The Hetero Ring Contains At Least Three Nitrogens Patents (Class 540/474)
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Publication number: 20140142298Abstract: The present invention embodiments relate to a compound with formula (V?) The invention also relates in certain embodiments to the synthesis method for compound (V?) and its use for the preparation of 1,4,7-triazacyclononane (tacn) and N- and/or C-functionalized derivatives thereof, particularly compounds with formula (I) The invention also relates in certain embodiments to metallic complexes comprising a ligand with formula (I) and a metal and their use for imaging.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE BOURGOGNEInventors: Franck Denat, Pauline Desogere, Claire Bernhard, Yoann Rousselin, Frederic Boschetti
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Patent number: 8722879Abstract: A device is presented having reversibly changeable and optically readable optical properties. The device comprises a substrate having an electrically conductive surface and carrying a redox-active layer structure. The redox-active layer structure may be a monolayer or a multi-layer structure and is configured to have at least one predetermined electronic property including at least one of electrodensity and oxidation state. The electronic property of the layer structure defines an optical property of the structure thereby determining an optical response of the structure to certain incident light. This at least one electronic property is changeable by subjecting the redox-active layer structure to an electric field or to a redox-active material. The device thus enables effecting a change in said electronic property that results in a detectable change in the optical response of the layer structure.Type: GrantFiled: March 5, 2007Date of Patent: May 13, 2014Assignee: Yeda Research & Development Company Ltd. at the Weizmann Institute of ScienceInventors: Milko E. Van Der Boom, Atindra D. Shukla, David Rosenblatt, Tarkeshwar Gupta
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Patent number: 8703937Abstract: Improved methods for synthesizing bifunctional chelates of tetraazamacrocycle derivatives and intermediates thereof are disclosed as well as novel tetraazamacrocycle derivatives and intermediates thereof.Type: GrantFiled: May 7, 2012Date of Patent: April 22, 2014Assignee: Mallinckrodt LLCInventor: Dennis A. Moore
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Publication number: 20140073631Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.Type: ApplicationFiled: September 10, 2013Publication date: March 13, 2014Applicant: Vymed CorporationInventor: B. Vithal SHETTY
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Publication number: 20140057877Abstract: This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan.Type: ApplicationFiled: October 18, 2011Publication date: February 27, 2014Inventors: Michael A. Murphy, Mitchell R. Malachowski
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Patent number: 8637620Abstract: The invention relates to a process for preparing a polymeric material doped with metal elements, comprising a step of polymerization of at least one monomer comprising at least one ethylenic function, said monomer being complexed with a metal element. Use of the materials obtained by means of this process as catalysts, or luminescent or magnetic materials, or as elements for laser targets.Type: GrantFiled: October 7, 2008Date of Patent: January 28, 2014Assignee: Commissariat A l'Energie Atomique et aux Energies AlternativesInventors: Alexia Balland Longeau, Louis Moreau, Jérôme Thibonnet, Emilie Velasquez
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Patent number: 8628978Abstract: A compound of formula (I) is provided: wherein: R1 is an optionally substituted 2-(1-azathiaxanthone); each —R2 is independently of the formula —CH2—C(?O)—R4, wherein R4 is an amino acid or a salt thereof, attached to the remainder of R2 through the nitrogen atom of the amino group; and R3 is hydrogen or a C1-6 alkyl group; or wherein: R1 is an optionally substituted 2-(1-azaxanthone); each R2 is independently an optionally substituted glutaric or succinic acid, or a salt or ester thereof; and R3 is hydrogen or a C1-6 alkyl group.Type: GrantFiled: January 29, 2010Date of Patent: January 14, 2014Assignee: University of DurhamInventors: David Parker, Robert Pal
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Publication number: 20130336888Abstract: A dendrimer conjugate according to Formula (I), or its pharmaceutically acceptable salt, or solvate thereof: and complexes of Formula I conjugates with metals radionuclides of elements such as rhenium, technetium, yttrium, lutetium and others to provide a complex for imaging tissues or for the radiotherapeutic treatment of cancer tissue. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.Type: ApplicationFiled: December 6, 2011Publication date: December 19, 2013Inventors: John W. Babich, John L. Joyal, Craig Zimmerman
