Molecular Insight Pharmaceuticals, Inc.

Biostream, Inc.

Molecular Insight Pharmaceuticlas, Inc.

Kevin P Maresca

John W Babich

Craig N Zimmerman

Genliang Lu

John L Joyal

Shawn Hillier

John Marquis

Jian-cheng Wang

David R Elmaleh

Timothy M Shoup

Chris Barone

James Kronauge

Jian-Cheng Wang

Compounds of Formula (Ia) wherein R is a C-Csubstituted or unsubstituted aryl, a C-Csubstituted or unsubstituted heteroaryl, a C-Csubstituted or unsubstituted alkyl or &#x2014;NR'R&#x2032;,

Heterodimers of glutamic acid

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

A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, 

Process for production of heterodimers of glutamic acid

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

Novel radiopharmaceuticals that are useful in diagnostic imaging and therapeutic treatment of disease characterized by over expression of CA-IX comprise a complex that contains a sulfonamide moiety which is capable of binding the active catalytic site of CA-IX, and a radionuclide adapted for radioimaging and/or radiotherapy: 

Inhibitors of carbonic anhydrase IX

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.

One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Technetium- 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 molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

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Tewksbury, MA, United States of America

Kevin P Maresca