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1. 发明授权

US06566336B1 Compounds alkylating specific base sequence of DNA and method for synthesizing the same 失效
标题翻译：烷基化DNA特异性碱基序列的化合物及其合成方法
公开(公告)号：US06566336B1
公开(公告)日：2003-05-20
申请号：US09486336
申请日：2000-05-30
申请人： Hiroshi Sugiyama , Zhi Fu Tao , Isao Saito
发明人： Hiroshi Sugiyama , Zhi Fu Tao , Isao Saito
IPC分类号： C07K1400
CPC分类号： C07D487/04 , C07D487/10
摘要： The invention provides a compound recognizing the minor group of hydrogen bonds between base pairs and being capable of forming a covalent bond with bases. The inventive compound can recognize a specific nucleotide sequence and can strongly bind to adjacent bases via covalent bonding, to regulate the expression of a DNA with the nucleotide sequence. The invention provides a DNA alkylating agent comprising a compound represented by the general formula I: wherein R represents a lower amyl group or a polyamide group; and X represents nitrogen or CH.
摘要翻译：本发明提供了识别碱基对之间的次要氢键的化合物并且能够与碱形成共价键的化合物。本发明化合物可以识别特定的核苷酸序列并且可以通过共价键强烈结合相邻的碱基，以调节DNA与核苷酸序列的表达。本发明提供一种DNA烷基化剂，其包含由通式I表示的化合物：其中R表示低级戊酰基或聚酰胺基; X表示氮或CH。

2. 发明授权

US06713633B1 Compounds capable of cleaving double-stranded DNA and method of utilization of the same 失效
标题翻译：能切割双链DNA的化合物及其利用方法
公开(公告)号：US06713633B1
公开(公告)日：2004-03-30
申请号：US09701264
申请日：2001-08-08
申请人： Hiroshi Sugiyama , Zhi-Fu Tao , Isao Saito
发明人： Hiroshi Sugiyama , Zhi-Fu Tao , Isao Saito
IPC分类号： A61K314164
CPC分类号： A61K31/407 , C07D487/04
摘要： Novel chemical species capable of simultaneously alkylating double-stranded DNA and cleaving the same; methods for alkylating and cleaving DNA by using these species; and anticancer agents with the use of these compounds. Compounds represented by the following general formula (I) which are capable of simultaneously alkylating double-stranded DNA and cleaving the same; a method for alkylating DNA and a method for cleaving double stranded DNA by using these compounds; and medicinal compositions with the use of these compounds: B—L—A(I) wherein B represents a chemical structure capable of recognizing the base sequence of DNA, for example, optionally substituted pyrrole-imidazole polyamide; A represents a chemical structure capable of binding to one base of DNA, for example, the alkylation moiety of duocarmycin A; and L represents a linker capable of binding the chemical structures A and B, for example, vinyl.
摘要翻译：能够同时烷化双链DNA并切割相同的新型化学物质; 通过使用这些物质烷基化和切割DNA的方法; 和使用这些化合物的抗癌剂。由以下通式（I）表示的化合物，其能够同时烷基化双链DNA并将其切割; 用于烷基化DNA的方法和通过使用这些化合物切割双链DNA的方法; 和使用这些化合物的药物组合物：B-L-A（I）其中B表示能够识别DNA碱基序列的化学结构，例如任选取代的吡咯 - 咪唑聚酰胺; A表示能够结合DNA的一个碱基的化学结构，例如二焦耳霉素A的烷基化部分; L表示能够结合化学结构A和B的接头，例如乙烯基。

