Patents by Inventor Martin W. Brechbiel
Martin W. Brechbiel has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 10858306Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.Type: GrantFiled: April 9, 2020Date of Patent: December 8, 2020Assignees: INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE NANTES, UNIVERSITE D'ANGERS, THE GOVERNMENT OF THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: François Guerard, Jean-François Gestin, Martin W. Brechbiel, Yong-Sok Lee
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Publication number: 20200239404Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.Type: ApplicationFiled: April 9, 2020Publication date: July 30, 2020Inventors: François GUERARD, Jean-François GESTIN, Martin W. BRECHBIEL, Yong-Sok LEE
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Patent number: 10703708Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.Type: GrantFiled: November 24, 2016Date of Patent: July 7, 2020Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE NANTES, UNIVERSITE D'ANGERS, THE GOVERNMENT OF THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: François Guerard, Jean-François Gestin, Martin W. Brechbiel, Yong-Sok Lee
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Publication number: 20190023646Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.Type: ApplicationFiled: November 24, 2016Publication date: January 24, 2019Inventors: François GUERARD, Jean-François GESTIN, Martin W. BRECHBIEL, Yong-Sok LEE
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Patent number: 10137212Abstract: Disclosed is a compound of formula (I) or (II) in which R1-R4, R1?-R5?, Z1+-Z4, and Z1?-Z4? are as described herein. Also disclosed are a 89Zr- or 90Nb-containing complex of a compound of formula (I) or (II) and a method for obtaining a diagnostic image, such as a positron emission tomography (PET) image.Type: GrantFiled: March 12, 2014Date of Patent: November 27, 2018Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Martin W. Brechbiel, Francois Guerard, Yong-Sok Lee
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Publication number: 20160022844Abstract: Disclosed is a compound of formula (I) or (II) in which R1-R4, R1?-R5?, Z1+-Z4, and Z1?-Z4? are as described herein. Also disclosed are a 89Zr- or 90Nb-containing complex of a compound of formula (I) or (II) and a method for obtaining a diagnostic image, such as a positron emission tomography (PET) image.Type: ApplicationFiled: March 12, 2014Publication date: January 28, 2016Applicant: The USA, as represented by the secretary, Department of Health & Human ServiceInventors: Martin W. Brechbiel, Francois Guerard, Yong-Sok Lee
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Patent number: 8535639Abstract: The present invention relates to trifunctional imaging agents that include an antibody for cell targeting, as well as a chelating moiety for sequestering radioisotopes and a fluorescing moiety for imaging. The invention also provides methods using the conjugates for medical diagnostic imaging.Type: GrantFiled: July 16, 2008Date of Patent: September 17, 2013Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu, Kwamena Baidoo
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Patent number: 8288530Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.Type: GrantFiled: November 6, 2007Date of Patent: October 16, 2012Assignee: The United States of America, as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Publication number: 20110014120Abstract: The present invention relates to trifunctional imaging agents that include an antibody for cell targeting, as well as a chelating moiety for sequestering radioisotopes and a fluorescing moiety for imaging. The invention also provides methods using the conjugates for medical diagnostic imaging.Type: ApplicationFiled: July 16, 2008Publication date: January 20, 2011Inventors: Martin W. Brechbiel, Heng Xu, Kwamena Baidoo
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Publication number: 20100092384Abstract: Provided is a multifunctional particle comprising: (a) an inner metallic core, (b) a biocompatible shell comprising an optical contrast agent embedded therein, and (c) a targeting biomolecule conjugated to the biocompatible shell through a multidentate ligand, wherein the multidentate ligand is chelated to an imaging agent. Also provided are compositions comprising the multifunctional particle and methods of using the multifunctional particle, including a method of diagnostic imaging and a method of treatment.Type: ApplicationFiled: March 17, 2008Publication date: April 15, 2010Applicants: The jUnited States of America as represented by Secretary, Dept. of Health and Human Service, University of OxfordInventors: Ambika Bumb, Martin W. Brechbiel, Peter Choyke, Lars Fugger, Peter James Dobson
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Publication number: 20100056776Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.Type: ApplicationFiled: November 6, 2007Publication date: March 4, 2010Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Patent number: 7371225Abstract: A method for monitoring and controlling convection enhanced delivery of a therapeutic agent to a target tissue is disclosed. A tracer that is detectable, for example, by magnetic resonance imaging (MRI) and/or by X-ray computed tomography (CT) is co-infused with the therapeutic agent and used to monitor the distribution of the therapeutic agent as it moves through the target tissue. The images obtained during delivery are used to confirm delivery of the therapeutic agent to the target tissue and to avoid exposure of tissue outside of the targeted area to the therapeutic agent. In addition, the signal intensity of the images may be used to confirm that the therapeutic agent has been delivered to the target tissue at a desired concentration.Type: GrantFiled: September 24, 2003Date of Patent: May 13, 2008Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Edward H. Oldfield, Russel R. Lonser, Kayhan Garmestani, Martin W. Brechbiel
