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公开(公告)号：US08883437B2
公开(公告)日：2014-11-11
申请号：US13387295
申请日：2010-07-29
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/26 , C12Q1/04 , C07D263/56 , C07D209/20 , C07D277/62
摘要： The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
摘要翻译： 本发明涉及式（I）化合物作为酶底物用于检测硝基还原酶活性的用途，其中：W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基 ，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; X是NR，CZ5Z6，S或O，R是H，烷基，芳烷基，芳基，链烷酸或烷基磺酸，Z5和Z6是烷基; Y是N或N + R，R是烷基，芳烷基，芳基，链烷酸或烷基磺酸; Z 1，Z 2，Z 3和Z 4独立地是H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括磺酰基或羧基酰胺或其酯 。
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公开(公告)号：US08535902B2
公开(公告)日：2013-09-17
申请号：US13386750
申请日：2010-07-27
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/37 , C07K4/00 , C07D213/00
摘要： The present invention relates to the use of a compound of the following formula (I) for detecting a peptidase activity and/or a variation in pH: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3 and Z4 being independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.
摘要翻译： 本发明涉及下式（I）的化合物用于检测肽酶活性和/或pH变化的用途：根据该化合物：Y1是肽，H或烷基; W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; X是NR，CZ5Z6，S或O，R是H，烷基，芳烷基，芳基，烷酰基或烷基磺酰基，Z5和Z6是烷基; Y是N或N + R，R是烷基，芳烷基，芳基，烷酰基或烷基磺酰基; Z 1，Z 2，Z 3和Z 4独立地为H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括羧基或磺酰基酯或酰胺及其盐。
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公开(公告)号：US20120122137A1
公开(公告)日：2012-05-17
申请号：US13387295
申请日：2010-07-29
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/26 , C07D209/20 , C07D263/56 , C07D209/12 , C07D235/06 , C07D277/64
摘要： The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonie, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
摘要翻译： 本发明涉及式（I）化合物作为酶底物用于检测硝基还原酶活性的用途，其中：W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基 ，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; X是NR，CZ5Z6，S或O，R是H，烷基，芳烷基，芳基，链烷酸或烷基磺酸，Z5和Z6是烷基; Y是N或N + R，R是烷基，芳烷基，芳基，链烷酸或烷基磺酸; Z 1，Z 2，Z 3和Z 4独立地是H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括磺酰基或羧基酰胺或其酯 。
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公开(公告)号：US20120129203A1
公开(公告)日：2012-05-24
申请号：US13386750
申请日：2010-07-27
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
摘要： The present invention relates to the use of a compound of the following formula (I) for detecting a peptidase activity and/or a variation in pH: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3 and Z4 being independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.
摘要翻译： 本发明涉及下式（I）的化合物用于检测肽酶活性和/或pH变化的用途：根据该化合物：Y1是肽，H或烷基; W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; X是NR，CZ5Z6，S或O，R是H，烷基，芳烷基，芳基，烷酰基或烷基磺酰基，Z5和Z6是烷基; Y是N或N + R，R是烷基，芳烷基，芳基，烷酰基或烷基磺酰基; Z 1，Z 2，Z 3和Z 4独立地为H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括羧基或磺酰基酯或酰胺及其盐。
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公开(公告)号：US20120122135A1
公开(公告)日：2012-05-17
申请号：US13386760
申请日：2010-07-28
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/37 , C07K5/083 , G01N21/80 , C07D215/12
摘要： The present invention relates to the use of a compound of the following formula (I), as an enzyme substrate for the detection of a peptidase activity or as a pH indicator: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or else V is N or N+R and U is CZ6; R is H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3, Z4 and Z5 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.
摘要翻译： 本发明涉及下述式（I）化合物作为检测肽酶活性的酶底物或作为pH指示剂的用途：其中：Y1为肽，H或烷基; W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; U是N或N + R，V是CZ6N或N + R，或者V是N或N + R，U是CZ6; R是H，烷基，芳烷基，芳基，烷酰基或烷基磺酰基; Z 1，Z 2，Z 3，Z 4和Z 5独立地为H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括羧基或磺酰基酯或酰胺及其盐。
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公开(公告)号：US08592175B2
公开(公告)日：2013-11-26
申请号：US13387280
申请日：2010-07-29
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/26 , C07K4/00 , C07D215/18
摘要： The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or V is N or N+R and U is CZ6, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; and Z1, Z2, Z3, Z4, Z5 and Z6 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
摘要翻译： 本发明涉及式（I）化合物作为酶底物用于检测硝基还原酶活性的用途，其中：W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基 ，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; U是N或N + R，V是CZ6N或N + R或V是N或N + R，U是CZ6，R是H，烷基，芳烷基，芳基，链烷基或烷基磺酸; 并且Z 1，Z 2，Z 3，Z 4，Z 5和Z 6独立地为H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括磺酰基或羧基酰胺或其酯， 和盐的相同。
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公开(公告)号：US08592174B2
公开(公告)日：2013-11-26
申请号：US13386760
申请日：2010-07-28
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/37 , C07D231/00 , A61K38/06
摘要： The present invention relates to the use of a compound of the following formula (I), as an enzyme substrate for the detection of a peptidase activity or as a pH indicator: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or else V is N or N+R and U is CZ6; R is H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3, Z4 and Z5 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.
