Patents Assigned to MOLECULAR INSIGHTS PHARMACEUTICALS, INC.
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Patent number: 9687572Abstract: 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.Type: GrantFiled: December 6, 2011Date of Patent: June 27, 2017Assignee: MOLECULAR INSIGHT PHARMACEUTICALS, INC.Inventors: John W. Babich, John L. Joyal, Craig Zimmerman
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Publication number: 20170044098Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2(CH2)p Y is C(O), O, NR?S, S(O)2, C(O)2(CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: ApplicationFiled: October 28, 2016Publication date: February 16, 2017Applicant: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20160346410Abstract: 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.Type: ApplicationFiled: August 10, 2016Publication date: December 1, 2016Applicant: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. BABICH, Craig ZIMMERMAN, John L. JOYAL, Genliang LU
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Patent number: 9447121Abstract: 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.Type: GrantFiled: January 10, 2014Date of Patent: September 20, 2016Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John L. Joyal, Genliang Lu
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Patent number: 9433594Abstract: 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.Type: GrantFiled: January 30, 2015Date of Patent: September 6, 2016Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Patent number: 9422251Abstract: 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 —(CH2)n—, —(CH2)n—O—, —(CH2)n—N(Rg)—, —(CH2)n—N(Rg)—C(O)— and —O—; Rg is hydrogen or (C1-C6)alkyl; G is —(CH(Rm))n—Rh—, or —(CH2)p—C(O)—Rh; G? is —(CH(Rm))n—Rh—, or —(CH2)p—C(O)—Rh; Rh is —H, —OH, NRaRb, or —CO2H; Rm is —H, —COOH, or substituted or unsubstituted —COO(C1-C6)alkyl; Ra and Rb are each independently H, substituted or unsubstituted (C1-C8)alkyl, or substituted or unsubstituted carboxy(C1-C8)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.Type: GrantFiled: August 7, 2015Date of Patent: August 23, 2016Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John L. Joyal, Genliang Lu, Shawn Hillier, Kevin P. Maresca, John Marquis
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Publication number: 20160222036Abstract: 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.Type: ApplicationFiled: January 30, 2015Publication date: August 4, 2016Applicant: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. BABICH, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Patent number: 9388144Abstract: 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.Type: GrantFiled: November 25, 2014Date of Patent: July 12, 2016Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John L. Joyal, Genliang Lu
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Publication number: 20160115267Abstract: The present disclosure provides purified forms of iobenguane and preparations of a precursor to iobenguane, such as a polymer, the polymer comprising a monomer of formula (I) or a pharmaceutically acceptable salt thereof, the preparation comprising leachable tin at a level of 0 ppm to 850 ppm.Type: ApplicationFiled: October 23, 2015Publication date: April 28, 2016Applicant: MOLECULAR INSIGHT PHARMACEUTICALS INC.Inventors: Jason Moss, Machinani Rao
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Patent number: 9309193Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: GrantFiled: October 12, 2011Date of Patent: April 12, 2016Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20160067361Abstract: 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.Type: ApplicationFiled: September 4, 2015Publication date: March 10, 2016Applicant: MOLECULAR INSIGHT PHARMACEUTICALS, INC.Inventors: John W. BABICH, Shawn HILLIER, John JOYAL
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Patent number: 9149547Abstract: 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, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; R? is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.Type: GrantFiled: May 9, 2013Date of Patent: October 6, 2015Assignee: MOLECULAR INSIGHT PHARMACEUTICALS, INC.Inventors: John W. Babich, Craig Zimmerman, Kevin P. Maresca
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Publication number: 20150110716Abstract: A method of evaluating a subject suspected of harboring a prostrate tumor includes administering to the subject an effective amount of a gamma-emitting transition metal complex conjugated to a targeting moiety that selectively binds to prostate-specific membrane antigen (PSMA), including PSMA expressed on the surface of a prostate tumor; subjecting the subject to a nuclear medicine tomographic imaging technique to obtain one or more images of at least a portion of prostate tissue that comprises tumor lesions; assessing a level of uptake of said gamma-emitting transition metal complex conjugated to a targeting moiety by said at least a portion of prostate tissue compared to a level of uptake by control tissue; and determining if a ratio of the level of uptake by said at least a portion of prostate tissue compared the level of uptake by control tissue is at or above a predetermined threshold.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: Molecular Insight Pharmaceuticals, Inc.Inventor: Thomas ARMOR
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Patent number: 8962799Abstract: 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.Type: GrantFiled: July 29, 2014Date of Patent: February 24, 2015Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Publication number: 20140341805Abstract: 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.Type: ApplicationFiled: July 29, 2014Publication date: November 20, 2014Applicant: MOLECULAR INSIGHT PHARMACEUTICALS, INC.Inventors: John W. BABICH, Craig ZIMMERMAN, John JOYAL, Kevin P. MARESCA, John MARQUIS, Genliang LU, Jian-cheng WANG, Shawn HILLIER
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Patent number: 8877970Abstract: 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:Type: GrantFiled: January 8, 2009Date of Patent: November 4, 2014Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: Craig Zimmerman, John W. Babich, John Joyal, Genliang Lu, Kevin P. Maresca, Chris Barone
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Patent number: 8840865Abstract: 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.Type: GrantFiled: September 30, 2013Date of Patent: September 23, 2014Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Publication number: 20140255306Abstract: 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.Type: ApplicationFiled: January 10, 2014Publication date: September 11, 2014Applicant: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. BABICH, Craig ZIMMERMAN, John L. JOYAL, Genliang LU
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Publication number: 20140179902Abstract: 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.Type: ApplicationFiled: September 30, 2013Publication date: June 26, 2014Applicant: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. BABICH, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Patent number: 8685369Abstract: 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.Type: GrantFiled: February 14, 2005Date of Patent: April 1, 2014Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John Babich, Kevin Maresca, James Kronauge