Agents for diagnosing and treating melanomas, aromatic halogenat

Details Agents for diagnosing and treating melanomas, aromatic halogenat Agents for diagnosing and treating melanomas, aromatic halogenat

1991-08-06

1993-03-02

Lovering, Richard D.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

564161, A61K 3100, A61K 4300

Patent

active

051907410

ABSTRACT:
##STR1## The invention concerns agents for diagnosing and treating malignant melanomas, of general formula (I), in which X denotes a hydrogen or halogen atom, Y denotes a Z--CONH--, Z--O--, Z--S(O)--.sub.n1 group, n.sub.1 being equal to 0,1,2 or 3, a Z--SO.sub.2 --NH-- Z--NHCO-- group, Z being a bond, a --CH.sub.2 -- or --CH(C.sub.6 H.sub.5)-- group, n is an integer between 2 and 4, and R.sub.1 and R.sub.2 each denote a hydrogen atom, a C.sub.1 to C.sub.6 alkyl group or a C.sub.6 to C.sub.12 aryl or aralkyl group, these compounds possibly being labelled by radioisotopes chosen from .sup.123 I, .sup.123 I, .sup.123 I, .sup.75 Br, .sup.77 Br, .sup.18 F, or .sup.11 C or by stable isotopes chosen from .sup.13 C and .sup.19 F, as well as their addition salts with pharmaceutically acceptable acids. The invention also concerns the use of these compounds to manufacture an agent for diagnosing and/or treating malignant melanomas.

REFERENCES:
patent: 4279887 (1981-07-01), Baldwin et al.
"Synthese etude chez le rat, de composes radioiodes utilisables pour l'exration du systeme nerveux central", Eur. J. Med. Chem. Chim. Ther., vol. 21, No. 5, 1986, by M.-F. Moreau et al., pp. 423-431.
"Interactions of the novel inhibitors of MAO-B Ro 19-6327 and Ro 16-6491 with the active site of the nezyme", Pharmacological Research Communications, vol. 20, suppl. IV, 1988, by A. M. Cesura et al, pp. 51-61.
"Ro 16-6491: A new reversible and highly selective MAO-B inhibitor protects mice from the dopaminergic neurotoxicity of MPTP", Advances in Neurology, vol. 45, 1987, by M. Da Prada et al., pp. 175-178.

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