3. 发明授权

US07456294B2 Hairpin polyamide 失效
标题翻译：发夹聚酰胺
公开(公告)号：US07456294B2
公开(公告)日：2008-11-25
申请号：US10507004
申请日：2003-03-03
申请人： Hiroshi Sugiyama , Toshikazu Bando , Isao Saito
发明人： Hiroshi Sugiyama , Toshikazu Bando , Isao Saito
IPC分类号： A61K31/407 , C07D403/14
CPC分类号： C07D487/04 , C07D403/14
摘要： It is intended to provide a pyrrole-imidazole polyamide type functional molecule having enhanced abilities of alkylating DNA and recognizing a sequence, compared with the existing functional molecules of this type, for a specific base sequence occurring on DNA. A hairpin polyamide having an alkylation site via a vinyl linker at the end of a pyrrole-imidazole polyamide. Drugs for inhibiting the expression of a specific gene and anticancer agents containing the above hairpin polyamide.
摘要翻译：旨在提供一种吡咯 - 咪唑聚酰胺型功能分子，其与DNA上存在的特定碱基序列相比，具有增强的DNA烷基化能力和识别序列，与此类型的现有功能分子相比。在吡咯 - 咪唑聚酰胺末端通过乙烯基接头具有烷基化位点的发夹聚酰胺。用于抑制特定基因表达的药物和含有上述发夹聚酰胺的抗癌剂。

4. 发明申请

US20050176647A1 Novel hairpin polyamide 失效
标题翻译：新型发夹聚酰胺
公开(公告)号：US20050176647A1
公开(公告)日：2005-08-11
申请号：US10507004
申请日：2003-03-03
申请人： Hiroshi Sugiyama , Toshikazu Bando , Isao Saito
发明人： Hiroshi Sugiyama , Toshikazu Bando , Isao Saito
IPC分类号： C12N15/09 , A61K31/4178 , A61P35/00 , A61P43/00 , C07D233/90 , C07D403/14 , C07D487/04 , C07D487/10 , A61K38/08 , C07K7/06 , C07D43/14
CPC分类号： C07D487/04 , C07D403/14
摘要： It is intended to provide a pyrrole-imidazole polyamide type functional molecule having enhanced abilities of alkylating DNA and recognizing a sequence, compared with the existing functional molecules of this type, for a specific base sequence occurring on DNA. A hairpin polyamide having an alkylation site via a vinyl linker at the end of a pyrrole-imidazole polyamide. Drugs for inhibiting the expression of a specific gene and anticancer agents containing the above hairpin polyamide.
摘要翻译：旨在提供一种吡咯 - 咪唑聚酰胺型功能分子，其与DNA上存在的特定碱基序列相比，具有增强的DNA烷基化能力和识别序列，与此类型的现有功能分子相比。在吡咯 - 咪唑聚酰胺末端通过乙烯基接头具有烷基化位点的发夹聚酰胺。用于抑制特定基因表达的药物和含有上述发夹聚酰胺的抗癌剂。

5. 发明授权

US06974668B1 Development of method for screening physiologically active pyrrole imidazole derivative 失效
标题翻译：开发用于筛选生理活性吡咯咪唑衍生物的方法
公开(公告)号：US06974668B1
公开(公告)日：2005-12-13
申请号：US09889379
申请日：2000-11-13
申请人： Hiroshi Sugiyama , Isao Saito , Hirokazu Iida
发明人： Hiroshi Sugiyama , Isao Saito , Hirokazu Iida
IPC分类号： C12N15/09 , A61K31/4178 , A61K31/70 , A61K39/395 , A61K49/00 , A61P35/00 , C07D487/04 , C07H21/04 , C12M1/26 , C12Q1/02 , C12Q1/04 , C12Q1/68 , G01N33/15 , G01N33/50 , G01N33/53 , G01N33/566
CPC分类号： G01N33/5011
摘要： A method for screening the effect of a segment A (chemical species A) on a substance (for example, a cell) containing DNA or RNA by using artificial chemical species. Namely, a method of detecting or identifying the function of a chemical species A on a substance containing DNA or RNA by using one or more chemical species represented by the following general formula (I) which are capable of recognizing a DNA base sequence; a kit therefor; and a plate to be used therein: B-L-A (I) wherein B represents a chemical structure containing an non-natural base capable of recognizing a DNA base sequence; A represents a chemical structure having an interaction with DNA; and L represents a linker whereby the chemical structures A and B can be linked together.
摘要翻译：通过使用人造化学物质筛选片段A（化学物质A）对含有DNA或RNA的物质（例如细胞）的影响的方法。即，通过使用能够识别DNA碱基序列的由以下通式（I）表示的一种或多种化学物质来检测或鉴定含有DNA或RNA的物质上的化学物质A的功能的方法; 一套工具; 和其中使用的板：B-L-A（I）其中B表示含有能够识别DNA碱基序列的非天然碱基的化学结构; A表示与DNA相互作用的化学结构; L表示连接物，化学结构A和B可以连接在一起。

