Australian Nuclear Science and Technology Organisation

The Australian National University

Australian Nuclear Science and Technology Organization

Suzanne V Smith

Gary James Perkins

Eskender Mume

Richard M Lambrecht

Fook-Thean Lee

Nadine M Di Bartolo

Peter F Schmidt

John M Harrowfield

Alan McLeod Sargeson

Therese M Donlevy

Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds. 

Cryptate compounds

There is provided a method of synthesis of a radiolabelled platinum chemotherapeutic agent comprising the steps of: converting a metal halide to a radiolabelled platinum halide wherein the radiolabel is a radioisotope of Pt; and synthesizing the radiolabelled platinum chemotherapeutic agent from the radiolabelled platinum halide.

Methods of synthesis and use of radiolabelled platinum chemotherapeutic agents

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

A physiologically acceptable, radiolabelled compound of general formula ##STR1## where k is an integer from 2 to 5

Growing community of inventors

Sylvania, Australia

Suzanne V Smith