Tri-aza macrocycles and processes for their preparation

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

540474, C07D25502, A61K 31395

Patent

active

052470776

ABSTRACT:
##STR1## Tri-aza macrocycles of formula (I), wherein m and n, which may be the same or different, is each zero or an integer 1, 2, or 3; p is zero or an integer 1 or 2; q is zero or an integer from 1 to 6 inclusive; R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen atom or a group --CO.sub.2 H or --P(O)(XH)R.sup.4 (where X is an oxygen or sulpher atom and R.sup.4 is a hydrogen atom or an alkyl or alkoxy group), with the proviso that at least one of R.sup.1, R.sup.2 and R.sup.3 is a --P(O)(XH)R.sup.4 group; L is a covalent bond or a linker group; Z is a hydrogen atom or a reactive functional group; and metal complexes and/or salts thereof; are described together with processes for their preparation and compositions containing them. The compounds are useful as imaging agents, and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and may be coupled to other molecules, such as proteins, for use in diagnosis and therapy.

REFERENCES:
patent: 4174319 (1979-11-01), Kobuke
patent: 4174428 (1979-11-01), Tabushi 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 (1987-07-01), Rodwell et al.
patent: 4678667 (1987-07-01), Meares
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.
Broan et al. Chemical Communications (1990) No. 23 pp. 1738-1739.
Chemical Abstracts vol. 114 (1991) Abstract 202872.
Abstracting FEBS Lett. (1991) 280(1) pp. 121-124 (Ramasamy et al.).
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 al., 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, p. 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).
Franz, J., et al., Abstract from Journal of Nuclear Medicine, Abstract No. 553, vol. 26, No. 5 (May 1985).
Franz et al., poster exhibited at 32nd Annual Meeting of the Society of Nuclear Medicine prior to May 1985.
Meares, 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).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Tri-aza macrocycles and processes for their preparation does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Tri-aza macrocycles and processes for their preparation, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Tri-aza macrocycles and processes for their preparation will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1051366

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.