Patent ID: 6517814
Filing Date: 2003-02-11
Classification: A61K

Abstract:
A macrocyclic chelant having the formula: and pharmaceutically acceptable salts thereof,wherein A1 and A2 are independently â€”(CH2)nâ€”, wherein n is 2 or 3; X is selected from the group consisting of O, NH and N(OH); R1, R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl substituted with 1-5 R6, C1-C10 fluoroalkyl substituted with 1-5 R6, C2-C10 alkenyl substituted with 1-5 R6, C2-C10 fluoroalkenyl substituted with 1-5 R6, and aryl substituted with 1-5 R6 and fluoroaryl substituted with 1-5 R6; R6 is selected from the group consisting of H, C(&boxH;O)R7, C(&boxH;O)OR8, C(&boxH;O)NR7R8, PO(OR7)(OR8) and S(O)2OR7; R7 and R8 are independently selected from the group consisting of H, C1-C10 alkyl substituted with 0-5 R9, C3-C10 cycloalkyl substituted with 0-5 R9, C1-C10 fluoroalkyl substituted with 0-5 R9, C2-C10 alkenyl substituted with 0-5 R9, C2-C10 fluoroalkenyl substituted with 0-5 R9, aryl substituted with 0-5 R9 and fluoroaryl substituted with 0-3 R9, or R7 and R8 may be taken together to form C3-C10 cycloalkyl or C3-C10 cycloalkenyl optionally interrupted with O, S, NH, S(O), S(O)2, P(O)(OR10)O, P(O)(NHR10)O, C(O)NH, NHC(O), NHC(O)NH, NHC(S)NH, or to form aryl substituted with 0-5 R10 or fluoroaryl substituted with 0-5 R10; said C1-C10 alkyl or C2-C10 alkenyl optionally interrupted with O, S, NR10 S(O), S(O)2, P(O)(OR10), P(O)(OR10)O, P(O)(NHR10), P(O)(NHR10)O, C(O)NH, NHC(O), NHC(O)NH or NHC(S)NH; R9 is selected from the group consisting of H, OH, NHR10, C(&boxH;O)R10, OC(&boxH;O)R10, OC(&boxH;O)OR10, C(&boxH;O)OR10, C(&boxH;O)NR102, PO3R102, SR10, SOR10, SO2R10, NHC(&boxH;O)R10, NHC(&boxH;O)NHR10, CH2OR10 and NHC(&boxH;S)NHR10; and R10 is selected from the group consisting of H, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 fluoroalkyl, C1-C6 alkenyl, C3-C6 cycloalkyl, C1-C6 fluoroalkenyl, benzyl, fluorobenzyl, phenyl and fluorophenyl.