Fluorine Patents (Class 424/1.89)
  • CANCER DIAGNOSIS AND IMAGING
    Publication number: 20120321561
    Abstract: The present invention provides a method for imaging a disease or condition in a mammal which includes the steps of; administering a therapeutically effective amount of a cell cycle inhibitor to effectively stop proliferation of eukaryotic cells at a cell cycle checkpoint between the G1 and S phase, stopping administration of the cell cycle inhibitor for a period of time, administering a marker to the mammal and imaging the mammal.
    Type: Application
    Filed: February 28, 2011
    Publication date: December 20, 2012
    Applicant: TAU THERAPEUTICS LLC
    Inventor: Lloyd S. Gray
  • Dose synthesis module for biomarker generator system
    Patent number: 8333952
    Abstract: A microfluidic radiopharmaceutical production system and process for synthesizing per run approximately, but not less than, one (1) unit dose of a radiopharmaceutical biomarker for use in positron emission tomography (PET). The radiopharmaceutical production system includes a reaction vessel that receives a radioisotope from an accelerator or other radioisotope generator. Organic and aqueous reagents are introduced into the reaction vessel, and the mixture is heated to synthesize a solution of a pre-selected radiopharmaceutical. The radiopharmaceutical solution is purified by passing the solution through a solid phase extraction column and a filter. The synthesis process produces per run a quantity of radiopharmaceutical approximately equal to, but not less than, one (1) unit dose of a radiopharmaceutical, reducing waste and allowing for the production of radiopharmaceutical on an as-needed basis.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: December 18, 2012
    Assignee: ABT Molecular Imaging, Inc.
    Inventors: Ronald Nutt, Anthony M. Giamis, Aaron McFarland
  • Locoregional internal radionuclide ablation of abnormal tissues
    Patent number: 8329141
    Abstract: The present disclosure provides methods of using unsealed and non-colloidal radiopharmaceuticals, for example beta emitting radiopharmaceuticals such as Yttrium-90 chloride, Indium-111 chloride, F-18-2-deoxy-2-fluoro-D-glucose, or combinations thereof, for locoregional ablation of cells in the abnormal tissue.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: December 11, 2012
    Assignee: Board of Regents, The University of Texas System
    Inventor: Franklin C. Wong
  • Compounds, compositions and methods for medical imaging of Parkinson's disease
    Patent number: 8329142
    Abstract: Compounds, compositions and methods for the detection and diagnosis of Parkinson's disease. Derivative lycerophosphocholine (GPC) compounds are used as a detection and diagnostic aid to measure progression of Parkinson's disease by detecting GPC binding to ?-synuclein. Derivative CPG compounds including non-radioactive, paramagnetic, and radioactive derivatives of GPC are presented. These compounds possess similar binding properties to original GPC molecules and are useful in medical magnetic resonance imaging (MRI) and/or positron emission tomography (PET) applications. By employing these radiological techniques in conjunction with the compositions of the present invention, the detection, diagnosis and assessment of the progression of Parkinson's disease may be achieved.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: December 11, 2012
    Inventors: Jay W. Pettegrew, Richard J. McClure, Kanagasabai Panchalingam
  • Solid-phase fluorination of benzothiazoles
    Patent number: 8323616
    Abstract: The invention provides a process for the production of an 18F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I) SOLID SUPPORT-LINKER-X-TRACER (I) wherein X is a group which promotes nucleophilic substitution at a specific site on the attached TRACER and the TRACER is of formula (A).
    Type: Grant
    Filed: December 19, 2003
    Date of Patent: December 4, 2012
    Assignees: GE Healthcare Limited, Hammersmith Imanet Limited
    Inventors: Frank Brady, Sajinder Kaur Luthra, Alexander Mark Gibson
  • METHOD FOR PRODUCTION OF RADIATION DIAGNOSTIC IMAGING AGENT
    Publication number: 20120301399
    Abstract: A method for producing a radioactive diagnostic imaging agent containing a radioactive 18 fluorine-labeled organic compound represented by the following formula (1): as an effective ingredient in which radiolysis of the effective ingredient is inhibited, involves providing a solution containing the radioactive 18fluorine-labeled organic compound represented by the above formula (1), adding an acid to the solution obtained in the first step in an amount sufficient for the solution to be kept within a pH of 2.0-5.9 in the following third step, and diluting the solution obtained in the second step in order to adjust the solution to a desired radioactive concentration within a pH of 2.0-5.9.
