Nycomed Salutar, Inc.

Salutar, Inc.

Other

Alan D Watson

Scott M Rocklage

Jo Klaveness

Jere D Fellmann

Arne Berg

William C Dow

Richard J Himmelsbach

Paul F Sieving

David B Love

Steven C Quay

Torsten Almen

Harald Dugstad

Pal Rongved

Michael Droege

John Varadarajan

Joan F Carvalho

Sook-Hui Kim

Jere D Fellman

Brent Segal

Gene Curtis Jamieson

Martha Garrity

C Allen Chang

Nils B Vogt

Michael David Koo

Michael Koo

Invention is directed to polychelants and their metal chelates which are useful in diagnostic imaging. The polychelants comprise a plurality of macrocyclic chelant moieties, eg. DOTA residues, conjugated by thiourea, urea or glycinamide linkages to a backbone moiety through a donor atom.

Polychelants

Liposomal agents

This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;

Dichelants

An x-ray contrast medium containing a multinuclear complex of the formula (M.sub.6 (.mu..sub.3 B).sub.8 A.sub.v).sub.x L.sub.w, wherein M is Mo, W, Re Tc, V, Nb, Ta, Ru, or Fe; .mu..sub.3 B represent a tridentate bridging atom; A is a non-bridging atom; L is a ligand coordinately bonded to at least one M atom; x is a positive integer; and v and w are independently zero or positive integers.

Multinuclear complexes for X-ray imaging

There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g. DOTA residues, conjugated to a dendritic polyamine backbone molecule, e.g. a starburst dendrimer. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein.

Polychelants containg amide bonds

Chelant moieties linked to an aryl moiety by an interrupted alkylene

Use of fullerenes in diagnostic and/or therapeutic agents

Linear oligomer polychelant compounds and chelates formed therewith have alternating chelant and linker moieties bound together by amide or ester moieties. The compounds have between 3 and 100 chelant moieties, at least one of which complexes a paramagnetic metal ion. The polychelants and especially their paramagnetic metal polychelates are particularly suitable for diagnostic imaging.

Linear oligomeric polychelant compounds

Macrocyclic polyaza dichelates linked through ring nitrogens via an

There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g. DOTA residues, conjugated to a polyamine backbone molecule, e.g. polylysine. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein. For example, adducts of a macrocyclic chelant can be formed by the process of (a) dispersing a carboxylic macrocyclic chelant in a polar, anhydrous solvent, (b) adding a base with a pKa sufficient to remove all carboxyl protons to create an amine salt of the chelant soluble in the solvent, (c) chilling the reaction mixture to between about 5.degree. C. and 55.degree. C. above the freezing point of the solvent, and (d) adding substantial equimolar amount of chilled alkylhaloformate under anhydrous conditions so as to form a slurry containing the mixture carboxycarbonic anhydride of the chelant.

Adducts of macrocyclic chelants

Multinuclear complexes for x-ray imaging

There are disclosed polychelant compounds, that is multi-site metal chelating agents, and chelates formed therewith. The polychelants and especially their paramagnetic metal, heavy metal or radioactive metal polychelates are particularly suitable for use in diagnostic imaging, heavy metal detoxification or radiotherapy. The polychelants have a linear or branched oligomeric structure comprising alternating chelant and linker moieties bound together by amide or ester moieties the carbonyl groups whereof being adjacent the chelant moieties, each polychelant comprising at least two said chelant moieties capable of complexing a metal ion.

Polychelant compounds

There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g, DOTA residues, conjugated to a polyamine backbone molecule, e.g, polylysine. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein.

Polychelants containing macrocyclic chelant moieties

Growing community of inventors

Campbell, CA, United States of America

Alan D Watson