Halogen Patents (Class 424/1.85)
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Publication number: 20130017150Abstract: The disclosure relates to a method for protecting a kidney from renal injury. For example, acute renal injury may be associated with decreased or blocked blood flow in the subject's kidney or exposure to a nephrotoxic agent, such as a radiocontrast dye. The methods include administering to the subject an effective amount of an aromatic-cationic peptide to a subject in need thereof.Type: ApplicationFiled: February 22, 2012Publication date: January 17, 2013Inventors: Hazel H. Szeto, Diane Felsen
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Publication number: 20130011336Abstract: Agents and methods for imaging a cell and/or a portion of tissue characterized by fibrosis, as well as to agents and methods for determining and/or diagnosing fibrotic diseases are disclosed herein. Also disclosed herein are polymer conjugates that can include a detectable label, a retinoid and a polymer. The polymer conjugates can be used to image a portion of tissue, deliver a detectable label to a portion of tissue or a cell and/or diagnosis a condition or disease.Type: ApplicationFiled: September 11, 2009Publication date: January 10, 2013Applicant: NITTO DENKO CORPORATIONInventors: Yoshiro Niitsu, Lei Yu, Gang Zhao, Sang Van, Xinghe Wang, Jian Liu, Sanjib Kumar Das, Yasunobu Tanaka, Keiko Kajiwara, Hirokazu Takahashi, Miyono Miyazaki
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Publication number: 20130004422Abstract: 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: ApplicationFiled: July 12, 2012Publication date: January 3, 2013Inventors: William E. KLUNK, Chester A. MATHIS, JR., Yanming WANG
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Publication number: 20130004420Abstract: The present invention relates to a compound having formula (I): wherein: X is in particular 125I Or 211At; R1 and R?1 are independently from each other chosen preferably from the group consisting of electron-withdrawing groups and alkyl groups; R2 is chosen from the group consisting of: H, alkyl groups, functional groups being able to bind a vector, and functional groups having targeting properties which make the compound of the invention a vector itself; Z is a heteroatom, R5, R8 and R9 are preferably H; Y is preferably an electron withdrawing group.Type: ApplicationFiled: February 20, 2011Publication date: January 3, 2013Inventors: Jean-Francois Gestin, Francois Guerard, Alain Faivre-Chauvet
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Patent number: 8343459Abstract: A method for producing a radioactive diagnostic imaging agent which contains a radioactive halogen-labeled amino acid compound as an effective ingredient and has a composition that can inhibit radiolysis of the effective ingredient, thereby further improving stability, is provided. Disclosed is a method for producing a radioactive diagnostic imaging agent, comprising a solution preparation step of preparing a solution containing a radioactive halogen-labeled amino acid compound, and a dilution step of diluting the solution containing the radioactive fluorine-labeled organic compound in order to adjust radioactive concentration thereof, which further comprises an acid addition step of adding an acid to the solution containing the radioactive fluorine-labeled organic compound, after the solution preparation step and before the dilution step, wherein the acid is added in the acid addition step in an amount sufficient to adjust the pH of the solution resulting from the dilution step to 2.0-5.Type: GrantFiled: February 12, 2008Date of Patent: January 1, 2013Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Daisaku Nakamura, Soichi Nakamura, Masahito Toyama, Akio Hayashi
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Patent number: 8337810Abstract: Oxidants (e.g., N-chlorosuccinimide) can be used to stabilize ?-particle emitters (e.g., 211 At) in solution, prior to their subsequent reaction to form ?-particle emitter labeled compounds (e.g., a radiolabeled pharmaceutical or a radiolabeled pre-cursor used to prepare it). In particular, the use of an oxidant has been found to maintain the ?-particle emitter in a chemical form that facilitates this reaction, which may involve a number of possible mechanisms including electrophilic substitution, nucleophilic substitution, complexation, exchange, or metallic bonding. Compounds labeled with ?-particle emitters in this manner have wide-ranging therapeutic applications, particularly in the treatment of cancer.Type: GrantFiled: December 22, 2006Date of Patent: December 25, 2012Assignee: Duke UniversityInventors: Michael Rod Zalutsky, Oscar Rodolfo Pozzi
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Patent number: 8329142Abstract: 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: GrantFiled: July 23, 2008Date of Patent: December 11, 2012Inventors: Jay W. Pettegrew, Richard J. McClure, Kanagasabai Panchalingam
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Patent number: 8329141Abstract: 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: GrantFiled: March 2, 2007Date of Patent: December 11, 2012Assignee: Board of Regents, The University of Texas SystemInventor: Franklin C. Wong
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Patent number: 8318132Abstract: 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: GrantFiled: February 17, 2009Date of Patent: November 27, 2012Assignee: 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
