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公开(公告)号：US07829714B2
公开(公告)日：2010-11-09
申请号：US10561817
申请日：2004-07-30
IPC分类号： C07D219/06 , C12Q1/25
CPC分类号： A61K31/565 , C12Q1/26 , G01N2333/90245 , G01N2500/00 , G01N2500/10 , G01N2500/20
摘要： The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods.
摘要翻译： 本发明涉及可用于测量芳香酶活性的化合物。 本发明还提供了测量芳香酶活性的方法和用于筛选调节芳香酶活性的测试剂。 还提供了一种用于这种筛选方法的试剂盒。
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公开(公告)号：US08334387B2
公开(公告)日：2012-12-18
申请号：US12892202
申请日：2010-09-28
IPC分类号： C07D471/04 , C12Q1/25
CPC分类号： A61K31/565 , C12Q1/26 , G01N2333/90245 , G01N2500/00 , G01N2500/10 , G01N2500/20
摘要： The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods.
摘要翻译： 本发明涉及可用于测量芳香酶活性的化合物。 本发明还提供了测量芳香酶活性的方法和用于筛选调节芳香酶活性的测试剂。 还提供了一种用于这种筛选方法的试剂盒。
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公开(公告)号：US20090325209A1
公开(公告)日：2009-12-31
申请号：US12500730
申请日：2009-07-10
IPC分类号： C12Q1/26 , C07D401/10 , C07D403/10
CPC分类号： C12Q1/26 , C09B57/007 , C12Q1/32 , G01N2500/00
摘要： Disclosed are nitro-substituted squaraine reporter dyes and methods using such dyes for detecting nitroreductase enzyme activity and nitroreductase gene expression in cellular assays. The dyes are of the structure: in which Z1 and Z2 independently represent a phenyl or a naphthyl ring system; X and Y are selected from oxygen, sulphur, —CH═CH— and the group: R1 and R2 are selected from C1-C4 alkyl, —(CH2)n—P, —{(CH2)2—O}p—R6 and group W; where P is selected from COOR7, SO3− and OH, W is mono- or di-substituted nitrobenzyl, R6 is methyl or ethyl, R7 is selected from H, C1-C4 alkyl and CH2OC(O)R8, where R8 is methyl, or t-butyl, n is an integer from 1 to 10, and p is an integer from 1 to 3; R3 and R4 are selected from hydrogen, NO2, halogen, SO3−, C1-C4 alkoxy and —(CH2)m—COOR7; where R7 is hereinbefore defined and m is 0 or an integer from 1 to 5; R5 is C1-C6 alkyl optionally substituted with COOR7, SO3−, or OH; where R7 is hereinbefore defined; and at least one of groups R1, R2, R3 and R4 comprises at least one NO2 group.Also provided are methods for screening for a test agent whose effect upon nitroreductase enzyme activity and nitroreductase gene expression is to be determined.