    Type: Application
    Filed: August 2, 2012
    Publication date: November 29, 2012
    Applicant: NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Daisaku NAKAMURA, Soichi Nakamura, Masahito Toyama, Akio Hayashi
  • Imaging agents for detecting neurological dysfunction
    Patent number: 8318132
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: November 27, 2012
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Peter J. H. Scott, Kai Chen, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha
  • CXCR4 ANTAGONISTS FOR IMAGING OF CANCER AND INFLAMMATORY DISORDERS
    Publication number: 20120294803
    Abstract: The invention provides radiolabeled CXCR4 antagonists, compositions and methods of use for imaging of chemokine CXCR4 receptors and biological conditions associated with the expression of CXCR4 receptors, including cancer, metastasis, and inflammatory disorders.
    Type: Application
    Filed: January 27, 2011
    Publication date: November 22, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Hyunsuk Shim, Dennis C. Liotta, Mark M. Goodman, Aizhi Zhu
  • RADIOLABELLING
    Publication number: 20120288445
    Abstract: Compounds of the formula (I) are disclosed: 18F—(CHR)n(CH2)mCHO??(I) in which n and m are independently 0 and 1 with at least one of n and m being 1, and R (if present) is a hydrogen atom or a methyl group, subject to the proviso that if n is 1 and R is methyl then m is 0. Synthesis of the compounds is described together with their use in radiolabelling reactions, e.g. for the radiolabelling of peptides to facilitate detection by Positron Emission Tomography (PET) imaging. The preferred compound is [18F]Fluoroacetaldehyde.
    Type: Application
    Filed: April 13, 2012
    Publication date: November 15, 2012
    Applicant: The University of Manchester
    Inventor: Christian PRENANT
  • SINGLE DIASTEREOMERS OF 4-FLUOROGLUTAMINE AND METHODS OF THEIR PREPARATION AND USE
    Publication number: 20120288444
    Abstract: The present invention is directed single diasteromers of 4-fluoroglutamine having a diastereomeric excess of at least 80%. Methods of preparing the single diastereomers are also described, as well as methods of using the single diastereomers of radiolabeled 4-fluoroglutamine as imaging agent is also described.
    Type: Application
    Filed: August 13, 2010
    Publication date: November 15, 2012
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Hank F. Kung, Craig B. Thompson, Wenchao Qu, Karl Ploessl
  • PET radiotracers
    Patent number: 8309055
    Abstract: The invention relates to novel 18F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. The 18F-labelled compounds of the invention comprise a [18F]fluoroalkenyl group.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: November 13, 2012
    Assignee: Hammersmith Imanet Limited
    Inventors: Erik Arstad, Edward George Robins
  • Method for the purification of radiolabelled compounds
    Patent number: 8309054
    Abstract: The invention relates to methods and apparatus for purifying a radiolabelled compound. The method comprises (i) passing a crude reaction mixture comprising the desired radiolabelled compound and one or more contaminants in a solvent through a narrow bore vessel at elevated temperature such that the organic solvent and either the radiolabelled compound or one or more contaminants is vaporised forming a vaporised component, and (ii) collecting the resulting vaporised component by condensing into a collection vessel.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: November 13, 2012
    Assignee: Hammersmith Imanet Limited
    Inventor: Erik Arstad
  • Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof
    Publication number: 20120282180
    Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration.
    Type: Application
    Filed: June 8, 2011
    Publication date: November 8, 2012
    Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
  • Alkoxy substituted imidazo[1,2-a]pyridines having affinity for amyloid
    Patent number: 8303935
    Abstract: The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.