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Patent number: 8309054Abstract: 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: GrantFiled: July 25, 2007Date of Patent: November 13, 2012Assignee: Hammersmith Imanet LimitedInventor: Erik Arstad
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Patent number: 8309055Abstract: 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: GrantFiled: January 27, 2012Date of Patent: November 13, 2012Assignee: Hammersmith Imanet LimitedInventors: Erik Arstad, Edward George Robins
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Publication number: 20120282180Abstract: 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: ApplicationFiled: June 8, 2011Publication date: November 8, 2012Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
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Patent number: 8303935Abstract: 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: GrantFiled: May 15, 2007Date of Patent: November 6, 2012Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki, Yuki Okumura
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Publication number: 20120276006Abstract: 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: ApplicationFiled: June 21, 2012Publication date: November 1, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
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Publication number: 20120269726Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C1-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: ApplicationFiled: October 12, 2011Publication date: October 25, 2012Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20120269727Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.Type: ApplicationFiled: June 22, 2012Publication date: October 25, 2012Applicant: GE HEALTHCARE ASInventors: ALAN CUTHBERTSON, MAGNE SOLBAKKEN
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Patent number: 8293208Abstract: 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: GrantFiled: May 15, 2009Date of Patent: October 23, 2012Assignee: The Governors of the University of AlbertaInventors: Chris Cheeseman, Frederick West, Tina Grant, Brendan Trayner, John Mercer, Andrei Manolescu
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Publication number: 20120251447Abstract: The present invention provides novel radio iodinated tropanes incorporating triazole or isoxazole rings. Also provided are methods of preparation of said tropanes from functionalised tropane precursors, using click cycloaddition chemistry, as well as radiopharmaceutical compositions comprising such radio iodinated tropanes. The invention also provides in vivo imaging methods using the radio iodinated tropanes.Type: ApplicationFiled: December 21, 2010Publication date: October 4, 2012Inventors: Michelle Emma Avory, Harry John Wadsworth, Robert James Domett Nairne
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Publication number: 20120251449Abstract: 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: ApplicationFiled: December 22, 2010Publication date: October 4, 2012Inventors: Vijaya Raj Kuniyil Kulangara, Alan Cuthbertson, Peter Iveson, Chitralekha Rangaswamy, Veena Rao, Rajiv Bhalla
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Publication number: 20120251448Abstract: 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: ApplicationFiled: March 2, 2012Publication date: October 4, 2012Inventors: 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
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Patent number: 8277777Abstract: 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: GrantFiled: June 21, 2007Date of Patent: October 2, 2012Assignees: Nihon Medi-Physics Co., Ltd., GE Healthcare LimitedInventors: Shigeyuki Tanifuji, Akio Hayashi, Daisaku Nakamura, Shinya Takasaki, Anthony Eamon Storey, Denis Raymond Christophe Bouvet
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Publication number: 20120244071Abstract: There are provided new iodo- and bromo-compounds, and their use as diagnostic agents and imaging agents for diseases and disorders wherein S1P receptor expression is altered.Type: ApplicationFiled: December 8, 2010Publication date: September 27, 2012Applicant: Novartis AGInventors: Yves Auberson, Emmanuelle Briard, David Orain
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Publication number: 20120244074Abstract: 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: ApplicationFiled: December 16, 2010Publication date: September 27, 2012Inventor: Magne Solbakken
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Publication number: 20120244072Abstract: The present invention relates to an improved synthesis of N-monofluoroalkyl tropanes using fluoroalkyl iodides or fluoroalkyl sulfonate esters. The invention also provides the use of such method to prepare the non-radioactive tropane intermediate FP-CIT, and its subsequent conversion to the 123I-labelled radiopharmaceutical DaTSCAN™ (123I-ioflupane). Also provided is the use of fluoroalkyl iodides or fluoroalkyl sulfonate esters in the alkylation method of the invention.Type: ApplicationFiled: December 15, 2010Publication date: September 27, 2012Inventors: Lorenzo Williams, Gunnar Keilen, Jarle Andre Haugan
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Publication number: 20120237445Abstract: 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: ApplicationFiled: April 15, 2010Publication date: September 20, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: James F. Castner, Dianne D. Zdankiewicz, James E. Anderson