6. 发明授权

US07378237B2 Development of method for screening physiologically active pyrrole imidazole derivative 失效
标题翻译：开发用于筛选生理活性吡咯咪唑衍生物的方法
公开(公告)号：US07378237B2
公开(公告)日：2008-05-27
申请号：US10285030
申请日：2002-11-01
申请人： Hiroshi Sugiyama , Isao Saito , Hirokazu Iida
发明人： Hiroshi Sugiyama , Isao Saito , Hirokazu Iida
IPC分类号： C12Q1/68 , A61K49/00 , A61K31/70 , A61K39/395
CPC分类号： G01N33/5011
摘要： A method for screening the effect of a segment A (chemical species A) on a substance (for example, a cell) containing DNA or RNA by using artificial chemical species. Namely, a method of detecting or identifying the function of a chemical species A on a substance containing DNA or RNA by using one or more chemical species represented by the following general formula (I) which are capable of recognizing a DNA base sequence; a kit therefor; and a plate to be used therein: B-L-A (I) wherein B represents a chemical structure containing an non-natural base capable of recognizing a DNA base sequence; A represents a chemical structure having an interaction with DNA; and L represents a linker whereby the chemical structures A and B can be linked together.
摘要翻译：通过使用人造化学物质筛选片段A（化学物质A）对含有DNA或RNA的物质（例如细胞）的影响的方法。即，通过使用能够识别DNA碱基序列的由以下通式（I）表示的一种或多种化学物质来检测或鉴定含有DNA或RNA的物质上的化学物质A的功能的方法; 一套工具; 和其中使用的板：B-L-A（I）其中B表示含有能够识别DNA碱基序列的非天然碱基的化学结构; A表示与DNA相互作用的化学结构; L表示连接物，化学结构A和B可以连接在一起。

7. 发明授权

US07067622B2 Method of the solid phase synthesis of pyrrole-imidazole polyamide 失效
标题翻译：吡唑咪唑聚酰胺的固相合成方法
公开(公告)号：US07067622B2
公开(公告)日：2006-06-27
申请号：US10481275
申请日：2002-02-27
申请人： Hiroshi Sugiyama , Hirokazu Iida , Isao Saito , Takashi Saito
发明人： Hiroshi Sugiyama , Hirokazu Iida , Isao Saito , Takashi Saito
IPC分类号： C07K1/02
CPC分类号： C07D403/14
摘要： It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.
摘要翻译：本发明提供一种制备吡咯 - 咪唑聚酰胺的方法，其中可以方便地合成较长的吡咯 - 咪唑聚酰胺，并且可以容易地转移肽（蛋白质）。根据该方法，可以在其末端从固相载体上切割出具有羧酸酯基的吡咯 - 咪唑聚酰胺，从而可以直接转移各种官能团，并且能够精确地区分DNA序列。一种合成吡咯 - 咪唑聚酰胺的方法，其特征在于使用肽合成仪通过固相Fmoc法进行自动合成; 通过该方法得到的具有羧基的吡咯 - 咪唑聚酰胺; 具有在上述吡咯 - 咪唑聚酰胺末端转移到羧基中的DNA烷基化剂的吡咯 - 咪唑聚酰胺; 特征在于使用上述化合物的序列特异性DNA烷基化方法。

