Fluorine Patents (Class 424/1.89)
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Patent number: 10004818Abstract: Methods and compositions utilizing ether and alkyl phospholipid ether analog compounds for treating cancer and imaging, monitoring, and detecting cancer stem cells in humans.Type: GrantFiled: April 15, 2016Date of Patent: June 26, 2018Assignee: CELLECTAR, Inc.Inventors: Jamey P. Weichert, Anatoly Pinchuk, Irawati Kandela, Marc Longino, William R. Clarke
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Patent number: 9999689Abstract: The present disclosure provides compositions and methods based on peptide-detectable agent conjugates that are useful for imaging beta cell mass.Type: GrantFiled: March 21, 2016Date of Patent: June 19, 2018Assignee: The General Hospital CorporationInventors: Ralph Weissleder, Thomas Reiner, Edmund J. Keliher
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Patent number: 9999692Abstract: The present invention relates to a novel composition comprising 1-amino-3-[18F]-fluorocyclobutanecarboxylic acid ([18F]-FACBC) wherein said composition has certain superior properties in comparison with known compositions comprising [18F]-FACBC. Also provided by the invention is a method to obtain said composition.Type: GrantFiled: March 28, 2014Date of Patent: June 19, 2018Assignee: GE Healthcare LimitedInventor: Torild Wickstrom
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Patent number: 9987380Abstract: A composition useful as a PET and/or fluorescence imaging probe a compound a compound of Formula I, including salts, hydrates and solvates thereof: wherein R1-R7 may be independently selected from hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, X is selected from the group consisting of C and N; and A is selected of hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, alkyl, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, including phenyl and aminophenyl, and heteroaryl.Type: GrantFiled: July 13, 2012Date of Patent: June 5, 2018Assignee: University of Southern CaliforniaInventors: Zibo Li, Francois P. Gabbai, Peter S. Conti, Todd W. Hudnall, Tzu-Pin Lin, Shuanglong Liu, Chiun-Wei Huang
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Patent number: 9951011Abstract: The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.Type: GrantFiled: September 19, 2014Date of Patent: April 24, 2018Assignee: GE HEALTHCARE LIMITEDInventors: William John Trigg, Paul Alexander Jones
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Patent number: 9856182Abstract: A method of conducting radiofluorination of a substrate, includes: (a) contacting an aqueous solution of [18F] fluoride with a polymer supported phosphazene base for sufficient time for trapping of [18F] fluoride on the polymer supported phosphazene base; and (b) contacting a solution of the substrate with the polymer supported phosphazene base having [18F] fluoride trapped thereon obtained in step (a) for sufficient time for a radiofluorination reaction to take place.Type: GrantFiled: July 30, 2013Date of Patent: January 2, 2018Assignee: TECHNICAL UNIVERSITY OF DENMARKInventors: Fedor Zhuravlev, Bente Mathiessen
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Patent number: 9833520Abstract: Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin ?v?3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin ?v?3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.Type: GrantFiled: July 26, 2013Date of Patent: December 5, 2017Assignee: The Methodist Hospital Research InstituteInventors: King Chuen Li, Zheng Li, Feng Li
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Patent number: 9789207Abstract: A PET imaging agent is made, by at first, washing out fluoride ions (F-18) adhered on an ion exchange resin to a reaction vessel with potassium carbonate/Kryptofix 2.2.2 in acetonitrile-water. After processing the first azeotropic distillation with helium while water is removed, the temperature is cooled down. Then, acetonitrile is added to the reaction vessel to be heated up. After processing the second azeotropic distillation with helium while water is removed, the temperature is cooled down and excess water is extracted. A precursor is then added to the reaction vessel to be heated up for processing a fluorination reaction. The reaction mixture obtained after the fluorination reaction is cooled down to be flown through a solid-phase extraction column with waste drained into a waste tank. Then, ethanol is used to wash out a product, i.e. [F-18]FEONM, adsorbed by the column, to be collected in a collection vial.Type: GrantFiled: June 16, 2016Date of Patent: October 17, 2017Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, Executive Yuan, R.O.C.Inventors: Li-Yuan Huang, Yean-Hung Tu, Jenn-Tzong Chen, Chyng-Yann Shiue
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Patent number: 9682159Abstract: The present invention relates to the use of a combination of several contrast agents having different properties with respect to imaging representation.Type: GrantFiled: September 21, 2015Date of Patent: June 20, 2017Assignee: nanoPET Pharma GmbHInventor: Ulrike Wiebelitz
