Halogen Patents (Class 424/1.85)
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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
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Patent number: 8852554Abstract: 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: GrantFiled: October 27, 2010Date of Patent: October 7, 2014Assignee: Janssen Pharmaceutica NVInventors: José Ignacio Andrés-Gil, Meri De Angelis, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen
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Publication number: 20140294725Abstract: The invention concerns various methods of using labeled HSP90 inhibitors to improve treatment of cancer patients with HSP90 inhibitors, including ex vivo and in vivo methods for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor. The disclosure provides a method for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor which comprises the following steps: (a) contacting the tumor or a sample containing cells from the tumor with a detectably labeled HSP90 inhibitor which binds preferentially to a tumor-specific form of HSP90; (b) measuring the amount of labeled HSP90 inhibitor bound to the tumor or the tumor cells in the sample; and (c) comparing the amount of labeled HSP90 inhibitor bound to the tumor or the tumor cells in the sample measured in step (b) to the amount of labeled-HSP90 inhibitor bound to a reference.Type: ApplicationFiled: July 6, 2012Publication date: October 2, 2014Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Nagavarakishore Pillarsetty, Jason S. Lewis, Steven M. Larson, Tony Taldone, Mary L. Alpaugh, Erica M. Gomes
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Publication number: 20140271471Abstract: A non-invasive injectable composition that contains type I collagen, an osteogenic growth factor (OSF), such as a bone morphogenetic protein and a reverse thermo-sensitive biodegradable polymer such as Poloxamer 407 in an aqueous vehicle. The formulation can be administered non-invasively, e.g., by injection, thus circumventing limitations of many currently marketed bone-inducing products. The injectable osteogenic formulation effectively induces bone formation at the desired locale. This injectable suspension could be used with bioresorbable bone mineral composites (e.g., Hydroxyapatite, Tri-calcium phosphate) and/or glycosaminoglycans (e.g., Hyaluronic acid, Heparin sulfate) to mold as putty and/slab as bone graft substitute implants to induce new bone formation in fracture healing and spine fusion procedures.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Genzyme CorporationInventors: Kuber T. Sampath, Michael Philbrook, Aviva Shiedlin, John M. McPherson
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Publication number: 20140271472Abstract: Lung volume reduction by isolating a target lung portion from the rest of the lung with a mass of extracellular matrix (“ECM”) material. The procedure can be performed by locating a tube within the lumen of an airway to be obstructed and depositing an amount of flowable or other ECM in the open space until the lumen is occluded. Optionally, the procedure may be performed by delivering a plug substantially comprised of ECM material into the lumen of an airway to be obstructed. Further optionally, the ECM plug may include a one-way valve to allow air and mucous to escape from the isolated lung portion.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: UMESH H. PATEL, BHAVIN SHAH, MICHELLE CHUTKA
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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
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Publication number: 20140255308Abstract: Compounds of formula: in which R4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.Type: ApplicationFiled: May 19, 2014Publication date: September 11, 2014Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTERInventors: Gavril Pasternak, Susruta Majumdar
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Publication number: 20140248213Abstract: The present invention provides for heptamethine cyanine dyes that possess both nuclear and near-infrared imaging capabilities. These dyes can be used for imaging, targeting and detecting tumors in patients.Type: ApplicationFiled: October 5, 2012Publication date: September 4, 2014Applicants: CEDARS-SINAI MEDICAL CENTER, UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Leland W. K. Chung, Dongfeng Pan
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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
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Publication number: 20140227183Abstract: Hsp90 inhibitors having are provided having the formula: (I) with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.Type: ApplicationFiled: April 18, 2014Publication date: August 14, 2014Applicant: MEMORIAL SLOAN KETTERING CANCER CENTERInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
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Patent number: 8795630Abstract: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.Type: GrantFiled: August 28, 2009Date of Patent: August 5, 2014Assignee: Treventis CorporationInventors: Sultan Darvesh, Eric Joy, Earl Martin, Ian Macdonald, Ian Pottie
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Patent number: 8795631Abstract: The present invention relates to 18F radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.Type: GrantFiled: October 20, 2009Date of Patent: August 5, 2014Assignees: HammerSmith Imanet Limited, GE Healthcare LimitedInventors: Robert James Domett Nairne, Erik Arstad, Matthias Eberhard Glaser
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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
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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
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Publication number: 20140178298Abstract: 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: December 9, 2013Publication date: June 26, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Amin I. Kassis, Ravi S. Harapanhalli
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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
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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
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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
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Patent number: 8741262Abstract: The present invention concerns a therapeutically labeled napthodianthrone or phenanthro[1,10,9,8-opqra]perylene-7,14-dione compound, which comprises a chemical element or an isotope that has an unstable nucleus and emits radiation during its decay to a stable form sufficient to destroy neighboring cells or tissues for use in a targeted radiotherapy to enhance curability of a warm-blooded animal that has been subjected to a necrosis-inducing antitumor therapy. A particular advantage of present invention is that viable rim resistant to a necrosis-inducing antitumor therapy such as vascular targeting agent (VTA) can be supplemented by one single or repeated doses of a therapeutically radiolabeled small molecule necrosis-avid chemical compound treatment to enhance the curability.Type: GrantFiled: November 26, 2008Date of Patent: June 3, 2014Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Yicheng Ni, Marie Van De Putte, Peter DeWitte, Alfons Verbruggen, Guy Marchal, Ziping Sun
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Publication number: 20140134106Abstract: The present invention describes oxidized avidin, suitable for inhalation, for conditioning the lung affected by inoperable/diffuse diseases, enabling the targeted delivery of biotinylated therapeutic agents to it.Type: ApplicationFiled: July 25, 2012Publication date: May 15, 2014Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.Inventor: Rita De Santis
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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
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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.
