Tetra-aza macrocycles, processes for their preparation and their

Details Tetra-aza macrocycles, processes for their preparation and their Tetra-aza macrocycles, processes for their preparation and their

1994-09-23

1997-08-05

Gupta, Yogendra N.

Drug, bio-affecting and body treating compositions

In vivo diagnosis or in vivo testing

Magnetic imaging agent

514 79, 514836, 534 15, 534 16, 540465, 540474, A61B 5055, A61K 4900, C07D25502, C07D25500

Patent

active

056539606

ABSTRACT:
##STR1## Metal complex of tetra-aza macrocycles of formula (1) wherein Alk.sup.1, Alk.sup.2, Alk.sup.3 and Alk.sup.4, which may be the same or different, is each a C.sub.1-4 alkylene chain optionally substituted by one or more optionally substituted C.sub.1-6 alkyl groups; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different is each a hydrogen atom or a group AlkR.sup.5 where Alk is an optionally substituted straight or branched C.sub.1-6 alkyl group and R.sup.5 is a hydrogen atom or a --CO.sub.2 H,--CONR.sup.6 R.sup.7 [where R.sup.6 and R.sup.7, which may be the same or different, is each a hydrogen atom or a C.sub.1-6 alkyl group] or --P(X.sup.1)(X.sup.2 R.sup.8)R.sup.9 group where X.sup.1 and X.sup.2, which may be the same or different is each an oxygen or sulphur atom, R.sup.8 is a hydrogen atom or an alkyl group and R.sup.9 is an aliphatic, aromatic or heteroaromatic group, with the proviso that at least two of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group -AlkP(X.sup.1)(X.sup.2 R.sup.8)R.sup.9 or one or R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group -AlkP(X.sup.1)(X.sup.2 R.sup.8)R.sup.9 and at least one of the remaining groups R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group -AlkCO.sub.2 H or -AlkCONR.sup.6 R.sup.7, or a salt thereof, for use as contrast agents in nuclear magnetic resonance imaging are described.

REFERENCES:
patent: 4174319 (1979-11-01), Kobuke
patent: 4174428 (1979-11-01), Tabushik et al.
patent: 4432907 (1984-02-01), Wieder et al.
patent: 4472509 (1984-09-01), Gansow et al.
patent: 4659839 (1987-04-01), Nicolotti et al.
patent: 4671958 (1987-06-01), Rodwell et al.
patent: 4678667 (1987-07-01), Meares
patent: 4702998 (1987-10-01), Tanaka et al.
patent: 4877600 (1989-10-01), Bonnemain et al.
patent: 4885363 (1989-12-01), Tweedle et al.
patent: 5049667 (1991-09-01), Schaefer et al.
patent: 5053503 (1991-10-01), Dean et al.
patent: 5342606 (1994-08-01), Sherry et al.
Broan et al., "Synthesis and Complexation Behaviour of an Effective Octadentate Complexone 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetrakis[methylene(methylphosphini c acid)]", J. Chem. Soc., Chem. Commun., pp. 1739-1741 (1st Dec. 1990).
Kabachnik et al., "Synthesis and Acid-Base and Complex-Forming Properties of 1,4,7,10-tetrakis(dihydroxyphosphorylmethyl)-1,4,7,10-tetraazacyclodode cane", Bull. Acad. Sci. USSR, 33(4), pp. 777-782 (1984).
Khaw et al., Science. 209, 295 (1980).
Krejcarek et al., Biochem. Biophys. Res. Comm., 77, 581 (1977).
Childs, R.L. and Hnatowich, D.J., J. Nuc. Med. 26, 293 (1985).
Stetter, H., et al., Angew. Chem. Int. Ed. Engl., 15, 686 (1976).
Loncin, J.F., et al., Inorg. Chem., 25, 2646 (1986).
Moi, C.F., et al., J. Am. Chem. Soc., 110 6266 (1988).
Tweedle, M.F., et al., J. Nuc. Med., 28, 705 (1988).
Goodwin, C.H., et a., J. Nuc. Med., 27, 959 (1986).
Paik, C.H., et al., J. Nuc. Med., 28, 572 (1987).
Paik, C.H., et al., J. Nuc. Med., 29, 889 (1988).
Haseman, C.F., et al., Eur. J. Nuc. Med., 12, 455 (1986).
Parker et al., Pure & Appl. Chem., vol. 61, No. 9, 1637-1641 (1989).
Craig et al., J. Chem. Soc. Chem. Commun. (1989), pp. 794-796.
Cox et al., J. Chem. Soc. Chem. Commun. (1989), pp. 797-798.
Paik et al., J. Nucl. Sci., vol. 30, No. 10, pp. 1693-1701 (Oct. 1989).
Paik et al., Nucl. Med. Biol., vol. 16, No. 5, pp. 475-481 (1989).
Deshpande et al., Nucl. Med. Biol., vol. 16, No. 6, pp. 587-597 (1989).
Deshpande et al., The Journal of Nuclear Medicine. "Copper-67-Labeled Monoclonal Antibody Lym-1, A Potential Radio-pharmaceutical for Cancer Therapy: Labeling and Biodistribution in RAJI Tumored Mice, " vol. 29, No. 2, pp. 217-225 (Feb. 1988).
Mears, Claude F., "Protein Tailoring for Food and Medicine Uses edited by R.E. Feeny et al., Attaching Metal Ions to Antibodies", pp. 339-352 (1986).
Goodwin, D.A., et al., Abstract of "In Complex of a New Macrocyclic Bifunctional Chelator TETA", presented at European Nuclear Medicine Congress Meeting at Barbican, London, Sep. 3-6 (1985).
Meares et al., Int. J. cancer Suppl., 2, 99-102 (1988).
Meares et al., Br. J. Cancer, 62, 21-26 (1990).
Gransow et al., ACS Symposium Series, No. 241, "Generator Produced Bi-212" (1984).
Moi et al., Anal. Biochem., 148, 249-253 (1985).
Lazar et al. Inorg. Chem. 30, pp. 5016-5019, 1991.

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