Abstract: The present invention provides a composition comprising anti-1-amino-3-18F-fluorocyclobutyl-1-carboxylic acid (18F-FACBC) having an improved impurity profile compared with previous such compositions. Also provided is a method to obtain said composition.
Type:
Grant
Filed:
June 30, 2015
Date of Patent:
August 3, 2021
Assignee:
GE HEALTHCARE LIMITED
Inventors:
Knut Richard Dyrstad, Torild Wickstrom, Thanushan Rajanayagam
Abstract: The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 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, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.
Type:
Grant
Filed:
December 16, 2016
Date of Patent:
June 29, 2021
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
José Ignacio Andrés-Gil, Michiel Luc Maria Van Gool, Guy Maurits R Bormans, Joost Verbeek
Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.
Type:
Grant
Filed:
December 9, 2019
Date of Patent:
June 15, 2021
Assignee:
The Trustees of Columbia University in the City of New York
Inventors:
Yan Feng, Mauro Fa, Ottavio Arancio, Shixian Deng, Donald W. Landry, Yitshak Francis
Abstract: The present invention relates to novel, radiolabelled mGluR2/3 ligands, selective 5 versus other mGlu receptors, which are useful for imaging and quantifying the metabotropic glutamate receptors mGlu2 and 3 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, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or 10 in vivo and to precursors of said compounds.
Type:
Grant
Filed:
December 16, 2016
Date of Patent:
June 15, 2021
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
José Ignacio Andrés-Gil, Michiel Luc Maria Van Gool, Guy Maurits R Bormans, Joost Verbeek
Abstract: The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: (A) at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; and (C) at least one dye moiety; wherein said compound has a molecular weight of not more than 5 kDa. Further, the invention refers to a method for producing such compound and to the in vivo and in vitro uses thereof.
Type:
Grant
Filed:
July 25, 2019
Date of Patent:
June 1, 2021
Assignee:
DEUTSCHES KREBSFORSCHUNGSZENTRUM
Inventors:
Matthias Eder, Klaus Kopka, Martin Schaefer, Ulrike Bauder-Wuest, Uwe Haberkorn
Abstract: Methods for detecting or ruling out a meningioma in a patient using a phenylbenzothiazole derivative or a stilbene derivative or a biphenylalkyne derivative, and a medical imaging technique such as positron emission tomography/computed tomography are disclosed.
Type:
Grant
Filed:
December 29, 2015
Date of Patent:
April 20, 2021
Assignee:
Mayo Foundation for Medical Education and Research
Inventors:
Geoffrey B. Johnson, Val J. Lowe, Mark A. Nathan, Joseph E. Parisi
Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
Type:
Grant
Filed:
May 1, 2019
Date of Patent:
April 13, 2021
Assignee:
MERCK & CIE
Inventors:
Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
Abstract: The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 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, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.
Type:
Grant
Filed:
December 2, 2015
Date of Patent:
April 6, 2021
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Michiel Luc Maria Van Gool, José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen, Joost Verbeek
Abstract: The invention provides a method for preparing a technetium-99m tricarbonyl intermediate. The method comprises reacting a manganese carbonyl compound used as a carbon monoxide source with pertechnetate and water to obtain the technetium-99m tricarbonyl intermediate. The method for preparing a technetium-99m tricarbonyl intermediate in an embodiment of the invention can complete the preparation of the intermediate at atmospheric pressure and room temperature. The method is easy to operate, uses easily obtained raw materials, has a high labeling yield, and can be used to prepare various types of technetium tricarbonyl labeled probes.
Type:
Grant
Filed:
December 28, 2016
Date of Patent:
April 6, 2021
Assignee:
Institute of High Energy Physics, Chinese Academy of Sciences
Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.
Type:
Grant
Filed:
September 21, 2017
Date of Patent:
March 30, 2021
Assignee:
MERCK & CIE
Inventors:
Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Tobias Ludwig Ross, Viola Groehn
Abstract: The present invention is related to a compound of formula (I) wherein R1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid; R2 is selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C5)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK is (C2-C5)alkylidene; R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and (C1-C4)alkyl under the proviso that one of R3, R4 and R5 is of the formula (II) wherein ALK? is (C2-C5)alkylidene; R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; and R7 is selected from the group consisting of H and an Effector moiety; or a pharmacologically acceptable salt, solvate or hydrate thereof.