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Patent number: 9592309Abstract: The invention disclosed herein discloses selected ribose isomers that are useful as PET probes (e.g. [18F]-2-fluoro-2-deoxy-arabinose). These PET probes are useful, for example, in methods designed to monitor physiological processes including ribose metabolism and/or to selectively observe certain tissue/organs in vivo. The invention disclosed herein further provides methods for making and using such probes.Type: GrantFiled: May 9, 2013Date of Patent: March 14, 2017Assignee: The Regents of the University of CaliforniaInventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
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Patent number: 9556114Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: GrantFiled: December 10, 2014Date of Patent: January 31, 2017Assignee: SciFluor Life Sciences, Inc.Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
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Patent number: 9517279Abstract: The invention features 2-alkoxy-11-hydroxyaporphine derivatives that selectively bind D2high receptors. The compounds are useful for imaging D2high receptors and for the treatment of diseases, such as Parkinson's disease, sexual dysfunction, and depressive disorders.Type: GrantFiled: April 14, 2011Date of Patent: December 13, 2016Assignee: The McLean Hospital CorporationInventors: John L. Neumeyer, Yu-Gui Si, Anna W. Sromek
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Patent number: 9481685Abstract: The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.Type: GrantFiled: October 2, 2009Date of Patent: November 1, 2016Assignee: GE Healthcare LimitedInventors: Harry John Wadsworth, Bo Shan, Dennis O'Shea, Joanna Marie Passmore, William John Trigg
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Patent number: 9468692Abstract: Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.Type: GrantFiled: January 23, 2014Date of Patent: October 18, 2016Assignee: General Electric CompanyInventors: Bruce Allan Hay, Jack Mathew Webster
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Patent number: 9346771Abstract: A diagnostic imaging agent useful for positron emission tomography (PET) imaging as well as to improved hardware for producing such imaging agents is described. Flutemetamol (18F) Injection for the imaging of ?-amyloid plaques in the brain and methods and devices for preparing same are described including the automated synthesis and purification of [18F]flutemetamol by means of solid phase extraction (SPE).Type: GrantFiled: February 11, 2015Date of Patent: May 24, 2016Assignee: GE HEALTHCARE LIMITEDInventors: Eric Horn, Steven Fairway, Dimitrios Mantzilas, Nigel Powell
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Patent number: 9308284Abstract: The invention is directed to formulations of lipophilic Amyloid beta ligand stilbene and more particularly to formulations which are capable to be administered parenterally e.g. intravenously, wherein the lipophilic Amyloid beta ligand stilbene is a fluorinated stilbene. Further, the invention is directed to a method for sterile filtration of formulations suitable for PET imaging of mammals pursuant to the invention.Type: GrantFiled: June 21, 2012Date of Patent: April 12, 2016Assignee: PIRAMAL IMAGING SAInventors: Carsten Olbrich, Michael Krause, Andreas Burkhard, Annett Richter, Rainer Braun
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Patent number: 9295738Abstract: Compounds and a method for imaging myocardial perfusion, including administering to a patient a compound linked to an imaging moiety, wherein the compound binds MC-1, and scanning the patient using diagnostic imaging. Kits including the compound or precursor compounds linked or not linked to an imaging moiety are also described.Type: GrantFiled: December 18, 2012Date of Patent: March 29, 2016Assignee: RESPIRATORIUS ABInventor: Martin Johansson
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Patent number: 9227943Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.Type: GrantFiled: January 7, 2015Date of Patent: January 5, 2016Assignee: University of Georgia Research Foundation, Inc.Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
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Patent number: 9211350Abstract: A compound represented by the following formula (1), or a salt thereof: wherein R1 is a radioactive halogen substituent, 0 to 2 of A1, A2, A3 and A4 represent N, and the rest represent —(CH)— is effective as a diagnostic imaging probe targeting amyloid. A diagnostic agent for Alzheimer's disease contains a compound represented by the above formula (1) or a salt thereof. After administration to a patient, the compound and the diagnostic agent for Alzheimer's disease transfer into the patient's brain, and indicate good accumulation on amyloid deposited in the brain.Type: GrantFiled: May 29, 2012Date of Patent: December 15, 2015Assignee: NIHON MEDI-PHYSICS CO., LTD.Inventors: Yuki Okumura, Yoshifumi Maya, Yoshinari Shoyama, Takako Onishi
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Patent number: 9179882Abstract: The present invention relates to the use of a combination of several contrast agents having different properties with respect to imaging representation.Type: GrantFiled: April 11, 2013Date of Patent: November 10, 2015Assignee: MIVENION GMBHInventor: Ulrike Wiebelitz
