Molecular Insight Pharmaceuticals, Inc.

John L Joyal

John W Babich

Craig N Zimmerman

Genliang Lu

Shawn Hillier

Kevin P Maresca

John Marquis

Jian-cheng Wang

Chris Barone

Jian-Cheng Wang

Craig Zimmerman

Metal complexes including a radionuclide and a compound of Formula I and Formula II are potent inhibitors of PSMA.

Triazine based radiopharmaceuticals and radioimaging agents

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

Metal complexes including a radionuclide and a compound of Formula I and Formula II are potent inhibitors of PSMA. 

Compounds according to Formula I and Formula II are potent inhibitors of PSMA.  Pharmaceutical compositions may include a complex of a radionuclide and a Formula I compound or a Formula II compound. Methods include using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

A dendrimer conjugate according to Formula (I), or its pharmaceutically acceptable salt, or solvate thereof: and complexes of Formula I conjugates with metals radionuclides of elements such as rhenium, technetium, yttrium, lutetium and others to provide a complex for imaging tissues or for the radiotherapeutic treatment of cancer tissue. 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. 

PSMA-targeted dendrimers

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

Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity:  Pharmaceutical compositions may include a complex of a radionuclide and a compound of Formula I or Formula II.

Radiolabeled prostate specific membrane antigen inhibitors

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

Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: The invention also provides pharmaceutical compositions of a complex of a radionuclide and a Formula I compound or a Formula II compound and methods of using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

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Melrose, MA, United States of America

John L Joyal