摘要翻译： 公开了硝基取代的方酸标记物染料和使用这种染料在细胞测定中检测硝基还原酶活性和硝基还原酶基因表达的方法。 染料具有以下结构：其中Z 1和Z 2独立地表示苯基或萘基环系; X和Y选自氧，硫，-CH-CH-，R 1和R 2选自C 1 -C 4烷基， - （CH 2）n P， - {（CH 2）2 -O} p -R 6和基团 W; 其中P选自COOR 7，SO 3 - 和OH，W是单取代或二取代的硝基苄基，R 6是甲基或乙基，R 7选自H，C 1 -C 4烷基和CH 2 OC（O）R 8，其中R 8是甲基， 或叔丁基，n为1至10的整数，p为1至3的整数; R3和R4选自氢，NO2，卤素，SO3-，C1-C4烷氧基和 - （CH2）m -COOR7; 其中R7如上定义，m为0或1至5的整数; R5是任选被COOR7，SO3-或OH取代的C1-C6烷基; 其中R7如上定义; 并且R 1，R 2，R 3和R 4中的至少一个包含至少一个NO 2基团。 还提供了筛选对硝基还原酶活性和硝基还原酶基因表达的影响的测试剂的方法。
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公开(公告)号：US07579140B2
公开(公告)日：2009-08-25
申请号：US11569682
申请日：2005-05-24
IPC分类号： C12Q1/00
CPC分类号： C12Q1/26 , C09B57/007 , C12Q1/32 , G01N2500/00
摘要： Disclosed are nitro-substituted squaraine reporter dyes and methods using such dyes for detecting nitroreductase enzyme activity and nitroreductase gene expression in cellular assays. The dyes are of the structure: in which Z1 and Z2 independently represent a phenyl or a naphthyl ring system; X and Y are selected from oxygen, sulphur, —CH═CH— and the group: R1 and R2 are selected from C1-C4 alkyl, —(CH2)n—P, —{(CH2)2—O}p—R6 and group W; where P is selected from COOR7, SO3− and OH, W is mono- or di-substituted nitrobenzyl, R6 is methyl or ethyl, R7 is selected from H, C1-C4 alkyl and CH2OC(O)R8, where R8 is methyl, or t-butyl, n is an integer from 1 to 10, and p is an integer from 1 to 3; R3 and R4 are selected from hydrogen, NO2, halogen, SO3−, C1-C4 alkoxy and —(CH2)m—COOR7; where R7 is hereinbefore defined and m is 0 or an integer from 1 to 5; R5 is C1-C6 alkyl optionally substituted with COOR7, SO3−, or OH; where R7 is hereinbefore defined; and at least one of groups R1, R2, R3 and R4 comprises at least one NO2 group. Also provided are methods for screening for a test agent whose effect upon nitroreductase enzyme activity and nitroreductase gene expression is to be determined.
摘要翻译： 公开了硝基取代的方酸标记物染料和使用这种染料在细胞测定中检测硝基还原酶活性和硝基还原酶基因表达的方法。 染料具有以下结构：其中Z 1和Z 2独立地表示苯基或萘基环系; X和Y选自氧，硫，-CH-CH-，R 1和R 2选自C 1 -C 4烷基， - （CH 2）n P， - {（CH 2）2 -O} p -R 6和基团 W; 其中P选自COOR 7，SO 3 - 和OH，W是单取代或二取代的硝基苄基，R 6是甲基或乙基，R 7选自H，C 1 -C 4烷基和CH 2 OC（O）R 8，其中R 8是甲基， 或叔丁基，n为1至10的整数，p为1至3的整数; R3和R4选自氢，NO2，卤素，SO3-，C1-C4烷氧基和 - （CH2）m -COOR7; 其中R7如上定义，m为0或1至5的整数; R5是任选被COOR7，SO3-或OH取代的C1-C6烷基; 其中R7如上定义; 并且R 1，R 2，R 3和R 4中的至少一个包含至少一个NO 2基团。 还提供了筛选对硝基还原酶活性和硝基还原酶基因表达的影响的测试剂的方法。
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公开(公告)号：US20080317674A1
公开(公告)日：2008-12-25
申请号：US11569682
申请日：2005-05-24
CPC分类号： C12Q1/26 , C09B57/007 , C12Q1/32 , G01N2500/00
摘要： Disclosed are nitro-substituted squaraine reporter dyes and methods using such dyes for detecting nitroreductase enzyme activity and nitroreductase gene expression in cellular assays. The dyes are of the structure: in which Z1 and Z2 independently represent a phenyl or a naphthyl ring system; X and Y are selected from oxygen, sulphur, —CH═CH— and the group: R1 and R2 are selected from C1-C4 alkyl, —(CH2)n—P, —{(CH2)2—O}p—R6 and group W; where P is selected from COOR7, SO3− and OH, W is mono- or di-substituted nitrobenzyl, R6 is methyl or ethyl, R7 is selected from H, C1-C4 alkyl and CH2OC(O)R8, where R8 is methyl, or t-butyl, n is an integer from 1 to 10, and p is an integer from 1 to 3; R3 and R4 are selected from hydrogen, NO2, halogen, SO3−, C1-C4 alkoxy and —(CH2)m, —COOR7; where R7 is hereinbefore defined and m is 0 or an integer from 1 to 5; R5 is C1-C6 alkyl optionally substituted with COOR7, SO3−, or OH; where R7 is hereinbefore defined; and at least one of groups R1, R2, R3 and R4 comprises at least one N02 group. Also provided are methods for screening for a test agent whose effect upon nitroreductase enzyme activity and nitroreductase gene expression is to be determined.