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Patent number: 9180209Abstract: Methods and materials for the imaging of cells and tissues containing active proteases such as cathepsin are disclosed. The present materials include activity based probes that bind to an enzyme and are subsequently cleaved. Cleavage results in covalent attachment of a fluorescent signal to a target protease due to removal of a quenching group which, when present on the probe causes altered or no fluorescence. The probes are non-peptidic, small molecule scaffolds linked to a reactive acyloxymethyl ketone group, a fluorophore and a quencher. The probes are cell permeable and may use, for example, a QSY21 (CAS 304014-13-9) quencher and a cyanine dye. The probes form covalent bonds with the active site of cysteine cathepsins, proteases that are upregulated at the tumor boundaries with normal tissue and at sites of inflammation.Type: GrantFiled: February 24, 2012Date of Patent: November 10, 2015Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Matthew S. Bogyo, Laura E. Edgington, Martijn Verdoes
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Patent number: 9134328Abstract: This invention provides benzothiazole derivative compounds, compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for detecting amyloid deposit(s) and for diagnosing a disease, disorder or condition characterized by amyloid deposit(s).Type: GrantFiled: April 7, 2014Date of Patent: September 15, 2015Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
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Patent number: 9125937Abstract: The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4)alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or a group of formula (?): —Y—Z—W—R11??(?) wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a —N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.Type: GrantFiled: September 19, 2013Date of Patent: September 8, 2015Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, UNIVERSITE D'AUVERGNE CLERMONT 1, LABORATORIES CYCLOPHARMAInventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
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Patent number: 9115172Abstract: The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.Type: GrantFiled: October 8, 2014Date of Patent: August 25, 2015Assignee: Immunomedics, Inc.Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
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Patent number: 9095631Abstract: The invention relates to a new class of compounds with high affinity and selectivity towards P-glycoprotein. The invention also relates to the utilization of such compounds in the in vivo diagnosis of neurodegenerative diseases and as medicaments for use in the prevention and treatment of neurodegenerative disease involving P-glycoprotein.Type: GrantFiled: May 24, 2011Date of Patent: August 4, 2015Assignee: UNIVERSITA DEGLI STUDI DI BARI “ALDO MORO”Inventors: Nicola Antonio Colabufo, Francesco Berardi, Mariangela Cantore, Marialessandra Contino, Marcello Leopoldo, Roberto Perrone
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Patent number: 9073802Abstract: The present invention aims at solving the problems of conventional methods for producing an 18F-labeled compound, that is, the problem of purification of a compound in a liquid phase synthesis method and the problem of an insufficient yield due to the reduction of reactivity in a solid phase synthesis method. There is provided a method for producing an 18F-labeled compound including: allowing a high molecular compound containing a residue of a precursor compound to be labeled and a residue of a phase transfer catalyst in the molecule thereof to react with 18F?; and removing the 18F-labeled compound from the high molecular compound.Type: GrantFiled: February 8, 2011Date of Patent: July 7, 2015Assignees: TOKYO INSTITUTE OF TECHNOLOGY, NIIGATA UNIVERSITYInventors: Takashi Takahashi, Hiroshi Tanaka, Tsutomu Nakada
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Patent number: 9072775Abstract: The invention relates to a fluorescent emulsion, to a diagnostic reagent containing the same, and to the use thereof in the preparation of a diagnostic reagent for in vivo fluorescence imaging.Type: GrantFiled: February 14, 2008Date of Patent: July 7, 2015Inventors: Mathieu Goutayer, Isabelle Texier-Nogues, Jacques Fattaccioli, Jérôme Bibette, Anabela Da Silva
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Patent number: 9061080Abstract: Imaging agents comprising an isolated polypeptide conjugated with a radionucleide and a chelator; wherein the isolated polypeptide binds specifically to HER2, or a variant thereof; and methods for preparing and using these imaging agents.Type: GrantFiled: December 19, 2011Date of Patent: June 23, 2015Assignee: GE HEALTHCARE LIMITEDInventors: Duncan Hiscock, Bard Indrevoll, Peter Iveson, Matthias Eberhard Glaser, Rajiv Bhalla, Anthony Wilson
