In An Organic Compound Patents (Class 424/1.65)
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Patent number: 8303935Abstract: The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.Type: GrantFiled: May 15, 2007Date of Patent: November 6, 2012Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki, Yuki Okumura
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Patent number: 8303936Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared (NIR) spectral range. The NIR is highly sensitive for tumor detection and tracking. The application discloses targeting a tumor-enriched cell surface receptor with a ligand-conjugated fluorescent probe, which specifically allows detection of the tumor relative to the negligible animal autofluorescence.Type: GrantFiled: June 15, 2012Date of Patent: November 6, 2012Assignee: Li-Cor, Inc.Inventors: Daniel R. Draney, Ananda G. Lugade, Narasimhachari Narayanan, Joy Kovar, D. Michael Olive
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Publication number: 20120276006Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: ApplicationFiled: June 21, 2012Publication date: November 1, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
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Publication number: 20120276001Abstract: 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: ApplicationFiled: May 21, 2012Publication date: November 1, 2012Applicant: Nordion (Canada) IncInventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso, Cara Ferreira
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Publication number: 20120269726Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C1-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: ApplicationFiled: October 12, 2011Publication date: October 25, 2012Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20120269724Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.Type: ApplicationFiled: December 13, 2011Publication date: October 25, 2012Applicant: President and Fellows of Harvard CollegeInventors: Ashfaq Mahmood, Alun G. Jones, Naengnoi Limpa-Amara, Yijie Peng, Zeynep Akgun
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Patent number: 8293207Abstract: An amino acid analog is provided, in syn-stereoisomeric form, anti-stereoisomeric form, or a combination thereof. The amino acid analog includes a cyclobutane ring with at least one of an amine group and a carboxyl group attached to one carbon node of the cyclobutane ring. A chain of moieties X, Y, and Z attached to one of remaining three carbon nodes of the cyclobutane ring. X is a chelating agent selected from a group comprising DCTA, DOTA, DTPA, EDTA, NOTA, PCTA, and TETA. Y is a linking moiety selected from a group comprising —NH—CO— and —NH-p-CHSN-Bn- where the linking moiety facilitates incorporation of the chelating agent into the amino acid analog. Z is a metal radioisotope selected from a group comprising Cu-60, Cu-61, Cu-62, Cu-64, Cu-67, Ga-67, Ga-68, Y-86, Y-88, Y-90, Sr-85, Sr-89, Gd-153, Gd-157, Sm-153, Lu-177, W-185, Re-186, Re-188, and Ir-192.Type: GrantFiled: September 18, 2009Date of Patent: October 23, 2012Inventors: Valery Zavarzin, Irving Weinberg
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Patent number: 8293209Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.Type: GrantFiled: October 22, 2009Date of Patent: October 23, 2012Assignee: Segev Laboratories LimitedInventor: David Segev
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Patent number: 8287840Abstract: This invention is directed to methods of treating solid tumor cancers, particularly refractory cancers by administration of two pluralities of microparticles, one comprising drug-carrying microparticles sized to lodge at the tumor preferably in the capillary bed of the tumor and the other comprising non-drug-carrying microparticles sized to lodge in the arterial system servicing the tumor so as to embolize the tumor.Type: GrantFiled: July 24, 2009Date of Patent: October 16, 2012Assignee: Abbott Cardiovascular Systems Inc.Inventors: Liangxuan Zhang, Florencia Lim
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Publication number: 20120251448Abstract: Provided are the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of pathological characteristics unique to synuclein diseases, such as Parkinson's disease.Type: ApplicationFiled: March 2, 2012Publication date: October 4, 2012Inventors: Franz F. Hefti, Geoffrey Golding, Ximin Li, Seok-Rye Choi, Luke Esposito, Marisa-Claire Yadon, Joel Cummings, F. Michael Hudson, Thomas Lake, Alan D. Snow
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Publication number: 20120251443Abstract: The present disclosure provides compositions and methods based on implantable contrast agents that are useful for imaging tissue and organs.Type: ApplicationFiled: October 1, 2010Publication date: October 4, 2012Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: C. Keith Ozaki, Jeffrey M. Karp, Frank Rybicki, Dimitrios Mitsouras, Praveen Kumar Vemula
