Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing – Magnetic imaging agent
Patent
1992-07-17
1994-06-21
Ford, John M.
Drug, bio-affecting and body treating compositions
In vivo diagnosis or in vivo testing
Magnetic imaging agent
534 15, 534 16, 540465, 540472, A61K 4900, C07F 1502, C07D49808
Patent
active
053226810
ABSTRACT:
The invention provides novel condensed macrocyclic chelants of formula [X(CR.sup.2 R.sup.3).sub.n ].sub.m, (wherein each X independently represents an oxygen or sulphur atom or a group of formula NH, N(CR.sup.2 R.sup.3).sub.p R.sup.4, N(CR.sup.2 R.sup.3).sub.p Y, or N(CR.sup.2 R.sup.3).sub.n- N((CR.sup.2 R.sup.3).sub.p Y).sub.2 ; each Y independently represents a group COZ, SO.sub.2 Z, POZ.sub.2, CON(OH)R.sup.2, CH.sub.2 SR.sup.2, CS.sub.2 R.sup.2 or CSZ; each Z independently represents a group OR.sup.2 or NR.sup.2 R.sup.2 ; n is an integer of 1 to 4; m is an integer of 3 to 8; p is an integer of 1 to 3; each R.sup.2 independently represents a hydrogen atom or a C.sub.1-8 alkyl group optionally mono- or poly-substituted by hydroxyl or C.sub.1-8 alkoxy groups and at least one pair of R.sup.2 groups, in each pair one being from a (CR.sup.2 R.sup.3).sub. n moiety and the other being from a (CR.sup.2 R.sup.3).sub.n or (CR.sup.2 R.sup.3).sub.p moiety, together with the intervening atoms represents a 5 to 8 membered, saturated fused ring optionally containing one or more ring heteroatoms selected from nitrogen, oxygen and sulphur, said fused ring optionally being substituted by a group R.sup.1 ; each R.sup.1 independently represents a group R.sup.4 or a nitrogen-attached group (CR.sup.2 R.sup.3).sub.p Y; each R.sup.3 independently represents a hydrogen atom or a C.sub.1-8 alkyl or C.sub.1-8 alkoxy group optionally mono or poly substituted by hydroxy or C.sub.1-8 alkoxy groups; and each R.sup.4 independently represents a hydrogen atom, a halogen atom or a hydroxyl group or an optionally mono- or poly-hydroxylated C.sub.1-8 alkyl, C.sub.1-8 alkoxy, (C.sub.1-8 alkoxy)-C.sub.1-8 alkyl or poly-(C.sub.1-8 alkoxy)-C.sub.1-8 alkyl group, a sulphonate group or a group (CR.sup.2 R.sup.3).sub.p Y; with the proviso that at least 2 Y groups are present). These chelants are useful in the preparation of diagnostic and therapeutic agents, in particular chelate complexes suitable for use as contrast agents for diagnostic imaging techniques, e.g. MRI.
REFERENCES:
patent: 2387976 (1945-09-01), Bersworth
patent: 2407645 (1946-09-01), Bersworth
patent: 2751390 (1956-06-01), Bersworth
patent: 4678667 (1987-07-01), Meares et al.
patent: 4880008 (1989-11-01), Lauffer
patent: 4957939 (1990-09-01), Gries et al.
Stetter et al. Tetrahedron Letters vol. 37 pp. 767-772, 1981.
Kodama J. Chem. Soc. Dalton Trans. 1980 pp. 327-333.
Lacoste et al., J. Am. Chem. Soc. 87, 2385-2388, 1965.
Alcock et al., J. Chem. Soc. Dalton Trans., 2959-2963, 1988.
Alcock et al., J. Chem. Soc., Chem. Commun., 1058-1059, 1985.
Hancock et al., J. Am. Chem. Soc., 110, 2788-2794, 1988.
Ramasubbu et al., J. Chem. Soc., Chem. Commun., 277-278, 1982.
Barefield et al., in Inorg. Chem., 25, 552-558, 1986.
Sabbatini et al., J. Phys. Chem., 91, 4681-4685, 1987.
Smith et al., J. Am. Chem. Soc., 111, 7437-7443, 1989.
Dhont et al., Bull. Soc. Chim. Belg., 98(8), 575-576, 1989.
Hosseini et al., Helvetica Chimica Acta, 72, 1066-1077, 1989.
Wagnon et al., Inorg. Chem., 28, 1923-1927, 1989.
Ford John M.
Nycomed Imaging AS
Sripada P. K.
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