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Publication number: 20130317196Abstract: The present invention relates to a triazanonane derivative indicated by the chemical formula 1 below, or a pharmaceutically acceptable salt thereof, and a method for preparing same, and the triazanonane derivative according to the present invention forms a complex with a metal-fluoride and displays an effect of increasing the labeling efficiency up to 78-90% when labeling F-18, thus enabling use in various radioactive medicine labeling (In the chemical formula 1, R1, R2, A. E. X, n and m are as defined in the present description.Type: ApplicationFiled: February 1, 2012Publication date: November 28, 2013Applicant: SNU R&DB FOUNDATIONInventors: Jae Min Jeong, Dinesh Shetty, Dong Soo Lee, June-Key Chung, Myung Chul Lee
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Publication number: 20130310555Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.Type: ApplicationFiled: May 17, 2013Publication date: November 21, 2013Applicant: Illinois Institute of TechnologyInventor: Hyun-Soon Chong
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Publication number: 20130261297Abstract: The present invention provides improved processes for the synthesis of 1,4-ditosyl-1,4,7-triazacyclonone and protected analogues thereof, and to synthesise bis(triazacyclononane) ligands.Type: ApplicationFiled: July 5, 2011Publication date: October 3, 2013Applicant: CATEXEL LIMITEDInventors: Ronald Hage, Jean Hypolites Koek, Stephen William Russell, Lodewijk Van der Wolf, Jianrong Zhang, Wei Zhao, Xiaohong Wang
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Patent number: 8540966Abstract: The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.Type: GrantFiled: June 28, 2005Date of Patent: September 24, 2013Assignee: Bracco Imaging S.p.A.Inventors: Silvio Aime, Matteo Galli, Luciano Lattuada, Pierfrancesco Morosini, Fulvio Uggeri, Kondareddiar Ramalingam
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Patent number: 8536162Abstract: Conjugates of 1,3-bis(1,4,7-triazacyclonon-1-yl)-2-hydroxypropanes with a variety of conjugating members are used in the formation of dinuclear metal complexes which bind to phosphate esters. By virtue of their conjugated forms, the complexes are incorporated into chromatographic media, affinity binding reagents, and dyes, which make the complexes useful in a wide range of assays, separations, and purifications. In addition, dinuclear metal complexes of 1,3-bis(1,4,7-triazacyclonon-1-yl)-2-hydroxypropanes that are not so conjugated are used in the detection of phosphate esters of biological species by either MALDI-TOF mass spectrometry or by dye displacement.Type: GrantFiled: March 9, 2011Date of Patent: September 17, 2013Assignee: Bio-Rad Laboratories, Inc.Inventors: Thomas R. Berkelman, Lisandra Martin, Rhiannon Jones, John Walker, II
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Publication number: 20130231475Abstract: The present invention relates to a magnetic resonance imaging (MRI) contrast agent including a gadolinium complex, more particularly to a DO3A-tranexamic acid or its ester compound, which is represented by the Chemical Formula 1. A DO3A-tranexamic acid or its ester compound may be prepared according to the present invention and a gadolinium complex may be prepared using the compound. An MRI contrast agent including the gadolinium complex prepared according to the present invention as an active ingredient has higher relaxivity as compared to the currently commercially available contrast agent. In addition, the MRI contrast agent according to the present invention has bifunctionality of liver-specific and blood-pool contrasting effect.Type: ApplicationFiled: December 21, 2010Publication date: September 5, 2013Applicant: KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATIONInventors: Tae-Jeong Kim, Yong Min Chang, Hee-Kyung Kim, Sung-Wook Gu
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Patent number: 8518715Abstract: A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111In or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.Type: GrantFiled: May 21, 2012Date of Patent: August 27, 2013Assignee: Nordion (Canada) Inc.Inventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso, Cara Ferreira
