Nonmetal Radionuclide Or Intended Radionuclide (e.g., Carbon) Patents (Class 424/1.81)
-
Patent number: 8906392Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.Type: GrantFiled: November 24, 2010Date of Patent: December 9, 2014Assignee: University of KansasInventors: Cory J. Berkland, Lianjun Shi, Nashwa El Gendy, Carl Plumley, Mark Bailey
-
Publication number: 20140348748Abstract: Derivatives of benzothiazolylbenzeneamines useful as imaging agents for nuclear imaging such as positron emission tomography of beta-amyloids are described. Methods of detecting amyloid using the compounds are described. Also disclosed is a radiolabeling method for selected compounds.Type: ApplicationFiled: September 13, 2012Publication date: November 27, 2014Inventors: Lisheng Cai, Victor W. Pike
-
Patent number: 8889100Abstract: The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.Type: GrantFiled: March 6, 2014Date of Patent: November 18, 2014Assignee: Immunomedics, Inc.Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
-
Patent number: 8877160Abstract: The present invention provides methods for treating, detecting and locating recurrence of cancer, radiation and chemo insensitive cancer or metastasis of cancer selected from the group consisting of Lung cancer, Adrenal cancer, Melanoma, Colon cancer, Colorectal cancer, Ovarian cancer, Prostate cancer, Liver cancer, Subcutaneous cancer, Squamous cell cancer, Intestinal cancer, Hepatocellular carcinoma, Retinoblastoma, Cervical cancer, Glioma, Breast cancer and Pancreatic cancer in subject using phospholipid ether analogs.Type: GrantFiled: August 12, 2013Date of Patent: November 4, 2014Assignee: Cellectar, Inc.Inventors: Jamey P. Weichert, Marc Longino, Anatoly Pinchuk
-
Patent number: 8877159Abstract: The present invention provides methods and uses of phospholipid ether analogs as diagnostic and therapeutic agents for numerous cancers.Type: GrantFiled: August 12, 2013Date of Patent: November 4, 2014Assignee: Cellectar, Inc.Inventors: Jamey P. Weichert, Marc Longino, Anatoly Pinchuk
-
Patent number: 8858911Abstract: Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particularly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.Type: GrantFiled: October 7, 2010Date of Patent: October 14, 2014Assignee: Intra-Cellular Therapies, Inc.Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
-
Publication number: 20140301947Abstract: A method for aiding in selecting or adjusting a dose of TSPO imaging or therapeutic agent for use with a subject, the method comprising the step of determining the subject's genotype for TSPO rs6971. A TSPO imaging or therapeutic agent for use in TSPO imaging or therapy in a subject, wherein the subject is a subject whose genotype at TSPO polymorphism position rs6971 is determined. The subject's genotype for TSPO may be taken into account when assessing the results of the TSPO imaging, for example normalising the subject's determined measure of binding of the TSPO agent to take account of the subject's determined genotype. The subject's genotype for TSPO may be taken into account when choosing the TSPO agent and/or the dose of TSPO agent. The subject may be a subject who has been determined to have genotype CC or CT at TSPO polymorphism position rs6971, for example when using a TSPO agent that binds with higher affinity to Aia147TSPO than to Thr147TSPO.Type: ApplicationFiled: May 31, 2012Publication date: October 9, 2014Applicant: IMPERIAL INNOVATIONS LIMITEDInventors: David Owen, Martin Wilkins
-
Patent number: 8846000Abstract: The present invention is directed to radiolabeled pyrimidinone compounds of general structural formula I which are useful as radiotracers for quantitative imaging of PDE10 in mammals.Type: GrantFiled: May 26, 2010Date of Patent: September 30, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Broc A. Flores, Eric Hostetler, Hong Fan
-
Patent number: 8834843Abstract: The present invention relates to a method useful in facilitating the identification of fibrogenesis in a subject. The method of the invention is particularly useful when applied as part of a method to diagnose fibrogenesis of the liver. The invention also provides a compound for use in a method for identification of fibrogenesis in a subject A further aspect of the invention is a compound for use in the preparation of a medicament for use in a method for identification of fibrogenesis in a subject.Type: GrantFiled: November 19, 2008Date of Patent: September 16, 2014Assignee: GE Healthcare LimitedInventors: Ben Newton, Salah Chettibi, Magne Solbakken
