Halogen Patents (Class 424/1.85)
  • Patent number: 10357576
    Abstract: The present invention is directed towards new 18F-folate/antifolate analog radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: July 23, 2019
    Assignee: MERECK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
  • Patent number: 10336757
    Abstract: Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 2, 2019
    Assignees: Sloan-Kettering Institute for Cancer Research, The Rockefeller University
    Inventors: Gabriela Chiosis, Paul Greengard, Fei Dou, Wenjie Luo, Huazhong He, Danuta Zatorska
  • Patent number: 10131627
    Abstract: 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, C6-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: Grant
    Filed: October 26, 2017
    Date of Patent: November 20, 2018
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Patent number: 9951324
    Abstract: Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical compositions containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: April 24, 2018
    Assignee: Purdue Research Foundation
    Inventors: Philip Stewart Low, Venkatesh Chelvam, Youngsoon Kim, Sumith A. Kularatne
  • Patent number: 9757483
    Abstract: 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: Grant
    Filed: October 17, 2014
    Date of Patent: September 12, 2017
    Assignee: Alseres Pharmaceuticals, Inc.
    Inventors: Chris Sterzinger, Cara Ferreira, David Leyh, Richard Thorn
  • Patent number: 9592308
    Abstract: This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.
    Type: Grant
    Filed: March 7, 2016
    Date of Patent: March 14, 2017
    Assignee: PIRAMAL IMAGING SA
    Inventors: Mathias Berndt, Matthias Friebe, Fabrice Samson, Rainer Braun, Gunnar Garke, Marianne Patt, Andreas Schildan, Christoph Smuda
  • Patent number: 9579406
    Abstract: 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: Grant
    Filed: September 30, 2014
    Date of Patent: February 28, 2017
    Assignee: CELLECTAR BIOSCIENCES, INC.
    Inventors: Jamey P. Weichert, Marc Longino, Anatoly Pinchuk
  • Patent number: 9550002
    Abstract: The present invention provides methods and uses of phospholipid ether analogs as diagnostic and therapeutic agents for numerous cancers.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: January 24, 2017
    Assignee: CELLECTAR BIOSCIENCES, INC.
    Inventors: Jamey P. Weichert, Marc Longino, Anatoly Pinchuk
  • Patent number: 9539220
    Abstract: Methods and compositions for the treatment of treatment-resistant depression are described. More specifically, the invention demonstrates that intranasal administration of ketamine is effective to ameliorate the symptoms of depression in a patient who has not responded to an adequate trial of one antidepressant in the current episode and has recurrent or chronic depressive symptoms (>2 years).
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: January 10, 2017
    Assignees: Icahn School of Medicine at Mount Sinai, Yale University, The United States of America, as represented by The Secretary, Department of Health and Human Services
    Inventors: Dennis S. Charney, Sanjay J. Mathew, Husseini K. Manji, Carlos A. Zarate, John H. Krystal
  • Patent number: 9492571
    Abstract: The invention relates to novel multi-modality probes for imaging, tracking and analyzing stem cells and related biological samples, and methods of preparation and use thereof. The molecular probes of the invention are constructed, for example, by utilizing (a) the high selectivity of long hydrocarbon chains for binding to plasma membranes of cells, (b) a near-infrared (NIR) dye for optical imaging, and (c) a radionuclide for PET or SPECT imaging. The in vitro and in vivo data of the optical and radiolabeled probes demonstrated their utility for detecting the presence of stem cells with multiple imaging modalities.
    Type: Grant
    Filed: May 27, 2013
    Date of Patent: November 15, 2016
    Assignee: University of Massachusetts
    Inventors: Brian D. Gray, Mary Rusckowski, Koon Y. Pak
  • Patent number: 9302018
    Abstract: Disclosed is a near-infrared fluorescent imaging agent comprising an indocyanine-based fluorescent dye and a liposome. The near-infrared fluorescent imaging agent of the present invention demonstrates high fluorescence intensity and a long anchoring time in sentinel lymph nodes, thereby making it useful for detecting sentinel lymph nodes in sentinel lymph node navigation surgery. Also disclosed is an indocyanine green derivative that is particularly suitable for use in the near-infrared fluorescent imaging agent of the present invention.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: April 5, 2016
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Hideki Hayashi, Masanori Fujinami, Taro Toyota, Yutaka Tamura, Akira Aoki, Yutaka Muraki, Kazuki Onoue
  • Patent number: 9290463
    Abstract: The present invention relates to Radiolabeled Compounds labeled with fluorine, bromine, iodine, carbon, or tritium isotopes and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: March 22, 2016
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Joseph John Mann, J. S. Dileep Kumar
  • Patent number: 9278146
    Abstract: A new peptide derivative is provided.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: March 8, 2016
    Assignees: Kyoto University, ARKRAY, Inc.