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Publication number: 20130202536Abstract: The invention relates to novel luminescent compositions of matter containing a fluorophore, synthetic methods for making the compositions, macromolecular conjugates of the compositions, and the use of the compositions in various methods of detection. The invention also provides kits containing the compositions and their conjugates for use in the methods of detection.Type: ApplicationFiled: January 13, 2011Publication date: August 8, 2013Applicants: NEW JERSEY INSTITUTE OF TECHNOLOGY, UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Arkady Mustaev, Maxim Kozlov, Salvatore Marras, Lev Krasnoperov, Laura Wirpsza, Shyamala Pillai
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Publication number: 20130156851Abstract: What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: When substituents R and R? that are hydrophobic substituents, the macrocyclic compound functions as a lipid and is compatible with lipid systems, including liposomes and lipid particles. When present in certain lipid systems, the macrocyclic compound enhances the ability of the lipid system to facilitate delivery of therapeutic molecules to target cells in a mammalian subject.Type: ApplicationFiled: August 26, 2011Publication date: June 20, 2013Inventors: Kunyuan Cui, Dong Liang
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Publication number: 20130149242Abstract: Described are bifunctional NOTA-based derivatives capable of conjugating with alginate and with metal ions, as well as NOTA-alginate conjugates which can be labeled with stable or radioactive metal ions. Also described are conjugation methods of the bifunctional NOTA-based linker with alginate, and methods of using radiometal-labeled NOTA-alginate conjugates or other radio-labeled alginate conjugates as imaging reagents.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Applicant: Ikaria Development Subsidiary One LLCInventor: Ikaria Development Subsidiary One LLC
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Publication number: 20130095035Abstract: The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations.Type: ApplicationFiled: January 31, 2011Publication date: April 18, 2013Applicant: MIVENION GMBHInventors: Kai Licha, Michael Schirner, Pia Welker, Rainer Haag, Marie Weinhart, Florian Paulus
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Publication number: 20130095076Abstract: Methods for increasing blood flow and/or regenerating tissue using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z???(1).Type: ApplicationFiled: July 5, 2012Publication date: April 18, 2013Applicant: Genzyme CorporationInventors: Gary J. BRIDGER, Simon P. FRICKER
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Patent number: 8389505Abstract: The invention relates to adamantane diaza-crown ether derivatives and the use of mono and diaza-crown ether adamantine derivatives in treatment, especially in tumor treatment. Adamantane aza-crown ethers were obtained by reaction of the corresponding adamantane derived tosylates or adamantane acid chlorides with mono- and diaza-18-crown-6. The prepared compounds showed moderate (monoaza-18-crown-6) to strong (diaza-18-crown-6) antiproliferative and cytotoxic activity on several tumor cell lines, revealing their potential for inhibiting the growth of other tumor cells.Type: GrantFiled: May 13, 2011Date of Patent: March 5, 2013Assignee: Rudjer Boskovic InstituteInventors: Marijeta Kralj, Kata Majerski, Tatjana Sumanovac Ramljak, Marko Marjanovic
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Publication number: 20130052130Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.Type: ApplicationFiled: August 30, 2012Publication date: February 28, 2013Applicants: UNIVERSITY OF WASHINGTON, QUANTA BIODESIGN, LTD.Inventors: Paul D. Davis, D. Scott Wilbur
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Publication number: 20130034494Abstract: 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: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Inventors: John W. BABICH, Craig Zimmerman, John L. Joyal, Genliang Lu
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Patent number: 8361438Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.Type: GrantFiled: January 8, 2009Date of Patent: January 29, 2013Assignee: Lantheus Medical Imaging, Inc.Inventors: Richard R. Cesati, Thomas D. Harris, Simon P. Robinson, Richard J. Looby, Edward H. Cheesman, Padmaja Yalamanchili, David S. Casebier
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Patent number: 8362164Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.Type: GrantFiled: October 12, 2011Date of Patent: January 29, 2013Assignee: Bridgestone CorporationInventor: Yan Yan-Yong