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Patent number: 7368100Abstract: Backbone-substituted 1,4,7,10-tetraaza cyclododecane-N,N?,N?,N??-tetraacetic acid compounds, metal complexes thereof, compositions thereof, conjugates thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.Type: GrantFiled: September 5, 2003Date of Patent: May 6, 2008Assignee: The United States of America, represented by the Secretary, Department of Health and Human ServicesInventors: Martin W. Brechbiel, Hyun-Soon Chong
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Patent number: 7163935Abstract: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid compounds with a pendant donor amino group, metal complexes thereof, compositions thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.Type: GrantFiled: June 3, 2003Date of Patent: January 16, 2007Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Hyun-Soon Chong
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Patent number: 7081452Abstract: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid compounds with a pendant donor amino group, metal complexes thereof, compositions thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.Type: GrantFiled: December 13, 2002Date of Patent: July 25, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Hyun-Soon Chong
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Patent number: 6995247Abstract: The present invention provides an ?-particle-emitting radioisotope chelation complex comprising 225Actinium (225Ac) and 1,4,7,10,13,16-hexaazacyclohexadecane-N,N?,N?,N?,N?,N?-hexaacetic acid (HEHA) (225Ac-HEHA). Also provided is a bifunctional HEHA, and a bifunctional 225Ac-HEHA. The bifunctional HEHA and the bifunctional 225Ac-HEHA can be conjugated to a targeting agent. In view of the above, the present invention provides a method of making HEHA and methods of making a bifunctional HEHA, including a conjugate thereof. Also provided are a method of treating disease, a method of treating cancer, a method of decontaminating a sample from 225Ac, a method of decontaminating a person who has been externally contaminated with 225Ac, and a method of detoxifying a person who has internalized 225Ac.Type: GrantFiled: January 28, 2004Date of Patent: February 7, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Kim Deal
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Patent number: 6852842Abstract: Small dendrimer-based MRI contrast agents are disclosed to accumulate in renal tubules. The accumulation enables visualization of renal structure and function, permitting assessment of structural and functional damage to the kidneys. In a disclosed embodiment, six, small dendrimer-based MRI contrast agents were synthesized, and their pharmacokinetics, whole body retention, and renal MRI images were evaluated in mice. Surprisingly, despite having unequal renal clearance properties, all of the dendrimer agents clearly visualized the renal anatomy and proximal straight tubules of the mice better than Gd-[DTPA]-dimeglumine. Dendrimer conjugate contrast agents prepared from PAMAM-G2D, DAB-G3D, and DAB-G2D dendrimers were excreted rapidly and may be acceptable for use in clinical applications.Type: GrantFiled: August 26, 2002Date of Patent: February 8, 2005Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Robert A. Star, Hisataka Kobayashi
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Publication number: 20040184991Abstract: The present invention provides an &agr;-particle-emitting radioisotope chelation complex comprising 225Actinium (225Ac) and 1,4,7,10,13,16-hexaazacyclohexadecane-N,N′,N′,N′,N′,N′-hexaacetic acid (HEHA) (225Ac-HEHA). Also provided is a bifunctional HEHA, and a bifunctional 225Ac-HEHA. The bifunctional HEHA and the bifunctional 225Ac-HEHA can be conjugated to a targeting agent. In view of the above, the present invention provides a method of making HEHA and methods of making a bifunctional HEHA, including a conjugate thereof Also provided are a method of treating disease, a method of treating cancer, a method of decontaminating a sample from 225Ac, a method of decontaminating a person who has been externally contaminated with 225Ac, and a method of detoxifying a person who has internalized 225Ac.Type: ApplicationFiled: January 28, 2004Publication date: September 23, 2004Applicant: The Government of the USA, as Represented by the Secretary, Dpt. of Health and Human ServicesInventors: Martin W. Brechbiel, Kim Deal
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Publication number: 20040037777Abstract: Small dendrimer-based MRI contrast agents are disclosed to accumulate in renal tubules. The accumulation enables visualization of renal structure and function, permitting assessment of structural and functional damage to the kidneys. In a disclosed embodiment, six, small dendrimer-based MRI contrast agents were synthesized, and their pharmacokinetics, whole body retention, and renal MRI images were evaluated in mice. Surprisingly, despite having unequal renal clearance properties, all of the dendrimer agents clearly visualized the renal anatomy and proximal straight tubules of the mice better than Gd-[DTPA]-dimeglumine. Dendrimer conjugate contrast agents prepared from PAMAM-G2D, DAB-G3D, and DAB-G2D dendrimers were excreted rapidly and may be acceptable for use in clinical applications.Type: ApplicationFiled: August 26, 2002Publication date: February 26, 2004Inventors: Martin W. Brechbiel, Robert A. Star, Hisataka Kobayashi
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Patent number: 6696551Abstract: The present invention provides an &agr;-particle-emitting radioisotope chelation complex comprising 225Actinium (225Ac) and 1,4,7,10,13,16-hexaazacyclohexadecane-N,N′,N″,N′″,N″″,N′″″-hexaacetic acid (HEHA) (225Ac-HEHA). Also provided is a bifunctional HEHA, and a bifunctional 225Ac-HEHA. The bifunctional HEHA and the bifunctional 225Ac-HEHA can be conjugated to a targeting agent. In view of the above, the present invention provides a method of making HEHA and methods of making a bifunctional HEHA, including a conjugate thereof. Also provided are a method of treating disease, a method of treating cancer, a method of decontaminating a sample from 225Ac, a method of decontaminating a person who has been externally contaminated with 225Ac, and a method of detoxifying a person who has internalized 225Ac.Type: GrantFiled: December 20, 2001Date of Patent: February 24, 2004Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Kim Deal