公开(公告)号：US20060142311A1

公开(公告)日：2006-06-29

申请号：US11135368

申请日：2005-05-24

申请人： Akimitsu Okamoto ,  Kazuki Tainaka ,  Isao Saito ,  Norihiko Takahashi

发明人： Akimitsu Okamoto ,  Kazuki Tainaka ,  Isao Saito ,  Norihiko Takahashi

IPC分类号： A61K31/522 ,  A61K31/513

CPC分类号： C07D239/54 ,  C07D473/34 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

摘要： A compound represented by formula (1): wherein R1 is a substituent represented by formula (2): wherein R2 is ═O or —NH2, with the proviso that when R2 is ═O, H is attached to the 1-position N of the pyrimidine ring, and the bond between the 1-position N and the 6-position C is a single bond; or a substituent represented by formula (3): wherein R3 is —OH, ═O, or —NH2, with the proviso that when R3 is —OH or —NH2, R4 is H; when R3 is ═O, R4 is —NH2; and when R3 is ═O, H is attached to the 1-position N of the purine ring, and the bond between the 1-position N and the 6-position C is a single bond.

摘要翻译： 由式（1）表示的化合物：其中R 1是由式（2）表示的取代基：其中R 2是-O或-NH 2， / SUB>，条件是当R 2为-O时，H与嘧啶环的1位氮连接，1位N和6位之间的键 C是单键; 或由式（3）表示的取代基：其中R 3是-OH，-O或-NH 2，条件是当R 3' / SUP>是-OH或-NH 2，R 4是H; 当R 3为-O时，R 4为-NH 2; 当R 3为-O时，H与嘌呤环的1位氮连接，1位N与6位C之间的键为单键。

公开(公告)号：US07563886B2

公开(公告)日：2009-07-21

申请号：US10567364

申请日：2004-08-02

申请人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

发明人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

IPC分类号： C07H19/22

CPC分类号： C07H19/173 ,  C07H19/20 ,  C12Q1/6823 ,  C12Q2525/101

摘要： A method of easily releasing a useful substance bonded to oligonucleotide without impairing a target nucleic acid; and a novel base therefore. A nucleoside of nucleotide (oligonucleotide containing thereof) represented by the formula (I) (wherein each of X and Y independently represents —O—, —NH—, —N(alkyl)- or —S—; R represents a functional unit, a reporter unit or a biofunctional molecule; each of R1 and R2 independently represents a hydrogen atom, a phosphate bond group, a phosphoramidite group or a nucleotide; and n is a numeral of 1 to 10). There is further provided a method of releasing the R group moiety at base portion by the use of the oligonucleotide comprising the nucleotide.

摘要翻译： 一种容易地释放与寡核苷酸结合而不损害目标核酸的有用物质的方法; 和一个新的基地。 由式（I）表示的核苷酸（其含有寡核苷酸）的核苷（其中X和Y各自独立地表示-O - ， - NH - ， - N（烷基） - 或-S-; R表示官能单元， 报告单元或生物功能分子; R 1和R 2各自独立地表示氢原子，磷酸键合基，亚磷酰胺基或核苷酸; n为1〜10的数）。 还提供了通过使用包含该核苷酸的寡核苷酸在碱基部分释放R基团部分的方法。

公开(公告)号：US07414117B2

公开(公告)日：2008-08-19

申请号：US10795436

申请日：2004-03-09

申请人： Isao Saito ,  Akimitsu Okamoto ,  Yoshio Saito ,  Yasuko Yoshida ,  Kousuke Niwa

发明人： Isao Saito ,  Akimitsu Okamoto ,  Yoshio Saito ,  Yasuko Yoshida ,  Kousuke Niwa

IPC分类号： C07H21/02 ,  C07H19/04 ,  C12Q1/68 ,  G01N33/53 ,  C07H21/00

CPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/067 ,  C07H19/16 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6837 ,  Y10S436/809 ,  C12Q2565/549

摘要： A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intendity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is a thymin/uracil derivative (1) emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; a cytosine derivative (2) emitting light most intensely when the confronting base is guanine; an adenine derivative (3) emitting light most intensely when the confronting base is cytosine; a guanine derivative (4) emitting light most intensely when the confronting base is cytosine or thymine/uracil; and an adrnine derivative (5) emitting light most intensely when the confronting base is thymine/uracil/.

