公开(公告)号：US20130023675A1

公开(公告)日：2013-01-24

申请号：US13521326

申请日：2011-01-12

申请人： Yasuteru Urano ,  Tetsuo Nagano ,  Masayo Sakabe

发明人： Yasuteru Urano ,  Tetsuo Nagano ,  Masayo Sakabe

IPC分类号： C07D493/10

CPC分类号： A61K49/0043 ,  A61K31/352 ,  A61K49/0041 ,  C07D493/10

摘要： An agent for diagnosing cancer comprising, as an active ingredient, a compound represented by the following formula (I) (R1 represents hydrogen atom, or a substituent; R2 to R7 represent hydrogen atom, hydroxyl group, an alkyl group, or a halogen atom; R8 and R9 represent hydrogen atom, or an alkyl group; and X represents a C1-C3 alkylene group), which specifically emits fluorescence in a cancerous tissue within a short time when applied to a part in which presence of a cancerous tissue is suspected.

摘要翻译： 作为活性成分的下述式（I）表示的化合物（R1表示氢原子或取代基），R2〜R7表示氢原子，羟基，烷基或卤素原子，作为活性成分 ; R8和R9表示氢原子或烷基，X表示C1-C3亚烷基），当在怀疑存在癌组织的部位应用时，在短时间内特异性地发生癌组织中的荧光 。

公开(公告)号：US08178669B2

公开(公告)日：2012-05-15

申请号：US12093479

申请日：2006-11-14

申请人： Tetsuo Nagano ,  Yasuteru Urano ,  Tasuku Ueno

发明人： Tetsuo Nagano ,  Yasuteru Urano ,  Tasuku Ueno

IPC分类号： C07F5/02

CPC分类号： C07F5/022 ,  C07F5/003 ,  G01N31/228

摘要： A compound represented by the following general formula (I): {R1, R3, R6 and R8 are methyl groups and the like, R2 and R7 are cyano groups and the like, R4 and R5 are fluorine atoms and the like, and X is a group represented by the formula (A) [R11 is a monocarboxy-substituted C1-8 alkoxy group and the like, R12, R14 and R15 are hydrogen atoms and the like, and R13 is hydroxy group and the like], provided that the combination of the aforementioned substituents is such a combination that the compound represented by the formula (I) can be substantially non-fluorescent before reacting with peroxynitrite, and the compound represented by the formula (I) in which the group represented by the formula (A) is nitrated after reacting with peroxynitrite can be substantially highly fluorescent}, or a salt thereof, which is useful as a fluorescent probe for peroxynitrite measurement.

摘要翻译： 由以下通式（I）表示的化合物：{R1，R3，R6和R8是甲基等，R2和R7是氰基等，R4和R5是氟原子等，X是 由式（A）表示的基团[R 11是单羧基取代的C 1-8烷氧基等，R 12，R 14和R 15为氢原子等，R 13为羟基等]，条件是 上述取代基的组合是这样的组合，即式（I）表示的化合物在与过氧亚硝酸盐反应之前可以基本上不发生荧光，而由式（I）表示的基团与式 ）与过氧亚硝酸盐反应后硝化可以是基本上高度荧光的}或其盐，其可用作过氧亚硝酸盐测量的荧光探针。

公开(公告)号：US20120052518A1

公开(公告)日：2012-03-01

申请号：US13201537

申请日：2010-02-19

申请人： Tetsuo Nagano ,  Yasuteru Urano ,  Masayo Sakabe

发明人： Tetsuo Nagano ,  Yasuteru Urano ,  Masayo Sakabe

IPC分类号： C12Q1/48 ,  C07D493/10

CPC分类号： C07D493/10 ,  C09B11/24

摘要： A compound represented by the formula (I) or a salt thereof (R1 represents hydrogen atom, or a substituent; R2 to R7 represent hydrogen atom, hydroxyl group, an alkyl group, or a halogen atom; R8 and R9 represent hydrogen atom, or an alkyl group; X represents a C1-C3 alkylene group; and R10 represents an acyl group), which promptly causes a structural change from a non-fluorescent closed ring structure to a strongly fluorescent open ring structure by hydrolysis of an acyl group, and is useful as a fluorescent probe for measuring a protease showing superior suitability for quantification.