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Publication number: 20150147273Abstract: A method for determining whether compound 0118 is a candidate treatment for a patient includes processing, via a processor, image data of tissue of interest of a patient including a cancer to determine whether a radiolabeled analog of compound 0118 is present in the tissue of interest represented in the image data and generating a signal indicating that compound 0118 is a candidate treatment for the patient in response to the determining that the radiolabeled analog of compound 0118 is present in a predetermined amount in the tissue of interest represented in the image data, wherein the presence of the radiolabeled analog of compound 0118 in the tissue of interest indicates presence of a sub-type of cancer having a galectin-1 molecular target, which is a sub-type of treatable by compound 0118.Type: ApplicationFiled: June 10, 2013Publication date: May 28, 2015Applicant: Koninklijke Philips N.V.Inventors: Tilman Lappchen, Holger Gruell, Marc Stefan Robillard, Johan Lub
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Patent number: 9040021Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.Type: GrantFiled: November 7, 2011Date of Patent: May 26, 2015Assignee: GE Healthcare LimitedInventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
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Publication number: 20150139903Abstract: Tracers targeting phosphodiesterase1 for use in gamma radiation detection-based diagnostic techniques, particularly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.Type: ApplicationFiled: September 22, 2014Publication date: May 21, 2015Inventors: Peng LI, Lawrence WENNOGLE, Jun ZHAO, Hailin ZHENG
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Publication number: 20150132223Abstract: One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammnonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.Type: ApplicationFiled: November 25, 2014Publication date: May 14, 2015Inventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
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Publication number: 20150133777Abstract: The invention disclosed herein discloses selected ribose isomers that are useful as PET probes (e.g. [18F]-2-fluoro-2-deoxy-arabinose). These PET probes are useful, for example, in methods designed to monitor physiological processes including ribose metabolism and/or to selectively observe certain tissue/organs in vivo. The invention disclosed herein further provides methods for making and using such probes.Type: ApplicationFiled: May 9, 2013Publication date: May 14, 2015Inventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
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Patent number: 9028800Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.Type: GrantFiled: May 8, 2014Date of Patent: May 12, 2015Assignee: Immunomedics, Inc.Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
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Publication number: 20150125390Abstract: The present invention is directed towards new 18F-folate/antifolate analogue radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.Type: ApplicationFiled: May 8, 2013Publication date: May 7, 2015Applicant: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
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Patent number: 9023316Abstract: A method for synthesizing an 18F-labeled probe. The method includes a step of eluting an amount of 18F with a first solvent which includes a predetermined amount of water and at least one organic solvent. In this step, the 18F elutes as an 18F solution. The method also includes a step of using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe. In the method, there is no step of drying the 18F starting from a time when the eluting step is performed and ending at a time when the 18F-labeling step is performed.Type: GrantFiled: April 8, 2011Date of Patent: May 5, 2015Assignee: Siemens Medical Solutions USA, Inc.Inventors: Umesh Gangadharmath, Joseph Walsh, Hartmuth Kolb
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Patent number: 9023318Abstract: Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.Type: GrantFiled: March 25, 2013Date of Patent: May 5, 2015Assignee: Siemens Medical Solutions USA, Inc.Inventors: Gang Chen, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Harmuth C. Kolb, Changhui Liu, Anjana Sinha, Anna Katrin Szardenings, Joseph C. Walsh, Eric Wang, Chul Yu, Wei Zhang, Klaus Kopka, Guenter Haufe, Michael Schaefers, Verena Hugenberg, Stefan Wagner, Sven Hermann, Hans-Joerg Breyholz, Andreas Faust
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Patent number: 9023317Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.Type: GrantFiled: February 25, 2013Date of Patent: May 5, 2015Assignee: University of Western OntarioInventors: Duncan H. Hunter, Mustafa Janabi
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Patent number: 9005578Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: GrantFiled: May 28, 2013Date of Patent: April 14, 2015Assignees: Fluoropharma, Inc., The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Patent number: 9005577Abstract: The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).Type: GrantFiled: April 30, 2009Date of Patent: April 14, 2015Assignee: Siemens Medical Solutions USA, Inc.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Kai Chen, Umesh B. Gangadharmath, Gang Chen, Vani P. Mocharla, Dhanalakshmi Kasi, Peter J. H. Scott, Qianwa Liang