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Patent number: 8277776Abstract: This disclosure relates to compositions for delivering agents to a subject, and in particular, to compositions for delivery of therapeutic agents or diagnostic agents in the presence or absence of targeting moieties. In part, this disclosure relates to compositions comprising a hydrophobic group with a first end and a second end, a first metal binding domain linked to the hydrophobic group, a metal ion capable of being chelated to the first metal binding domain, and an agent linked to a second metal binding domain capable of chelating to the metal ion.Type: GrantFiled: November 24, 2009Date of Patent: October 2, 2012Assignee: PharmaIN CorporationInventors: Elijah M. Bolotin, Gerardo M. Castillo
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Patent number: 8277777Abstract: A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.Type: GrantFiled: June 21, 2007Date of Patent: October 2, 2012Assignees: Nihon Medi-Physics Co., Ltd., GE Healthcare LimitedInventors: Shigeyuki Tanifuji, Akio Hayashi, Daisaku Nakamura, Shinya Takasaki, Anthony Eamon Storey, Denis Raymond Christophe Bouvet
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Publication number: 20120244074Abstract: The present invention provides alternative in vivo imaging agents suitable for use in the detection of ?v?6 expressed in a subject. The invention also provides a method for obtaining said in vivo imaging agents, and use of the in vivo imaging agents in determining ?v?6 expressed in a subject.Type: ApplicationFiled: December 16, 2010Publication date: September 27, 2012Inventor: Magne Solbakken
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Patent number: 8273325Abstract: The present invention provides novel compounds and pharmaceutical compositions containing such compounds, wherein the compounds have affinity for proteoglycans. The compounds comprise an amino acid based core unit linked to positively charged moieties. The compounds further comprise at least one imaging moiety detectable in in vivo imaging making the compounds useful as diagnostic contrast agents for imaging of proteoglycans, such as heparan sulphate proteoglycans.Type: GrantFiled: December 19, 2007Date of Patent: September 25, 2012Assignee: GE Healthcare ASInventors: Helge Tolleshaug, Alan Cuthbertson, Hege Karlsen
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Publication number: 20120237445Abstract: Radiopharmaceutical compositions, and related methods, useful for medical imaging are provided. The radiopharmaceutical compositions include one or more radiopharmaceutical compounds, together with a stabilizer comprising ascorbic acid, wherein the pH of said composition is within the range of about 3.5-5.5.Type: ApplicationFiled: April 15, 2010Publication date: September 20, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: James F. Castner, Dianne D. Zdankiewicz, James E. Anderson
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Patent number: 8263039Abstract: Use of DKK-1 protein or the nucleic acid sequence in preparation of cancer diagnostic agents or kits, method to detect liver cancer with the monoclonal antibody thereof, the kit comprising anti-DKK-1 antibody or protein specific nucleic acid probes, together with a label, and method to detecting specific DKK-1 protein expression are disclosed.Type: GrantFiled: November 11, 2008Date of Patent: September 11, 2012Assignee: Shanghai Cancer InstituteInventors: Wenxin Qin, Haitao Zhang, Yanjun Yu, Haiyan You, Shengli Yang, Jianren Gu, Gang Huang, Shile Sheng, Tao Chen
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Patent number: 8263040Abstract: The invention relates to the subjects characterized in the patent claims, namely metal chelates having a perfluorinated PEG radical, processes for their preparation, and their use, processes for their preparation and their use in NMR and X-ray diagnosis, radiodiagnosis and radiotherapy, and in MRT lymphography.Type: GrantFiled: October 17, 2007Date of Patent: September 11, 2012Assignee: Bayer Schering Pharma AGInventors: Johannes Platzek, Heiko Schirmer, Hanns-Joachim Weinmann, Bernd Misselwitz, Ludwig Zorn
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Patent number: 8263042Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: GrantFiled: December 19, 2008Date of Patent: September 11, 2012Assignee: Lantheus Medical Imaging, Inc.Inventors: Heike S. Radeke, David S. Casebier, Michael T. Azure, Douglas D. Dischino
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Patent number: 8263098Abstract: This invention relates to a “high lower alcohol content” (>40% v/v of a C1-4 alcohol) liquid composition able to be dispensed as a stable foam with the use of non-propellant foam dispensing devices from non-pressurized containers. The liquid compositions comprise an alcohol, C1-4 (>40% v/v), a silicone-based surfactant of at least 0.001% by weight to prepare a foamable composition, 0-10% w/w of additional minor components added to obtain the desired performance (a foamable composition), and the balance being purified water. The compositions may include emulsifier-emollients and mosturizers, secondary surfactants, foam stabilizers, fragrances, antimicrobial agents, other type of medicinal ingredients, and the like ingredients or additives or combinations thereof commonly added to alcohol gels or foams, aerosol compositions or to toiletries, cosmetics, pharmaceuticals and the like.Type: GrantFiled: March 7, 2006Date of Patent: September 11, 2012Assignee: Deb Worldwide Healthcare Inc.Inventors: Maria Teresa Fernandez de Castro, Bruce Michael Koivisto, Francisco Munoz