摘要翻译： 由式（I）表示的化合物或其盐（R1表示氢原子或取代基; R2表示氢原子，羟基，烷基或卤素原子; R8和R9表示氢原子或 烷基; X表示C1-C3亚烷基; R10表示酰基），其通过酰基水解迅速导致从非荧光闭环结构向强荧光开环结构的结构变化，以及 作为用于测定显示出优异的定量适用性的蛋白酶的荧光探针是有用的。

公开(公告)号：US20090263910A1

公开(公告)日：2009-10-22

申请号：US12493995

申请日：2009-06-29

申请人： Ken-Ichi Setsukinai ,  Yasuteru Urano ,  Tetsuo Nagano

发明人： Ken-Ichi Setsukinai ,  Yasuteru Urano ,  Tetsuo Nagano

IPC分类号： G01N33/00

CPC分类号： G01N21/6428 ,  G01N2021/7786 ,  Y10T436/14 ,  Y10T436/19 ,  Y10T436/196666 ,  Y10T436/200833

摘要： A method for measuring hypochlorite ion, which comprises the steps of:(A) reacting, with hypochlorite ion, a compound represented by the following general formula (I): wherein R1 represents a 2-carboxyphenyl group which may be substituted; R2 represents a phenyl group which is substituted with a substituted or unsubstituted amino group; X1 and X2 each independently represents either hydrogen atom or a halogen atom; or a salt thereof; and (B) measuring fluorescence of a dearylated compound generated in the aforementioned step (A) or a salt thereof.

摘要翻译： 一种测定次氯酸根离子的方法，包括以下步骤：（A）与次氯酸根离子反应由以下通式（I）表示的化合物：其中R1表示可被取代的2-羧基苯基; R2表示被取代或未取代的氨基取代的苯基; X1和X2各自独立地表示氢原子或卤素原子; 或其盐; 和（B）测量在上述步骤（A）中产生的脱芳基化合物的荧光或其盐。

公开(公告)号：US20090258434A1

公开(公告)日：2009-10-15

申请号：US12093479

申请日：2006-11-14

申请人： Tetsuo Nagano ,  Yasuteru Urano ,  Tasuku Ueno

发明人： Tetsuo Nagano ,  Yasuteru Urano ,  Tasuku Ueno

IPC分类号： G01N33/566 ,  C07F5/02

CPC分类号： C07F5/022 ,  C07F5/003 ,  G01N31/228

摘要： A compound represented by the following general formula (I): {R1, R3, R6 and R8 are methyl groups and the like, R2 and R7 are cyano groups and the like, R4 and R5 are fluorine atoms and the like, and X is a group represented by the formula (A) [R11 is a monocarboxy-substituted C1-8 alkoxy group and the like, R12, R14 and R15 are hydrogen atoms and the like, and R13 is hydroxy group and the like], provided that the combination of the aforementioned substituents is such a combination that the compound represented by the formula (I) can be substantially non-fluorescent before reacting with peroxynitrite, and the compound represented by the formula (I) in which the group represented by the formula (A) is nitrated after reacting with peroxynitrite can be substantially highly fluorescent}, or a salt thereof, which is useful as a fluorescent probe for peroxynitrite measurement.

摘要翻译： 由以下通式（I）表示的化合物：{R1，R3，R6和R8是甲基等，R2和R7是氰基等，R4和R5是氟原子等，X是 由式（A）表示的基团[R 11是单羧基取代的C 1-8烷氧基等，R 12，R 14和R 15为氢原子等，R 13为羟基等]，条件是 上述取代基的组合是这样的组合，即式（I）表示的化合物在与过氧亚硝酸盐反应之前可以基本上不发生荧光，而由式（I）表示的基团与式 ）与过氧亚硝酸盐反应后硝化可以是基本上高度荧光的}或其盐，其可用作过氧亚硝酸盐测量的荧光探针。