摘要翻译： 公开了硝基取代的方酸标记物染料和使用这种染料在细胞测定中检测硝基还原酶活性和硝基还原酶基因表达的方法。 染料具有以下结构：其中Z 1和Z 2独立地表示苯基或萘基环系; X和Y选自氧，硫，-CH-CH-，R 1和R 2选自C 1 -C 4烷基， - （CH 2）n P， - {（CH 2）2 -O} p -R 6和基团 W; 其中P选自COOR 7，SO 3 - 和OH，W是单取代或二取代的硝基苄基，R 6是甲基或乙基，R 7选自H，C 1 -C 4烷基和CH 2 OC（O）R 8，其中R 8是甲基， 或叔丁基，n为1至10的整数，p为1至3的整数; R3和R4选自氢，NO2，卤素，SO3-，C1-C4烷氧基和 - （CH2）m，-COOR7; 其中R7如上定义，m为0或1至5的整数; R5是任选被COOR7，SO3-或OH取代的C1-C6烷基; 其中R7如上定义; R 1，R 2，R 3和R 4中的至少一个包含至少一个N02基团。 还提供了筛选对硝基还原酶活性和硝基还原酶基因表达的影响的测试剂的方法。
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公开(公告)号：US07101719B2
公开(公告)日：2006-09-05
申请号：US09992111
申请日：2001-11-05
IPC分类号： G01N33/534 , C12N5/00 , B32B5/02 , G01N33/557
CPC分类号： G01N33/5008 , G01N33/542 , G01N33/60 , Y10T436/13
摘要： Disclosed is a method for the measurement of a cellular process, or for the measurement of the effect of a test compound on a cellular process, in one or more different populations of cells. The method comprises providing separate samples of one or more different populations of cells adhering to support particles, the support particles comprising a scintillant substance and being adapted for cell growth. In one embodiment, different samples of cells are introduced into separate reaction vessels in a fluid medium, together with a reagent labelled with a radioisotope, in the presence or the absence of the test compound, under conditions so as to cause a portion of said radiolabelled reagent to become associated with the cells. In another embodiment, multiparameter analysis may be performed to determine the effect of a test compound on a cellular process using two or more different cell populations present in the same well. Measurement of the cellular process, or the effect of a test compound on a cellular process may be made by detecting light emission from the scintillant particles caused by radioactive decay of the radioisotope.
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公开(公告)号：US08378120B2
公开(公告)日：2013-02-19
申请号：US12500730
申请日：2009-07-10
IPC分类号： C07D209/02 , C07D277/62 , C07D263/62
CPC分类号： C12Q1/26 , C09B57/007 , C12Q1/32 , G01N2500/00
摘要： Disclosed are nitro-substituted squaraine reporter dyes and methods using such dyes for detecting nitroreductase enzyme activity and nitroreductase gene expression in cellular assays. The dyes are of the structure: in which Z1 and Z2 independently represent a phenyl or a naphthyl ring system; X and Y are selected from oxygen, sulphur, —CH═CH— and the group: R1 and R2 are selected from C1-C4 alkyl, —(CH2)n—P, —{(CH2)2—O}p—R6 and group W; where P is selected from COOR7, SO3− and OH, W is mono- or di-substituted nitrobenzyl, R6 is methyl or ethyl, R7 is selected from H, C1-C4 alkyl and CH2OC(O)R8, where R8 is methyl, or t-butyl, n is an integer from 1 to 10, and p is an integer from 1 to 3; R3 and R4 are selected from hydrogen, NO2, halogen, SO3−, C1-C4 alkoxy and —(CH2)m—COOR7; where R7 is hereinbefore defined and m is 0 or an integer from 1 to 5; R5 is C1-C6 alkyl optionally substituted with COOR7, SO3−, or OH; where R7 is hereinbefore defined; and at least one of groups R1, R2, R3 and R4 comprises at least one NO2 group. Also provided are methods for screening for a test agent whose effect upon nitroreductase enzyme activity and nitroreductase gene expression is to be determined.