    Type: Grant
    Filed: May 15, 2007
    Date of Patent: November 6, 2012
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki, Yuki Okumura
  • Radiolabeled affibody molecules
    Patent number: 8303960
    Abstract: The invention provides a radiolabeled affibody molecule comprising a fragment of an IgG-binding domain of protein A from Staphylococcus aureus, a bifunctional linker, and a radiolabel comprising 18F or 76Br, wherein the bifunctional linker links the fragment and the radiolabel. The affibody molecule binds with high affinity to select receptors, which are over-expressed in certain cancers. Since the radionuclides emit a positron, the in vitro and in vivo binding characteristics of the radiolabeled affibody can be assessed using diagnostic imaging.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: November 6, 2012
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Jacek Capala, Dale O. Kiesewetter, Gabriela Kramer-Marek, Sang Bong Lee
  • CONTRAST AGENTS FOR MYOCARDIAL PERFUSION IMAGING
    Publication number: 20120276006
    Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
    Type: Application
    Filed: June 21, 2012
    Publication date: November 1, 2012
    Applicant: Lantheus Medical Imaging, Inc.
    Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
  • IMAGING AGENTS AND METHODS OF IMAGING NAALADASE OR PSMA
    Publication number: 20120276007
    Abstract: 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: Application
    Filed: June 29, 2012
    Publication date: November 1, 2012
    Applicants: Georgetown University, The Johns Hopkins University
    Inventors: Martin Gilbert Pomper, Jiazhong Zhang, John L. Musachio, Alan P. Kozikowski
  • Separation process
    Patent number: 8298414
    Abstract: The present invention relates to a process for separating a target radiolabelled compound from an impurity, apparatus for performing such a process and a removable cassette for use in such apparatus. Also provided are methods for using the target radiolabelled compound obtained by a method comprising the separating process of the invention.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: October 30, 2012
    Assignee: GE Healthcare Limited
    Inventor: Mette Husbyn
  • IMAGING AGENTS WITH IMPROVED PHARMACOKINETIC PROFILES
    Publication number: 20120269727
    Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 25, 2012
    Applicant: GE HEALTHCARE AS
    Inventors: ALAN CUTHBERTSON, MAGNE SOLBAKKEN
  • Fluorinated fructose derivatives for PET imaging
    Patent number: 8293208
    Abstract: The present invention is directed to fructose-based radiopharmaceuticals, pharmaceutical compositions comprising same, precursors and methods for preparing same, and methods of using same for diagnostic imaging of cancer cells and non-imaging tracer studies.
    Type: Grant
    Filed: May 15, 2009
    Date of Patent: October 23, 2012
    Assignee: The Governors of the University of Alberta
    Inventors: Chris Cheeseman, Frederick West, Tina Grant, Brendan Trayner, John Mercer, Andrei Manolescu
  • IMAGING AGENTS AND THEIR USE FOR THE DIAGNOSTIC IN VIVO OF NEURODEGENERATIVE DISEASES, NOTABLY ALZHEIMER'S DISEASE AND DERIVATIVE DISEASES
    Publication number: 20120263646
    Abstract: Disclosed are new imaging agents and their use for the in vivo diagnostic of neurodegenerative diseases, notably Alzheimer's disease and related diseases.
    Type: Application
    Filed: October 15, 2010
    Publication date: October 18, 2012
    Applicant: GUERBET
    Inventors: Sarah Catoen, Thierry Gautheret
  • Compounds for Use in the Detection of Neurodegenerative Diseases
    Publication number: 20120251448
    Abstract: Provided are the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of pathological characteristics unique to synuclein diseases, such as Parkinson's disease.
    Type: Application
    Filed: March 2, 2012
    Publication date: October 4, 2012
    Inventors: Franz F. Hefti, Geoffrey Golding, Ximin Li, Seok-Rye Choi, Luke Esposito, Marisa-Claire Yadon, Joel Cummings, F. Michael Hudson, Thomas Lake, Alan D. Snow
  • ALDH: A COMPOUND FOR CANCER STEM CELL IMAGING
    Publication number: 20120251449
    Abstract: The present invention claims fluoro- & iodo-containing aldehydes as ALDH substrates for use as diagnostic imaging agents or as therapeutic agents. The aldehydes are both directly and indirectly attached to an aromatic or a straight chain ring. ALDH activity was monitored either by the formation of acid-product or consumption of aldehyde substrates.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 4, 2012
    Inventors: Vijaya Raj Kuniyil Kulangara, Alan Cuthbertson, Peter Iveson, Chitralekha Rangaswamy, Veena Rao, Rajiv Bhalla
  • Compound having affinity for amyloid
    Patent number: 8277777
    Abstract: A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: October 2, 2012
    Assignees: Nihon Medi-Physics Co., Ltd., GE Healthcare Limited
    Inventors: Shigeyuki Tanifuji, Akio Hayashi, Daisaku Nakamura, Shinya Takasaki, Anthony Eamon Storey, Denis Raymond Christophe Bouvet
  • ARYLOXYANILIDE IMAGING AGENTS
    Publication number: 20120244073
    Abstract: The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
    Type: Application
    Filed: December 16, 2010
    Publication date: September 27, 2012
    Inventors: Harry John Wadsworth, Dennis O' Shea
  • LABELLED INTEGRIN BINDERS
    Publication number: 20120244074
    Abstract: The present invention provides alternative in vivo imaging agents suitable for use in the detection of ?v?6 expressed in a subject. The invention also provides a method for obtaining said in vivo imaging agents, and use of the in vivo imaging agents in determining ?v?6 expressed in a subject.