公开(公告)号：US07524974B2

公开(公告)日：2009-04-28

申请号：US10519682

申请日：2003-07-07

申请人： Tetsuo Nagano ,  Yasuteru Urano ,  Suguru Kenmoku ,  Kohjiro Kanda

发明人： Tetsuo Nagano ,  Yasuteru Urano ,  Suguru Kenmoku ,  Kohjiro Kanda

IPC分类号： C07D311/90

CPC分类号： G01N27/44726 ,  C07D311/82 ,  C09B11/06 ,  C09B11/245 ,  G01N31/22

摘要： A fluorescent probe which is represented by the following formula (I): (wherein, R1 and R2 represent hydrogen atom, or a substituent for trapping proton, a metal ion, or an active oxygen species, or the like; R3 represents a monovalent substituent; R4 and R5 represent hydrogen atom or a halogen atom; R6 represents hydrogen atom, an alkylcarbonyl group, or an alkylcarbonyloxymethyl group, provided that a combination of R1, R2, and R3 provides (1) substantially high electron density of the benzene ring to which said groups bind, so that the compound represented by the formula (I) is substantially no fluorescent before the trapping of proton, or the like, and (2) substantially reduced electron density of the benzene ring to which said groups bind, so that a compound after the trapping, which is derived from the compound represented by the formula (I) is substantially highly fluorescent after the trapping of proton or the like). A fluorescent probe having an excellent fluorescence property is provided.

摘要翻译： 由下式（I）表示的荧光探针：（其中，R1和R2表示氢原子，或用于捕获质子的取代基，金属离子或活性氧等）; R3表示一价取代基 R 4和R 5表示氢原子或卤素原子; R 6表示氢原子，烷基羰基或烷基羰氧基甲基，条件是R 1，R 2和R 3的组合提供（1）苯环的电子密度基本上高到 所述基团结合，使得由式（I）表示的化合物在捕获质子之前基本上不发荧光等，和（2）所述基团所结合的苯环的电子密度基本上降低，使得 衍生自由式（I）表示的化合物捕获后的化合物在质子等的捕获之后基本上是高度荧光的）。 提供具有优异荧光性能的荧光探针。

公开(公告)号：US20060211122A1

公开(公告)日：2006-09-21

申请号：US10531664

申请日：2003-10-15

申请人： Tetsuo Nagano ,  Ken-ichi Setsukinai ,  Yasuteru Urano

发明人： Tetsuo Nagano ,  Ken-ichi Setsukinai ,  Yasuteru Urano

IPC分类号： G01N33/00

CPC分类号： G01N31/227 ,  C09K11/06 ,  C09K2211/1011 ,  C09K2211/1022 ,  C09K2211/1088 ,  Y10T436/17 ,  Y10T436/173076

摘要： A reagent for measuring peroxynitrite comprising a compound represented by the following general formula (I): wherein R1 represents an amino group, or hydroxy group; R2 represents a 2-carboxyphenyl group; and X1 and X2 independently represent hydrogen atom, or a halogen atom (e.g., 2-[6-(4′-hydroxy)phenoxy -3H-xanthen-3-on-9-yl]benzoic acid, or 2-[6-(4′-amino)phenoxy-3H-xanthen-3-on-9-yl]benzoic acid) or a salt thereof, which does not react with superoxide or nitrogen monoxide, a precursor of peroxynitrite, and specifically reacts with peroxynitrite.

摘要翻译： 一种用于测量过氧亚硝酸盐的试剂，其包含由以下通式（I）表示的化合物：其中R 1表示氨基或羟基; R 2表示2-羧基苯基; 和X 1和X 2独立地表示氢原子或卤素原子（例如2- [6-（4'-羟基）苯氧基-3H-呫吨-3 - 壬-9-基]苯甲酸或2- [6-（4'-氨基）苯氧基-3H-呫吨-3-基-9-基]苯甲酸）或其盐与超氧化物反应 或一氧化氮，过氧亚硝酸盐的前体，并与过氧亚硝酸盐特异性反应。