    Inventors: Hideo Saji, Nobuya Inagaki, Hiroyuki Kimura, Kentaro Toyoda, Konomu Hirao, Hirokazu Matsuda
  • Patent number: 9259398
    Abstract: A composition of bioactive agent-loaded micelles with tissue-targeting properties and methods of using the same are disclosed.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: February 16, 2016
    Assignee: ABBOTT CARDIOVASCULAR SYSTEMS INC.
    Inventors: Kyle Klein, Katsuyuki Murase, Jinping Wan, Dariush Davalian
  • Patent number: 9149547
    Abstract: 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: Grant
    Filed: May 9, 2013
    Date of Patent: October 6, 2015
    Assignee: MOLECULAR INSIGHT PHARMACEUTICALS, INC.
    Inventors: John W. Babich, Craig Zimmerman, Kevin P. Maresca
  • Patent number: 9107952
    Abstract: The invention relates to novel liquid preparation comprising a substituted benzimidazol, preferably pimobendan as pharmaceutically active compound. In particular, the present invention relates to liquid preparation comprising an etherified cyclodextrin derivative, preferably in a concentration of about 20 to 70% (w/v) and said substituted benzimidazol, preferably in a concentration of about 0.005 to 0.15% (w/w).
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: August 18, 2015
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin Folger, Stefan Lehner
  • Patent number: 9028800
    Abstract: 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: Grant
    Filed: May 8, 2014
    Date of Patent: May 12, 2015
    Assignee: Immunomedics, Inc.
    Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
  • Publication number: 20150125389
    Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R5, X1, X2, X3 and X4 are as defined herein, and wherein the compound comprises at least one F, Cl, Br, I or 123I moiety, are provided. Uses of such compounds for imaging diagnostics in cancer and therapeutics methods for treatment of subjects in need thereof, including prostate cancer as well as methods and intermediates for preparing such compounds are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: May 7, 2015
    Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, BRITISH COLUMBIA CANCER AGENCY BRANCH
    Inventors: Raymond John Andersen, Carmen Adriana Banuelos, Javier GARCIA FERNANDEZ, Yusuke IMAMURA, Jian KUNZHONG, Nasrin R. MAWJI, Marianne Dorothy Sadar, Jun Wang, Amy (Hsing Chen) Tien
  • Patent number: 9023317
    Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.
    Type: Grant
    Filed: February 25, 2013
    Date of Patent: May 5, 2015
    Assignee: University of Western Ontario
    Inventors: Duncan H. Hunter, Mustafa Janabi
  • Patent number: 9005577
    Abstract: The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: April 14, 2015
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Kai Chen, Umesh B. Gangadharmath, Gang Chen, Vani P. Mocharla, Dhanalakshmi Kasi, Peter J. H. Scott, Qianwa Liang
  • Patent number: 9005578
    Abstract: 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: Grant
    Filed: May 28, 2013
    Date of Patent: April 14, 2015
    Assignees: Fluoropharma, Inc., The General Hospital Corporation
    Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
  • Patent number: 8986652
    Abstract: 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: Grant
    Filed: February 1, 2013
    Date of Patent: March 24, 2015
    Assignee: National Tsing Hua University
    Inventors: 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
  • Patent number: 8986653
    Abstract: 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: Grant
    Filed: October 2, 2013
    Date of Patent: March 24, 2015
    Assignee: Alseres Pharmaceuticals, Inc.
    Inventors: Chris Sterzinger, Cara Ferreira, David Leyh, Richard Thorn
  • Publication number: 20150079000
    Abstract: The present invention relates to the compound of formula (I), in which R1 represents Sn(R)3, B(OH)2, B(OR)2, a halogen atom, NO2, a radionuclide or a —N+(R)3 group, where R is a (C1-C6) alkyl group, R2 represents a hydrogen atom or a (C1-C6)alkyl group, R3 represents: a —(CH2CH2O)n2—(CH2)n3—X group, or a —(CH2CH2O)n4—(CH2)n5—Y group with Y representing a —C?C—H, a —N3 or a —Ar—(CH2)n6—(OCH2CH2)n7—X group, and X represents a halogen atom, a radionuclide or a —OSO2R? group, where R? is a CF3, CH3, t-Bu, Ph, p-NO2Ph, p-BrPh or p-CH3Ph group, and their addition salts with pharmaceutically acceptable acids, The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT or PET imaging and in therapy of melanoma, via targeted radionuclide therapy.