    Type: Application
    Filed: December 16, 2010
    Publication date: September 27, 2012
    Inventor: Magne Solbakken
  • Imaging infection with compounds that bind to thymidine kinase
    Patent number: 8273326
    Abstract: The instant invention provides a method for diagnosing an infection in a subject by administering to the subject a compound suitable for imaging which binds to a thymidine kinase present in the infecting organism, and obtaining an image of the subject to determine the presence and location of the compound, wherein a localization of the compound is indicative that the subject has an infection.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: September 25, 2012
    Assignee: The Johns Hopkins University
    Inventors: Martin G. Pomper, Chetan Bettegowda, Catherine Foss, Shibin Zhou, Kenneth Kinzler, Bert Vogelstein
  • Radio-opaque compounds, compositions containing same and methods of their synthesis and use
    Patent number: 8273327
    Abstract: Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: September 25, 2012
    Assignee: Pathak Holdings, LLC
    Inventors: Chandrashekhar P. Pathak, Sanjay M. Thigle
  • Compounds for binding and imaging amyloid plaques and their use
    Publication number: 20120237446
    Abstract: The present invention relates to novel compounds (3-aminopropen-1-ones) useful for binding and imaging beta amyloid deposits and their use in detecting or treating Alzheimer's disease and amyloidosis.
    Type: Application
    Filed: March 26, 2012
    Publication date: September 20, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrike Röhn, Hermann Künzer, Tobias Heinrich, Markus Berger, Damian Brockschnieder, Sabine Krause, Thomas Dyrks, Andrea Thiele, Ursula Mönning, Ulf Bömer
  • STABILIZATION OF RADIOPHARMACEUTICAL COMPOSITIONS USING ASCORBIC ACID
    Publication number: 20120237445
    Abstract: Radiopharmaceutical compositions, and related methods, useful for medical imaging are provided. The radiopharmaceutical compositions include one or more radiopharmaceutical compounds, together with a stabilizer comprising ascorbic acid, wherein the pH of said composition is within the range of about 3.5-5.5.
    Type: Application
    Filed: April 15, 2010
    Publication date: September 20, 2012
    Applicant: Lantheus Medical Imaging, Inc.
    Inventors: James F. Castner, Dianne D. Zdankiewicz, James E. Anderson
  • LABELING COMPOUND FOR PET
    Publication number: 20120230914
    Abstract: A labeling compound of the present invention includes a structure represented by formula (1) wherein X1 is 11CH3, CH218F, CF218F, 18F, 76Br or 124I, X2 is CN or NO2, and R is any one of groups represented by or a structure represented by formula (2) wherein X3 is CH3, CH2F, CF3, F, Br or I, and R is defined equally as in the formula (1). This allows realizing a labeling compound for PET, capable of quantifying aromatase with high accuracy.
    Type: Application
    Filed: July 5, 2010
    Publication date: September 13, 2012
    Applicant: RIKEN
    Inventors: Yasuyoshi Watanabe, Hirotaka Onoe, Kayo Takahashi, Masaaki Suzuki, Hisashi Doi, Takamitsu Hosoya
  • Use of DKK-1 protein in the cancer diagnosis
    Patent number: 8263039
    Abstract: Use of DKK-1 protein or the nucleic acid sequence in preparation of cancer diagnostic agents or kits, method to detect liver cancer with the monoclonal antibody thereof, the kit comprising anti-DKK-1 antibody or protein specific nucleic acid probes, together with a label, and method to detecting specific DKK-1 protein expression are disclosed.