摘要翻译： 公开了硝基取代的方酸标记物染料和使用这种染料在细胞测定中检测硝基还原酶活性和硝基还原酶基因表达的方法。 染料具有以下结构：其中Z 1和Z 2独立地表示苯基或萘基环系; X和Y选自氧，硫，-CH = CH-，且R 1和R 2选自C 1 -C 4烷基， - （CH 2）n -P， - {（CH 2）2 -O} p -R 6 和W组; 其中P选自COOR 7，SO 3 - 和OH，W是单取代或二取代的硝基苄基，R 6是甲基或乙基，R 7选自H，C 1 -C 4烷基和CH 2 OC（O）R 8，其中R 8是甲基， 或叔丁基，n为1至10的整数，p为1至3的整数; R3和R4选自氢，NO2，卤素，SO3-，C1-C4烷氧基和 - （CH2）m -COOR7; 其中R7如上定义，m为0或1至5的整数; R5是任选被COOR7，SO3-或OH取代的C1-C6烷基; 其中R7如上定义; 并且R 1，R 2，R 3和R 4中的至少一个包含至少一个NO 2基团。 还提供了筛选对硝基还原酶活性和硝基还原酶基因表达的影响的测试剂的方法。
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公开(公告)号：US20110014641A1
公开(公告)日：2011-01-20
申请号：US12892202
申请日：2010-09-28
CPC分类号： A61K31/565 , C12Q1/26 , G01N2333/90245 , G01N2500/00 , G01N2500/10 , G01N2500/20
摘要： The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods.
摘要翻译： 本发明涉及可用于测量芳香酶活性的化合物。 本发明还提供了测量芳香酶活性的方法和用于筛选调节芳香酶活性的测试剂。 还提供了一种用于这种筛选方法的试剂盒。
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公开(公告)号：US07235401B2
公开(公告)日：2007-06-26
申请号：US10491762
申请日：2002-09-12
申请人： Jonathon Noe Pines , Nicholas Thomas , Anne Elizabeth Jones , Ian David Goodyer , Michael John Francis , Rahman Aziz Ismail , Jonathan Mark Kendall
发明人： Jonathon Noe Pines , Nicholas Thomas , Anne Elizabeth Jones , Ian David Goodyer , Michael John Francis , Rahman Aziz Ismail , Jonathan Mark Kendall
CPC分类号： C07K14/4738 , C12N15/63
摘要： The invention provides a novel, non-destructive and dynamic process for determining the cell cycle position of living cells. The invention also provides DNA constructs, and cell lines containing such constructs, that exhibit activation and deactivation of a detectable reporter molecule in a cell cycle specific manner. The invention thus allows greater precision in determining cell cycle phase status than existing techniques and further provides a method for continuous monitoring of cell cycle progression in individual cells.
摘要翻译： 本发明提供了用于确定活细胞的细胞周期位置的新颖的，非破坏性和动态的方法。 本发明还提供DNA构建体和含有此类构建体的细胞系，其以细胞周期特异性方式表现出可检测报道分子的活化和失活。 因此，本发明允许比现有技术更高的确定细胞周期相位状态的精确性，并进一步提供用于连续监测各个细胞中的细胞周期进程的方法。
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