte growth promoting agent, and drug 有权
标题翻译：环丁基嘌呤衍生物，血管生成促进剂，管腔形成促进剂，神经细胞生长促进剂和药物
公开(公告)号：US09273050B2
公开(公告)日：2016-03-01
申请号：US13130952
申请日：2009-11-27
申请人： Ikuko Tsukamoto , Ryoji Konishi , Masaaki Tokuda , Yasuo Kubota , Tokumi Maruyama , Hiroaki Kosaka , Junsuke Igarashi
发明人： Ikuko Tsukamoto , Ryoji Konishi , Masaaki Tokuda , Yasuo Kubota , Tokumi Maruyama , Hiroaki Kosaka , Junsuke Igarashi
IPC分类号： C07D473/34 , C07D473/40 , C07D473/18 , C07D473/24
CPC分类号： C07D473/18 , C07D473/24 , C07D473/34 , C07D473/40
摘要： Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight. A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.
摘要翻译：本发明提供一种化学稳定的低分子量物质，其具有选自细胞生长促进活性，血管生成促进活性，管腔形成促进活性，细胞迁移促进活性和神经细胞生长促进活性的至少一种化合物具有高吸收性，由于其低分子量，可以以低成本稳定地供给。根据本发明的环丁基嘌呤衍生物，其互变异构体或立体异构体或其盐，溶剂化物或水合物是由以下通式（1）表示的环丁基嘌呤衍生物，其互变异构体或立体异构体，或其盐，溶剂合物或水合物。

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