摘要翻译： 在存在单链序列成员的情况下，新的核苷酸衍生物依赖于与单链序列杂交的伴侣链中的相应碱基类型而经历荧光信号意图的变化，并且其是 当与单链核苷酸序列杂交的伴侣链中的相对的碱基是腺嘌呤时，最强烈地发射光的甲氨喋呤/尿嘧啶衍生物（1） 当相对的碱是鸟嘌呤时，胞嘧啶衍生物（2）最强地发射光; 当面对的碱基是胞嘧啶时，腺苷衍生物（3）最强地发光; 当面对的碱基是胞嘧啶或胸腺嘧啶/尿嘧啶时，最强烈地发射光的鸟嘌呤衍生物（4） 和当相对底物是胸腺嘧啶/尿嘧啶时最强烈地发光的腺苷衍生物（5）。

公开(公告)号：US20070270582A1

公开(公告)日：2007-11-22

申请号：US10567364

申请日：2004-08-02

申请人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

发明人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

IPC分类号： C07H19/16

CPC分类号： C07H19/173 ,  C07H19/20 ,  C12Q1/6823 ,  C12Q2525/101

摘要： A method of easily releasing a useful substance bonded to oligonucleotide without impairing a target nucleic acid; and a novel base therefore. A nucleoside of nucleotide (oligonucleotide containing thereof) represented by the formula (I) (wherein each of X and Y independently represents —O—, —NH—, —N(alkyl)- or —S—; R represents a functional unit, a reporter unit or a biofunctional molecule; each of R1 and R2 independently represents a hydrogen atom, a phosphate bond group, a phosphoramidite group or a nucleotide; and n is a numeral of 1 to 10). There is further provided a method of releasing the R group moiety at base portion by the use of the oligonucleotide comprising the nucleotide.

摘要翻译： 一种容易地释放与寡核苷酸结合而不损害目标核酸的有用物质的方法; 和一个新的基地。 由式（I）表示的核苷酸（其含有寡核苷酸）的核苷（其中X和Y各自独立地表示-O - ， - NH - ， - N（烷基） - 或-S-; R表示官能单元， 报告单元或生物功能分子; R 1和R 2各自独立地表示氢原子，磷酸键合基团，亚磷酰胺基团或核苷酸; n为 数字1〜10）。 还提供了通过使用包含该核苷酸的寡核苷酸在碱基部分释放R基团部分的方法。

公开(公告)号：US07323555B2

公开(公告)日：2008-01-29

申请号：US10746157

申请日：2003-12-24

申请人： Isao Saito ,  Akimitsu Okamoto ,  Yasuko Yoshida

发明人： Isao Saito ,  Akimitsu Okamoto ,  Yasuko Yoshida

IPC分类号： C07H21/02 ,  C07H21/04 ,  G01N33/53 ,  C12Q1/68

CPC分类号： C07H19/067 ,  C07H21/04 ,  Y10S436/809

摘要： A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intensity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is (1) a thymine/uracil derivative emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; (2) a cytosine derivative emitting light most intensely when the confronting base is guanine; (3) an adenine derivative emitting light most intensely when the confronting base is cytosine; and, (4) a guanine derivative emitting light most intensely when the confronting base is cytosine or thymine/uracil.

摘要翻译： 在存在单链序列成员的情况下，新的核苷酸衍生物根据与单链序列杂交的伴侣链中的相应碱基类型经历荧光信号强度的变化，并且其是 （1）当与单链核苷酸序列杂交的配对链中的相对碱基是腺嘌呤时，最强烈地发射光的胸腺嘧啶/尿嘧啶衍生物; （2）当对面的碱是鸟嘌呤时，最强烈地发射光的胞嘧啶衍生物; （3）当面对的碱基是胞嘧啶时，最强烈地发光的腺嘌呤衍生物; 和（4）当对面的碱基是胞嘧啶或胸腺嘧啶/尿嘧啶时，最强烈地发光的鸟嘌呤衍生物。

公开(公告)号：US20050142554A1

公开(公告)日：2005-06-30

申请号：US10508138

申请日：2002-08-15

申请人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

发明人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

IPC分类号： C07H19/14 ,  C07H19/04 ,  C07H19/22 ,  C07H19/23 ,  C07H21/04 ,  H01L51/30 ,  C12Q1/68 ,  C12M1/34

CPC分类号： C07H21/04 ,  B82Y10/00 ,  C07H19/04 ,  C07H19/22 ,  C07H19/23 ,  H01L51/0072 ,  H01L51/0093

摘要： A nucleic acid base for hole transportation in DNAs which does not cause oxidative decomposition; and an artificial DNA molecule which can realize effective hole transportation in DNAs while maintaining the double spiral structure of the DNAs. Provided are: a nucleic acid which contains a benzodeazaadenine derivative base represented by the general formula (I): (wherein R1, R2, R3, R4, R5, and R6 each independently represents hydrogen, amino, mono (lower alkyl) amino, di (lower alkyl) amino, hydroxy, lower alkoxy, halogeno, cyano, mercapto, lower alkylthio, or aryl; and R7 and R8 each independently represents hydrogen or a group bonded to phosphoric acid); and a polynucleotide comprising the nucleic acid.

