The Hetero Ring Contains At Least Three Nitrogens Patents (Class 540/474)
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Patent number: 8110679Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.Type: GrantFiled: July 31, 2008Date of Patent: February 7, 2012Assignee: Covalent Partners LLCInventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas, Mark Micklatcher, Serena Joshi
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Publication number: 20120028291Abstract: The present invention relates to compositions for and methods of optically imaging tissues or cells using imaging agents having desirable in vivo properties that result in improved signal-to-background ratio.Type: ApplicationFiled: February 5, 2010Publication date: February 2, 2012Applicants: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC., BETH ISRAEL DEACONESS MEDICAL CENTER, INC.Inventors: John V. Frangioni, Maged M. Henary
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Publication number: 20120029177Abstract: The present invention relates to novel amino acid derivatives containing heterocyclic chelating residues thereof; radioactive or nonradioactive metal complexes thereof; methods for preparation thereof; and apyrogenic and sterile preparative kits of the composition for targeting cancer cells. The compounds of the present invention can easily be taken up to cancer cells as they contain amino acid residues thereof; radioactive or nonradioactive metals can be labeled easily as they contain heterocyclic chelating residues thereof; cancer lesion can be imaged easily by targeting using the present invention.Type: ApplicationFiled: March 31, 2010Publication date: February 2, 2012Applicant: SNU R&DB FOUNDATIONInventors: Jae Min Jeong, Dinesh Shetty, Dong Soo Lee, June Key Chung, Myung Chul Lee
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Publication number: 20120021253Abstract: [Problem] Provided is a novel lubricant composition that is useful as a material of a lubricating layer of a magnetic recording medium. [Means for Resolution] The lubricant composition contains at least one kind of compound represented by the following Formula (1). In the formula, X represents a cyclic group that may be substituted, and Y represents a single bond or a linking group having a valency of 2 or more. Here, at least one of X and Y includes 1 or more polar groups such as a hydroxyl group; Z represents a linking group having a valency of 2 or more and constituted with a carbon atom (C), a fluorine atom (F), and 1 or 2 kinds of arbitrary atoms (here, a hydrogen atom is excluded); n represents a real number of 1 to 10; m represents a real number of 0 to 1; and s and t independently represent a real number of 1 or greater.Type: ApplicationFiled: March 3, 2010Publication date: January 26, 2012Applicant: FUJIFILM CORPORATIONInventors: Hiyoku Nakata, Akiko Hattori, Atsushi Tatsugawa, Ken Kawata
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Publication number: 20120009121Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.Type: ApplicationFiled: March 19, 2010Publication date: January 12, 2012Applicant: The Johns Hopkins UniversityInventors: Martin Pomper, Ronnie Charles Mease, Ray Sangeeta, Ying Chen
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Patent number: 8092782Abstract: The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.Type: GrantFiled: September 10, 2008Date of Patent: January 10, 2012Assignee: The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Alan J. Fischman
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Publication number: 20110287558Abstract: 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: ApplicationFiled: January 29, 2010Publication date: November 24, 2011Inventors: David Parker, Robert Pal
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Patent number: 8063032Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: GrantFiled: February 11, 2010Date of Patent: November 22, 2011Assignee: Sunovion Pharmaceuticals Inc.Inventors: Milan Chytil, Qun Kevin Fang, Kerry L. Spear
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Publication number: 20110280802Abstract: A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N—O—P-Q, wherein M is the diagnostic or therapeutic moiety, N—O—P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N—O—P-M, wherein M is independently a diagnostic or therapeutic moiety and N—O—P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Applicant: Bracco Imaging S.p.A.Inventors: Christoph De Haen, Adrian D. Nunn, Rolf E. Swenson
