Abstract: The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (?-, ?-)dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.
Type:
Grant
Filed:
November 30, 2012
Date of Patent:
June 21, 2016
Assignee:
THE JOHNS HOPKINS UNIVERSITY
Inventors:
Martin Gilbert Pomper, Sangeeta Ray, Ronnie C. Mease, Hassan Shallal
Abstract: The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi.
Type:
Grant
Filed:
August 17, 2012
Date of Patent:
May 24, 2016
Assignee:
PIRAMAL IMAGING SA
Inventors:
Markus Berger, Martin Kruger, Jessica Lohrke, Michael Reinhardt, Holger Siebeneicher
Abstract: The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogs, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
Abstract: Methods and compositions utilizing ether and alkyl phospholipid ether analog compounds for treating cancer and imaging, monitoring, and detecting cancer stem cells in humans.
Type:
Grant
Filed:
May 6, 2013
Date of Patent:
May 17, 2016
Assignee:
CELLECTAR, INC.
Inventors:
Jamey P. Weichert, Anatoly Pinchuk, Irawati Kandela, Marc Longino, William R. Clarke
Abstract: Novel fluorogenic compounds designed such that upon a chemical event, compounds capable of emitting NIR light are generated, are disclosed. The compounds comprise two or more acceptor-containing moieties and a cleavable donor-containing moiety, being in complete pi-electrons conjugation and being such that no delocalization of pi-electrons is enabled. Also disclosed are fluorescent compounds generated upon subjecting the fluorogenic compounds to a chemical event (e.g., deprotonation). Also disclosed are uses of the fluorogenic compounds as NIR probed with a Turn-ON mechanism in monitoring presence and/or level of various analytes.
Abstract: The invention provides novel biocompatible upconversion nanoparticle (UCNP) that comprises a core of cubic nanocrystals (e.g., comprising ?-Na Lna, Lnb Lnc F4) and an epitaxial shell (e.g., formed from CaF2; wherein Lnb is Yb), and related methods of preparation and uses thereof.
Abstract: The present invention provides a method useful in the diagnosis and monitoring of cancer wherein there is an abnormal expression of PBR. The method of the invention is particularly useful in evaluating the severity of the cancer, e.g. PBR expression correlates with cell proliferation rates, metastatic potential, tumor aggressiveness, malignancy progression. The method of the invention can therefore be applied in the determination of likely disease progression and in making an associated prognosis. Furthermore, the method of the invention can find use in determining the likely success of certain therapeutic approaches, or in the evaluation of the efficacy of certain proposed new treatments.
Abstract: AIE (aggregation-induced emission)-active TPE derivatives, TPE-TPP, TPE-MitoR and TPE-IQ are contemplated. These specific TPE derivatives are useful as fluorescent agents for mitochondrial imaging and as apoptosis inducers. Possessing high specificity to mitochondria, superior photostability and appreciable tolerance to microenvironment change, TPE derivatives are well-suited imaging agents for mitochondrial targeting and morphological change tracking. Because of their synthetic flexibility, TPE derivatives can be further modified as dual-functional probes for an array of applications such as sensing of ROS, metal ions, or pH change in mitochondria.
Type:
Grant
Filed:
January 27, 2014
Date of Patent:
April 19, 2016
Assignee:
THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY
Abstract: Disclosed is a near-infrared fluorescent imaging agent comprising an indocyanine-based fluorescent dye and a liposome. The near-infrared fluorescent imaging agent of the present invention demonstrates high fluorescence intensity and a long anchoring time in sentinel lymph nodes, thereby making it useful for detecting sentinel lymph nodes in sentinel lymph node navigation surgery. Also disclosed is an indocyanine green derivative that is particularly suitable for use in the near-infrared fluorescent imaging agent of the present invention.
Abstract: Compounds and uses of the compounds are provided. The compounds can be used as Fe(II) sequestering compounds. For example, these compounds can be used to sequester Fe(II) in cells, organs, vasculature, or tissues. Also, provided are compositions and methods of using the them for sequestering Fe(II) in an individual. The compounds can be used as MRI paraCEST contrast agents.
Type:
Grant
Filed:
May 11, 2012
Date of Patent:
April 5, 2016
Assignee:
The Research Foundation for The State University of New York
Abstract: The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.
Type:
Grant
Filed:
August 10, 2012
Date of Patent:
March 29, 2016
Assignee:
MERCK & CIE
Inventors:
Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Harriet Struthers, Viola Groehn, Simon Mensah Ametamey, Cindy Ramona Fischer
Abstract: Compounds and a method for imaging myocardial perfusion, including administering to a patient a compound linked to an imaging moiety, wherein the compound binds MC-1, and scanning the patient using diagnostic imaging. Kits including the compound or precursor compounds linked or not linked to an imaging moiety are also described.
Abstract: The present invention relates to a pharmaceutical composition comprising an effective amount of silver nanoparticles and extracts of Polygonum Multiflorum Thunb, a method for increasing hair growth by administering the pharmaceutical composition locally to a host, and use thereof.
Abstract: The present invention relates to Radiolabeled Compounds labeled with fluorine, bromine, iodine, carbon, or tritium isotopes and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.
Type:
Grant
Filed:
November 5, 2012
Date of Patent:
March 22, 2016
Assignee:
The Trustees of Columbia University in the City of New York
Abstract: Compounds of formula (I) in which: >R is a linear or branched (C1-C6) alkyl, >L is a spacer group, >A is a diagnostic agent, and >m is equal to 1 or 2.
Type:
Grant
Filed:
July 12, 2012
Date of Patent:
March 8, 2016
Assignee:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
Abstract: Contemplated compositions and methods are drawn to use of various boron-containing compounds to temporarily and transiently increase endogenous blood calcitriol concentration. The boron-containing compound is preferably a carbohydrate-boron complex having sufficient stability to achieve measurable quantities of the complex in blood upon oral administration of the complex.
Abstract: The present disclosure provides functionalized magnetic nanoparticles (MNPs) comprising a functional group that binds to ?-amyloid deposits and/or neurofibrillary tangles. The present disclosure provides compositions comprising the functionalized MNPs, and methods of using the functionalized MNPs in imaging ?-amyloid deposits and neurofibrillary tangles.
Type:
Grant
Filed:
April 4, 2012
Date of Patent:
March 1, 2016
Assignee:
The Regents of the University of California
Abstract: Embodiments of the present disclosure provide for a compound, methods of making a compound, a probe, methods of making a probe, pharmaceutical compositions including a probe or a compound, methods of using a probe, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a disease (e.g., cancer, diseases caused by inflammation (e.g., arthritis, cardiovascular disease, and the like)), and the like, and/or related biological events using a probe, kit for imaging, diagnosing, localizing, monitoring, and/or assessing a disease, and/or related biological events, using a probe, and the like.
Type:
Grant
Filed:
November 7, 2013
Date of Patent:
February 23, 2016
Assignee:
VANDERBILT UNIVERSITY
Inventors:
Wellington Pham, Donald D. Nolting, John C. Gore
Abstract: 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:
Grant
Filed:
September 2, 2014
Date of Patent:
February 23, 2016
Assignee:
Lantheus Medical Imaging, Inc.
Inventors:
Richard R. Cesati, Thomas D. Harris, Simon P. Robinson, Richard J. Looby, Edward H. Cheesman, Padmaja Yalamanchili, David S. Casebier