-
Patent number: 8834841Abstract: The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).Type: GrantFiled: April 5, 2013Date of Patent: September 16, 2014Assignee: Emory UniversityInventor: Mark M. Goodman
-
Patent number: 8808665Abstract: The present application discloses compositions and methods of synthesis and use involving click chemistry reactions for in vivo or in vitro formation of therapeutic and/or diagnostic complexes. Preferably, the diagnostic complex is of use for 18F imaging, while the therapeutic complex is of use for targeted delivery of chemotherapeutic drugs or toxins. More preferably, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment, using a click chemistry reaction involving cyclooctyne, nitrone or azide reactive moieties. In most preferred embodiments, the click chemistry reaction occurs in vivo. In vivo click chemistry is not limited to 18F labeling but can be used for delivering a variety of therapeutic and/or diagnostic agents.Type: GrantFiled: November 18, 2013Date of Patent: August 19, 2014Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
-
Patent number: 8802053Abstract: Radiotracer vorozole compounds for in vivo and in vitro assaying, studying and imaging cytochrome P450 aromatase enzymes in humans, animals, and tissues and methods for making and using the same are provided. [N-radio-methyl] vorozole substantially separated from an N-3 radio-methyl isomer of vorozole is provided. Separation is accomplished through use of chromatography resins providing multiple mechanisms of selectivity.Type: GrantFiled: March 19, 2013Date of Patent: August 12, 2014Assignee: Brookhaven Science Associates, LLCInventors: Sung Won Kim, Anat Biegon, Joanna S. Fowler
-
Patent number: 8795629Abstract: Radiotracer vorozole compounds for in vivo and in vitro assaying, studying and imaging cytochrome P450 aromatase enzymes in humans, animals, and tissues and methods for making and using the same are provided. [N-radio-methyl] vorozole substantially separated from an N-3 radio-methyl isomer of vorozole is provided. Separation is accomplished through use of chromatography resins providing multiple mechanisms of selectivity.Type: GrantFiled: February 11, 2010Date of Patent: August 5, 2014Assignee: Brookhaven Science Associates, LLCInventors: Sung Won Kim, Anat Biegon, Joanna S. Fowler
-
Patent number: 8778304Abstract: Translocator protein (TSPO) targeting compounds are described. Methods of making the compounds, and uses of the compounds for imaging are also described.Type: GrantFiled: February 24, 2011Date of Patent: July 15, 2014Assignee: The Johns Hopkins UniversityInventors: Martin G. Pomper, Haofan Wang, Tomas R. Guilarte
-
Patent number: 8778305Abstract: Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.Type: GrantFiled: July 31, 2009Date of Patent: July 15, 2014Assignee: The Johns Hopkins UniversityInventors: Martin Pomper, Ronnie Charles Mease, Ying Chen
-
Patent number: 8778303Abstract: The invention encompasses radiopharmaceutical compounds that can be used in imaging cell death associated with either apoptosis or necrosis. Phosphatidylethanolamine (PtdE) is externalized to the surface of apoptotic cells, and also becomes accessible in necrotic cells due to compromised plasma membrane integrity. Duramycin, a 19 amino acid polypeptide, binds PtdE at a 1:1 ratio with high affinity and exclusive specificity. Novel Duramycin-based radiopharmaceuticals and non-radioactively labeled compounds are disclosed herein. Such compounds facilitate detection of cell apoptosis and/or necrosis by binding to PtdE. The location of the bound compound can then be pinpointed using standard imaging techniques.Type: GrantFiled: January 10, 2011Date of Patent: July 15, 2014Assignee: The Medical College of Wisconsin, Inc.Inventor: Ming Zhao
-
Publication number: 20140178304Abstract: The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.Type: ApplicationFiled: August 21, 2012Publication date: June 26, 2014Inventors: Takahiko Taniguchi, Shotaro Miura, Tomoaki Hasui, Christer Halldin, Vladimir Stepanov, Akihiro Takano
-
Patent number: 8758726Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.Type: GrantFiled: August 28, 2013Date of Patent: June 24, 2014Assignee: Immunomedics, Inc.Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