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Patent number: 8044081Abstract: Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.Type: GrantFiled: November 27, 2007Date of Patent: October 25, 2011Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Giovanni Paganelli, Marco Chinol, Mauro Ginanneschi
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Patent number: 8034800Abstract: A compound of Formulae (1), (2) or (3), A1-Ph (1) or A1-Ar-A2 (2) or A1-(A2)A?-A3 (3) wherein A1, A2 and A3 are selected from Formulae 4, 5 and 6: or a salt whereof; wherein Ar is selected from the group consisting of 1,2-phenyl, 1,3-phenyl and 1,4-phenyl optionally substituted with one or more methyl groups; m and n are independently integers from 0 to 1; Ph is phenyl, optionally substituted with one or more methyl groups; Ar1 is trisubstituted phenyl optionally substituted with one or more phenyl groups; and R1, R2 and R3 are independently selected from the group consisting of H, Me and linear chain C2-C4 alkyl.Type: GrantFiled: June 10, 2005Date of Patent: October 11, 2011Assignee: University of HullInventors: Stephen James Archibald, Elizabeth Amie Lewis, Timothy J. Hubin
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Publication number: 20110236312Abstract: The invention provides compounds that comprise a 4?-thio nucleoside that is a derivative of 4?-thiothymidine or 4?-thio-2?-deoxyuridine comprising a positron or single photon emitting radioisotope or corresponding non-radioactive isotope attached via a triazole link to the N-3 position. Methods for preparing such compounds and uses of the compounds in medicine are also provided.Type: ApplicationFiled: August 28, 2009Publication date: September 29, 2011Applicant: IMPERIAL INNOVATIONS LIMITEDInventors: Eric Ofori Aboagye, Graham Smith
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Publication number: 20110165075Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.Type: ApplicationFiled: March 13, 2009Publication date: July 7, 2011Inventors: Milind Rajopadhye, Guojie Ho, Bohumil Bednar, Le T. Duong, Paul J. Coleman
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Publication number: 20110137000Abstract: 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: ApplicationFiled: October 7, 2008Publication date: June 9, 2011Inventors: Balland Longeau Alexia, Moreau Louis, Thibonnet Jérôme, Velasquez Emilie
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Publication number: 20110129425Abstract: The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount of free macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.Type: ApplicationFiled: February 18, 2009Publication date: June 2, 2011Inventors: Dominique Meyer, Claire Corot, Marc Port, Vincent Barbotin, Bruno Bonnemain
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Publication number: 20110112289Abstract: The invention relates to the use of compounds comprising at least one 2-(1H-tetrazol-5-yl)pyridine unit, of formula (I) below: as ligands for lanthanides and, more especially, as organic chromophores for complexing these elements. It also relates to lanthanide complexes using these compounds as complexing organic chromophores, and to new compounds containing one or more 2-(1H-tetrazol-5-yl)pyridine units, which are useful as ligands for lanthanides and, in particular, as organic chromophores for complexing these elements. Applications: photonics and optoelectronics, especially for forming light-emitting devices such as electroluminescent diodes; biology, as for example for the preparation of luminescent probes.Type: ApplicationFiled: September 17, 2008Publication date: May 12, 2011Inventors: Marion Giraud, Renaud Demadrille, Marinella Mazzanti, Eugen Sorin Andreiadis
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Patent number: 7935692Abstract: Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed.Type: GrantFiled: November 8, 2005Date of Patent: May 3, 2011Assignee: Genzyme CorporationInventors: Gary J. Bridger, Michael J. Abrams, Geoffrey W. Henson, Ronald Trevor MacFarland, Gary B. Calandra, Hal E. Broxmeyer, David C. Dale
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Publication number: 20110092533Abstract: The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER? and ER?). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors.Type: ApplicationFiled: December 14, 2010Publication date: April 21, 2011Applicant: STC. UNMInventors: Eric R. PROSSNITZ, Sergey E. Tkatchenko, Chetana M. Revankar, Larry A. Sklar, Jeffrey B. Arterburn, Daniel F. Cimino, Tudor I. Oprea, Cristian-George Bologa, Bruce S. Edwards, Alexander Kiselyov, Susan M. Young