    Type: Application
    Filed: April 19, 2013
    Publication date: March 19, 2015
    Inventors: Jean-Michel Chezal, Latifa Rbah-Vidal, Emilie Billaud, Philippe Auzeloux, Jean-Claude Madelmont, Aurélien Vidal, Elisabeth Miot-Noirault, Janine Papon, Aurélie Maisonial
  • Publication number: 20150056138
    Abstract: The invention features compounds and methods relating to hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters useful for diagnostic purposes. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention include radiolabeled inhibitors that can be used in research or clinical applications (e.g., for the treatment of cancer or ischemia-related central nervous system injury).
    Type: Application
    Filed: October 15, 2014
    Publication date: February 26, 2015
    Inventor: Stephanie Lynn Martinelli
  • Publication number: 20150031988
    Abstract: The present invention provides a therapeutic system that is widely applicable to general solid cancers, can achieve both a reduction in side effects of cancer therapy and suppression of cancer recurrence and metastasis, and requires no expensive drug such as an antibody; and a nanoparticle for internal radiation therapy. A system for internal radiation therapy of a vascular lesion site comprising: a device comprising a means for acquiring image data showing a position of a vascular lesion site, and a means for positioning a needle, which should be punctured into the vascular lesion site, at the vascular lesion site based on the image data; and a nanoparticle comprising an amphiphilic block polymer comprising a hydrophilic block having a sarcosine unit and a hydrophobic block having a lactic acid unit, and a substance labeled with a ?-ray emitting nuclide. The nanoparticle for internal radiation therapy.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 29, 2015
    Inventors: Eri Takeuchi, Isao Hara, Ryo Yamahara, Eiichi Ozeki, Shunsaku Kimura, Kensuke Kurihara
  • Patent number: 8940274
    Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are functionalised BTMs useful in the method, as well as methods of preparing such functionalised BTMs under mild conditions.
    Type: Grant
    Filed: November 23, 2011
    Date of Patent: January 27, 2015
    Assignee: GE Healthcare Limited
    Inventors: Michelle Avory, Harry John Wadsworth, Robert James Domett Nairne
  • Patent number: 8936777
    Abstract: The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comprising a radioisotope (e.g., 18F). Various embodiments of the invention may be useful as sensors, diagnostic tools, and the like. In some cases, methods for evaluating perfusion, including myocardial perfusion, are provided. Synthetic methods of the invention have also been incorporated into an automated synthesis unit to prepare and purify imaging agents that comprise a radioisotope. In some embodiments, the present invention provides a novel methods and systems comprising imaging agent 1, including methods of imaging in a subject comprising administering a composition comprising imaging agent 1 to a subject by injection, infusion, or any other known method, and imaging the area of the subject wherein the event of interest is located.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: January 20, 2015
    Assignee: Lantheus Medical Imaging, Inc.