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Publication number: 20150098902Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: ApplicationFiled: December 10, 2014Publication date: April 9, 2015Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
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Publication number: 20150098903Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Patent number: 8986652Abstract: The present invention provides a method of preparing [123I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/?mol and radiochemical purity of 95%. The present invention further provides a method of applying [123I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.Type: GrantFiled: February 1, 2013Date of Patent: March 24, 2015Assignee: National Tsing Hua UniversityInventors: Chung-Shan Yu, Ho-Lien Huang, Chun-Nan Yeh, Wei-Yuan Lee, Kang-Wei Chang, Ying-Cheng Huang, Kun-Ju Lin, Ching-Shiuann Yang, Shu-Fan Tien, Wen-Chin Su, Jenn-Tzong Chen, Wuu-Jyh Lin, Shiou-Shiow Farn
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Patent number: 8986654Abstract: The present invention relates to certain labelled or un-labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives and their medical use. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).Type: GrantFiled: April 3, 2012Date of Patent: March 24, 2015Assignee: DanPET ABInventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen
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Publication number: 20150079001Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.Type: ApplicationFiled: May 22, 2014Publication date: March 19, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: MARTIN GILBERT POMPER, JIAZHONG ZHANG, ALAN P. KOZIKOWSKI, JOHN L. MUSACHIO
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Patent number: 8980221Abstract: The invention relates to methods for processing [18F]-fluoride target water using a solid-support bound Cryptand of formula (I) and to apparatus for performing such methods. The resultant [18F]-fluoride is useful for preparation of radiopharmaceuticals by nucleophilic fluorination, specifically for use in Positron Emission Tomography (PET).Type: GrantFiled: December 22, 2008Date of Patent: March 17, 2015Assignee: GE Healthcare LimitedInventors: Alexander Jackson, Rajiv Bhalla
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Publication number: 20150064111Abstract: The invention relates to compounds and use thereof in the diagnosis and/or in treatment of medical disorders. In some embodiments, the compounds may be used for detecting a cancer. The compound may include a di-acid moiety. In some embodiments the di-acid moiety comprises a di-carboxylic acid and in some embodiments the di-acid moiety comprises a di-tetrazole.Type: ApplicationFiled: April 3, 2013Publication date: March 5, 2015Applicant: APOSENSE LTD.Inventors: Joel M. Van Gelder, Menashe Levy, Mirit Argov, Miri Ben-Ami, Ilan Ziv
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Patent number: 8968701Abstract: The invention relates to a process for the production of radiotracers. In particular, this invention relates the isolation of radiotracers with containers filled with a stationary phase.Type: GrantFiled: July 6, 2010Date of Patent: March 3, 2015Assignee: Piramal Imaging SAInventors: Holger Siebeneicher, Keith Graham, Mathias Berndt
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Publication number: 20150056137Abstract: Provided is an activatable probe that undergoes intramolecular cyclization and subsequent aggregation in apoptotic tumor cells upon peptidase-initiated, and most advantageously caspase-3, activation. These caspase-sensitive nano-aggregation probes (C-SNAFs) are generally biocompatible, possess NIR spectral properties or may serve as PET or MRI imaging agents, and have a mechanism of target-mediated nanostructure self-assembly amenable to in vivo use. The probes encompass biocompatible condensation chemistry products that comprise D-cysteine and 2-cyano-6-hydroxyquinoline (CHQ) moieties linked to an amino-luciferin scaffold, and which can be activated by a two-step reaction requiring caspase-3/7-mediated cleavage of an aspartate-glutamate-valine-aspartate (L-DEVD) capping peptide and the free intracellular thiol-mediated reduction of the disulfide bond.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Inventors: Jianghong Rao, Deju Ye, Adam Shuhendler, Frederick Te-Ning Chin, Jongho Jeon, Bin Shen
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Publication number: 20150056138Abstract: The invention features compounds and methods relating to hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters useful for diagnostic purposes. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention include radiolabeled inhibitors that can be used in research or clinical applications (e.g., for the treatment of cancer or ischemia-related central nervous system injury).Type: ApplicationFiled: October 15, 2014Publication date: February 26, 2015Inventor: Stephanie Lynn Martinelli