Macrocyclic polyaza compounds containing 5 or 6 membered...

C - Chemistry – Metallurgy – 07 – D

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167/101, 167/119

C07D 471/08 (2006.01) A61K 49/00 (2006.01) A61K 49/06 (2006.01) A61K 51/00 (2006.01) C07D 255/04 (2006.01) C07D 487/08 (2006.01) C07D 498/08 (2006.01) C07D 513/08 (2006.01) C07F 5/00 (2006.01)

Patent

CA 1341035

The macrocyclic compounds of the following formula I and their salts with inorganic and/or organic bases, amino acids or amino acid amides are valuable diagnostic and therapeutic agents: Image in which ~~stands for a single bond or double bond, q stands for the numbers 0-5, A and B, which are the same or different, each stand for a straight chain or branched alkylene group with 2 to 6 carbon atoms, D stands for a nitrogen atom, oxygen atom, the group ~C~O, =NR2 with R2 meaning a hydrogen atom or a C1-C6-alkyl group, the group Image or ,IMG> with R3 meaning a hydrogen atom or a halogen atom, a phenyl or a C1-C6 -alkyl group, which optionally is substituted by one or more phenyl and/or hydroxy 2/3 group(s), the radical OR5, in which R5 stands for a C1-C6-alkyl radical optionally substituted by 1 to 3 hydroxy groups, substituent Image , whereby m stands for the numbers 0 and 1 and R6 and R7 independently from one another for hydrogen atoms, for the radical R5, for phenyl or benzyl radicals optionally substituted by 1 to 3 hydroxy groups or R6 and R7 together with the nitrogen atom for a saturated or unsaturated 5 or 6 ring optionally containing an additional nitrogen atom, oxygen atom, sulfur atom or a carbonyl group, which is optionally substituted by 1 to 3 radicals R5, or one of the substituents R6 or R7 stand for the radical Image , or substituent G, wherein G represents a second macrocycle of general formula II bonded by a direct bond, a bis(carbonylaminol) group (-NH-CO-CO-NH-) or by a C1-C20-alkylene group, which optionally carries carbonyl (CO) groups or carbonylamino (-NH-CO-) groups or oxygen atoms on the ends and optionally contains one or more oxygen atom(s), Z-, acyl groups or hydroxyacyl substituted imino groups or one to two C-C double bonds and/or C-C triple bonds, Image in which 3/3 D1 has the same meaning as D, with the exception that D~ does not contain the substituent G, or stands for the radical Image and F1 has the same meaning as F, with the exception that F1 does not contain the substituent G, or stands for the radical Image , E stands for a nitrogen atom, sulfur atom, oxygen atom, the Image or NR4 group with R4 meaning Image a hydroxy group, R2 an optionally hydroxylated or carboxylated C1-C6-alkyl group, F stands for (-CHR8-)n or (=CR8-)n with n meaning the numbers 0 or 1 and R8 meaning R1 or G, R1 stands for a hydrogen atom or a halogen atom or a C1-C6 alkylgroup, Z stands for a hydrogen atom or the group -CH2COOY with Y meaning a hydrogen atom and/or a metal ion equivalent of an element with atomic numbers 21-29, 31, 32, 37-39, 42-44, 49 or 57-83, provided that at least two of substituents Z stand for the radical -CH2COOY and the macrocyclic compound of general formula I contains not more than one radical G.

606159

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