公开(公告)号：US08258171B2

公开(公告)日：2012-09-04

申请号：US12447723

申请日：2007-11-15

申请人： Tetsuo Nagano ,  Yasuteru Urano ,  Daisuke Asanuma

发明人： Tetsuo Nagano ,  Yasuteru Urano ,  Daisuke Asanuma

IPC分类号： A61K31/40 ,  C07D209/56

CPC分类号： C07F5/022 ,  G01N21/80

摘要： A compound represented by the following general formula (I): wherein R1 represents an amino group which may be substituted with one or two alkyl groups; R2, R3, R4 and R5 independently represent an alkyl group; and R6 and R7 independently represent a monocarboxyalkyl group, a salt thereof, or an ester thereof, which is useful as a pH-sensitive fluorescent probe which emits intense fluorescence in an acidic region.

摘要翻译： 由以下通式（I）表示的化合物：其中R1表示可被一个或两个烷基取代的氨基; R2，R3，R4和R5独立地表示烷基; 并且R6和R7独立地表示单羧基烷基，其盐或其酯，其可用作在酸性区域发射强荧光的pH敏感荧光探针。

公开(公告)号：US20110251404A1

公开(公告)日：2011-10-13

申请号：US12991750

申请日：2009-05-15

申请人： Tetsuo Nagano ,  Yasuteru Urano ,  Saki Izumi

发明人： Tetsuo Nagano ,  Yasuteru Urano ,  Saki Izumi

IPC分类号： C07D311/82 ,  C07D311/90

CPC分类号： G01N31/225 ,  C07D311/82 ,  C07D493/10 ,  G01N2021/7786

摘要： A compound represented by the formula (I) (R1 represents an aryl group such as hydroxyphenyl group, R2 represents 2-carboxyphenyl group etc., and R3 and R4 represent —(CH2)p—N(R5)(R6) (R5 and R6 represent —(CH2)n—COOH), a salt thereof, or an ester thereof, which is useful as a reagent for highly sensitive measurement of reactive oxygen such as hydroxy radical present at a trace amount in living bodies or tissues by a bioimaging technique over a long period of time.

摘要翻译： 由式（I）表示的化合物（R 1表示芳基如羟基苯基，R 2表示2-羧基苯基等，R 3和R 4表示 - （CH 2）p -N（R 5）（R 6）（R 5和 R6表示 - （CH2）n-COOH），其盐或其酯，可用作活性氧如活体或组织中微量存在的活性氧的高灵敏度测定的试剂，通过生物成像 技术在很长一段时间内。

公开(公告)号：US20090318707A1

公开(公告)日：2009-12-24

申请号：US12066323

申请日：2006-09-13

申请人： Takuya Matsumoto ,  Takuji Shoda ,  Yasuteru Urano ,  Tetsuo Nagano

发明人： Takuya Matsumoto ,  Takuji Shoda ,  Yasuteru Urano ,  Tetsuo Nagano

IPC分类号： C07F5/02

CPC分类号： C07F5/022 ,  C09B23/04 ,  C09B57/10 ,  G01N21/6428 ,  G01N2021/6439

摘要： A compound represented by the following general formula (I): [wherein R1 and R2 independently represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 and X2 represent hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom), provided that R1 and R2 do not simultaneously represent hydrogen atom; R3 and R6 represent an alkyl group; R4 and R7 represent hydrogen atom, an alkyl group, carboxy group, an alkoxycarbonyl group, or sulfo group; and R5 and R8 represents an alkyl group, an aryl group, an alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group], or a salt thereof, which is usable for efficient screening for a chemical substance having applicability as a catalyst of the reaction of Michael addition.

摘要翻译： 由以下通式（I）表示的化合物：[其中R 1和R 2独立地表示氢原子或由下式（A）表示的基团：（其中X 1和X 2表示氢原子，烷基，烷氧基 或卤素原子），条件是R 1和R 2不同时表示氢原子; R3和R6表示烷基; R4和R7表示氢原子，烷基，羧基，烷氧基羰基或磺基; R5和R8表示烷基，芳基，烷氧基羰基，乙烯基，噻吩基或吡咯基]或其盐，其可用于有效筛选具有适用性的化学物质作为 催化剂的迈克尔加成反应。