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    • 3. 发明授权
    • Peptidase substrates
    • 肽酶底物
    • US08535902B2
    • 2013-09-17
    • US13386750
    • 2010-07-27
    • Olivier FabregaArthur JamesSylvain OrengaJohn PerryVindhya SalwaturaStephen Stanforth
    • Olivier FabregaArthur JamesSylvain OrengaJohn PerryVindhya SalwaturaStephen Stanforth
    • C12Q1/37C07K4/00C07D213/00
    • C12Q1/37C12Q1/04
    • 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.
    • 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。
    • 10. 发明授权
    • Nitroreductase enzymatic substrates
    • 硝基还原酶酶底物
    • US08535903B2
    • 2013-09-17
    • US13387636
    • 2010-07-29
    • Arthur JamesSylvain OrengaJohn PerryVindhya SalwaturaStephen Stanforth
    • Arthur JamesSylvain OrengaJohn PerryVindhya SalwaturaStephen Stanforth
    • C12Q1/04C07D211/72
    • C12Q1/26C12Q1/04
    • The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity or as an enzymatic substrate for the detection of a nitroreductase activity and indicator of pH, 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 and V are N, N+R, CZ4, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, preferably if U is CZ4, V is N or N+R and, if V is CZ4, U is N or N+R; and 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.
    • 本发明涉及具有式(I)化合物作为酶底物的用途,用于检测硝基还原酶活性或用作检测硝基还原酶活性和pH指示剂的酶底物,其中:W1,W2,W3和 W4独立地是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和V是N,N + R,CZ4,R是H,烷基,芳烷基,芳基,链烷酸或烷基磺酸,优选如果U是CZ4,V是N或N + R,并且如果V是CZ4,则U是N或 N + R; 并且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 相同。