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Patent number: 8697032Abstract: The present invention relates to compositions and methods for preparing radiopharmaceutical compounds in high chemical-purity and isotopic-purity. The present invention provides polymer-bound precursors to radiopharmaceutical compounds that can be converted to radiopharmaceutical compounds in one step. In a preferred embodiment, a radiopharmaceutical precursor is bound to a polymeric support via a prosthetic group comprising an alkenyl-tin bond. The radiopharmaceutical precursor is converted to a radiopharmaceutical compound in one step involving cleavage of the alkenyl-tin bond and incorporation of a radioisotope to form the radiopharmaceutical compound. Importantly, the polymeric support containing the toxic tin by-product can be easily removed from the radiopharmaceutical compound by filtration. The present invention can be used to install a large number of different radioisotopes. In a preferred embodiment, the radioisotope is 211At, 123I, or 131I.Type: GrantFiled: April 3, 2013Date of Patent: April 15, 2014Assignee: University of Western OntarioInventors: Duncan Hunter, M. Karen J. Gagnon
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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
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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
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Publication number: 20140093453Abstract: The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4)alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or a group of formula (?): —Y—Z—W—R11??(?) wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a —N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.Type: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), LABORATOIRES CYCLOPHARMA, UNIVERSITE D'AUVERGNE CLERMONT 1, COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVESInventors: Jean-Michel CHEZAL, Frederic DOLLE, Jean-Claude MADELMONT, Aurelie MAISONIAL, Elisabeth MIOT-NOIRAULT, Nicole MOINS, Janine PAPON, Bertrand KUHNAST, Bertrand TAVITIAN, Raphael BOISGARD
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Publication number: 20140079633Abstract: The present invention provides a method of preparing [123I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/?mol and radiochemical purity of 95%. The present invention further provides a method of applying [123I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.Type: ApplicationFiled: February 1, 2013Publication date: March 20, 2014Applicant: NATIONAL TSING HUA UNIVERSITYInventors: Chung-Shan Yu, Ho-Lien Huang, Chun-Nan Yeh, Wei-Yuan Lee, Kang-Wei Chang, Ying-Cheng Huang, Kun-Ju Lin, Ching-Shiuann Yang, Shu-Fan Tien, Wen-Chin Su, Jenn-Tzong Chen, Wuu-Jyh Lin, Shiou-Shiow Farn
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Publication number: 20140079634Abstract: A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-N-(3-iodoprop-2E-enyl)-2?-carbomethoxy-3?-(4-methylphenyl) nortropane.Type: ApplicationFiled: September 13, 2013Publication date: March 20, 2014Applicant: NAVIDEA BIOPHARMACEUTICALS INC.Inventors: Stephen B. Haber, Richard Thorn
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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
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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
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Publication number: 20140065070Abstract: The present application relates to methods of preparing radiohalogenated compounds, to compounds useful in such methods and to radiohalogenated compounds useful for imaging and/or therapy.Type: ApplicationFiled: August 28, 2013Publication date: March 6, 2014Applicant: MCMASTER UNIVERSITYInventors: John Valliant, Alla Darwish, Stephanie Rathmann, Afaf Genady
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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
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Publication number: 20140050663Abstract: Contemplated compositions and methods are employed to bind in vitro and in vivo to an ?4?2 nicotinic acetylcholine receptor in a highly selective manner. Where such compounds are labeled, compositions and methods employing such compounds can be used for PET and SPECT analysis. Alternatively, and/or additionally contemplated compounds can be used as antagonists, partial agonists or agonists in the treatment of diseases or conditions associated with ?4?2 dysfunction.Type: ApplicationFiled: February 6, 2013Publication date: February 20, 2014Applicant: The Regents of the University of CaliforniaInventors: Jogeshwar Mukherjee, Sharon A. Kuruvilla
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Publication number: 20140037544Abstract: A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-2?-carbomethoxy-3?-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: Alseres Pharmaceuticals, Inc.Inventors: Chris Sterzinger, Cara Ferreira, David Leyh, Richard Thorn
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Patent number: 8641903Abstract: The present invention is related to a method to obtain reactive [18F] fluorides in an organic medium suitable for radiolabelling without any azeotropic evaporation step, by the use of a solid phase extraction column containing a modified non-ionic solid support.Type: GrantFiled: April 22, 2008Date of Patent: February 4, 2014Assignees: Trasis S.A., Universite de LiègeInventors: Samuel Voccia, Joël Aerts, Christian Lemaire, André Luxen, Jean-Luc Morelle, Gauthier Philippart
