The Australian National University

Australian Nuclear Science and Technology Organization

Alan McLeod Sargeson

John M Harrowfield

Suzanne V Smith

Nadine M Di Bartolo

Anthony J Herlt

The present invention relates to cryptate compounds useful as chelating agents. In particular, the present invention relates to functionalized derivatives of certain cryptate compounds. These functionalized derivatives are suitable for use in radiolabelling and similar applications. The present invention also relates to a method for diagnosis or therapy of a disease utilizing functionalized derivatives of cryptase compounds. In one embodiment, the present invention relates to a compound which is capable of being radiolabelled of general formula (I) in which n represents an integer from 2 to 4, where each Rand Ris independently selected from &#x2014;H, CH, COOH, NO, CHOH, HPO, HSO, CN, C&#x2550;ONHand CHO; X and Y are the same or different and are selected from the group of C&#x2014;R, N, P and C&#x2014;Z in which R represents a hydrogen or halogen atom or a hydroxyl, nitro, nitroso, amino, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl or cyano group, or a group of the formula &#x2014;COOR', COCOOR&#x2032;, NH&#x2014;COCHBr, &#x2014;NH&#x2014;CO&#x2014;CH&#x2550;CH&#x2014;COOR&#x2032; in which R&#x2032; is a hydrogen atom or alkyl group; or, W is selected from the group of NH, S and O; and Z is a functionalized linkage group which is capable of binding said compound of formula (I) to a molecular recognition unit and wherein at least one of X and Y is C&#x2014;Z; or a pharmaceutically acceptable salt thereof

Cryptate compounds and methods for diagnosis and therapy

Hydrogen peroxide is produced by oxidation of a coordination complex of a metal ion capable of existing in at least two oxidation states and a ligand, the coordination complex being sufficiently stable for the metal ion to be oxidized and reduced without decomposition of the complex and the metal ion being in its lower oxidation state. In a cyclic process, the step of reduction of the complex with the metal ion in its higher oxidation state precedes the oxidation step, and the reduction and oxidation steps are repeated sequentially. Novel coordination complexes which may be used in the process have the formula: ##STR1## in which n represents an integer; M represents a cobalt ion or other metal ion having at least two oxidation states; x and y, which may be the same or different, each represent .tbd.N, .tbd.P or .tbd.C--R', in which R' represents a hydrogen or halogen atom, or a hydroxyl, nitro, nitroso, amino, alkyl, or cyano group, or a group of the formula --COOR', --COCOOR' or --NH--COCH--CHCOOR' in which R' is a hydrogen atom or alkyl group; provided that when M represents a cobalt ion and n is 2, x and y do not both represent .tbd.N.

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Curtin, Australia

Alan McLeod Sargeson