The Dow Chemical Company

University of Texas System

Barnes Jewish Hospital

Dow Global Technolgoies LLC

Nordion (canada) Inc.

Texas Tech University System

Orano Med

Radiomedixinc.

F. Hoffmann-la Roche Ag

Radiomedix Inc.

Orano Med Sas

Garry E Kiefer

Christian Klein

David A Wilson

Pablo Umana

Jaime Simon

Joseph R Garlich

A Dean Sherry

Phillip S Athey

Samuel A Wickline

Gregory M Lanza

R Keith Frank

William Jack Kruper, Jr

Darryl J Bornhop

William A Fordyce

Kenneth McMillan

Roberta C Cheng

Gyongyi Gulyas

Zoltan Kovacs

Corinne Bensimon

Richard Keith Frank

Julien Torgue

William F Goeckeler

Izabela Tworowska

Ebrahim S Delpassand

Cara L Ferreira

Tania A Stallons

Sharon Baughman

Sharon Braughman

William F Goeckleler

Nilesh Wagh

Federico Rojas-Quijano

Paul Jurek

Amal Saidi

Won D Kim

Tapan Nayak

Alexander Haas

Sofia Frost

Christian Gerdes

Olivier Freytag

A cancer targeting composition, kit, and method for treatment of cancer cells overexpressing somatostatin receptors is disclosed. The composition includes a radioisotope, a chelator, and a targeting moiety. The chelator includes a nitrogen ring structure including a tetraazacyclododecane, a triazacyclononane, and/or a tetraazabicyclo [6.6.2] hexadecane derivative. The targeting moiety includes a somatostatin receptor targeting peptide. The somatostatin receptor targeting peptide includes an octreotide derivative. The targeting moiety is chelated to the radioisotope by the chelator whereby the cancer cells are targeted for elimination.

Treatment of cancer cells overexpressing somatostatin receptors using ocreotide derivatives chelated to radioisotopes

A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q, X, Y, Z, Z, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion ofY,In orLu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.

Bifunctional polyazamacrocyclic chelating agents

A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q, X, Y, Z, Z, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion ofY,Li orLu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.

MRI contrast agents that employ paramagnetic agents and chemical exchange saturation transfer (paraCEST) and which are coupled to targeted particulate delivery vehicles provide sufficient concentration of the paraCEST contrast agents to obtain useful images of target tissues or organs. In addition, the image contrast may be switched on or off with a presaturation radio frequency pulse, avoiding the necessity obtaining pre-injection and post-injection images.

Targeted MR imaging agents

Compounds useful for associating with nanoparticle or microparticle emulsions to obtain magnetic resonance images permit control of the relaxivity of the signal and readily associate with the particulate components.

Chelating agents with lipophilic carriers

Fluorescent chelates of lanthanide, terbium, europium and dysprosium with tetraazamacrocyclic compounds are discussed which can be used as fluorescent in vitro or in vivo diagnostic agents. These chelates are tissue specific imaging agents for soft tissue cancers.

Tissue specific fluorescent chelates possessing long wavelength UV excitation

Actinium-225 complexes comprising functionalized polyazamacrocyclic chelant compounds are disclosed. Such complexes show improved stability and can be conjugated to a biological carrier.

Actinium-225 complexes and conjugates for targeted radiotherapy

Fluorescent chelates of terbium and europium with tri- and tetra-cyclopolyazamacrocyclic compounds are discussed which can be used as fluorescent in vitro or in vivo diagnostic agents. These chelates are tissue specific imaging agents.

Fluorescent chelates as visual tissue specific imaging agents

Polyazamacrocyclofluoromonoalkylphosphonic acid compounds are disclosed which form inert complexes with Gd, Mn, Fe or La ions. The complexes are useful as contrast agents for diagnostic purposes.

Polyazamacrocyclofluoromonoalkylphosphonic acids, and their complexes,

Bicyclopolyazamacrocyclophosphonic acid compounds are disclosed which may form inert complexes with Gd, Mn or Fe ions. The overall charge of the complex can be varied to alter the in vivo biolocalization. Such complexes can be covalently attached to an antibody, antibody fragment or other biologically active molecule to form conjugates. The complexes and conjugates are useful as contrast agents for diagnostic purposes.

Bicyclopolyazamacrocyclophosphonic acid half esters

Bicyclopol yazamacrocyclophosphonic acid complexes for use as contrast

A novel process for the preparation of azamacrocyclic or acyclic aminophosphonate ester derivatives is disclosed. The process concerns the reaction of an appropriate azamacrocyclic or acyclic primary or secondary amine with trialkyl phosphite and paraformaldehyde.

Process for the preparation of azamacrocyclic or acyclic

The present invention describes a process to reduce the volume and/or weight of magnesium slag when the magnesium slag contains radioactive thorium. The process contacts the magnesium slag as an aqueous slurry with an acid in a pH range from about 4.0 to about 8.0, preferably from about 5.0 to about 5.5, followed by separating insoluble solids from the aqueous solution. Optionally, the acid digested solids are heated, either before or after the acid digestion, at a temperature from about 350.degree. to about 500.degree. C. The solid waste can then be further compacted, if desired, prior to disposal.

Process for concentrating thorium containing magnesium slag

A group of functionalized polyaminocarboxylate chelants that form complexes with rare earth-type metal ions are disclosed. The complexes, covalently attached to an antibody or antibody fragment, can be used for therapeutic and/or diagnostic purposes.

Macrocyclic ligands and complexes

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Lake Jackson, TX, United States of America

Garry E Kiefer