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Publication number: 20120225015Abstract: The inventive method relates to a method for the determination of susceptibility or diagnosis of autism or autism spectrum disorders. Diagnosis or determination of susceptibility determinations are predicated on quantitative analysis of endocannibinoid levels or endocannibinoid receptor expression.Type: ApplicationFiled: March 3, 2012Publication date: September 6, 2012Inventors: Stephen T. Schultz, Mauris N. DeSilva, Georgianna G. Gould
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Patent number: 8257682Abstract: This disclosure relates to compositions for delivering agents to a subject, and in particular, to compositions for delivery of therapeutic agents or diagnostic agents in the presence or absence of targeting moieties. In part, this disclosure relates to compositions comprising a hydrophobic group with a first end and a second end, a first metal binding domain linked to the hydrophobic group, a metal ion capable of being chelated to the first metal binding domain, and an agent linked to a second metal binding domain capable of chelating to the metal ion.Type: GrantFiled: August 31, 2009Date of Patent: September 4, 2012Assignee: PharmaIn CorporationInventors: Elijah M. Bolotin, Gerardo M. Castillo
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Patent number: 8258101Abstract: This invention relates to new peptide-based compounds and their use in therapeutically effective treatments as well as for diagnostic imaging techniques. More specifically the invention relates to the use of such peptide-based compounds used as targeting vectors that bind to receptors associated with angiogenesis, in particular the ?v?3 integrin receptor. Such contrast agents may thus be used for diagnosis of for example malignant diseases, heart diseases, inflammation-related diseases, rheumatoid arthritis and Kaposi's sarcoma. Moreover such compounds may also be used in therapeutic treatment of these diseases.Type: GrantFiled: June 14, 2010Date of Patent: September 4, 2012Assignee: GE Healthcare ASInventor: Alan Cuthbertson
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Patent number: 8257684Abstract: Disclosed herein are methods for identifying and targeting autonomic and autonomic-related brain regions. In one embodiment, a method of identifying a brain region in a patient comprises administering to the patient a targeting agent that activates or inhibits a brain region and imaging the brain region.Type: GrantFiled: March 26, 2009Date of Patent: September 4, 2012Assignee: Neurosigma, Inc.Inventors: Alejandro Covalin, Antonio Afonso Ferreira De Salles
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Patent number: 8257683Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.Type: GrantFiled: October 23, 2009Date of Patent: September 4, 2012Assignee: Mallinckrodt LLCInventors: Gary L. Cantrell, B. Daniel Burleigh
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Publication number: 20120219496Abstract: The invention relates to nanocluster compositions and uses thereof. Specifically, the invention relates to gadolinium-linked nanocluster compositions and their use in diagnosis and prognosis of diseases. The nanocluster compositions of the invention are effective in enhancing the payload of a gadolinium and thereby increasing the longitudinal relaxivity of each particle in the cluster.Type: ApplicationFiled: August 30, 2010Publication date: August 30, 2012Inventors: Andrew Tsourkas, Zhiliang Cheng
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Publication number: 20120219497Abstract: A polymeric material comprised of (i) at least one random copolymer comprised of ethylene oxide and one or more other alkylene oxide(s) and (ii) at least one non-random polymer comprised of one or more poly(alkylene oxide)s has been discovered. Preferably, it is a polymer alloy. Alkylene oxide homo-polymers or block copolymers may be the non-random polymer. In a related discovery, an adhesive material can be made by suspending (a) particles in (b) a matrix of at least one poly(ethylene oxide) copolymer of ethylene oxide and propylene oxide, or a combination thereof. The handling characteristics may be adjusted for different utilities (e.g., from runny oil to hard wax). Applications include use as adhesive, cohesive, filler, lubricant, surfactant, or any combination thereof. In particular, the hard materials may be used for cleaning or waxing.Type: ApplicationFiled: February 27, 2012Publication date: August 30, 2012Applicant: SYNCERA, INC.Inventors: Tadeusz WELLISZ, Timothy C. Fisher, Jonathan K. Armstrong, John Cambridge
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Synthetic C-glycolipid and its use for treating cancer, infectious diseases, and autoimmune diseases
Patent number: 8252909Abstract: The invention is directed to compounds of formula (I) wherein X is O or NH; R? is a hydrocarbon chain; R3 and R4 are hydrogen, OH or a monosaccharide; R5 is hydrogen or a monosaccharide; Q? is optionally present and may be a C1-10 hydrocarbon; X? is optionally present and may be O, S or NR8; and Q3 may be a hydrocarbon or hydrogen. The invention is also directed to the use of the compounds for treating cancer, infectious diseases and autoimmune diseases. The invention is also directed to syntheses of the compounds of formula (I).Type: GrantFiled: July 29, 2005Date of Patent: August 28, 2012Assignees: New York University, The Research Foundation of the City University of New YorkInventors: Moriya Tsuji, Guangwu Chen, Richard Franck, Guangli Yang -
Publication number: 20120213702Abstract: The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3? and R3? is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention.Type: ApplicationFiled: August 31, 2010Publication date: August 23, 2012Inventors: Christoph Bremer, Carsten Höltke
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Patent number: 8246930Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.Type: GrantFiled: October 23, 2009Date of Patent: August 21, 2012Assignee: Mallinckrodt LLCInventors: Gary L. Cantrell, B. Daniel Burleigh
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Publication number: 20120207674Abstract: The cancer-imaging agent and method of radioimaging relates to the use of a radioimaging agent for the imaging increased choline uptake to detect cancerous tissue. The radioimaging agent includes choline or a pharmaceutically acceptable salt thereof labeled with technetium-99m. Preferably, the radioimaging agent is [methyl]-choline chloride labeled with 99mTcO4, which carries technetium-99m. In use, a patient is administered an effective amount of the radioimaging agent by injection and then scanned with a radioimaging device. The radioimaging agent is used to image select soft tissues in the patient, such as the liver or gallbladder, the upper abdominal organs, or the like, and to detect increased choline uptake. Choline is known to accumulate in cancerous cells. Thus, the radioimaging agent is particularly effective in the detection of potentially cancerous tissues.Type: ApplicationFiled: February 15, 2011Publication date: August 16, 2012Applicant: KUWAIT UNIVERSITYInventor: FATMA JASSAB FALEH MARZOOQ AL-SAEEDI
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Patent number: 8241607Abstract: This invention relates to compositions, methods utilizing fructose and other monosaccharides for the diagnosis of cancer. Cancer cells have shown a higher level of fructose utilization as compared to glucose. Further, cancer cells have shown a preferential use of fructose for nucleic acid synthesis. The present invention takes advantage of these features and provides for fructose or fructose-based compositions for the diagnosis of cancer using imaging techniques such as positron emission tomography.Type: GrantFiled: August 24, 2006Date of Patent: August 14, 2012Assignee: Cedars-Sinai Medical CenterInventors: Anthony P. Heaney, Hongxiang Hui, Alan Waxman
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Publication number: 20120201754Abstract: Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particulaly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.Type: ApplicationFiled: October 7, 2010Publication date: August 9, 2012Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
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Patent number: 8236283Abstract: This invention relates to a method for imaging of wet age-related macular degeneration (AMD) using a contrast agent comprising a vector attached to an optical imaging reporter, wherein the vector has affinity for receptors associated with angiogenesis. The invention further provides such methods for monitoring the effect of treatment of AMD.Type: GrantFiled: January 6, 2006Date of Patent: August 7, 2012Assignee: GE Healthcare ASInventors: Alan Cuthbertson, Maria E. Verdugo-Gazdik
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Patent number: 8236282Abstract: This invention provides benzothiazole derivative compounds, compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for detecting amyloid deposit(s) and for diagnosing a disease, disorder or condition characterized by amyloid deposit(s).Type: GrantFiled: September 30, 2009Date of Patent: August 7, 2012Assignee: University of Pittsburgh—of the Commonwealth System of Higher EducationInventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
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Patent number: 8236279Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.Type: GrantFiled: September 21, 2009Date of Patent: August 7, 2012Assignee: Board of Regents, The University of Texas SystemInventors: David J. Yang, Chun W. Liu, Dong-Fang Yu, E. Edmund Kim
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Publication number: 20120195832Abstract: 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: March 7, 2012Publication date: August 2, 2012Applicant: KTB Tumorforschungs GMBHInventor: Felix Kratz
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Patent number: 8231859Abstract: This disclosure relates to compositions for delivering agents to a subject, and in particular, to compositions for delivery of therapeutic agents or diagnostic agents in the presence or absence of targeting moieties. In part, this disclosure relates to compositions comprising a hydrophobic group with a first end and a second end, a first metal binding domain linked to the hydrophobic group, a metal ion capable of being chelated to the first metal binding domain, and an agent linked to a second metal binding domain capable of chelating to the metal ion.Type: GrantFiled: November 23, 2009Date of Patent: July 31, 2012Assignee: PharmaIN CorporationInventors: Elijah M. Bolotin, Gerardo M. Castillo
