Title: New multifunctional ligands for potential use in the design therapeutic or diagnostic radiopharmaceutical imaging agents

Abstract

A class of diagnostic and therapeutic compounds derived from phosphinimines that include ligands containing either a single phosphinimine functionality or both a phosphinimine group and a phosphine or arsine group, or an aminato group, or a second phosphinimine moiety. These phosphinimine ligands are complexed to early transition metal radionuclides (e.g. .sup.99m Tc or .sup.186 Re/.sup.188 Re) or late transition metals (e.g., .sup.105 Rh or .sup.109 Pd). The complexes with these metals .sup.186 Re/.sup.188 Re, .sup.99m Tc and .sup.109 Pd exhibit a high in vitro and high in vivo stability. The complexes are formed in high yields and can be neutral or charged. These ligands can also be used to form stable compounds with paramagnetic transition metals (e.g. Fe and Mn) for potential use as MRI contrast agents. Applications for the use of ligands and making the ligands are also disclosed.

Inventors:

Katti, Kattesh V ^[1]; Volkert, Wynn A ^[1]; Ketring, Alan R ^[1]; Singh, Prahlad R ^[1]

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1. Columbia, MO

Issue Date:

Wed Jan 01 00:00:00 EST 1997

Research Org.:

Univ. of Missouri, Columbia, MO (United States)

OSTI Identifier:

870821

Patent Number(s):

5601800

Assignee:

Curators of University of Missouri (Columbia, MO)

Patent Classifications (CPCs):

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07B - GENERAL METHODS OF ORGANIC CHEMISTRY

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A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A61K2123/00 - Preparations for testing in vivo
A61K51/1093 - {conjugates with carriers being antibodies}

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07B - GENERAL METHODS OF ORGANIC CHEMISTRY

C07B59/004 - {Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium}

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07F - ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM

C07F13/005 - {Compounds without a metal-carbon linkage}
C07F15/0013 - {without a metal-carbon linkage}

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DOE Contract Number:  

FG02-89ER60875

Resource Type:

Patent

Country of Publication:

United States

Language:

English

Subject:

multifunctional; ligands; potential; design; therapeutic; diagnostic; radiopharmaceutical; imaging; agents; compounds; derived; phosphinimines; containing; single; phosphinimine; functionality; phosphine; arsine; aminato; moiety; complexed; transition; metal; radionuclides; 99m; tc; 186; 188; metals; 105; 109; pd; complexes; exhibit; vitro; vivo; stability; formed; yields; neutral; charged; form; stable; paramagnetic; mn; mri; contrast; applications; disclosed; form stable; imaging agents; transition metals; transition metal; stable compound; radiopharmaceutical imaging; imaging agent; contrast agents; contrast agent; therapeutic compounds; multifunctional ligand; diagnostic radiopharmaceutical; /424/999/