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Patent number: 8268291Abstract: The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.Type: GrantFiled: February 23, 2009Date of Patent: September 18, 2012Assignee: The General Hospital CorporationInventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
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Patent number: 8257684Abstract: 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: GrantFiled: March 26, 2009Date of Patent: September 4, 2012Assignee: Neurosigma, Inc.Inventors: Alejandro Covalin, Antonio Afonso Ferreira De Salles
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Publication number: 20120219500Abstract: 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: ApplicationFiled: October 25, 2010Publication date: August 30, 2012Applicant: FUJIFILM RI PHARMA CO., LTD.Inventors: Kazuhisa Sakurai, Akio Nagano
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Publication number: 20120213702Abstract: 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: ApplicationFiled: August 31, 2010Publication date: August 23, 2012Inventors: Christoph Bremer, Carsten Höltke
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Publication number: 20120213701Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.Type: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Applicant: President and Fellows of Harvard CollegeInventors: Amin I. Kassis, Ravi S. Harapanhalli
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Publication number: 20120207679Abstract: 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: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Applicant: ASTRAZENECA ABInventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmström, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Ström, David Wensbo
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Publication number: 20120201754Abstract: 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: ApplicationFiled: October 7, 2010Publication date: August 9, 2012Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
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Patent number: 8236282Abstract: 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: September 30, 2009Date of Patent: August 7, 2012Assignee: 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: 8231858Abstract: The present invention relates to the field of diagnostic imaging. Specifically, the invention relates to the diagnostic imaging of diseases where specific matrix metalloproteinases are known to be involved. One embodiment of the invention is a compound having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the diagnostic imaging agent of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention. The pharmaceutical composition of the invention may be used in the diagnosis of diseases where specific matrix metalloproteinases are known to be involved.Type: GrantFiled: February 10, 2004Date of Patent: July 31, 2012Assignee: GE Healthcare LimitedInventors: Anthony Storey, Julie Davis, Sally-Ann Ricketts, Marivi Mendizabal, Alan Cuthbertson, Joseph Arukwe, Kirsty Heywood, Ian Wilson, Duncan Wynn, Michael Schafers, Bodo Levkau, Stefan Wagner, Hans-Jörg Breyholz, Klaus Kopka
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Publication number: 20120189548Abstract: 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: ApplicationFiled: April 5, 2012Publication date: July 26, 2012Applicant: The University of SydneyInventors: Michael Kassiou, Michelle Louise James
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Patent number: 8226929Abstract: 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: GrantFiled: January 15, 2008Date of Patent: July 24, 2012Assignee: Lantheus Medical Imaging, Inc.Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
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Patent number: 8226927Abstract: 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: GrantFiled: May 21, 2007Date of Patent: July 24, 2012Inventors: Farhad Karimi, Bengt Langstrom
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Patent number: 8221720Abstract: The invention relates to novel processes for the purification of radiolabelled tracers, using a solid-support bound scavenger group.Type: GrantFiled: May 11, 2005Date of Patent: July 17, 2012Assignees: Hammersmith Imanet Limited, GE Healthcare Limited, GE Healthcare ASInventors: Sajinder Kaur Luthra, Frank Brady, Nicholas Toby Jeffery, Erik Arstad, Alexander Mark Gibson, Duncan Wynn, Alan Cuthbertson, Magne Solbakken
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Publication number: 20120177572Abstract: The present method for determining the efficacy of therapy in the treatment of amyloidosis involves administering to a patient in need thereof a compound of formula (I) or formula (II) or structures 1-45 and imaging the patient. After said imaging, at least one anti-amyloid agent is administered to said patient. Then, an effective amount of a compound of formula (I) or formula (II) or structures 1-45 is administered to the patient and the patient is imaged again. Finally, baseline levels of amyloid deposition in the patient before treatment with the anti-amyloid agent are compared with levels of amyloid deposition in the patient following treatment with the anti-amyloid agent.Type: ApplicationFiled: March 6, 2012Publication date: July 12, 2012Inventors: William E. KLUNK, Chester A. MATHIS, JR.