-
Patent number: 8753605Abstract: In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein, embodiments of the present disclosure, in one aspect, relate to methods of detecting the over-expression of epidermal growth factor receptor (EGFR) in a subject or sample, methods of diagnosing the presence of one or more angiogenesis related diseases or related biological events in a subject or sample, method of monitoring the progress of one or more angiogenesis related diseases or related biological events in a subject or sample, a 18F-FBEM-CYS-ZEGFR:1907 probe, compositions including a 18F-FBEM-CYS-ZEGFR:1907 probe, and pharmaceutical compositions including a 18F-FBEM-CYS-ZEGFR:1907 probe and the like.Type: GrantFiled: August 30, 2011Date of Patent: June 17, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Zhen Cheng, Sanjiv Sam Gambhir, Zheng Miao, Hongguang Liu, Gang Ren
-
Publication number: 20140154182Abstract: The invention is directed to a N,N-substituted guanidine compound or a salt or solvate thereof according to formula (1), R1RNC(NH)NR2R3, wherein R1 is methyl and R2 is hydrogen. R3 is a organic group comprising a halogen and thiomethyl substituted phenyl group. R is an organic group comprising a substituted aryl group Z wherein the substituent group is —Y—R4, wherein Y is a heteroatom chosen from the group consisting of O, S and N and R4 is a fluorinated organic group.Type: ApplicationFiled: May 30, 2012Publication date: June 5, 2014Applicant: STICHTING VU-VUMCInventors: Pieter Jacob Klein, Athansios Metaxas, Albert Dirk Windhorst, Johannes Antonius Maria Christiaans, Bart Nicolaas Maria van Berckel
-
Patent number: 8741261Abstract: Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.Type: GrantFiled: March 22, 2005Date of Patent: June 3, 2014Assignee: GE Healthcare LimitedInventors: Bengt Langstrom, Julien Barletta, Hisashi Doi, Masaaki Suzuki, Ryoji Noyori, Yasuyoshi Watanabe, Farhad Karimi
-
Publication number: 20140134105Abstract: The present invention relates to a composition and method for the detection of a detectable product formed from a compound of the present invention in the body of an individual. The detectable product may include a halide or a benzenetriol-based or benzenetetrol-based product of a dehalogenation reaction in the presence of FROS. In many embodiments, an indigo-like product formed from an indigogenic compound of the present invention may also be a detectable product for diagnostic purposes. This indigo-like product may have a higher residence time in tissues where it is formed, thus providing a detectable product localized to sites of high FROS. An indigogenic compound containing one or more radioactive isotopes is further provided for therapeutic purposes.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Inventor: Keith R. Latham
-
Publication number: 20140120036Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by 5-HT6 receptor ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as 5-HT6 positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 21, 2012Publication date: May 1, 2014Inventor: Lawrence A. Black
-
Patent number: 8709381Abstract: The present disclosure relates to a compound comprising at least one of a carbon or an oxygen isotope and a process for preparing the compound. The process comprises irradiating a compound comprising at least one of a carbon or an oxygen atom using photons or particles having an energy in the range of 20 MeV-430 MeV. The carbon and/or the oxygen atom is then allowed to be converted into a carbon and/or an oxygen positron nuclide through a photonuclear reaction. Provided that the molecular structure of the compound is not disrupted, the compound comprising the carbon and/or the oxygen isotope is prepared. The compound may be used in positron and/or other nuclide imaging to obtain a distribution and/or metabolic image of the compound in a human and/or animal body.Type: GrantFiled: September 25, 2011Date of Patent: April 29, 2014Assignee: Beijing Top Grade Medical Equipment Co., LtdInventors: Jun Zeng, Qiyin Sun
-
Patent number: 8709382Abstract: The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.Type: GrantFiled: May 20, 2013Date of Patent: April 29, 2014Assignee: Immunomedics, Inc.Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
