Fluorine Patents (Class 424/1.89)
  • Patent number: 10406164
    Abstract: The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: September 10, 2019
    Assignee: The General Hospital Corporation
    Inventor: David R. Elmaleh
  • Patent number: 10358437
    Abstract: The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R3-R6, X, and each Re have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: July 23, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Alexandre Cote, Terry Crawford, Martin Duplessis, Andrew Charles Good, Yves LeBlanc, Steven Magnuson, Christopher G. Nasveschuk, Richard Pastor, F. Anthony Romero, Alexander M. Taylor
  • Patent number: 10335503
    Abstract: The present invention provides a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof. (In the formula, each of A and Z independently represents CO, SO or SO2; each of X and Y independently represents S or O; each of R1-R4 independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group or a halogen group; each R5 independently represents an alkyl group, an alkenyl group, an alkynyl group or a halogen group; and n represents an integer of 0-4.) This compound is capable of specifically binding to an AMPA receptor, and shows extremely high brain uptake.
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: July 2, 2019
    Assignee: Public University Corporation Yokohama City University
    Inventors: Takuya Takahashi, Tomoyuki Miyazaki, Tetsuya Suhara, Makoto Higuchi, Meiei Cho
  • Patent number: 10316023
    Abstract: The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R3-R6, X, and each Re have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: June 11, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Alexandre Cote, Terry Crawford, Martin Duplessis, Andrew Charles Good, Yves LeBlanc, Steven Magnuson, Christopher G. Nasveschuk, Richard Pastor, F. Anthony Romero, Alexander M. Taylor
  • Patent number: 10259781
    Abstract: Provided herein is technology relating to imaging agents and particularly, but not exclusively, to methods of manufacturing fluorine-18-labeled phenethylguanidines and uses thereof.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: April 16, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: David M. Raffel, Yong-Woon Jung, Keun-Sam Jang
  • Patent number: 10183082
    Abstract: 18F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-mino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an 18F. The 18F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: January 22, 2019
    Assignee: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
    Inventors: Haibin Tian, Robert J. Gillies
  • Patent number: 10179117
    Abstract: The present technology is directed to compounds, compositions, medicaments, and methods related to the treatment of cancers expressing PSMA. The compounds are of Formulas I & II or pharmaceutically acceptable salts thereof. The present technology is especially well-suited for use in treating prostate cancer.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: January 15, 2019
    Assignee: Cornell University
    Inventors: John W. Babich, James M. Kelly, Alejandro Amor-Coarasa, Shashikanth Ponnala
  • Patent number: 10081630
    Abstract: The present invention relates to a radioactive halogen-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a specific general formula or a salt thereof, or a radiopharmaceutical comprising the same.
    Type: Grant
    Filed: February 24, 2016
    Date of Patent: September 25, 2018
    Assignees: KYOTO UNIVERSITY, NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Masahiro Ono, Hideo Saji, Masafumi Ihara, Hiroki Matsumoto, Ikuya Seki
  • Patent number: 10004818
    Abstract: 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: Grant
    Filed: April 15, 2016
    Date of Patent: June 26, 2018
    Assignee: CELLECTAR, Inc.
    Inventors: Jamey P. Weichert, Anatoly Pinchuk, Irawati Kandela, Marc Longino, William R. Clarke
  • Patent number: 9999692
    Abstract: 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: Grant
    Filed: March 28, 2014
    Date of Patent: June 19, 2018
    Assignee: GE Healthcare Limited
    Inventor: Torild Wickstrom
  • Patent number: 9999689
    Abstract: The present disclosure provides compositions and methods based on peptide-detectable agent conjugates that are useful for imaging beta cell mass.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: June 19, 2018
    Assignee: The General Hospital Corporation
    Inventors: Ralph Weissleder, Thomas Reiner, Edmund J. Keliher
  • Patent number: 9987380
    Abstract: 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: Grant
    Filed: July 13, 2012
    Date of Patent: June 5, 2018
    Assignee: University of Southern California
    Inventors: Zibo Li, Francois P. Gabbai, Peter S. Conti, Todd W. Hudnall, Tzu-Pin Lin, Shuanglong Liu, Chiun-Wei Huang
  • Patent number: 9951011
    Abstract: 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: Grant
    Filed: September 19, 2014
    Date of Patent: April 24, 2018
    Assignee: GE HEALTHCARE LIMITED
    Inventors: William John Trigg, Paul Alexander Jones
  • Patent number: 9856182
    Abstract: 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: Grant
    Filed: July 30, 2013
    Date of Patent: January 2, 2018
    Assignee: TECHNICAL UNIVERSITY OF DENMARK
    Inventors: Fedor Zhuravlev, Bente Mathiessen
  • Patent number: 9833520
    Abstract: 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: Grant
    Filed: July 26, 2013
    Date of Patent: December 5, 2017
    Assignee: The Methodist Hospital Research Institute
    Inventors: King Chuen Li, Zheng Li, Feng Li
  • Patent number: 9789207
    Abstract: 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: Grant
    Filed: June 16, 2016
    Date of Patent: October 17, 2017
    Assignee: 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
  • Patent number: 9682159
    Abstract: The present invention relates to the use of a combination of several contrast agents having different properties with respect to imaging representation.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: June 20, 2017
    Assignee: nanoPET Pharma GmbH
    Inventor: Ulrike Wiebelitz
  • Patent number: 9592309
    Abstract: 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: Grant
    Filed: May 9, 2013
    Date of Patent: March 14, 2017
    Assignee: The Regents of the University of California
    Inventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
  • Patent number: 9556114
    Abstract: 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: Grant
    Filed: December 10, 2014
    Date of Patent: January 31, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Patent number: 9517279
    Abstract: 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: Grant
    Filed: April 14, 2011
    Date of Patent: December 13, 2016
    Assignee: The McLean Hospital Corporation
    Inventors: John L. Neumeyer, Yu-Gui Si, Anna W. Sromek
  • Patent number: 9481685
    Abstract: 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: Grant
    Filed: October 2, 2009
    Date of Patent: November 1, 2016
    Assignee: GE Healthcare Limited
    Inventors: Harry John Wadsworth, Bo Shan, Dennis O'Shea, Joanna Marie Passmore, William John Trigg
  • Patent number: 9468692
    Abstract: 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: Grant
    Filed: January 23, 2014
    Date of Patent: October 18, 2016
    Assignee: General Electric Company
    Inventors: Bruce Allan Hay, Jack Mathew Webster
  • Patent number: 9346771
    Abstract: 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: Grant
    Filed: February 11, 2015
    Date of Patent: May 24, 2016
    Assignee: GE HEALTHCARE LIMITED
    Inventors: Eric Horn, Steven Fairway, Dimitrios Mantzilas, Nigel Powell
  • Patent number: 9308284
    Abstract: 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: Grant
    Filed: June 21, 2012
    Date of Patent: April 12, 2016
    Assignee: PIRAMAL IMAGING SA
    Inventors: Carsten Olbrich, Michael Krause, Andreas Burkhard, Annett Richter, Rainer Braun
  • Patent number: 9295738
    Abstract: 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: Grant
    Filed: December 18, 2012
    Date of Patent: March 29, 2016
    Assignee: RESPIRATORIUS AB
    Inventor: Martin Johansson
  • Patent number: 9227943
    Abstract: 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: Grant
    Filed: January 7, 2015
    Date of Patent: January 5, 2016
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
  • Patent number: 9211350
    Abstract: 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: Grant
    Filed: May 29, 2012
    Date of Patent: December 15, 2015
    Assignee: NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Yuki Okumura, Yoshifumi Maya, Yoshinari Shoyama, Takako Onishi
  • Patent number: 9180209
    Abstract: 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: Grant
    Filed: February 24, 2012
    Date of Patent: November 10, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Laura E. Edgington, Martijn Verdoes
  • Patent number: 9179882
    Abstract: The present invention relates to the use of a combination of several contrast agents having different properties with respect to imaging representation.
    Type: Grant
    Filed: April 11, 2013
    Date of Patent: November 10, 2015
    Assignee: MIVENION GMBH
    Inventor: Ulrike Wiebelitz
  • Patent number: 9134328
    Abstract: 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: Grant
    Filed: April 7, 2014
    Date of Patent: September 15, 2015
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
  • Patent number: 9125937
    Abstract: 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: Grant
    Filed: September 19, 2013
    Date of Patent: September 8, 2015
    Assignees: 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 CYCLOPHARMA
    Inventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
  • Patent number: 9115172
    Abstract: 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: Grant
    Filed: October 8, 2014
    Date of Patent: August 25, 2015
    Assignee: Immunomedics, Inc.
    Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
  • Patent number: 9095631
    Abstract: 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: Grant
    Filed: May 24, 2011
    Date of Patent: August 4, 2015
    Assignee: UNIVERSITA DEGLI STUDI DI BARI “ALDO MORO”
    Inventors: Nicola Antonio Colabufo, Francesco Berardi, Mariangela Cantore, Marialessandra Contino, Marcello Leopoldo, Roberto Perrone
  • Patent number: 9072775
    Abstract: 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: Grant
    Filed: February 14, 2008
    Date of Patent: July 7, 2015
    Inventors: Mathieu Goutayer, Isabelle Texier-Nogues, Jacques Fattaccioli, Jérôme Bibette, Anabela Da Silva
  • Patent number: 9073802
    Abstract: 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: Grant
    Filed: February 8, 2011
    Date of Patent: July 7, 2015
    Assignees: TOKYO INSTITUTE OF TECHNOLOGY, NIIGATA UNIVERSITY
    Inventors: Takashi Takahashi, Hiroshi Tanaka, Tsutomu Nakada
  • Patent number: 9061080
    Abstract: 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: Grant
    Filed: December 19, 2011
    Date of Patent: June 23, 2015
    Assignee: GE HEALTHCARE LIMITED
    Inventors: Duncan Hiscock, Bard Indrevoll, Peter Iveson, Matthias Eberhard Glaser, Rajiv Bhalla, Anthony Wilson
  • Publication number: 20150147273
    Abstract: 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: Application
    Filed: June 10, 2013
    Publication date: May 28, 2015
    Applicant: Koninklijke Philips N.V.
    Inventors: Tilman Lappchen, Holger Gruell, Marc Stefan Robillard, Johan Lub
  • Patent number: 9040021
    Abstract: 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: Grant
    Filed: November 7, 2011
    Date of Patent: May 26, 2015
    Assignee: GE Healthcare Limited
    Inventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
  • Publication number: 20150139903
    Abstract: 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: Application
    Filed: September 22, 2014
    Publication date: May 21, 2015
    Inventors: Peng LI, Lawrence WENNOGLE, Jun ZHAO, Hailin ZHENG
  • Publication number: 20150132223
    Abstract: 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: Application
    Filed: November 25, 2014
    Publication date: May 14, 2015
    Inventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
  • Publication number: 20150133777
    Abstract: 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: Application
    Filed: May 9, 2013
    Publication date: May 14, 2015
    Inventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
  • Patent number: 9028800
    Abstract: 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: Grant
    Filed: May 8, 2014
    Date of Patent: May 12, 2015
    Assignee: Immunomedics, Inc.
    Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
  • Publication number: 20150125390
    Abstract: 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: Application
    Filed: May 8, 2013
    Publication date: May 7, 2015
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
  • Patent number: 9023316
    Abstract: 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: Grant
    Filed: April 8, 2011
    Date of Patent: May 5, 2015
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Umesh Gangadharmath, Joseph Walsh, Hartmuth Kolb
  • Patent number: 9023317
    Abstract: 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: Grant
    Filed: February 25, 2013
    Date of Patent: May 5, 2015
    Assignee: University of Western Ontario
    Inventors: Duncan H. Hunter, Mustafa Janabi
  • Patent number: 9023318
    Abstract: 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: Grant
    Filed: March 25, 2013
    Date of Patent: May 5, 2015
    Assignee: 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
  • Patent number: 9005577
    Abstract: 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: Grant
    Filed: April 30, 2009
    Date of Patent: April 14, 2015
    Assignee: 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
  • Patent number: 9005578
    Abstract: 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: Grant
    Filed: May 28, 2013
    Date of Patent: April 14, 2015
    Assignees: Fluoropharma, Inc., The General Hospital Corporation
    Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
  • Publication number: 20150098902
    Abstract: 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: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20150098903
    Abstract: 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: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu