In An Organic Compound Patents (Class 424/1.65)
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Publication number: 20100329978Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: May 21, 2010Publication date: December 30, 2010Applicants: University of Mississippi, I'Universite catholique de LouvainInventors: Christopher R. McCurdy, Christophe Mesangeau, Rae Reiko Matsumoto, Jacques Henri Poupaert, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem
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Patent number: 7858072Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.Type: GrantFiled: December 19, 2005Date of Patent: December 28, 2010Assignee: The Trustees of the University of PennsylvaniaInventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
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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: 20100322854Abstract: Described herein are compositions and methods for diagnosing and/or monitoring pathogenic disease states using positron emission tomography, wherein the pathogenic cells uniquely express, preferentially express, or overexpress vitamin receptors. Also described herein are 18F conjugates of vitamins and vitamin receptor-binding analogs and derivatives.Type: ApplicationFiled: February 7, 2008Publication date: December 23, 2010Applicant: PURDUE RESEARCH FOUNDATIONInventors: Philip Stewart Low, Sumith K. Kularatne
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Patent number: 7854920Abstract: 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: GrantFiled: July 26, 2007Date of Patent: December 21, 2010Assignee: University of PittsburghInventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
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Patent number: 7854918Abstract: By preliminarily dissolving a basic organic compound in an aqueous solvent in which a peptide usable in metal-labeling is to be dissolved, the solubility of the peptide is improved and thus metal-labeling can be carried out without heating. A composition for medical use containing a peptide usable in metal-labeling and a basic organic compound acceptable as a pharmaceutical additive can be utilized as a preparation useful in image diagnosis, radiotherapy and so on.Type: GrantFiled: March 23, 2005Date of Patent: December 21, 2010Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Takayoshi Kawaguchi, Ikuya Seki, Marino Maemura
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Patent number: 7854919Abstract: The invention provides compositions and methods for therapeutic and diagnostic applications.Type: GrantFiled: January 19, 2007Date of Patent: December 21, 2010Assignees: Bracco, Suisse SA, Dyax CorporationInventors: Christophe Arbogast, Philippe Bussat, Hong Fan, Karen E. Linder, Edmund R. Marinelli, Palaniappa Nanjappan, Adrian Nunn, Radhakrishna Pillai, Sibylle Pochon, Kondareddiar Ramalingam, Bo Song, Rolf E. Swenson, Mathew A. Von Wronski, Aaron Sato, Sharon Michele Walker, Daniel T. Dransfield, Ajay Shrivastava
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Publication number: 20100316566Abstract: The present invention concerns methods and compositions related to a chelator and a HHRT ligand. In specific embodiments of the invention the chelator is conjugated to the HHRT ligand. In another specific embodiment of the invention, the chelator is chelated to a metal. In a particular embodiment of the invention, there is a metal species that is chelated to a chelator, which is then directly or indirectly conjugated to a HHRT ligand. In some embodiments, the composition further comprises a therapeutic agent. In particular cases, the compositions are employed for cancer diagnosis and/or therapy.Type: ApplicationFiled: February 27, 2009Publication date: December 16, 2010Applicant: RADIOMEDIX INC.Inventors: Jennifer Sims-Mourtada, Ali Azhdarinia, Izabela Tworowska, Hitomi Saso
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Patent number: 7850946Abstract: The sensitivity and specificity of the optical modality can be enhanced by the use of highly absorbing compounds as contrast agents. Novel macrocyclic cyanine and indocyanine bioconjugates that absorb and emit light in the near infrared region of electromagnetic spectrum are disclosed. These compounds are especially useful for endoscopic, localized photoacoustic, and sonofluorescence imaging, detection and therapy of tumors and other abnormalities.Type: GrantFiled: June 1, 2004Date of Patent: December 14, 2010Assignee: Washington University in St. LouisInventors: Samuel Achilefu, Yunpeng Ye
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Patent number: 7850948Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: GrantFiled: September 10, 2008Date of Patent: December 14, 2010Assignee: Bayer Schering Pharma AGInventors: Matthias Friebe, Peter Muschick, Andreas Huth
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Patent number: 7850947Abstract: New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are define herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.Type: GrantFiled: February 10, 2006Date of Patent: December 14, 2010Assignee: Bracco Imaging S.p.A.Inventors: Enrico Cappelletti, Luciano Lattuada, Karen E. Linder, Edmund Marinelli, Palaniappa Nanjappan, Adrian D. Nunn, Natarajan Raju, Kondareddiar Ramalingam, Rolf E. Swenson, Michael F. Tweedle
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Patent number: 7842278Abstract: The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.Type: GrantFiled: October 27, 2006Date of Patent: November 30, 2010Assignee: Natural Pharmacia International, Inc.Inventors: David Y-W Lee, Xiao-Shen Ji, James A. Raleigh
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Patent number: 7842279Abstract: F-18 radiolabeled peptides are prepared by reacting a peptide comprising a hydroxylamine, a thiosemicarbazide, a hydrazine or a free amine group with 4-[18F]Fluorobenzaldehyde. Specific, non-limiting examples of F-18 radiolabeled peptides are described herein. The labeled peptides are useful, for example, in clinical positron emission tomography.Type: GrantFiled: August 8, 2006Date of Patent: November 30, 2010Assignee: Immunomedics, Inc.Inventors: William J. McBride, Carl F. Noren
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Publication number: 20100297007Abstract: The present invention provides nanoparticles, methods of making the nanoparticles, and methods of using the nanoparticles to deliver therapeutic agents and/or imaging agents.Type: ApplicationFiled: October 9, 2008Publication date: November 25, 2010Applicant: THE WASHINGTON UNIVERSITYInventors: Gregory M. Lanza, Samuel A. Wickline, Dipanjan Pan
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Patent number: 7837981Abstract: Provided herein are agents that bind to soluble beta-amyloid. Also provided are in vivo and in vitro methods for detecting soluble beta-amyloid in a sample that may include brain tissue.Type: GrantFiled: December 11, 2006Date of Patent: November 23, 2010Assignee: General Electric CompanyInventors: Tiberiu Mircea Siclovan, Michael Christopher Montalto, Kenneth Michael Fish, Eric Dustin Agdeppa, Cristina Tan Hehir
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Patent number: 7837982Abstract: 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-[18F]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).Type: GrantFiled: June 19, 2006Date of Patent: November 23, 2010Assignee: Emory UniversityInventor: Mark M. Goodman
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Publication number: 20100290986Abstract: The present invention relates generally to methods and materials for use in the treatment or prophylaxis of diseases, for example cognitive disorders, using diaminophenothiazines. In particular it relates to treatments having optimised pharmacokinetic properties, and dosage forms are intended to improve the relative cognitive or CNS benefits of the diaminophenothiazines, for instance compared to haematological effects.Type: ApplicationFiled: October 1, 2008Publication date: November 18, 2010Inventors: Claude Michel Wischik, Damon Jude Wischik, John Mervyn David Storey, Charles Robert Harrington
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Publication number: 20100284913Abstract: Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analogue binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.Type: ApplicationFiled: May 7, 2010Publication date: November 11, 2010Applicant: The Board of Trustees of the Leland Stanford JunioInventors: Justin Du Bois, John Mulcahy, Brian Andresen, David C. Yeomans, Sandip Biswal
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Publication number: 20100278730Abstract: We disclose methods of detecting histone deacetylase activity in a mammal by administering to the mammal a compound comprising at least one atom having a nucleus detectable by magnetic resonance spectroscopy, wherein the compound is a substrate of histone deacetylase; and observing the compound or a cleavage product thereof in at least a portion of the body of the mammal by magnetic resonance spectroscopy (MRS). We also disclose methods of detecting histone deacetylase activity in a mammal by administering to the mammal a compound comprising at least one positron-emission-decaying radioisotope, wherein the compound is a substrate of histone deacetylase; and observing the compound or a cleavage product thereof in at least a portion of the body of the mammal by positron emission tomography (PET). We also disclose compounds useful as histone deacetylase substrates.Type: ApplicationFiled: April 8, 2008Publication date: November 4, 2010Inventors: Sabrina Ronen, Juri Gelovani, William Tong, Mian Alauddin, Uday Mukhopadhyay, Madhuri Sankaranatayanapillai, Ashutosh Pal
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Publication number: 20100278731Abstract: Compositions for imaging pancreatic beta cells comprise chelator-antidiabetic agent conjugates and optionally chelated metals.Type: ApplicationFiled: November 2, 2009Publication date: November 4, 2010Inventors: David J. Yang, Chang-Sok Oh, Saady Kohanim, Dong-Fang Yu, Ali Azhdarinia, Jerry Bryant
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Patent number: 7824661Abstract: One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.Type: GrantFiled: February 14, 2005Date of Patent: November 2, 2010Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Kevin B. Maresca, James F. Kronauge, Jr.
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Publication number: 20100272642Abstract: Disclosed are: a PET probe compound having an alkoxy group substituted by a fluorine and a hydroxy group, which is useful for the early diagnosis of a conformational disease; a pharmaceutical composition for the treatment and/or prevention of a conformational disease, which comprises the compound; and others.Type: ApplicationFiled: June 17, 2008Publication date: October 28, 2010Applicant: TOHOKU UNIVERSITYInventors: Yukitsuka Kudo, Syozo Furumoto, Nobuyuki Okamura
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Publication number: 20100272641Abstract: Imaging agents that comprise labeled substrates of the cystine/glutamate antiporter of cells, whereby the methods of use comprise introducing the labeled agents into cells via the cystine/glutamate antiporter, which are then reduced to a labeled cysteine, and subsequently detected in the cell.Type: ApplicationFiled: April 27, 2009Publication date: October 28, 2010Applicant: GENERAL ELECTRIC COMPANYInventors: JACK MATHEW WEBSTER, FAISAL AHMED SYUD, BRIAN DUH-LAN LEE, PAUL SCHAFFER, RONG ZHANG, JENNIFER LYNNE HUNTINGTON, KANDE KANKANAMALAGE DAYARATHNA AMARASINGHE
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Patent number: 7820144Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methods for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoids. The disclosed compounds may include radioactive atoms. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual, to treat a condition in an animal or individual and for use in radioimaging.Type: GrantFiled: January 5, 2007Date of Patent: October 26, 2010Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Hongfeng Deng
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Patent number: 7815894Abstract: Compounds, compositions and methods for the diagnosis of Alzheimer's disease. Synthesized Glycerophosphocholine (GPC) may be used as a diagnostic aid to measure progression of Alzheimer's disease. GPC is a membrane phospholipid metabolite that is capable of binding specifically to the ?-turn of beta amyloid (A?) peptide. Compounds including non-radioactive, paramagnetic, and radioactive derivatives of GPC are presented. These compounds possess similar binding properties to original GPC molecules and are useful in medical magnetic resonance imaging and/or positron emission tomography applications. By employing these radiological techniques in conjunction with the compositions of the present invention, the diagnosis and assessment of the progression of Alzheimer's disease may be achieved.Type: GrantFiled: May 27, 2004Date of Patent: October 19, 2010Inventors: Jay W. Pettegrew, Richard J. McClure, Kanagasabai Panchalingam, Billy W. Day
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Publication number: 20100260671Abstract: The invention is in general directed to compounds, such as tannic acid, nicotine, nicotine derivatives and pyrrolid derivatives of nicotine, and methods for diagnosing, preventing or alleviating the symptoms of amyloid-associated diseases, for example, neuronal diseases, such as, for example, Alzheimer's disease, compounds and methods for inhibiting ion channel activity of beta amyloid, and methods of diagnostic imaging of A/3 fibrils.Type: ApplicationFiled: May 30, 2008Publication date: October 14, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Jerry Yang, Petra Inbar, Mahealani Bautista, Michael Mayer
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Publication number: 20100254900Abstract: Compositions and methods for manufacturing polymers are disclosed. Compositions include novel plastics, including films and shaped forms comprising polymer matrices that are biologically compatible and biodegradable. Such plastics may comprise polymers derived from natural sources. Further, such plastics are useful in biological systems for wound repair, implants, stents, drug encapsulation and delivery, and other applications. The disclosed methods comprise mild manufacturing processes such that various additives, such as biologically active proteins, sugars, lipids, and the like may be incorporated into the polymer matrix without subsequent loss of bioactivity during processing. Additionally, methods of manufacture for controlling mechanical properties, such as elasticity, pliancy, and the porosity of such plastics are disclosed.Type: ApplicationFiled: July 28, 2006Publication date: October 7, 2010Inventors: Phil G. Campbell, Lee E. Weiss, Jason Smith
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Patent number: 7807133Abstract: Dimers of avidin and streptavidins (diavidins) are described wherein the linker is suberate, which in turn, is bound to different functional groups (—NH2 o-COOH) of avidin. As compared to avidin, the diavidins have shown the ability to increase the amount of labelled biotin on the target, when used in an in vitro pretargeting test using supported human tenascin, the biotinylated anti-tenascin monoclonal antibody (Mab-B), avidin/diavidin, and biotin-3H. The use of such diavidins is also described in cancer diagnosis and anticancer therapy based on the three-step pretargeted radioimmunotherapy procedure.Type: GrantFiled: July 3, 2008Date of Patent: October 5, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: De Santis Rita, Lindstedt Ragnar, Nuzzolo Carlo Antonio
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Patent number: 7807135Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.Type: GrantFiled: December 19, 2005Date of Patent: October 5, 2010Assignee: The Trustees of the University of PennsylvaniaInventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
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Patent number: 7807140Abstract: Polymeric chelating agents and metal chelates, particularly those of lanthanide metals and more specifically those of Gd(III), useful as contrast agents in magnetic resonance imaging (MRI) for therapeutic and diagnostic applications as well as clinical and biomedical research applications. The polymeric chelates are generated using ring-opening metathesis polymerization (ROMP). Polymers can have multiple sites for functionalization allowing for the synthesis of multimodal and targeted contrast agents. Hydroxypyridonate (HOPO)-based chelating moieties are integrated into a ROMP-derived polymer. More specifically, the HOPO-based chelating moiety is integrated into a benzonorbornadiene unit that constitutes the backbone of the polymer. The ROMP-derived polymer chelators can comprise multiple metal ions, particularly Gd(III) ions, in polymers of varying lengths to provide a series of agents with controlled relaxivites. Polymer chelates include those that are water-soluble.Type: GrantFiled: May 3, 2007Date of Patent: October 5, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Laura L. Kiessling, Ronald T. Raines, Matthew J. Allen
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Publication number: 20100247433Abstract: The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handle” to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.Type: ApplicationFiled: October 16, 2006Publication date: September 30, 2010Applicant: California Institute of TechnologyInventors: David Tirrell, Daniela C. Dieterich, Aaron J. Link, Erin Schuman
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Patent number: 7803351Abstract: Novel blood-brain barrier permeant amyloid-targeting peptides and peptide conjugates are described. The peptide conjugates include a radioisotope or other label in a stable complex that translocates across brain capillary endothelial cell monolayers. The labeled peptide conjugate binds to amyloid plaques (A?) associated with Alzheimer's disease, and is useful for the targeted delivery of therapeutic and diagnostic molecules into the brain.Type: GrantFiled: August 19, 2005Date of Patent: September 28, 2010Assignee: Washington UniversityInventors: Vijay Sharma, David Piwnica-Worms
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Patent number: 7803352Abstract: A method for visualizing a blood clot or plaque disposed within a body lumen comprising: binding a contrasting complex comprising a contrast material and a thrombolytic material or a clot dissolving agent to the blood clot or plaque; and visualizing the blood clot or plaque over a period time by a visualizing system.Type: GrantFiled: November 5, 2004Date of Patent: September 28, 2010Inventor: John Steele Fisher
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Publication number: 20100239496Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: March 23, 2010Publication date: September 23, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharia, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
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Patent number: 7794691Abstract: Methods of using Th-226 or mother radionuclides thereof, namely U-230 or Th-226, in medicine. These radionuclides are particularly appropriate for the treatment of human and/or non-human mammals, in particular for therapeutic, diagnostic (detection/imaging), prophylactic and pain palliation purposes. These radionuclides may be used in various forms for treatment and/or diagnostic purposes, in particular in cationic form or in the form of radioconjugates or bone-targeting complexes. Methods of making such radionuclides.Type: GrantFiled: June 25, 2004Date of Patent: September 14, 2010Assignee: The European Community, represented by the European CommissionInventors: Alfred Morgenstern, Christos Apostolidis, Roger Molinet, Klaus Luetzenkirchen
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Patent number: 7790142Abstract: 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: GrantFiled: October 11, 2007Date of Patent: September 7, 2010Assignee: The General Hospital CorporationInventors: David R. Elmaleh, Alan J. Fischman, Timothy M. Shoup
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Patent number: 7790144Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologes. The compounds are be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1,300 nm, the exact range being dependent upon the particular dye. The use of a biocompatible organic solvent such as dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.Type: GrantFiled: March 15, 2004Date of Patent: September 7, 2010Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph Bugaj, Muthunadar P. Periasamy
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Patent number: 7790140Abstract: In part, the present invention is directed to biocompatible compositions comprising a carrier with a first metal binding domain, a metal ion, an active agent with second metal binding domain and optionally a protective chain covalently attached to the polymeric carrier.Type: GrantFiled: July 5, 2006Date of Patent: September 7, 2010Assignee: PharmaIN CorporationInventor: Elijah M. Bolotin
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Patent number: 7790141Abstract: Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.Type: GrantFiled: August 9, 2004Date of Patent: September 7, 2010Assignee: Pathak Holdings, LLCInventors: Chandrashekhar P. Pathak, Sanjay M. Thigle
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Publication number: 20100221180Abstract: A molecular probe for labeling myelin includes a fluorescent stilbenzene derivative.Type: ApplicationFiled: September 2, 2008Publication date: September 2, 2010Inventors: Yanming Wang, Chunying Wu
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Publication number: 20100221181Abstract: The present invention relates to a method of differentially diagnosing different types of dementia. In particular, the method relates to the use of specific SPECT tracers for differentially diagnosing Alzheimer's disease, Lewy-Body Dementia, and Frontotemporal Dementia.Type: ApplicationFiled: September 23, 2008Publication date: September 2, 2010Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V.Inventor: Frank Olaf Thiele
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Patent number: 7785566Abstract: The invention comprises pharmaceuticals of formula (I) Z-(L)n-V, wherein V denotes a peptide, L denotes an optional linker, Z denotes a group that optionally can carry an imaging moiety M, n denotes 0 or 1. The pharmaceuticals are active as therapeutic agents for the treatment of heart failure, cardiac arrhythmias and diseases were fibrosis is prominent such as COPD, liver fibrosis and atherosclerosis and are also useful as diagnostic agents for the diagnosis of heart failure and diseases were fibrosis is prominent such as COPD, liver fibrosis and atherosclerosis.Type: GrantFiled: November 5, 2004Date of Patent: August 31, 2010Assignee: GE Healthcare, Inc.Inventors: Alan Cuthbertson, Bard Indrevoll, Morten Eriksen
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Patent number: 7785565Abstract: Metal chelators of Formula I and Formula II are disclosed: or a pharmaceutically acceptable salt thereof. Also disclosed are metal chelator-targeting moiety complexes, metal chelator-targeting moiety-metal conjugates, kits, and methods of their preparation and use in diagnosis and/or treatment of diseases and conditions, including, inter alia, cancer and thrombosis.Type: GrantFiled: August 9, 2005Date of Patent: August 31, 2010Assignee: The United States of America as represented by the Secretary, Department of Health and Human ServicesInventors: Martin Wade Brechbiel, Thomas Clifford
