Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – Molecular bilayer structure
Patent
1992-11-17
1994-12-20
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
Molecular bilayer structure
424 165, 424 4, 424 71, 424 9, 436173, 534 10, 534 11, 534 13, 534 14, 534 15, 534 16, 540465, 540474, 1286534, A61K 4900, A61K 4904, C07D40304, C07D40306
Patent
active
053744160
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to new nitrogenous cyclic ligands and metal complexes formed by these ligands and to the diagnostic and therapeutic applications of these complexes, in particular in nuclear magnetic resonance imaging, in X-ray radiology, as in-vivo chemical shift agents and in nuclear medicine.
The invention also relates to a process for the preparation of these ligands.
The invention thus relates to ligands of formula I ##STR4## in which A.sub.1, A.sub.2, A.sub.3 and A.sub.4, which may be identical or different, independently of one another represent a group: ##STR5## m and n being identical or different integers such that the sum of m and n is between 1 and 5, R.sub.4 and R.sub.5, which may be identical or different, represent a hydrogen atom, a straight-chain or branched C.sub.1 -C.sub.6 alkyl group, a straight-chain or branched C.sub.1 -C.sub.6 hydroxyalkyl or polyhydroxyalkyl group, a functional group enabling the macrocycle of formula I to be attached to a macromolecule, a straight-chain or branched C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl group, a straight-chain or branched hydroxy-C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 alkyl group or a straight-chain or branched polyhydroxy-C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 -alkyl group an aryl group or an aryl group substituted by one or more identical or different substituents chosen from a halogen atom, a hydroxyl group, a nitro group or a C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 polyhydroxyalkyl, C.sub.1 -C.sub.6 alkoxy and C.sub.1 - C.sub.6 alkoxy-C.sub.1 -C.sub.6 -alkyl group, an aralkyl group or an aralkyl group substituted by one or more identical or different substituents chosen from a halogen atom, a hydroxyl group, a nitro group or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 polyhydroxyalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 -alkyl group, the alkyl radical of the aralkyl group being C.sub.1 -C.sub.6 and straight-chain or branched, R.sub.10 represents the group R.sub.4 or R.sub.5, a hydroxyl group or a C.sub.1 -C.sub.5 alkoxy group, R.sub.1, R.sub.2 and R.sub.3, which may be identical or different, are chosen from a hydrogen atom and the ##STR6## groups, R.sub.9 representing a hydrogen atom, a straight-chain or branched C.sub.1 -C.sub.6 alkyl group, a straight-chain or branched C.sub.1 -C.sub.6 hydroxyalkyl group, a straight-chain or branched C.sub.1 -C.sub.6 polyhydroxyalkyl group or a straight-chain or branched C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 -alkyl group and R.sub.13 representing a straight-chain or branched C.sub.1 -C.sub.6 -hydroxyalkyl group, a straight-chain or branched C.sub.1 -C.sub.6 -hydroxyalkyl or-polyhydroxyalkyl group, a straight-chain or branched C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl group or a straight-chain or branched C.sub.1 -C.sub.6 -hydroxyalkoxy- or -polyhydroxyalkoxy-C.sub.1 -C.sub.6 group, B represents the group ##STR7## W representing the group ##STR8## in which p and q are identical or different integers from 0 to 6, R.sub.11 and R.sub.12, which may be identical or different, have the same meaning as R.sub.10 when p is other than 0 and have the same meaning as R.sub.4 and R.sub.5 when p is equal to 0 and X represents a group ##STR9## R.sub.6 and R.sub.7 forming, with the carbon atom to which they are attached, a heterocycle, optionally composed of 2 fused rings, containing up to 12 members, 1 to 4 of which are heteroatoms chosen from oxygen, ##STR10## R.sub.8 representing a hydrogen atom, a straight-chain or branched C.sub.1 -C.sub.6 alkyl group, a straight-chain or branched C.sub.1 -C.sub.6 hydroxyalkyl group, a straight-chain or branched C.sub.1 -C.sub.6 polyhydroxyalkyl group or a straight-chain or branched C.sub.1 -C.sub.6 alkoxy group, phosphorus and sulphur, the heterocycle being optionally substituted by one or more groups chosen from hydroxyl, mercapto, straight-chain or branched C.sub.1 -C.sub.6 alkyl, straight-chain or branched C.sub.1 -C.sub.6 hydroxyalkyl, straight-chain
REFERENCES:
patent: 4174319 (1979-11-01), Kobuke
March, Advanced Organic Chemistry, 2d ed., (1977), pp. 326, 377-378.
Kodama et al., Inorganic Chemistry, vol. 30, No. 6, (1991), pp. 1270-1273.
Helps et al.: "General routes for the synthesis of mono, di and tri-N-substituted derivatives of cyclam", Tetrahedron, vol. 45, No. 1, Jan. 1989, pp. 219-226.
Cox et al.: "Synthesis of a kinetically stable yttrium-90 labelled macrocycle-Antibody conjugate" J. Chem Soc., Chemical Communications, No. 12, Jun. 1989, pp. 797-798.
Bouillot Anne
Meyer Dominique
Rousseaux Olivier
Schaefer Michel
Datlow Philip I.
Guerbet S.A.
Shah Mukund J.
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