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Patent number: 7928096Abstract: The present invention provides compound of the formula (I): in which at least two of R1, R2, R3, R4, R5, and R6 are N2O2M and related compounds, substrates, compositions, and methods of using such compounds and compositions to treat biological disorders in which a polyphasic release of nitric oxide would be beneficial.Type: GrantFiled: November 11, 2008Date of Patent: April 19, 2011Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: David J. Waterhouse, Preeya Kapur, Larry K. Keefer, Joseph A. Hrabie, Frank De Rosa
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Publication number: 20110079557Abstract: The present invention relates to a material notably adapted for the extraction of metal cations in an aqueous medium, comprising a solid support on which are attached polyazacycloalkane compounds having a ring including at least 4 nitrogen atoms, and wherein the nitrogen atoms of the ring are substituted with coordinating groups, which each are independently: a coordinating group of formula: —(CH2)n—C(?O)—NR1R2 ?or else a both coordinating and binding group, fitting the formula: —(CH2)p—C(?O)—NR3-(A)-[support]. The invention also relates to methods for preparing the aforementioned materials and to different uses thereof, notably for the extraction of Pb2+ cations in an aqueous medium.Type: ApplicationFiled: February 20, 2009Publication date: April 7, 2011Inventors: Michel Meyer, Arnaud Bucaille, Francois Cuenot, Franck Denat, Frédéric Boschetti, Roger Guilard
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Patent number: 7917188Abstract: A method for mapping a physico-chemical parameter using a chemical exchange saturation transfer contrast agent in Magnetic Resonance Imaging is used with agents having only one exchangeable entity pool, e.g. proton pool, by applying two different RF frequencies for pre-saturation of the contrast agent.Type: GrantFiled: April 21, 2006Date of Patent: March 29, 2011Assignee: Koninklijke Philips Electronics N.V.Inventors: Rene Theodorus Wegh, Jeroen Alphons Pikkemaat, Nicolaas Petrus Willard
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Publication number: 20110064657Abstract: The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.Type: ApplicationFiled: June 26, 2008Publication date: March 17, 2011Applicant: The Johns Hopkins UniversityInventors: Martin Gilbert Pomper, Ray Sangeeta, Ronnie C. Mease, Catherine Foss
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Publication number: 20110054066Abstract: Radically polymerizable macrocyclic polyethers or macrocyclic heteroanalogous polyethers, preferably crown ethers, heteroanalogous crown ethers and cryptands for use in dental materials is disclosed.Type: ApplicationFiled: January 8, 2010Publication date: March 3, 2011Applicant: IVOCLAR VIVADENT AGInventors: Norbert MOSZNER, Frank ZEUNER, Urs Karl FISCHER, Volker M. RHEINBERGER, Iris LAMPARTH
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Patent number: 7897590Abstract: Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed.Type: GrantFiled: August 20, 2007Date of Patent: March 1, 2011Assignee: Genzyme CorporationInventors: Gary J. Bridger, Michael J. Abrams, Geoffrey W. Henson, Ronald Trevor MacFarland, Gary B. Calandra, Hal E. Broxmeyer, David C. Dale
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Publication number: 20110039854Abstract: The present invention relates to linear and cyclic guanidine derivatives, method of preparation and uses thereof, pharmaceutical compositions to be used as antifungal agents, in particular against Candida species.Type: ApplicationFiled: March 12, 2009Publication date: February 17, 2011Applicant: UNIVERSITÀ DEGLI STUDI DI SIENAInventors: Maurizio Botta, Francesco Raffi, Paolo Visca
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Publication number: 20110028714Abstract: A cell population expressing folate receptors is selectively targeted with a folate mimetic. The folate mimetic is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.Type: ApplicationFiled: May 7, 2010Publication date: February 3, 2011Inventors: Mark A. Green, Chun-Yen Ko, Christopher P. Leamon