-
Publication number: 20140112868Abstract: The invention relates to a new class of compounds with high affinity and selectivity towards P-glycoprotein. The invention also relates to the utilization of such compounds in the in vivo diagnosis of neurodegenerative diseases and as medicaments for use in the prevention and treatment of neurodegenerative disease involving P-glycoprotein.Type: ApplicationFiled: May 24, 2011Publication date: April 24, 2014Applicant: UNIVERSITA' DEGLI STUDI DI BARI "ALDO MORO"Inventors: Nicola Antonio Colabufo, Francesco Berardi, Mariangela Cantore, Marialessandra Contino, Marcello Leopoldo, Roberto Perrone
-
Publication number: 20140112867Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes. The invention further provides a radio-labelled derivative thereof.Type: ApplicationFiled: June 4, 2012Publication date: April 24, 2014Inventors: Edilio Borroni, Luca Gobbi, Hans Hilpert, Michael Honer, Dieter Muri, Robert Narquizian, Alessandra Polara
-
Publication number: 20140105820Abstract: 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: October 9, 2013Publication date: April 17, 2014Applicant: University of Pittsburgh-of the Commonwealth System of Higher EducationInventors: William E. Klunk, Chester A. Mathis, JR.
-
Patent number: 8691187Abstract: Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: GrantFiled: February 25, 2011Date of Patent: April 8, 2014Assignee: Eli Lilly and CompanyInventors: Anna Katrin Szardenings, Wei Zhang, Dhanalakshmi Kasi, Anjana Sinha, Umesh B. Gangadharmath, Joseph C. Walsh
-
Patent number: 8691185Abstract: 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: July 12, 2012Date of Patent: April 8, 2014Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
-
Publication number: 20140086836Abstract: The present invention provides methods for predicting whether a subject will develop a disease capable of affecting cognitive function. More specifically, the present invention relates to the predictive detection of neurological diseases in a subject. The methods and systems provided enable a quantitative assessment and theoretical predictions of neocortical amyloid loading or amyloid beta levels based on the measurement of biomarkers in biological fluids that will provide an indication of whether a subject is likely to develop a neurological disease, such as Alzheimer's disease (AD).Type: ApplicationFiled: May 3, 2012Publication date: March 27, 2014Applicants: MENTAL HEALTH RESEARCH INSTITUTE, Commonweath Scientific and Industrial Research Organisation, NATIONAL AGEING RESEARCH INSTITUTE, EDITH COWAN UNIVERSITYInventors: Samantha C. Burnham, Noel Faux, Simon M. Laws
-
Patent number: 8679452Abstract: Methods and reagents for miniaturized carboxylation with carbon-isotope labeled carbon dioxide using Grignard reagents or other organometallic reagents in a closable reaction loop or reactor are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals or precursors for radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.Type: GrantFiled: December 19, 2006Date of Patent: March 25, 2014Assignee: GE Healthcare LimitedInventors: Tor Kihlberg, Bengt Langstrom
-
Publication number: 20140079635Abstract: A method of detecting myelin in a subject includes administering to the subject a molecular probe that includes a fluorescent trans stilbene derivative and detecting the amount or distribution of the molecular probe in a tissue of interest of the subject.Type: ApplicationFiled: April 29, 2013Publication date: March 20, 2014Applicant: Case Western Reserve UniversityInventor: Case Western Reserve University
-
Patent number: 8668900Abstract: The cancer-imaging agent and method of radioimaging relates to the use of a radioimaging agent for the imaging increased choline uptake to detect cancerous tissue. The radioimaging agent includes choline or a pharmaceutically acceptable salt thereof labeled with technetium-99m. Preferably, the radioimaging agent is [methyl]-choline chloride labeled with 99mTcO4, which carries technetium-99m. In use, a patient is administered an effective amount of the radioimaging agent by injection and then scanned with a radioimaging device. The radioimaging agent is used to image select soft tissues in the patient, such as the liver or gallbladder, the upper abdominal organs, or the like, and to detect increased choline uptake. Choline is known to accumulate in cancerous cells. Thus, the radioimaging agent is particularly effective in the detection of potentially cancerous tissues.Type: GrantFiled: February 15, 2011Date of Patent: March 11, 2014Assignee: Kuwait UniversityInventor: Fatma Jassab Faleh Marzooq Al-Saeedi
