Patent ID: 6761878
Filing Date: 2004-07-13
Classification: A61K,A61P,C07D,C09B

Abstract:
A compound having the carbocyanine dye bioconjugate of formula 2 wherein W1 and W2 may be the same or different and are selected from the group consisting of â€”CR10R11; Y1, Y2, Z1, and Z2 are independently selected from the group consisting of hydrogen, tumor-specific agent, phototherapy agent, â€”CONH-Bm, â€”NHCO-Bm, â€”(CH2)aâ€”CONH-Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONH-Bm, â€”(CH2)aâ€”NHCO-Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCO-Bm, â€”(CH2)aâ€”N(R12)â€”(CH2)bâ€”CONH-Bm, (CH2)aâ€”N(R12)â€”(CH2)câ€”NHCO-Bm, â€”(CH2)aâ€”N(R12)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONH-Bm, â€”(CH2)aâ€”N(R12)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCO-Bm, â€”CH2â€”(CH2OCH2) bâ€”CH2â€”N(R12)â€”(CH2)aâ€”CONH-Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R12)â€”(CH2)aâ€”NHCO-Bm, â€”CH2(CH2OCH2)bâ€”CH2â€”N(R12)â€”CH2â€”(CH2OCH2)dâ€”CONH-Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R12)â€”CH2â€”(CH2OCH2)dâ€”NHCO-Bm, â€”CONH-Dm, â€”NHCO-Dm, â€”(CH2)aâ€”CONH-Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONH-Dm, â€”(CH2)aâ€”NHCO-Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCO-Dm, â€”(CH2)aâ€”N(R12) â€”(CH2)bâ€”CONH-Dm, â€”(CH2)aâ€”N(R12)â€”(CH2)câ€”NHCO-Dm, â€”(CH2)aâ€”N(R12)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONH-Dm, â€”(CH2)aâ€”N(R12)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCO-Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R12)â€”(CH2)aâ€”CONH-Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R12)â€”(CH2)aâ€”NHCO-Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R12)â€”CH2â€”(CH2OCH2)dâ€”CONH-Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R12)â€”CH2â€”(CH2OCH2)dâ€”NHCO-Dm, â€”(CH2)aâ€”N R12R13, and â€”CH2(CH2OCH2)bâ€”CH2N R12R13; K1and K2 are independently selected from the group consisting of C1-C30 alkyl, C5-C30 aryl, C1-C30 alkoxyl, C1-C30 polyalkoxyalkyl, C5-C30 polyhydroxyalkyl, C5-C30 polyhydroxyaryl, C1-C30 aminoalkyl, saccharide, peptide, â€”CH2(CH2OCH2)bâ€”CH2, â€”(CH2)aâ€”COâ€”, â€”(CH2)aâ€”CONH, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONHâ€”, â€”(CH2)aâ€”NHCOâ€”, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”, â€”(CH2)aâ€”Oâ€”, and â€”CH2â€”(CH2OCH2)bâ€”COâ€”; X1 and X2 are single bonds, or are independently selected from the group consisting of nitrogen, saccharide, â€”CR14â€”, â€”CR14R15, â€”NR16R17;C5-C30 aryl; Q is a single bond or is selected from the group consisting of â€”Oâ€”, â€”Sâ€”, â€”Seâ€”, and â€”NR18; a1 and b1 independently vary from 0 to 5; R10 to R13, and R18 to R31 are independently selected from the group consisting of hydrogen, C1-C10 alkyl, C1-C20 aryl, C1-C10 alkoxyl, C1-C10 polyalkoxyalkyl, C1-C20 polyhydroxyalkyl, C5-C20 polyhydroxyaryl, C1-C10 aminoalkyl, cyano, nitro, halogen, saccharide, peptide, â€”CH2(CH2OCH2)bâ€”CH2â€”OH, â€”(CH2)aâ€”CO2H, â€”(CH2)aâ€”CONH-Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONH-Bm, â€”(CH2)aâ€”NHCO-Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCO-Bm, â€”(CH2)aâ€”OH and â€”CH2â€”(CH2OCH2)bâ€”CH2H; R14 to R17 are independently selected from the group consisting of hydrogen, C1-C10 alkyl, C5-C20 aryl, C1-C10 alkoxyl, C1-C10 polyalkoxyalkyl, C1-C20 polyhydroxyalkyl, C5-C20 polyhydroxyaryl, C1-C10 aminoalkyl, saccharide, peptide, â€”C2(CH2OCH2)bâ€”CH2â€”, â€”(CH2)aâ€”COâ€”, â€”(CH2)aâ€”CONHâ€”, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONHâ€”, â€”(CH2)aâ€”NHCOâ€”, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”, â€”(CH2)aâ€”Oâ€”, and â€”CH2â€”(CH2OCH2)bâ€”COâ€”; Bm and Dm are independently selected from the group consisting of bioactive peptide, protein, cell, antibody, antibody fragment, saccharide, glycopeptide, peptidomimetic, drug, drug mimic, hormone, metal chelating agent, radioactive or nonradioactive metal complex, echogenic agent, photoactive molecule, and phototherapy agent; a and c independently vary from 1 to 20; b and d independently vary from 1 to 100.