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Publication number: 20110028713Abstract: A core of a cyclic structure represented by (—N—(CH2)n—)k is bonded to a dendrimer-type side chain with a specific branched structure at all nitrogen atoms in the core to produce a compound with a specific structure for producing a metal complex that exhibits a T1-reducing effect, and the resulting compound is coordinated to a metal ion that has a T1-reducing effect to obtain a metal complex that exhibits an excellent T1-reducing effect which is useful as an effective component of an MRI contrast agent and an MRI contrast agent using the same.Type: ApplicationFiled: November 28, 2008Publication date: February 3, 2011Applicants: KYOTO UNIVERSITY, CANON KABUSHIKI KAISHAInventors: Teruyuki Kondo, Hiroshi Tsujita, Zainul Abedin Siddique, Shingo Matsuki, Hiroki Miura, Hidehito Tochio, Tetsuya Matsuda, Michiko Narazaki, Hidetoshi Tsuzuki, Katsuaki Kuge, Yoshinori Tomida, Kimihiro Yoshimura, Tetsuya Yano
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Publication number: 20110021765Abstract: The invention provides a paramagnetic lanthanide (III) complex comprising a lanthanide (III) ion and a polydentate ligand wherein the polydentate ligand comprises one or more fluorine atoms in which the distance of at least. one of the fluorine atoms to the lanthanide ion is less than 7, said polydentate ligand not being a DPTA bisamide of p-CF3-aniline.Type: ApplicationFiled: April 11, 2008Publication date: January 27, 2011Inventors: David Parker, Padma Kanthi Senanayake
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Publication number: 20100322855Abstract: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N?,N?,N??-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.Type: ApplicationFiled: August 20, 2010Publication date: December 23, 2010Applicant: Illinois Institute of TechnologyInventor: Hyun-soon Chong
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Publication number: 20100311962Abstract: The invention provides MRI detectable species of formula (I) Dp-Sn-Nm??(I) wherein D is a MRI detectable moiety S is a spacer N is a molecule of a nutrient or pseudo-nutrient n is 0 or an integer m is an integer and p is an integer. These compounds are useful for internalising into tumor cells an amount of the MRI detectable moiety that is distinguishably higher than the amount internalised in normal healthy cells thus allowing the diagnosis of tumors. The internalisation of the MRI detectable moiety involves the nutrients or pseudo-nutrients transporting system. Preferred compounds of formula (I) are those wherein D is the chelated complex of a paramagnetic metal ion.Type: ApplicationFiled: July 2, 2010Publication date: December 9, 2010Inventors: Silvio AIME, Valentina MAINERO, Simonetta Chrich GENINATTI, Claudia CABELLA
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Publication number: 20100256178Abstract: The present invention relates to compounds which are effective as catalysts for dismutating superoxide and, more particularly, the manganese or iron complexes of substituted, unsaturated heterocyclic 16-membered macrocyclic complexes that catalytically dismutate superoxide. It also relates to methods of using these complexes to reduce the concentration or the effects of superoxide, pharmaceutical compositions comprising these compounds or their metal complexes, and methods of treating conditions associated with excessive superoxide activity.Type: ApplicationFiled: November 14, 2008Publication date: October 7, 2010Inventor: Dennis P. Riley
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Publication number: 20100247448Abstract: The present invention relates to a ligand for metals, in particular lanthanides, of the general formula (I) A corresponds to an organic acid radical, to an alkyl or aryl ester. R1 and R2 correspond, individually and independently of one another, to an H, an alkyl radical or an aryl radical. Z1 and Z2, identical or different, are of the general formula (ZA) or (ZB): G represents an O, N, P, S or a C substituted independently with an H, an alkyl radical or an aryl radical. R3 to R8 correspond, individually and independently of one another, to an H, an alkyl radical or an aryl radical. The present invention also relates to co-ordinating complexes of the general formula: [Ln(L)(H2O)n] wherein Ln is a lanthanide, L corresponds to a ligand, as well as the grafting thereof to a molecule of interest and their preparation method. The present invention relates moreover to a contrast agent and a pharmaceutical composition including at least one ligand and/or complex and/or molecule of interest.Type: ApplicationFiled: January 19, 2007Publication date: September 30, 2010Applicant: COMMISSARIAT A L'ENERGIE ATOMIQUEInventors: Christelle Gateau, Marinella Mazzanti, Aline Nonat
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Patent number: 7777029Abstract: The present invention relates to a method for preparing a bifunctional chelator for lanthanide. The method comprises the steps of providing a starting material which has an amino and carboxyl group; protecting the amino with an amino protecting group and the carboxyl with a carboxyl protecting group to produce a protected compound; reacting the protected compound with cyclen to generate a monoalkylated cyclen; reacting the monoalkylated cyclone with an activated compound to generated tetra-alkylated cyclone; removing the amino protecting group with a first protecting group removal reagent; and removing the carboxyl protecting groups with a second protecting group removal reagent to yield a bifunctional chelator having three more carboxyl groups and one or more amino groups.Type: GrantFiled: May 2, 2007Date of Patent: August 17, 2010Assignee: San Diego State University (SDSU) FoundationInventors: Douglas Grotjahn, Erik Wiener
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Publication number: 20100190967Abstract: The invention relates to an improved method of dynamic nuclear polarisation (DNP) of carboxylic acids and to compounds and compositions for use in the method.Type: ApplicationFiled: August 29, 2007Publication date: July 29, 2010Inventors: Christian Gloegaard, Rolf Servin, Mikkel Thaning
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Publication number: 20100184972Abstract: A process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as a base.Type: ApplicationFiled: May 31, 2006Publication date: July 22, 2010Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Mauro Marzi, Maria Di Marzo
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Publication number: 20100179116Abstract: The present invention relates to arene connected polyamine macrocyclic derivatives represented by general formula I, pharmaceutically acceptable salts or hydrates thereof which have anti-HIV activities, in which the definitions of substituents are as defined in the description; to preparation methods of the compounds of formula I; to pharmaceutical compositions containing the compounds of formula I or their pharmaceutically acceptable salts or hydrates; to the use of the compounds of formula I or their pharmaceutically acceptable salts or hydrates for the preparation of a medicament for the treatment and prevention of HIV-associated diseases.Type: ApplicationFiled: May 30, 2008Publication date: July 15, 2010Inventors: Song Li, Jing Su, Yao Liu, Junhai Xiao, Lili Wang, Wu Zhong, Zhibing Zheng, Yunde Kie, Xingzhou Li, Guoming Zhao, Xiaokui Wang, Xinbo Zhou, Hongying Liu
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Publication number: 20100111875Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a saturated triaza cyclic central moiety containing carbonyl functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.Type: ApplicationFiled: April 3, 2008Publication date: May 6, 2010Inventor: Veronique Morrison-Iveson
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Publication number: 20100111858Abstract: The present invention provides conjugates useful for the diagnosis and treatment of diseases associated with the over-expression of COX-2. The conjugates comprise a selective COX-2 targeting carrier, a metal coordinating moiety, and a linker chemically linking the metal coordinating moiety to the carrier. The metals coordinated by the metal coordinating moiety are selected from paramagnetic or radioisotopes. The invention also includes kits comprising a conjugate and a radioisotope solution.Type: ApplicationFiled: January 17, 2008Publication date: May 6, 2010Inventors: Carol P. Howard, Dennis A. Moore
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Patent number: 7709486Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.Type: GrantFiled: July 29, 2008Date of Patent: May 4, 2010Assignee: Genzyme CorporationInventors: Gary J. Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
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Publication number: 20100099649Abstract: Site-specific modifications of proteins at their N-termini are provided. In particular, a chemical modification of proteins at their N-termini via a transamination reaction to form homogeneous adducts such as, the corresponding oxime derivatives is provided. Methods of making and using the adducts in radio-labelling, molecular imaging applications, and treatment of disorders such as cancer, Crohn's disease, arthritis, atherothrombosis and plaque rupture are also provided.Type: ApplicationFiled: October 5, 2009Publication date: April 22, 2010Inventors: Alexander KRANTZ, Peng YU
