Patent ID: 6503745
Filing Date: 2003-01-07
Classification: C07C,C07D,G01N

Abstract:
A compound selected from the group represented by the following formula: wherein:U is CH; Z is â€”CHâ€”CH(R3)nR2; R1 is H; R9 is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, esters thereof, or salts thereof; R2 is NHC(O)R5, NHC(S)R5, or NHSO2R5; R3 is H, (CH2)nCO2R10, (CH2)mOR10, C(O)N(R10)m, (CH2)nN(R10)m, CH(R10)m, (CH2)n(R10)m, CH2CH(OR10)CH2OR10, CH(OR10)CH(OR10)CH2OR10, CH2OR10, CH(OR10)CH2NHR10, CH2CH(OR10)CH2NHR10, CH(OR10)CH(OR10)CH2NHR10, C(&boxH;NR10)N(R10)m, NHR10, NHC(&boxH;NR10)N(R10)m, (CH2)m-Xâ€”Wâ€”Y, CH2CH(Xâ€”Wâ€”Y)CH2OR10, CH(Xâ€”Wâ€”Y)CH(OR10)CH2OR10, CH(Xâ€”Wâ€”Y)CH2(OR10), CH(OR10)CH(Xâ€”Wâ€”Y)CH2OR10, CH(OR10)CH2(Xâ€”Wâ€”Y), CH2CH(Xâ€”Wâ€”Y)CH2NHR10, CH(Xâ€”Wâ€”Y)CH(OR10)CH2NHR10, CH(Xâ€”Wâ€”Y)CH2(NHR10), CH(OR10)CH(Xâ€”Wâ€”Y)CH2NHR10, or CH(NHR10)CH2(Xâ€”Wâ€”Y); R4 is (CH2)nOH, (CH2)nNR10R11, (CH2)nNH2, (CH2)nC(&boxH;NH)(NH2), (CH2)nNHC(&boxH;NR11)NH2, (CH2)nNHC(&boxH;NR7)NH2, (CH2)nCN, (CH2)nN3, C(&boxH;NH)NH2, C(NR7)NH2, or C(NR11)NH2; R5 is H, lower alkyl, branched chain alkyl, cyclic alkyl, halogen substituted alkyl, aryl, substituted aryl, or CF3; R7 is H, (CH2)nOH, (CH2)nCN, (CH2)nNH2, or (CH2)nNO2; R10 is H, lower alkyl, lower alkylene, branched alkyl, cyclic alkyl, (CH2)n aromatic, (CH2)n substituted aromatic, or when m is 2 both R10 groups can also be interconnected to form an N substituted heterocyclic ring, or other 5 or 6 membered heterocyclic ring; R11 is lower alkyl, branched alkyl, (CH2)m aromatic, or C(O)OR10; R12 is (CH2)nOH, (CH2)nNH2, (CH2)nNR10R11, (CH2)nOR11, (CH2)nF, (CH2)nOC(O)R11, (CH2)nNHC(O)R11, or Xâ€”Wâ€”Y; R13 is H or R12; m is 1 or 2; n is 0-4; p is 1; X is O, S, CH2, or NH; W is a spacer group made up of a chain of 4 to 100 atoms, and optionally also comprising of substituted carbon and/or nitrogen atoms and optionally including oxygen or sulphur atoms; Y is OH, SH, NH2, CH&boxH;O, CH&boxH;CH2, CO2H, CONHNH2, or NH-biotinyl, or a protected form of one of these end functionalities.