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Patent number: 8642008Abstract: To provide a molecular probe for imaging of pancreatic islets. A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe includes any one of the following polypeptides: polypeptides represented by the following formulae (1), (5), and (9); and polypeptides having homology with the foregoing polypeptides: Z-DLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2? (1) Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2? (5) B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2? (9) where X in the formulae (1) and (5) and B- in the formula (9) indicate that an amino group is labeled with a group represented by the formula (I) below having an aromatic ring, wherein A represents either an aromatic hydrocarbon group or an aromatic heterocyclic group, R1 represents a substituent that contains radioactive iodine, R2 represents either a hydrogen atom or a substituent different from that represented by R1, and R3 represents any one of a bond, a methylene group, and an oxymethylene group.Type: GrantFiled: August 31, 2010Date of Patent: February 4, 2014Assignees: Kyoto University, ARKRAY, Inc.Inventors: Nobuya Inagaki, Hideo Saji, Kentaro Toyoda, Hiroyuki Kimura, Yu Ogawa, Konomu Hirao, Kenji Nagakawa, Hirokazu Matsuda
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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
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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
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Publication number: 20140030188Abstract: A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; 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; R? is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.Type: ApplicationFiled: May 9, 2013Publication date: January 30, 2014Applicant: Molecular Insight Pharmaceuticals, Inc.Inventor: Molecular Insight Pharmaceuticals, Inc.
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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
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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
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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
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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
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Publication number: 20130336889Abstract: A nanoparticle for detecting or treating a tumor is provided. The nanoparticle includes a plurality of polymer backbones and at least one first detectable substance, of which each of the polymer backbones includes a hydrophobic region, a hydrophilic region and a chelating region, and the first detectable substance is bound to the chelating region of the polymer backbone. The hydrophobic regions of the polymer backbones form a core block, and the hydrophilic regions of the polymer backbones form a shell block surrounding the core block. A method for detecting or treating a tumor using the nanoparticle is also provided.Type: ApplicationFiled: June 14, 2012Publication date: December 19, 2013Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Ming-Jium Shieh, Cheng-Liang Peng, Tsai-Yueh Luo
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Patent number: 8597613Abstract: A radiolabeled lymphatic staining agent is mixed on site with a much larger amount, on a weight basis, of a non-radiolabeled lymphatic staining agent to form an injectable radiolabeled lymphatic staining agent suitable for surgical use in humans. Preferably, the radiolabel is I-125, because it has a 60-day half-life which enables it to be made off-site. The preferred radiolabeled lymphatic staining agent is iodinated methylene blue, because it can be mixed with a range of non-radioactive lymphatic staining agents, for example isosulfan blue, methylene blue, patent blue, and patent blue V, to provide the injected agent with sufficient radioactivity to enable machine detection. A method for making radioiodinated methylene blue is also disclosed.Type: GrantFiled: July 2, 2004Date of Patent: December 3, 2013Assignee: Iso-Tex Diagnostics, IncInventors: Thomas J. Maloney, Arthur E. Camp, Jr., Jesse J. Hernandez
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Publication number: 20130315825Abstract: Derivatives of phenothiazine, phenoxazine, and phenazine compounds and their use as ?-synuclein ligands are described. Also described are methods of using these compounds and their radiolabeled analogs for the detection, monitoring, and treatment of synucleinopathies, including Parkinson's disease.Type: ApplicationFiled: May 3, 2013Publication date: November 28, 2013Applicant: Washington UniversityInventors: Zhude Tu, Robert Mach, Lihai Yu, Paul Kotzbauer
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Publication number: 20130315827Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: ApplicationFiled: May 28, 2013Publication date: November 28, 2013Applicants: Fluoropharma, Inc., The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Publication number: 20130302246Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.Type: ApplicationFiled: February 7, 2013Publication date: November 14, 2013Inventor: The General Hospital Corporation
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Patent number: 8574545Abstract: A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [123I]-2?-carbomethoxy-3?-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane.Type: GrantFiled: March 24, 2009Date of Patent: November 5, 2013Assignee: Alseres Pharmaceuticals, Inc.Inventors: Chris Sterzinger, Cara Ferreira, David Leyh, Richard Thorn
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Publication number: 20130287687Abstract: The present disclosure relates to organic chemistry and in particular to a series of corticotropin releasing factor type-1 (CRF1) receptor ligand compounds and compositions, as well as methods of preparation and treatment.Type: ApplicationFiled: April 30, 2013Publication date: October 31, 2013Inventor: EMORY UNIVERSITY