    Inventors: Richard R. Cesati, Edward H. Cheesman, Joel Lazewatsky, Heike S. Radeke, Enrico Mongeau, Dianne D. Zdankiewicz, Marybeth Devine
  • Patent number: 8926944
    Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: The invention also provides pharmaceutical compositions of a complex of a radionuclide and a Formula I compound or a Formula II compound and methods of using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: January 6, 2015
    Assignee: Molecular Insight Pharmaceuticals
    Inventors: John W. Babich, Craig Zimmerman, John L. Joyal, Genliang Lu
  • Patent number: 8916132
    Abstract: Use of benzimidazole-derived compounds of formula (I) according to the following structure, wherein x is a heteroatom selected from N, S, O, P, SO, SO2 and SO3, preferably from N, S and SO3 and most preferably from N and SO3; n may be 0 or 1, R1 is a group selected from formula (II) and formula (III) and R2 is a group selected from H and formula (IV) since the aforesaid serves for the production of a formulation used as a specific marker in the case of neurodegenerative diseases and tau pathologies.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: December 23, 2014
    Assignee: Servicios Cientificos Neuroinnovation Ltda
    Inventors: Rodrigo Kuljis Azocar, Ricardo Maccioni Baraona, Leonel Rojo
  • Patent number: 8916131
    Abstract: The present invention relates to radiopharmaceuticals and in particular to a radiopharmaceutical composition comprising a compound of Formula (I): and polysorbate as an excipient. The radiopharmaceutical composition of the invention reduces problems encountered with prior art compositions comprising the same class of compounds. Also provided by the invention is a method for the preparation of the radiopharmaceutical composition of the invention as well as particular uses of the radiopharmaceutical composition.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: December 23, 2014
    Assignee: GE Healthcare Limited
    Inventors: Line Roed, Sarah Elizabeth Peterson
  • Patent number: 8911707
    Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: December 16, 2014
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
  • Patent number: 8906343
    Abstract: A PAA nanoparticle containing a covalently linked fluorescent dye and a post-loaded tetrapyrrolic photosensitizer.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: December 9, 2014
    Assignees: Health Research, Inc., The Research Foundation of State University of New York, Regents of the University of Michigan
    Inventors: Ravindra K. Pandey, Raoul Kopelman, Anurag Gupta, Munawwar Sajjad
  • Publication number: 20140348748
    Abstract: 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: Application
    Filed: September 13, 2012
    Publication date: November 27, 2014
    Inventors: Lisheng Cai, Victor W. Pike
  • Patent number: 8889100
    Abstract: 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: Grant
    Filed: March 6, 2014
    Date of Patent: November 18, 2014
    Assignee: Immunomedics, Inc.
    Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
  • Publication number: 20140335019
    Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
  • Patent number: 8877160
    Abstract: 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: Grant
    Filed: August 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Cellectar, Inc.
    Inventors: Jamey P. Weichert, Marc Longino, Anatoly Pinchuk
  • Patent number: 8877159
    Abstract: The present invention provides methods and uses of phospholipid ether analogs as diagnostic and therapeutic agents for numerous cancers.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Cellectar, Inc.
    Inventors: Jamey P. Weichert, Marc Longino, Anatoly Pinchuk
  • Publication number: 20140322133
    Abstract: Translocator protein (TSPO) targeting compounds are described. Methods of making the compounds, and uses of the compounds for imaging are also described.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: MARTIN G. POMPER, HAOFAN WANG, TOMAS R. GUILARTE
  • Patent number: 8871179
    Abstract: 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: Grant
    Filed: August 27, 2012
    Date of Patent: October 28, 2014
    Assignee: The General Hospital Corporation
    Inventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
  • Patent number: 8865125
    Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: October 21, 2014
    Assignee: GE Healthcare Limited
    Inventors: Michelle Avory, William John Trigg
  • Patent number: 8858911
    Abstract: 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: Grant
    Filed: October 7, 2010
    Date of Patent: October 14, 2014
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
  • Patent number: 8852554
    Abstract: The present invention relates to novel, selective, radiolabelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: October 7, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Ignacio Andrés-Gil, Meri De Angelis, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen
  • Publication number: 20140294725
    Abstract: 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: Application
    Filed: July 6, 2012
    Publication date: October 2, 2014
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Gabriela Chiosis, Nagavarakishore Pillarsetty, Jason S. Lewis, Steven M. Larson, Tony Taldone, Mary L. Alpaugh, Erica M. Gomes
  • Publication number: 20140271471
    Abstract: 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: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Genzyme Corporation
    Inventors: Kuber T. Sampath, Michael Philbrook, Aviva Shiedlin, John M. McPherson
  • Publication number: 20140271472
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: UMESH H. PATEL, BHAVIN SHAH, MICHELLE CHUTKA
  • Patent number: 8834841
    Abstract: 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: Grant
    Filed: April 5, 2013
    Date of Patent: September 16, 2014
    Assignee: Emory University
    Inventor: Mark M. Goodman
  • Publication number: 20140255308
    Abstract: 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: Application
    Filed: May 19, 2014
    Publication date: September 11, 2014
    Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Gavril Pasternak, Susruta Majumdar
  • Publication number: 20140248213
    Abstract: 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: Application
    Filed: October 5, 2012
    Publication date: September 4, 2014
    Applicants: CEDARS-SINAI MEDICAL CENTER, UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Leland W. K. Chung, Dongfeng Pan
  • Patent number: 8808665
    Abstract: 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: Grant
    Filed: November 18, 2013
    Date of Patent: August 19, 2014
    Assignee: Immunomedics, Inc.
    Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg