Molecular Insight Pharmaceuticals, Inc.

Shawn Hillier

John W Babich

John L Joyal

Craig N Zimmerman

Genliang Lu

Kevin P Maresca

John Marquis

Jian-cheng Wang

John Joyal

Jian-Cheng Wang

Craig Zimmerman

A method of reducing radiation exposure of a non-cancerous tissue of a patient diagnosed with a cancer includes administering to the patient an agent capable of competing for binding sites on a surface of the non-cancerous tissue, provided that the administration is carried out after a waiting period that follows administration of a compound including a radionuclide to the patient, the compound having affinity for both a cancerous tissue and the non-cancerous tissue, and, further provided that the binding sites have an affinity for both the agent and the compound.

Organ protection in PSMA-targeted radionuclide therapy of prostate cancer

A method of imaging a region in a subject includes administering to the subject a complex of a metal chelated to a compound, and obtaining an image of the region in the subject.

Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof

A ligand, a pharmaceutically acceptable salt, tautomer, or ester thereof, may be represented as: In the formula, X is selected from the group consisting of &#x2014;(CH)&#x2014;, &#x2014;(CH)&#x2014;O&#x2014;, &#x2014;(CH)&#x2014;N(R)&#x2014;, &#x2014;(CH)&#x2014;N(R)&#x2014;C(O)&#x2014; and &#x2014;O&#x2014;; Ris hydrogen or (C-C)alkyl; G is &#x2014;(CH(R))&#x2014;R&#x2014;, or &#x2014;(CH)&#x2014;C(O)&#x2014;R; G' is &#x2014;(CH(R))&#x2014;R&#x2014;, or &#x2014;(CH)&#x2014;C(O)&#x2014;R; Ris &#x2014;H, &#x2014;OH, NRR, or &#x2014;COH; Ris &#x2014;H, &#x2014;COOH, or substituted or unsubstituted &#x2014;COO(C-C)alkyl; Rand Rare each independently H, substituted or unsubstituted (C-C)alkyl, or substituted or unsubstituted carboxy(C-C)alkylene; m is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; and p is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

Metal complexes of poly(carboxyl)amine-containing ligands having an affinity for carbonic anhydrase IX

The present invention is directed to CA IX inhibitors that conform to Formula I where the substituents X, A, B, D, E, E' and G are as defined above.  Also described are Pt,Cu,Re,Re andTc metal complexes of Formula I compounds which find use as candidate agents for imaging tumors.

Technetium&#x2014;and rhenium-bis(heteroaryl) complexes and methods of use thereof

Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecu le, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV. 

CA-IX specific radiopharmaceuticals for the treatment and imaging of cancer

A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.

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Danvers, MA, United States of America

Shawn Hillier