摘要翻译： DNA不会引起氧化分解的空穴传输核酸碱基; 以及能够在保持DNA的双螺旋结构的同时实现DNA中有效空穴传输的人造DNA分子。 提供：含有由通式（I）表示的苯并恶唑腺苷衍生物碱的核酸：其中R 1，R 2，R 3， R 3，R 5，R 5和R 6各自独立地表示氢，氨基，单（低级烷基）氨基，二（低级 烷基）氨基，羟基，低级烷氧基，卤代，氰基，巯基，低级烷硫基或芳基; R 7和R 8各自独立地表示氢或键合到 磷酸）; 和包含该核酸的多核苷酸。

公开(公告)号：US07205396B2

公开(公告)日：2007-04-17

申请号：US10508138

申请日：2002-08-15

申请人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

发明人： Isao Saito ,  Akimitsu Okamoto ,  Kazuo Tanaka

IPC分类号： C07H21/00 ,  C07H21/02 ,  C12Q1/68

CPC分类号： C07H21/04 ,  B82Y10/00 ,  C07H19/04 ,  C07H19/22 ,  C07H19/23 ,  H01L51/0072 ,  H01L51/0093

摘要： A nucleic acid base for hole transportation in DNAs which does not cause oxidative decomposition; and an artificial DNA molecule which can realize effective hole transportation in DNAs while maintaining the double spiral structure of the DNAs. Provided are: a nucleic acid which contains a benzodeazaadenine derivative base represented by the general formula (I): (wherein R1, R2, R3, R4, R5, and R6 each independently represents hydrogen, amino, mono (lower alkyl) amino, di (lower alkyl) amino, hydroxy, lower alkoxy, halogeno, cyano, mercapto, lower alkylthio, or aryl; and R7 and R8 each independently represents hydrogen or a group bonded to phosphoric acid); and a polynucleotide comprising the nucleic acid.

摘要翻译： DNA不会引起氧化分解的空穴传输核酸碱基; 以及能够在保持DNA的双螺旋结构的同时实现DNA中有效空穴传输的人造DNA分子。 提供：含有由通式（I）表示的苯并恶唑烷衍生物碱的核酸：

公开(公告)号：US20080302674A1

公开(公告)日：2008-12-11

申请号：US11667980

申请日：2005-12-21

申请人： Akimitsu Okamoto ,  Taku Kamei ,  Isao Saito

发明人： Akimitsu Okamoto ,  Taku Kamei ,  Isao Saito

IPC分类号： G01N33/487

CPC分类号： G01N33/5438 ,  C12Q1/6825 ,  C12Q2565/519 ,  C12Q2563/113

摘要： A probe unit for identifying a target nucleotide region in a target nucleic acid, the unit being provided with an electrode, a probe bound to the electrode and recognizes the target nucleic acid, and a hole-transfer-inducing agent bound to the probe, wherein a nucleotide region corresponding to the target nucleotide region is located between the hole-transfer-inducing-agent-binding site and the electrode-binding end of the probe. A state of the target nucleotide region in the target nucleic acid can be identified by comparing electrochemical signal levels by energy-induced hole transfers before and after the hybridization of such a probe unit with the target nucleic acid.

摘要翻译： 用于鉴定目标核酸中的靶核苷酸区域的探针单元，所述单元设置有电极，与电极结合并识别靶核酸的探针和与探针结合的空穴传递诱导剂，其中 与靶核苷酸区域对应的核苷酸区域位于探针的空穴传递诱导剂结合位点和电极结合末端之间。 可以通过在这种探针单元与靶核酸的杂交之前和之后通过能量诱导的空穴转移比较电化学信号水平来鉴定靶核酸中靶核苷酸区的状态。

公开(公告)号：US20050059037A1

公开(公告)日：2005-03-17

申请号：US10795436

申请日：2004-03-09

申请人： Isao Saito ,  Akimitsu Okamoto ,  Yoshio Saito ,  Yasuko Yoshida ,  Kousuke Niwa

发明人： Isao Saito ,  Akimitsu Okamoto ,  Yoshio Saito ,  Yasuko Yoshida ,  Kousuke Niwa

IPC分类号： C07H19/04 ,  C07H19/067 ,  C07H21/00 ,  C07H21/04 ,  C12N15/09 ,  C12Q1/68 ,  G01N33/58

CPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/067 ,  C07H19/16 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6837 ,  Y10S436/809 ,  C12Q2565/549

摘要： A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intensity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is a thymine/uracil derivative (1) emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; a cytosine derivative (2) emitting light most intensely when the confronting base is guanine; an adenine derivative (3) emitting light most intensely when the confronting base is cytosine; a guanine derivative (4) emitting light most intensely when the confronting base is cytosine or thymine/uracil; and an adenine derivative (5) emitting light most intensely when the confronting base is thymine/uracil.

摘要翻译： 在存在单链序列成员的情况下，新的核苷酸衍生物根据与单链序列杂交的伴侣链中的相应碱基类型经历荧光信号强度的变化，并且其是 当与单链核苷酸序列杂交的伴侣链中的相对的碱基是腺嘌呤时，最强烈地发射光的胸腺嘧啶/尿嘧啶衍生物（1） 当相对的碱是鸟嘌呤时，胞嘧啶衍生物（2）最强地发射光; 当面对的碱基是胞嘧啶时，腺苷衍生物（3）最强地发光; 当面对的碱基是胞嘧啶或胸腺嘧啶/尿嘧啶时，最强烈地发射光的鸟嘌呤衍生物（4） 和当面对的碱是胸腺嘧啶/尿嘧啶时最强烈地发光的腺嘌呤衍生物（5）。

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。