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Publication number: 20120189543Abstract: Methods and compositions for detecting, diagnosing, and treating osteolysis and implant loosening are disclosed.Type: ApplicationFiled: September 9, 2010Publication date: July 26, 2012Inventors: Dong Wang, Steven R. Goldring, Edward V. Fehringer
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Patent number: 8226927Abstract: The present invention relates to new 11C/18F-labeled inhibitor compounds for over-expressed GSK-3 prepared from the GMP synthesis method. The present invention provides novel 11C/18F inhibitor compounds for over-expressed GSK-3 that are suitable for use as an in vivo imaging agent. A pharmaceutical comprising the compound and a kit for the preparation of the pharmaceutical are also provided.Type: GrantFiled: May 21, 2007Date of Patent: July 24, 2012Inventors: Farhad Karimi, Bengt Langstrom
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Patent number: 8221719Abstract: This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid supports conjugated with said chelates, chelating agents or labeled biomolecules. Especially the invention relates to novel chelating agents useful in solid phase synthesis of oligonucleotides or oligopeptides and the oligonucleotides and oligopeptides so obtained.Type: GrantFiled: September 5, 2008Date of Patent: July 17, 2012Assignee: Wallac OyInventors: Jari Peuralahti, Jari Hovinen, Janne Ketola, Lassi Jaakkola, Veli-Matti Mukkala, Päivi Liitti
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Patent number: 8221720Abstract: The invention relates to novel processes for the purification of radiolabelled tracers, using a solid-support bound scavenger group.Type: GrantFiled: May 11, 2005Date of Patent: July 17, 2012Assignees: Hammersmith Imanet Limited, GE Healthcare Limited, GE Healthcare ASInventors: Sajinder Kaur Luthra, Frank Brady, Nicholas Toby Jeffery, Erik Arstad, Alexander Mark Gibson, Duncan Wynn, Alan Cuthbertson, Magne Solbakken
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Publication number: 20120177569Abstract: The present invention provides radioactive gallium complexes which comprise DOTA-biotin conjugates, incorporating a linker group. Also described are radiopharmaceutical compositions, and methods and uses of the complexes for in vivo imaging involving pre-targeting with avidin.Type: ApplicationFiled: September 16, 2010Publication date: July 12, 2012Applicants: HAMMERSMITH IMANET LMITED, GE HEALTHCARE LIMITEDInventors: Irina Velikyan, Elisabeth Blom, Bengt Langstrom
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Publication number: 20120177570Abstract: The invention relates to compounds of formula IA? and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: February 14, 2012Publication date: July 12, 2012Applicant: Purdue Pharma L.P.Inventor: Laykea TAFESSE
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Patent number: 8216547Abstract: The present invention is directed to radiolabelled ligands, useful for the labeling and imaging of TRP M8 (transient receptor potential M8 channel) functionality. The present invention is further directed to pharmaceutical compositions comprising the radiolabelled ligands and methods for the preparation of the radiolabelled ligands.Type: GrantFiled: July 9, 2009Date of Patent: July 10, 2012Assignee: Janssen Pharmaceutica NVInventors: Paul D. Acton, Dennis J. Hlasta, Jay M. Matthews, James J. McNally
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Publication number: 20120171116Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.Type: ApplicationFiled: July 26, 2011Publication date: July 5, 2012Inventors: Bruce Edward Tomczuk, Gary Lee Olson, Richard Scott Pottorf, Jane Wang, Bhaskara Rao Nallaganchu
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Patent number: 8211402Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.Type: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Patent number: 8211401Abstract: A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. 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: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Publication number: 20120164070Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: ApplicationFiled: March 1, 2012Publication date: June 28, 2012Applicant: ABBOTT LABORATORIESInventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
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Patent number: 8202509Abstract: The present application discloses compositions and methods of synthesis and use of 68Ga, 18F or 19F labeled molecules of use in PET or MRI imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a chelating moiety, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 68Ga, 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. In more preferred embodiments, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment.Type: GrantFiled: December 2, 2010Date of Patent: June 19, 2012Assignee: Immunomedics, Inc.Inventors: William J. McBride, Christopher A. D'Souza, David M. Goldenberg