Type:
Grant
Filed:
December 6, 2013
Date of Patent:
March 30, 2021
Assignee:
3B PHARMACEUTICALS GMBH
Inventors:
Frank Osterkamp, Christiane Smerling, Ulrich Reineke, Christian Haase, Jan Ungewiß
Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.
Abstract: It has been found that efficient screening for a compound having anticancer activity can be achieved by selecting a compound having activity to induce alternative autophagy using, as an index, formation of fluorescent bright spots due to aggregation of a lysosomal protein to which a fluorescent protein is attached in cells expressing the lysosomal protein.
Type:
Grant
Filed:
February 7, 2013
Date of Patent:
March 23, 2021
Assignee:
National University Corporation Tokyo Medical and Dental University
Inventors:
Shigeomi Shimizu, Takamitsu Hosoya, Michiko Murohashi, Suguru Yoshida
Abstract: An imaging agent and a method of its use for imaging a necrosis in a tissue of a subject. The imaging method may be positron emission tomography (PET). In at least one embodiment the imaging agent comprises 2-deoxy-2-[18F]fluoroglucaric acid (18F-FGA), or a pharmaceutically-acceptable salt thereof. The imaging agent may be disposed in a pharmaceutically-acceptable excipient, carrier, diluent, or vehicle. The imaging agent may be contained within a kit. The disclosure includes in at least one embodiment a method of preparing a radiopharmaceutical such as 18F-FGA for use in imaging.
Type:
Grant
Filed:
November 30, 2017
Date of Patent:
March 23, 2021
Assignee:
THE BOARD OF REGENTS OF THE UNIVERSITY OF OKLAHOMA
Abstract: A method and composition for treating a meningioma in a subject are disclosed. The method includes the step of administering to the subject a therapeutically effective amount of a composition including a cytotoxic agent associated with a phenylbenzothiazole derivative or a stilbene derivative or a biphenylalkyne derivative that accumulates within meningiomas.
Type:
Grant
Filed:
March 29, 2017
Date of Patent:
March 9, 2021
Assignee:
Mayo Foundation for Medical Education and Research
Inventors:
Geoffrey B. Johnson, Val J. Lowe, Mark A. Nathan, Joseph E. Parisi
Abstract: A process for the preparation of a radionuclide imaging agent includes providing an imaging agent including a chelated place-holder metal; loading the imaging agent onto an acid stable stationary phase; replacing the chelated place-holder metal of the imaging agent loaded on the stationary phase with a replacement radioactive metal under mild reaction conditions; and eluting the imaging agent including the chelated replacement radioactive metal from the stationary phase to provide a radionuclide imaging agent suitable for positron emission tomography (PET) or single-photon emission computed tomography (SPECT). The imaging agent can include a targeting agent that is directly conjugated to the imaging agent or by means of a linker. The process may also apply to other metals that are non-radioactive but used as diluent metals or other metals that are strongly bound to DOTA.
Type:
Grant
Filed:
February 26, 2016
Date of Patent:
February 23, 2021
Assignee:
Rochester Institute of Technology
Inventors:
Hans F. Schmitthenner, Anne M. Sweeney-Jones, Scott Williams
Abstract: The present invention relates to new and improved methods of synthesizing radiolabelling agents which can be used to label biomolecules for use as radiopharmaceuticals. It further relates to certain novel radiolabelling agents and their use in such methods. PET imaging methods and methods of diagnosis employing such radiolabelling agents form a further aspect of the invention.
Abstract: The present invention relates to novel compounds of the formula (I) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.
Type:
Grant
Filed:
July 21, 2017
Date of Patent:
December 15, 2020
Assignees:
AC IMMUNE S.A., LIFE MOLECULAR IMAGING SA
Inventors:
Heiko Kroth, Jérôme Molette, Hanno Schieferstein, Andre Müller, Heribert Schmitt-Willich, Mathias Berndt, Felix Oden
Abstract: The present invention relates to novel compounds of the formula (II) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.
Type:
Grant
Filed:
July 21, 2017
Date of Patent:
November 17, 2020
Assignees:
AC IMMUNE S.A., LIFE MOLECULAR IMAGING SA
Inventors:
Heiko Kroth, Jérôme Molette, Vincent Darmency, Hanno Schieferstein, Andre Müller, Heribert Schmitt-Willich, Mathias Berndt, Felix Oden, Emanuele Gabellieri