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Patent number: 8216547Abstract: The present invention is directed to radiolabelled ligands, useful for the labeling and imaging of TRP M8 (transient receptor potential M8 channel) functionality. The present invention is further directed to pharmaceutical compositions comprising the radiolabelled ligands and methods for the preparation of the radiolabelled ligands.Type: GrantFiled: July 9, 2009Date of Patent: July 10, 2012Assignee: Janssen Pharmaceutica NVInventors: Paul D. Acton, Dennis J. Hlasta, Jay M. Matthews, James J. McNally
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Publication number: 20120171118Abstract: The present invention provides conjugates and methods of using the same for the treatment of cerebral, meningeal, and neural diseases, disorders, and conditions. Provided methods include administering conjugates directly into the cerebrospinal fluid space of an animal.Type: ApplicationFiled: June 11, 2010Publication date: July 5, 2012Applicant: THE GENERAL HOSPITAL CORPORATIONInventor: Mikhail I. Papisov
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Patent number: 8211403Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I): with a compound of formula (II) or, a compound of formula (III): with a compound of formula (IV): in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.Type: GrantFiled: June 20, 2007Date of Patent: July 3, 2012Assignee: Hammersmith Imanet LimitedInventors: Matthias Eberhard Glaser, Erik Arstad
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Patent number: 8202509Abstract: The present application discloses compositions and methods of synthesis and use of 68Ga, 18F or 19F labeled molecules of use in PET or MRI 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 chelating moiety, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 68Ga, 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. In more preferred embodiments, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment.Type: GrantFiled: December 2, 2010Date of Patent: June 19, 2012Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
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Patent number: 8187573Abstract: The invention provides methods and products, such as kits, useful for determining the apoptotic state of cells in an organism, comprising detecting the presence or abundance of at least one caspase affinity labeling agent in the cells of an animal into which at least one caspase affinity labeling agent has been introduced, wherein the presence or abundance of the caspase affinity labeling agent correlates with the apoptotic state of the cells.Type: GrantFiled: October 12, 2006Date of Patent: May 29, 2012Assignee: Immunochemistry Technologies, LLCInventors: Gary L. Johnson, Brian W. Lee
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Patent number: 8163928Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] 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: GrantFiled: January 25, 2007Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Patent number: 8153101Abstract: The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen.Type: GrantFiled: June 17, 2009Date of Patent: April 10, 2012Assignee: Immunomedics, Inc.Inventors: William J. McBride, David M. Goldenberg
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Patent number: 8153100Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F labeled molecules of use in PET or MRI imaging. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a metal complex and binding of the 18F- or 19F-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the 18F or 19F bound to the metal. 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 18F or 19F labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET or MRI imaging.Type: GrantFiled: April 30, 2009Date of Patent: April 10, 2012Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
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Patent number: 8147800Abstract: The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled by the described methods. Preferably, the F-18 may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other embodiments, the F-18 labeled moiety may comprise a targetable construct used in combination with a bispecific or multispecific antibody to target F-18 to a disease-associated antigen, such as a tumor-associated antigen. The F-18 labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET imaging analysis.Type: GrantFiled: June 17, 2011Date of Patent: April 3, 2012Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
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Patent number: 8148559Abstract: Disclosed are processes for development and recovery of lipids from biomass. A plant or microorganism-based biomass can be developed to encourage a desired lipid profile. Following development, ecologically friendly normally gaseous fluids such as carbon dioxide can be pressurized to a supercritical state followed by rapid expansion. The fluid is first contacted with a biomass source including oil-containing microorganisms and/or agricultural products. For instance, fungi or algae can be bioconverted from another biomass sources such as canola seed or corn syrup and then contacted with the high pressure fluid. During a contact period, the fluid can diffuse into the biomass, and in particular through the cell walls of the biomass. The fluid undergoes rapid release of pressure and opens the cell structure for improved release of oil. The fluid can optionally be utilized for extraction following the explosion process. For instance, the fluid can be re-pressurized in the same vessel for extraction processes.Type: GrantFiled: August 28, 2008Date of Patent: April 3, 2012Assignee: Clemson University Research FoundationInventors: Terry H. Walker, Meidui Dong, Keri B. Cantrell, Mark C. Thies
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Patent number: 8147799Abstract: The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen.Type: GrantFiled: August 14, 2009Date of Patent: April 3, 2012Assignee: Immunomedics, Inc.Inventors: William J. McBride, David M. Goldenberg