8. 发明授权

US06946455B2 Interstrand crosslinking agents for DNA and compounds therefor 失效
标题翻译： Interstrand交联剂用于DNA及其化合物
公开(公告)号：US06946455B2
公开(公告)日：2005-09-20
申请号：US10030678
申请日：2001-05-01
申请人： Hiroshi Sugiyama , Toshikazu Bando , Hirokazu Iida , Isao Saito
发明人： Hiroshi Sugiyama , Toshikazu Bando , Hirokazu Iida , Isao Saito
IPC分类号： C12N15/00 , A61K31/407 , A61P35/00 , C07D487/04 , C07D487/10 , C07D519/00 , C12N15/01 , C12N15/09 , A61K31/33 , A01N43/38 , A01N43/90 , A61K31/44 , C07D209/56
CPC分类号： C07D487/04 , C07D487/10
摘要： Compounds represented by the general formula (I): which two DNA strands can be interstrand-crossliked: A-L-B-X-B-L-A (I) wherein B represents a chemical structure capable of recognizing the nucleotide sequence of DNA; A represents a chemical structure capable of binding to one of the bases of DNA; L represents a linker by which the chemical structures of A and B can be linked to each other; X represents a spacer by which the A-L-B components can be linked to each other. A method of interstrand-crosslinking DNA by using these compounds; and medicinal compositions containing interstarand-crosslinking agents of DNA.
摘要翻译：由通式（I）表示的化合物：两个DNA链可以是交联的：<？in-line-formula description =“In-line Formulas”end =“lead”？> ALBXBLA（I） line-formula description =“In-line Formulas”end =“tail”？>其中B表示能识别DNA核苷酸序列的化学结构; A表示能够结合DNA的一个碱基的化学结构; L表示A和B的化学结构可以彼此连接的连接体; X表示可以将A-L-B成分彼此连接的间隔物。通过使用这些化合物进行链间交联DNA的方法; 以及含有星际交联剂的DNA的药物组合物。

9. 发明授权

US5770715A Hammerhead-like nucleic acid analogues and their synthesis 失效
标题翻译：锤头样核酸类似物及其合成
公开(公告)号：US5770715A
公开(公告)日：1998-06-23
申请号：US618960
申请日：1996-03-20
申请人： Hiroshi Sugiyama , Ken Hatano , Isao Saito , Takayoshi Uchida , Yoko Matsuda , Kiyoshi Uchida
发明人： Hiroshi Sugiyama , Ken Hatano , Isao Saito , Takayoshi Uchida , Yoko Matsuda , Kiyoshi Uchida
IPC分类号： C07F9/204 , C07F9/24 , C07H19/10 , C07H19/20 , C07H21/00 , C07J63/00
CPC分类号： C07H19/10 , C07F9/204 , C07F9/2416 , C07H19/20 , C07H21/00 , C07J63/008
摘要： The present invention provides nucleic acid compounds which have a non-nucleic acid structure with ring skeleton to which two functional groups are bound with fixed state and are able to point to substantially the same direction, nucleic acid compounds which can form triple strands with third nucleotide chains, nucleic acid compounds which have improved permeability, and synthetic methods thereof.
摘要翻译：本发明提供了具有环状骨架的非核酸结构的核酸化合物，两个官能团以固定状态结合并且能够指向基本上相同的方向，可以与第三核苷酸形成三链的核酸化合物链，具有改善的渗透性的核酸化合物及其合成方法。

10. 发明申请

US20110160399A1 HISTONE MODIFICATION INHIBITOR SPECIFIC TO TARGET GENE 审中-公开
标题翻译： HISTONE修饰抑制剂特异性靶向基因
公开(公告)号：US20110160399A1
公开(公告)日：2011-06-30
申请号：US13000950
申请日：2009-07-01
申请人： Hiroki Nagase , Hiroshi Sugiyama , Tukasa Suzuki , Toshikazu Bando , Makoto Kimura , Akimichi Ohtsuki
发明人： Hiroki Nagase , Hiroshi Sugiyama , Tukasa Suzuki , Toshikazu Bando , Makoto Kimura , Akimichi Ohtsuki
IPC分类号： C08G69/48
CPC分类号： C07D403/14 , A61K45/06 , A61K47/595 , A61K47/60 , A61K47/62
摘要： The present invention provides a target gene-specific histone modification regulator, which comprises a conjugate between a histone modification regulator and a polyamide capable of recognizing a regulatory region in a target gene. This enables the provision of a target gene-specific histone modification regulator.
摘要翻译：本发明提供了靶基因特异性组蛋白修饰调节剂，其包含组蛋白修饰调节剂和能够识别靶基因中调节区的聚酰胺之间的缀合物。这使得能够提供靶基因特异性组蛋白修饰调节剂。

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