    Type: Grant
    Filed: November 11, 2008
    Date of Patent: September 11, 2012
    Assignee: Shanghai Cancer Institute
    Inventors: Wenxin Qin, Haitao Zhang, Yanjun Yu, Haiyan You, Shengli Yang, Jianren Gu, Gang Huang, Shile Sheng, Tao Chen
  • Catalytic radiofluorination
    Patent number: 8257680
    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 arylammonium 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: Grant
    Filed: August 18, 2006
    Date of Patent: September 4, 2012
    Assignee: The General Hospital Corporation
    Inventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
  • Methods for identifying and targeting autonomic brain regions
    Patent number: 8257684
    Abstract: Disclosed herein are methods for identifying and targeting autonomic and autonomic-related brain regions. In one embodiment, a method of identifying a brain region in a patient comprises administering to the patient a targeting agent that activates or inhibits a brain region and imaging the brain region.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: September 4, 2012
    Assignee: Neurosigma, Inc.
    Inventors: Alejandro Covalin, Antonio Afonso Ferreira De Salles
  • DIAGNOSTIC AGENT FOR INFECTIOUS DISEASES
    Publication number: 20120219500
    Abstract: A diagnostic agent for infectious diseases which is capable of distinguishing among different kinds of bacterial species and which allows simple and non-invasive measurement and/or imaging in a short period of time is provided; and a screening method for a therapeutic agent for infectious diseases caused by microorganisms are provided. A diagnostic agent for infectious diseases caused by nitroimidazole susceptible microorganisms, containing an imidazole derivative or a fused imidazole derivative having at least one nitro group on an imidazole ring, or a labeled form thereof as an active ingredient is provided.
    Type: Application
    Filed: October 25, 2010
    Publication date: August 30, 2012
    Applicant: FUJIFILM RI PHARMA CO., LTD.
    Inventors: Kazuhisa Sakurai, Akio Nagano
  • RADIOLABELLED PDE10 LIGANDS
    Publication number: 20120213703
    Abstract: The present invention relates to novel, selective, radiolabelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.
    Type: Application
    Filed: October 27, 2010
    Publication date: August 23, 2012
    Inventors: José Ignacio Andrés-Gil, Meri De Angelis, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen
  • NOVEL DIAGNOSTIC AGENTS FOR THE NON-INVASIVE IN VIVO IMAGING OF AMINOPEPTIDASE N (APN/CD13)
    Publication number: 20120213702
    Abstract: The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3? and R3? is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention.
    Type: Application
    Filed: August 31, 2010
    Publication date: August 23, 2012
    Inventors: Christoph Bremer, Carsten Höltke
  • CATALYTIC RADIOFLUORINATION
    Publication number: 20120207677
    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 arylammonium 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: August 18, 2006
    Publication date: August 16, 2012
    Inventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
  • Labeled Adenosine for Use in Positron Emission Tomography
    Publication number: 20120207678
    Abstract: Radiolabeled adenosine or radiolabeled adenosine containing molecules for use in positron emission tomography for assessing alterations in adenylate metabolism in a patient are provided.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 16, 2012
    Inventor: Edward H. Abraham
  • Novel Heteroaryl Substituted Benzothiazoles
    Publication number: 20120207679
    Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 16, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmström, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Ström, David Wensbo
  • Synthesis of a radiofluorinated peptide using photolabile protecting groups
    Patent number: 8241606
    Abstract: The present invention encompasses a method of preparing a radiofluorinated compound by adding a photolabile protecting group, R, to an aminoxy group of a peptide based compound wherein the peptide based compound reacts with a light of a specified wavelength in an automated radiosynthesis apparatus to form a radiofluorinated compound. The present invention further relates to a photolabile peptide based compound.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: August 14, 2012
    Assignee: GE Healthcare AS
    Inventor: Lorenzo Williams
  • Use of fructose-based compounds for the diagnosis of cancer
    Patent number: 8241607