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Publication number: 20130004423Abstract: According to the present invention, a novel polyazamacrocyclic compound which is used as a bifunctional chelating agent (BFC) can be synthesized selectively and in high yield. The novel polyazamacrocyclic compound synthesized by this method chelates with metals and thus can be conjugated with bioactive molecules such as peptides, and can be used in the diagnosis and treatment of medical conditions.Type: ApplicationFiled: February 14, 2011Publication date: January 3, 2013Inventors: Jeongsoo Yoo, Darpan Navinchandra Pandya
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Publication number: 20120328514Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.Type: ApplicationFiled: July 8, 2010Publication date: December 27, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: Richard R. Cesati, Thomas D. Harris, Simon P. Robinson, Richard J. Looby, Edward H. Cheesman, Padmaja Yalamanchili, David S. Casebier
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Publication number: 20120309962Abstract: The invention concerns a process for the preparation of the calcium complex of 0-(2,3-Dihydroxy-1-(hydroxymethyl)propyl)-1,4,7,10-tetraazacyclodecane-4,7-triacetic acid, also known as Calcobutrol, starting from the pure gadolinium complex (Gadobutrol). The invention furthermore concerns Calcobutrol with a hitherto unknown level of purity.Type: ApplicationFiled: November 2, 2010Publication date: December 6, 2012Applicant: Bayer Intellectual Property GmbHInventors: Johannes Platzek, Wilhelm Trentmann
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Patent number: 8323621Abstract: Cyclen-based chelates can be used as contrast agents for multi-modal imaging of tissue cells. The cyclen-based chelates are preferably polyazamacrocyclic molecules formed from 1,4,7,10 tetraazacyclododecane (“cyclen”) having varying chelating ions, phosphoester chains, and light harvesting moieties. By changing the chelating ion, phosphoester chain length and/or the light harvesting moiety different imaging techniques, such as MRI, CT, fluorescence and absorption, x-ray and NIR, may be employed to image the tissue cells. Additionally, the cyclen-based chelates may be conjugated to provide for site-specific delivery of the cyclen-based chelate to the desired tissue cells. The cyclen-based chelates may also be delivered to the tissue cells by attaching the cyclen-based to a polymeric delivery vehicle. Although these cyclen-based chelates have a wide variety of application, the preferred use is for imaging of cancer cells, such as brain cancer, for improving resection of a cancerous tissue.Type: GrantFiled: March 4, 2008Date of Patent: December 4, 2012Assignees: Vanderbilt University, Texas Tech University SystemInventors: Darryl J. Bornhop, H. Charles Manning, Timothy Goebel
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Publication number: 20120294809Abstract: The invention relates to compositions of DOTA derivative compounds, lanthanoid-DOTA derivative molecular complex, and lanthanoid-complex encapsulated solid lipid particles or capsules, and methods of making and using the compositions. The solid lipid particles or capsules contain micelle cores stabilized by a hyperbranched polymer shell based from a crosslinked DOTA derivative compound or crosslinked lanthanoid-DOTA derivative complex. These solid lipid particles or capsules can be used in various applications, such as contrast agents or drug delivery vehicles.Type: ApplicationFiled: May 4, 2012Publication date: November 22, 2012Applicant: NEW YORK UNIVERSITYInventor: Marc Anton WALTERS
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Publication number: 20120289454Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.Type: ApplicationFiled: May 12, 2012Publication date: November 15, 2012Applicant: METALLOPHARM LLCInventors: James A. Cowan, Ada S. Cowan, Donna T. Palmer
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Publication number: 20120282178Abstract: 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: ApplicationFiled: May 17, 2012Publication date: November 8, 2012Applicant: IMMUNOMEDICS, INC.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
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Publication number: 20120277421Abstract: Improved methods for synthesizing bifunctional chelates of tetraazamacrocycle derivatives and intermediates thereof are disclosed as well as novel tetraazamacrocycle derivatives and intermediates thereof.Type: ApplicationFiled: May 7, 2012Publication date: November 1, 2012Applicant: Mallinckrodt LLCInventor: Dennis A. Moore
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Patent number: 8288530Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.Type: GrantFiled: November 6, 2007Date of Patent: October 16, 2012Assignee: The United States of America, as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Publication number: 20120251560Abstract: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.Type: ApplicationFiled: March 23, 2012Publication date: October 4, 2012Applicant: Massachusetts Institute of TechnologyInventors: James E. Dahlman, Avraham D. Schroeder, Daniel Griffith Anderson, Robert S. Langer, Christopher G. Levins
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Publication number: 20120231297Abstract: Disclosed is a lubricant composition comprising at least one kind of compound represented by following formula (1): where X represents a cyclic group that may be substituted; Y represents a divalent or higher-valent linking group having at least one polar group and having no aromatic cyclic group; p1 represents an integer of 1 to 4; p2, p3, and p4 each represent an integer of 0 to 4; q represents an integer of 0 to 30; n represents an integer of 1 to 10; s represents an integer of 1 to 4; and t represents an integer of 2 to 10.Type: ApplicationFiled: March 7, 2012Publication date: September 13, 2012Applicant: FUJIFILM CORPORATIONInventors: Hiroki SUGIURA, Masayuki HARADA, Ken KAWATA, Akiko HATTORI, Atsushi TATSUGAWA
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Publication number: 20120190795Abstract: Provided is a low-cost, highly active, environmentally friendly living radical polymerization catalyst which does not require a radical initiator. An organic compound having an oxidation-reduction capability is used as a catalyst. Even if a radical initiator is not used, a monomer can be subjected to a radical polymerization to obtain a polymer having narrow molecular weight distribution. The cost of the living radical polymerization can be remarkably reduced. It is made possible to prevent adverse effects of using a radical initiator. The present invention is significantly more environmentally friendly and economically excellent than conventional living radical polymerization methods, due to advantages of the catalyst such as low toxicity of the catalyst, low amount of the catalyst necessary, high solubility of the catalyst, mild reaction conditions, and no coloration/no odor (which do not require a post-treatment for a molded article), etc.Type: ApplicationFiled: May 10, 2010Publication date: July 26, 2012Inventors: Atsushi Goto, Yoshinobu Tsujii, Takeshi Fukuda
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Publication number: 20120148492Abstract: Disclosed is a radioactive bone diagnostic agent which gives a high ratio of radioactivity accumulation in bone to that in blood from an early stage after administration of the agent and allows capturing an image in a short time after administration. Also disclosed is a bisphosphonic acid derivative represented by the following chemical formula (II) or a salt thereof, wherein X represents —(CH2)mCO—, Y represents —(CH2)n—, R represents H, OH, or a halogen atom, m and n are independent of each other and m represents an integer of 1 to 3, and n represents an integer of 0 to 4.Type: ApplicationFiled: August 19, 2010Publication date: June 14, 2012Applicant: FUJIFILM RI PHARMA CO., LTD.Inventor: Hiroyuki Dozono
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Patent number: 8198101Abstract: A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111Li or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.Type: GrantFiled: March 6, 2007Date of Patent: June 12, 2012Assignee: Nordion (Canada) Inc.Inventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso
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Patent number: 8193347Abstract: Improved methods for synthesizing bifunctional chelates of tetraazamacrocycle derivatives and intermediates thereof are disclosed as well as novel tetraazamacrocycle derivatives and intermediates thereof.Type: GrantFiled: March 14, 2007Date of Patent: June 5, 2012Assignee: Mallinckrodt LLCInventor: Dennis A. Moore
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Publication number: 20120134920Abstract: 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: ApplicationFiled: December 12, 2011Publication date: May 31, 2012Applicant: IMMUNOMEDICS, INC.Inventors: Christopher A. D'Souza, William J. McBride, David M. Goldenberg
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Patent number: 8158782Abstract: This invention concerns novel labeling reactants based on azacycloalkanes, wherein a suitable group is linked to the molecule allowing introduction of the said molecules to bioactive molecules in solution or on solid phase.Type: GrantFiled: May 4, 2007Date of Patent: April 17, 2012Assignee: Wallac OyInventor: Jari Hovinen