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Patent number: 7785564Abstract: Aminophosphinic acid derivatives were synthesized as potential inhibitors of renal dipeptidase, an enzyme overexpressed in benign and malignant colon tumors. Several compounds showed potent enzyme-inhibitory activity. These compounds can be used therapeutically and diagnostically for treatment and detection of tumors.Type: GrantFiled: July 7, 2005Date of Patent: August 31, 2010Assignee: The Johns Hopkins UniversityInventors: Saeed R. Khan, Bert Vogelstein, Kenneth W. Kinzler, Hallur Gurulingappa, Phillip Buckhaults
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Publication number: 20100215574Abstract: The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.Type: ApplicationFiled: October 22, 2009Publication date: August 26, 2010Inventor: FELIX KRATZ
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Patent number: 7780952Abstract: The invention provides MRI detectable species of formula (I): Dp-Sn-Nm, 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 internalizing into tumor cells an amount of the MRI detectable moiety that is distinguishably higher than the amount internalized in normal healthy cells thus allowing the diagnosis of tumors. The internalization 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: GrantFiled: June 2, 2003Date of Patent: August 24, 2010Assignee: Bracco Imaging SpAInventors: Silvio Aime, Valentina Mainero, Simonetta Chirich Geninatti, Claudia Cabella
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Patent number: 7780947Abstract: New bifunctional chelation complexes are described. These are based on the structure of the so-called “TAME-HexA” molecule. The compounds are especially useful for forming chelation complexes with metal ions, including radioisotopes.Type: GrantFiled: December 3, 2004Date of Patent: August 24, 2010Assignees: Sloan-Kettering Institute for Cancer Research, Ludwig Institute for Cancer ResearchInventors: Enver Arslantas, Richard R. Schmidt, Peter M. Smith-Jones, Gerd Ritter
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Patent number: 7771704Abstract: The present invention provides radioactive metal heterocomplexes of formula (I): [(Me=N—R)L1L2]+Z? wherein Me, R, L1L2 and Z? have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium-or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me=N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me=N—R)Y2L1)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final [(Me=N—R)L1L2]+ Z?heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.Type: GrantFiled: June 23, 2008Date of Patent: August 10, 2010Assignee: Bracco Imaging S.p.A.Inventors: Francesco Tisato, Cristina Bolzati, Marina Porchia, Fiorenzo Refosco
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Patent number: 7771706Abstract: Disclosed is a method for monitoring early treatment response of a cancer treatment comprising measuring by magnetic resonance spectroscopy (MRS), for example, proton MRS, the amount of Choline present in the tissue adjoining or surrounding the cancerous tissue before and after treatment; the treatment comprises administration of an angiogenesis inhibitor, for example, a VEGF inhibitor, whereby a decrease in the amount of Choline after treatment is indicative of a positive response. The decrease in the amount of Choline represents the decrease in the internal cell membrane as a result of down regulation of the organelles and their secretory granules and their transport vesicles. Disclosed also is a method for determining effectiveness of an angiogenesis inhibitor in the treatment of cancer. Also disclosed are methods of monitoring early treatment response in diseases where an angiogenesis effector, i.e., an inhibitor or promoter of angiogenesis, is employed.Type: GrantFiled: January 11, 2007Date of Patent: August 10, 2010Assignee: Receptomon, LLCInventor: Joseph F. Norfray
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Publication number: 20100196269Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the ?-opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other ?-opioid receptor-mediated diseases, disorders, and/or conditions.Type: ApplicationFiled: July 27, 2009Publication date: August 5, 2010Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Guo-Hua Chu