    Abstract: This invention relates to compositions, methods utilizing fructose and other monosaccharides for the diagnosis of cancer. Cancer cells have shown a higher level of fructose utilization as compared to glucose. Further, cancer cells have shown a preferential use of fructose for nucleic acid synthesis. The present invention takes advantage of these features and provides for fructose or fructose-based compositions for the diagnosis of cancer using imaging techniques such as positron emission tomography.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: August 14, 2012
    Assignee: Cedars-Sinai Medical Center
    Inventors: Anthony P. Heaney, Hongxiang Hui, Alan Waxman
  • PHOSPHODIESTERASE 1-TARGETING TRACERS AND METHODS
    Publication number: 20120201754
    Abstract: Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particulaly 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: October 7, 2010
    Publication date: August 9, 2012
    Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
  • Benzothiazole derivative compounds, compositions and uses
    Patent number: 8236282
    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: September 30, 2009
    Date of Patent: August 7, 2012
    Assignee: University of Pittsburgh—of the Commonwealth System of Higher Education
    Inventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
  • [18F] LABELLED ANALOGUES OF FLUMAZENIL AS IN VIVO IMAGING AGENTS
    Publication number: 20120189547
    Abstract: The present invention provides radiofluorinated compounds useful for in vivo imaging GABAA receptors. Also provided by the present invention is a method of synthesis for the radiofluorinated compounds of the invention, in particular an automated method of synthesis. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention.
    Type: Application
    Filed: October 8, 2010
    Publication date: July 26, 2012
    Inventors: John Woodcraft, Clare L. Jones, Alessandra Gaeta, William John Trigg, Paul Alexander Jones, Stuart Plant
  • 2-ARYLPYRAZOLO[L,5-ALPHA]PYRIMIDIN-3-YL ACETAMIDE DERIVATIVES AS LIGANDS FOR TRANSLOCATOR PROTEIN (18 KDA)
    Publication number: 20120189548
    Abstract: The invention provides compounds of formula (I) radiolabelled with 18F, 123I, 76Br, 124I or 75Br and salts thereof, and a method of imaging translocator protein (18 kDa) (TSPO) in a subject comprising administering a compound of formula (I) radiolabelled with 18F, 123I, 76Br, 124I or 75 Br or a pharmaceutically acceptable salt thereof. The invention further provides fluoro-substituted compounds of formula (II) and salts thereof, and a method of treating a neurodegenerative disorder, inflammation or anxiety in a subject comprising administering a compound of formula (II) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: The University of Sydney
    Inventors: Michael Kassiou, Michelle Louise James
  • Radiolabelling Method Using Cycloalkyl Groups
    Publication number: 20120189546
    Abstract: This invention relates to novel cyclo alkyl compounds suitable for labeling by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: July 9, 2010
    Publication date: July 26, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Heribert Schmitt-Willich, Dominic Franck
  • C/F-labeled inhibitors of glycogen synthase kinase-3
    Patent number: 8226927
    Abstract: The present invention relates to new 11C/18F-labeled inhibitor compounds for over-expressed GSK-3 prepared from the GMP synthesis method. The present invention provides novel 11C/18F inhibitor compounds for over-expressed GSK-3 that are suitable for use as an in vivo imaging agent. A pharmaceutical comprising the compound and a kit for the preparation of the pharmaceutical are also provided.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: July 24, 2012
    Inventors: Farhad Karimi, Bengt Langstrom
  • Contrast agents for myocardial perfusion imaging
    Patent number: 8226929
    Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
    Type: Grant
    Filed: January 15, 2008
    Date of Patent: July 24, 2012
    Assignee: Lantheus Medical Imaging, Inc.
    Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
  • Methods and System for Detecting Soluble Amyloid-Beta
    Publication number: 20120183474
    Abstract: The present invention provides methods of detecting soluble amyloid ? using curcumin-derived near infrared (NIR) imaging probes. Upon interacting with soluble amyloid ?, these probes undergo a range of changes, qualifying them as “smart” probes. In addition, the invention provides methods of detecting soluble amyloid ? by positron emission tomography (PET), magnetic resonance imaging (MRI) and multimodal imaging based on the curcumin-derived NIR imaging probes and derivatives thereof.
    Type: Application
    Filed: July 29, 2010
    Publication date: July 19, 2012
    Inventors: Chongzhao Ran, Anna Moore