摘要翻译： 本发明涉及下述式（I）化合物作为检测肽酶活性的酶底物或作为pH指示剂的用途：其中：Y1为肽，H或烷基; W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; U是N或N + R，V是CZ6N或N + R，或者V是N或N + R，U是CZ6; R是H，烷基，芳烷基，芳基，烷酰基或烷基磺酰基; Z 1，Z 2，Z 3，Z 4和Z 5独立地为H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括羧基或磺酰基酯或酰胺及其盐。
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公开(公告)号：US20120129204A1
公开(公告)日：2012-05-24
申请号：US13387280
申请日：2010-07-29
申请人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Sylvain Orenga , John Perry , Vindhya Salwatura , Stephen Stanforth
IPC分类号： C12Q1/26 , C07D215/12
摘要： The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; U is N or N+R and V is CZ6 N or N+R or V is N or N+R and U is CZ6, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; and Z1, Z2, Z3, Z4, Z5 and Z6 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
摘要翻译： 本发明涉及式（I）化合物作为酶底物用于检测硝基还原酶活性的用途，其中：W1，W2，W3和W4独立地为H，Br，Cl，F，I，烷基，烷氧基 ，硫代甲基，全氟烷基，硝基，氰基，羧基（包括其酯或酰胺）或其任何组合; n = 0,1或2; U是N或N + R，V是CZ6N或N + R或V是N或N + R，U是CZ6，R是H，烷基，芳烷基，芳基，链烷基或烷基磺酸; 并且Z 1，Z 2，Z 3，Z 4，Z 5和Z 6独立地为H，Br，Cl，F，I，烷基，芳基，烷氧基，全氟烷基，硝基，氰基，羧基，磺酰基，包括磺酰基或羧基酰胺或其酯， 和盐的相同。
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公开(公告)号：US20100221764A1
公开(公告)日：2010-09-02
申请号：US12451293
申请日：2008-05-29
申请人： Olivier Fabrega , Arthur James , Vindhya Lakshika Salwatura , Sylvain Orenga , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Vindhya Lakshika Salwatura , Sylvain Orenga , Stephen Stanforth
IPC分类号： C12Q1/26 , C07D209/04 , C07D401/04 , C07D261/20 , C07D263/52
CPC分类号： C07D235/18 , C07D241/44 , C07D263/57 , C07D277/66 , C12Q1/26 , C12Q2326/00 , G01N2333/90209
摘要： The present invention relates to an enzyme substrate for detecting nitroreductase activity of formula (I) below: in which X is S, NX1, O or NX1-CO; R1 is nothing or a substituent selected from Cl, CH3, Br, F, I, alkyl, aryl and carboxyl; R2 is nothing or a substituent selected from Cl, O—CH2—O, O—CH3, F, diethylenediamine-CH3, NR3R4, Br, I, alkyl, aryl, carboxyl, NO2 and R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms; and X1 is selected from H, CH3, C2H4Ph, OH, alkyl and aryl.
摘要翻译： 本发明涉及用于检测以下式（I）的硝基还原酶活性的酶底物：其中X是S，NX1，O或NX1-CO; R 1不是选自Cl，CH 3，Br，F，I，烷基，芳基和羧基的取代基; R 2不是选自Cl，O-CH 2 -O，O-CH 3，F，二乙二胺-CH 3，NR 3 R 4，Br，I，烷基，芳基，羧基，NO 2的取代基，R 3和R 4独立地为H或烷基 含有1至4个碳原子; X 1选自H，CH 3，C 2 H 4 Ph，OH，烷基和芳基。
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10.发明授权公开(公告)号：US08216800B2
公开(公告)日：2012-07-10
申请号：US12451291
申请日：2008-05-29
申请人： Olivier Fabrega , Arthur James , Vindhya Lakshika Salwatura , Sylvain Orenga , Stephen Stanforth
发明人： Olivier Fabrega , Arthur James , Vindhya Lakshika Salwatura , Sylvain Orenga , Stephen Stanforth
IPC分类号： C12Q1/37
CPC分类号： C12Q1/04 , C07D235/18 , C07D241/44 , C07D263/57 , C07D277/66 , C12Q1/045 , C12Q1/37
摘要： An enzyme substrate of formula (I) detects peptidase activity: Methods of detecting peptidase activity of a microorganism may include incubating a biological sample with the enzyme substrate of formula (I), and detecting peptidase activity if a microorganism having peptidase activity is present in the biological sample. The enzyme substrate may be included in a reaction medium.
摘要翻译： 式（I）的酶底物检测肽酶活性：检测微生物肽酶活性的方法可包括将生物样品与式（I）的酶底物孵育，并检测肽酶活性，如果具有肽酶活性的微生物存在于 生物样品。 酶底物可以包括在反应介质中。
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