The Dupont Merck Pharmaceutical Company

Bristol-myers Squibb Pharma Company

Other

The Dow Chemical Company

Dupont Pharmaceuticals Company

David Scott Edwards

Shuang Liu

Milind Rajopadhye

Thomas David Harris

Edward H Cheesman

Michael Sworin

Donald A Tomalia

William Jack Kruper, Jr

Ian A Tomlinson

Michael J Fazio

Larry R Wilson

David M Hedstrand

Roberta C Cheng

Donald A Kaplan

Chu W Jung

Christopher E Orvig

Michael J Poirier

Detectably labeled macrophage scavenger receptor antagonists useful for the diagnosis and monitoring of various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque, coronary artery disease, renal disease, thrombosis, transient ischemia due to clotting, stroke, myocardial infarction, organ transplant, organ failure and hypercholesterolemia.

Labeled macrophage scavenger receptor antagonists for imaging atherosclerosis and vulnerable plaque

The present invention provides novel radiopharmaceuticals comprising one to three pentapeptides, X X X X X , independently attached to a metal chelator or bonding moiety, C , to which is attached a Tc-99m, Re-186, or Re-188, optionally further comprising a linking group, L , between-the peptides and the chelator or bonding moiety. The pentapeptide sequence binds to the tuftsin receptor and is attached at the N-terminus to L or C . These radiopharmaceuticals are useful for the diagnosis of infection and inflammation, reagents and kits useful for preparing the radiopharmaceuticals, methods of imaging sites of infection and/or inflammation in a patient, and methods of diagnosing diseases associated with infection or inflammation in patients in need of such diagnosis.

Radiopharmaceuticals for imaging infection and inflammation and for imaging and treatment of cancer

This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.

Stable reagents for the preparation of radio pharmaceuticals

This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure:

Ternary radiopharmaceutical complexes

This invention relates to novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer, and to kits useful for their preparation. The radiopharmaceuticals of this invention are comprised of a transition metal radionuclide, a transition metal chelator, a biologically active group connected to said chelator, a first ancillary ligand, a second ancillary ligand capable of stabilizing the radiopharmaceutical, optionally having a linking group between said chelator and said biologically active group. Preferred radiopharmaceuticals of this invention have the formula:

Stable hydrazones linked to a peptide moiety as reagents for the

Tris(isonitrile) copper(I) sulfate complexes and their use in synthetic methods for making radionuclide isonitrile coordination complexes such as �.sup.99m Tc(1-isocyano-2-methoxy-2-methylpropane).sub.6 !.sup.+. The coordination complexes are useful as radiopharmaceutical imaging agents.

Tris(isonitrile) copper(I) sulfates for preparing radionuclide complexes

Dense star polymer conjugates which are composed of at least one dendrimer in association with at least one unit of a carried agricultural, pharmaceutical, or other material have been prepared. These conjugates have particularly advantageous properties due to the unique characteristics of the dendrimer.

Dense star polymer conjugates

Tris(isonitrile)copper(I) sulfate complexes and their use in synthetic methods for making radionuclide isonitrile coordination complexes such as [.sup.99m Tc(1-isocyano-2-methoxy-2-methylpropane).sub.6 ].sup.+. The coordination complexes are useful as radiopharmaceutical imaging agents.

Tris(isonitrile)copper(i) sulfates for preparing radionuclide complexes

Disclosed are cationic complexes of Tc-99m and ligands having the structure: ##STR1## wherein: R.sup.1 is hydrogen or is selected from the group consisting of C.sub.1 to C.sub.20 alkyl; C.sub.3 to C.sub.12 cycloalkyl; C.sub.7 to C.sub.24 aralkyl; C.sub.2 to C.sub.16 alkyl ethers, thioethers, ketones or esters; C.sub.7 to C.sub.27 aralkyl ethers;

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Burlington, MA, United States of America

David Scott Edwards