-
Patent number: 8663602Abstract: The invention enables high-throughput screening of compounds in living systems to detect unanticipated or unintended biological actions. The invention also allows for screening, detection, and confirmation of new indications for approved drugs. Screening and detection of toxic effects of compounds also can be achieved by using the methods of the invention. The methods comprise administering isotope-labeled substrates to a living system so that the label is incorporated into molecules in a manner that reveals flux rates through metabolic pathways thought to be involved in a disease. Comparisons between living systems exposed to compounds and living systems not so exposed reveals the effects of the compounds on the flux rates through the metabolic pathways. Combinations or mixtures of compounds can be systematically screened to detect unanticipated or unintended biological actions, including synergistic actions, in the same manner.Type: GrantFiled: February 18, 2011Date of Patent: March 4, 2014Assignee: The Regents of the University of CaliforniaInventor: Marc K. Hellerstein
-
Patent number: 8658132Abstract: 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: GrantFiled: August 2, 2012Date of Patent: February 25, 2014Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Daisaku Nakamura, Soichi Nakamura, Masahito Toyama, Akio Hayashi
-
Patent number: 8658129Abstract: The present invention relates to agents capable of binding to myelin basic protein in a subject. Also provided are methods for the detection of myelin-associated neuropathy comprising identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, administering to a subject an agent that binds specifically to myelin basic protein, and determining myelination in the subject by detecting the agent present in the subject. A kit containing the agent or its derivatives for use in detecting myelin basic protein is also provided.Type: GrantFiled: February 21, 2011Date of Patent: February 25, 2014Assignee: General Electric CompanyInventors: Rong Zhang, Tiberiu Mircea Siclovan, Cristina Abucay Tan Hehir, Victoria Eugenia Cotero, Bruce Fletcher Johnson
-
Patent number: 8658131Abstract: Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for ?1 receptors. Some compounds are also highly selective for ?1 receptor compared to ?2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of ?1 receptor in a subject such as a human using positron emission tomography (PET) scanning.Type: GrantFiled: June 21, 2011Date of Patent: February 25, 2014Assignee: Washington UniversityInventors: Zhude Tu, Robert H. Mach, Wei Wang, Stanley M. Parsons
-
Patent number: 8652440Abstract: The present invention relates to methods for determining whether a mammal has a disease, such as diabetes, using PET data analysis techniques. These methods include administering to a mammal a PET-compatible tracer, such as a radioligand specific for a vesicular monoamine transporter 2 (VMAT2) receptor, and measuring total functional ?-cell capacity (volume) of the mammal's pancreas using PET data analysis techniques. Methods for tracking the efficacy of a treatment for diabetes, for evaluating the regeneration of ?-cells in a pancreas, and for monitoring a patient with a transplanted pancreas are also provided.Type: GrantFiled: May 9, 2008Date of Patent: February 18, 2014Assignee: The Trustees of Columbia University in the City of New YorkInventor: Masanori Ichise
-
Publication number: 20140030191Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.Type: ApplicationFiled: April 20, 2012Publication date: January 30, 2014Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
-
Publication number: 20140030189Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.Type: ApplicationFiled: June 12, 2013Publication date: January 30, 2014Inventors: Ajay Purohit, Thomas D. Harris, Heike S. Radeke, Simon P. Robinson, Ming Yu, David S. Casebier, Michael T. Azure
-
