The Australian National University

Australian Nuclear Science and Technology Organisation

Australian Nuclear Science and Technology Organization

Nadine M Di Bartolo

Suzanne V Smith

Richard M Lambrecht

John M Harrowfield

Peter F Schmidt

Fook-Thean Lee

Alan McLeod Sargeson

Therese M Donlevy

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

A physiologically acceptable, radiolabelled compound of general formula (I) consisting of a compound of the ##STR1## where k is an integer from 2 to 5 l is an integer from 1 to 5 X and Y are independently selected from phenyl, naphthyl, pyridine or quinoline radical, each having at position 2 one of --OH, --SH, --NH.sub.2 or --COOH and each of X and Y can be optionally substituted by one or more amino, halogen, hydroxy, mercapto, nitro, cyano, thiocyano, alkyl, alkoxy, halogenoalkyl, acyl, acylamino, acyloxy, carboxyl, alkoxycarbonyl, carbamoyl, pyridoylamino, N-carboxyalkyl-carbamoyl, sulpho, sulphamoyl, mono- or dialkylated or phenylated sulphamoyl which can also carry one or more substituents R', alkylsulphonyl, alkoxysulphonyl, or by an optionally hydroxy-containing phenylsulphonyl or phenoxysulphonyl; where R' is as defined for X and Y; or pharmaceutically acceptable salts thereof.

Metal complexes of hydroxyaryl containing aminocarboxylic acid chelating

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Sutherland, Australia

Nadine M Di Bartolo