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Patent number: 8148359Abstract: The present invention relates to compounds that can be used as metal-ion-chelating agents or as depolluting agents, corresponding to general formula (I) below: and also to precursor compounds of formula (II) and labelled compounds of formula (III) deriving from the compounds of formula (I). The present invention also relates to the use of the compounds (I), (II) or (III) as a medicament, and also the use thereof for the diagnosis, prevention and treatment of neurodegenerative diseases such as Wilson's disease and Alzheimer's disease.Type: GrantFiled: March 13, 2009Date of Patent: April 3, 2012Assignee: Commissariat a l'Energie AtomiqueInventors: Pascale Delangle, Christelle Gateau, Anaïs Pujol
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Patent number: 8138332Abstract: The invention relates to an improved process for preparation of protected DO3A, such as DO3A-tri-t-butyl ester (1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid tri-t-butyl ester). The compound is prepared as a salt. The process includes a work-up procedure giving DO3A-tri-t-butyl ester as a salt of excellent purity.Type: GrantFiled: April 18, 2006Date of Patent: March 20, 2012Assignee: GE Healthcare ASInventors: Oskar Axelsson, Andreas Olsson
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Publication number: 20120064003Abstract: The present invention concerns a Ga68 complex of formula FOLATE-(LINKER)i-NOTA-Ga68 in which: 1) FOLATE is a folate compound or a derivative thereof capable of targeting a folate receptor, 2) NOTA is a chelate capable of complexing Ga68 having a NOTA scaffold or derivatives thereof 3) LINKER is a chemical group linking FOLATE and NOTA 4) i is an integer chosen between 0 and 1 wherein NOTA is complexing Ga68Type: ApplicationFiled: August 8, 2011Publication date: March 15, 2012Applicant: GUERBETInventors: Marc PORT, Claire COROT, Thierry GAUTHERET
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Publication number: 20120058565Abstract: Conjugates of 1,3-bis(1,4,7-triazacyclonon-1-yl)-2-hydroxypropanes with a variety of conjugating members are used in the formation of dinuclear metal complexes which bind to phosphate esters. By virtue of their conjugated forms, the complexes are incorporated into chromatographic media, affinity binding reagents, and dyes, which make the complexes useful in a wide range of assays, separations, and purifications. In addition, dinuclear metal complexes of 1,3-bis(1,4,7-triazacyclonon-1-yl)-2-hydroxypropanes that are not so conjugated are used in the detection of phosphate esters of biological species by either MALDI-TOF mass spectrometry or by dye displacement.Type: ApplicationFiled: March 9, 2011Publication date: March 8, 2012Applicant: BIO-RAD LABORATORIES, INC.Inventors: Thomas R. Berkelman, Lisandra Martin, Rhiannon Jones, John Walker, II
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Publication number: 20120039803Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an alkene or alkyne dienohile.Type: ApplicationFiled: April 12, 2010Publication date: February 16, 2012Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventors: Marc Stefan Robillard, Raffaella Rossin, Johan Lub, Pascal Renart Verkerk, Dirk Burdinski
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Patent number: 8114863Abstract: The present invention relates to a compound of formula (II) chosen from (IIa) and (IIb) or of formula (VI) chosen from (VIa) and (VIb) of following general formulae: in which: X1, X2, X3, X4 and X5 represent, independently of one another, L-Y in which L represents a C1-C3 alkyl group, preferably (CH2)n with n=1 to 3, Y represents —CONH2, —CO—NR7R8 or —NR8-CO—R8, or an isomer, an enantiomer or a diastereoisomer of these or their mixtures or a pharmaceutically acceptable salt of the compounds of formulae (VIa) and (VIb). It also relates to a complex of these compounds with a paramagnetic metal or a radionuclide and their use in diagnostic methods.Type: GrantFiled: October 9, 2006Date of Patent: February 14, 2012Assignee: GuerbetInventor: Marc Port
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Publication number: 20120035255Abstract: The present invention relates to compounds having general formula (I), i.e. poly-alkyl-bis-maltolic molecules and in particular to derivates of [(3-hydroxy-4-pyron-2-yl)methyl]-amine and pharmaceutically acceptable salts thereof, and to the use thereof as anti-neoplastic drugs, in particular, for the preparation of a medicament for the treatment of neoplastic diseases.Type: ApplicationFiled: November 27, 2009Publication date: February 9, 2012Applicant: Universita' Degli Studi Di UrbinoInventors: Mirco Fanelli, Vieri Fusi
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Publication number: 20120035159Abstract: The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH?CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.Type: ApplicationFiled: June 18, 2010Publication date: February 9, 2012Applicant: D. WESTERN THERAPEUTICS INSTITUTE, INCInventors: Hiroyoshi Hidaka, Kouichi Takahashi, Yoshihiro Inoue, Kengo Sumi, Ryohei Nakamura