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Publication number: 20100081799Abstract: A compound of the formula: wherein R1 is selected from H, methyl, ethyl, carboxyl protecting groups and hydrophilic moieties, R2 and R3 are independently selected from H, methyl, ethyl and carboxyl protecting groups, R4 is selected from H, methyl, ethyl, hydrophilic moieties and carboxyl protecting groups, and R5 is an aryl, heteroaryl, alkyl or a combination of these groups and is substituted with a carbonyl group, an aminooxy group or a functional group suitable for participating in a cycloaddition reaction. The compounds of the invention may be useful as bifunctional chelating agents which allow chemoselective attachment to targeting molecules.Type: ApplicationFiled: December 10, 2007Publication date: April 1, 2010Inventors: Sebastian Knör, Armin Modlinger, Hans-Jürgen Wester, Horst Kessler
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Publication number: 20100056776Abstract: 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: ApplicationFiled: November 6, 2007Publication date: March 4, 2010Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Publication number: 20100055043Abstract: In certain aspects, the present invention relates to metal coordinating complexes for use as imaging contrast agents. For instance, in some embodiments, the present invention is directed to an imaging contrast agent including a metal chelator and a halogen-substituted phenol, thiophenol, resorcinol, thioresorcinol, or dithioresorcinol derivative.Type: ApplicationFiled: October 30, 2007Publication date: March 4, 2010Inventor: Dennis A. Moore
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Publication number: 20100008857Abstract: A label with which labeling is easy when labeling a molecule, i.e., a label that has a high reaction rate upon labeling and that produces a high reaction yield, as well as a precursor for the production of the label are provided. This is achieved by a hexatriene-?-carbonyl compound represented by Formula (I), a hexatriene-?-carbonyl compound represented by Formula (II), a hexatriene-?-carbonyl compound represented by Formula (III) and a hexatriene-?-carbonyl compound represented by Formula (IV).Type: ApplicationFiled: February 5, 2008Publication date: January 14, 2010Applicants: OSAKA UNIVERSITY, RIKENInventors: Koichi Fukase, Katsunori Tanaka, Yasuyoshi Watanabe, Tsuyoshi Tahara, Koki Hasegawa
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Publication number: 20090326176Abstract: 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: ApplicationFiled: December 29, 2008Publication date: December 31, 2009Inventor: Yuan-Yong Yan
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Publication number: 20090252676Abstract: 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: January 8, 2009Publication date: October 8, 2009Applicant: Lantheus Medical Imaging, IncInventors: 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: 20090246130Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F labeled molecules of use in PET or MRI imaging. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a metal complex and binding of the 18F- or 19F-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the 18F or 19F bound to the metal. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The 18F or 19F labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET or MRI imaging.Type: ApplicationFiled: April 30, 2009Publication date: October 1, 2009Applicant: IMMUNOMEDICS, INC.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg
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Patent number: 7582280Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.Type: GrantFiled: July 8, 2008Date of Patent: September 1, 2009Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
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Publication number: 20090216011Abstract: 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: ApplicationFiled: April 18, 2006Publication date: August 27, 2009Inventors: Oskar Axelsson, Andreas Olsson
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Patent number: RE42152Abstract: Polyamine macrocyclic compounds, e.g. of 10 to 15 ring members and 3 to 6 ring amine nitrogens, linked through methylene groups to an aromatic moiety, show high selective activity against HIV.Type: GrantFiled: December 16, 1992Date of Patent: February 15, 2011Assignee: Genzyme CorporationInventors: Gary J. Bridger, Sreenivasan Padmanbhan, Renato Skerlj, David M. Thornton