Patent number: 8632752Abstract: The present application discloses compositions and methods of synthesis and use involving click chemistry reactions for in vivo or in vitro formation of therapeutic and/or diagnostic complexes. Preferably, the diagnostic complex is of use for 18F imaging, while the therapeutic complex is of use for targeted delivery of chemotherapeutic drugs or toxins. More preferably, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment, using a click chemistry reaction involving cyclooctyne, nitron or azide reactive moieties. In most preferred embodiments, the click chemistry reaction occurs in vivo. In vivo click chemistry is not limited to 18F labeling but can be used for delivering a variety of therapeutic and/or diagnostic agents.Type: GrantFiled: June 14, 2013Date of Patent: January 21, 2014Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
-
Patent number: 8628750Abstract: Provided herein are compounds or conjugates useful for diagnostic imaging and/or therapeutic purposes. Each compound or conjugate comprises a ligand for the chemokine receptor CXCR4 and a detectable label. The ligand has a binding affinity for the CXCR4 receptor, measured as IC50 in the presence of 125I-CPCR4, of 250 nM or lower, and the ligand comprises a cyclic oligopeptide moiety having the motif B-Arg or B-(Me)Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine, provided that the motif is B-Arg when B is a N?-methyl derivative of a basic amino acid.Type: GrantFiled: February 27, 2007Date of Patent: January 14, 2014Assignee: Technische Universitat MunchenInventors: Hans Jürgen Wester, Norman Koglin, Markus Schwaiger, Horst Kessler, Burkhardt Laufer, Oliver Demmer, Martina Anton
-
Publication number: 20140004044Abstract: The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including for the treatment of demyelinating diseases and/or in vivo imaging of the central nervous system to diagnose and/or assess the progression of MS or other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: The University of ChicagoInventors: Pedro Brugarolas, Brian Popko, Daniel Appelbaum
-
Publication number: 20140004043Abstract: The present invention relates to the cryptophane derivatives of formula (I) capable of encapsulating small molecules such as noble gases for biological and environmental use. In particular, the invention relates to cryptophane derivatives with high affinity for xenon, which can be used as biosensors in clinical imaging.Type: ApplicationFiled: October 12, 2011Publication date: January 2, 2014Applicant: Georgetown UniveristyInventor: Kevin Holman
-
Patent number: 8617518Abstract: 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: March 26, 2013Date of Patent: December 31, 2013Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
-
Patent number: 8617515Abstract: The present invention relates to methods for myelin basic protein detection comprises identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, parenterally administering to the subject the agent, and determining myelination in the subject by detecting binding to myelin basic protein. Methods for the detection of myelin and a quantitative measurement of its local concentration in a sample using an agent with specific binding to myelin basic protein are also provided as is a kit containing the agent or its derivatives for use in detecting myelin basic protein.Type: GrantFiled: June 4, 2009Date of Patent: December 31, 2013Assignee: General Electric CompanyInventors: Cristina Abucay Tan Hehir, Tiberiu Mircea Siclovan, Nicole Evelyn Barnhardt, Kenneth Michael Fish, Randall Lee Carter, Bruce Fletcher Johnson
-
Publication number: 20130343993Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by 5-HT6 receptor ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as 5-HT6 positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 21, 2012Publication date: December 26, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
-
Publication number: 20130343992Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 21, 2012Publication date: December 26, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
-
Publication number: 20130315826Abstract: Various compounds, compositions, and methods for binding to ?-amyloid plaque and norepinephrine transporters are presented. Especially preferred compounds include those with a PET-detectable label.Type: ApplicationFiled: May 22, 2013Publication date: November 28, 2013Applicant: The Regents of the University of CaliforniaInventors: Jogeshwar Mukherjee, Min-Liang Pan