Abstract: A method of reducing radiation exposure of a non-cancerous tissue of a patient diagnosed with a cancer includes administering to the patient an agent capable of competing for binding sites on a surface of the non-cancerous tissue, provided that the administration is carried out after a waiting period that follows administration of a compound including a radionuclide to the patient, the compound having affinity for both a cancerous tissue and the non-cancerous tissue, and, further provided that the binding sites have an affinity for both the agent and the compound.
Type:
Grant
Filed:
April 28, 2020
Date of Patent:
November 9, 2021
Assignee:
Molecular Insight Pharmaceuticals, Inc.
Inventors:
John W. Babich, Shawn Hillier, John Joyal
Abstract: An object of this invention is to provide a streptavidin mutant reduced in affinity to the naturally-occurring biotin, and to provide a modified biotin which shows a high affinity to such streptavidin mutant reduced in affinity to the naturally-occurring biotin. This invention can provide a compound composed of a dimer of modified biotin, a streptavidin mutant, angsd usage of them.
Abstract: There is provided a radiolabelled peptide-based compound for diagnostic imaging using positron emission tomography (PET). The compound may thus be used for diagnosis of malignant diseases. The compound is particularly useful for imaging of somatostatin overexpression in tumors, wherein the compound is capable of being imaged by PET when administered with a target dose in the range of 150-350 MBq, such as 150-250 MBq, preferable in the range of 191-210 MBq.
Type:
Grant
Filed:
June 27, 2019
Date of Patent:
November 2, 2021
Assignee:
SOMSCAN APS
Inventors:
Andreas Kjaer, Ulrich Knigge, Liselotte Højgaard, Palle Rasmussen
Abstract: The present disclosure relates to compounds of Formula I and II, wherein R1-R20 and FL are defined herein. Also provided are methods of targeting alpha-radiation to poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, reducing proliferation of cancer cells, reducing proliferation of cancer cells, detecting intact and enzymatically active poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, detecting PARP-1 enzyme expression in a subjects tissue sample, monitoring cancer treatment in a subject, or detecting a PARP-1 receptive cancer in a subject.
Type:
Grant
Filed:
May 24, 2018
Date of Patent:
November 2, 2021
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
Robert H. Mach, Sean Reilly, Mehran Makvandi, Kuiying Xu, Daniel A. Pryma, Roger A. Greenberg
Abstract: Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.
Abstract: Provided herein are conjugates, compositions and methods for use in photoimmunotherapy, such as photoimmunotherapy induced by activation of a phthalocyanine dye conjugated to a targeting molecule that binds a protein on cell, for example, an IR700-antibody conjugate. In some embodiments, the phthalocyanine-dye conjugate can be activated by irradiation with near-infrared light. Features of the conjugates, compositions and methods, including the dose of the conjugate, provide various advantages, such as lower toxicity and/or improved efficacy. In some embodiments, also provided is a dual label phthalocyanine-dye conjugate in which the targeting molecule is conjugated to an additional fluorescent dye, which can be used for photoimmunotherapy while, for example, also exhibiting improved performance for imaging or detection. Also provided are therapeutic methods using the conjugates and compositions for treatment of diseases and conditions, including tumors or cancers.
Type:
Grant
Filed:
August 18, 2016
Date of Patent:
October 26, 2021
Assignee:
Rakuten Medical, Inc.
Inventors:
Miguel Garcia-Guzman, Eileen Sun Chin, Deepak Yadav, Jerry Fong
Abstract: Embodiments of the present disclosure pertain to methods of opening a lipid bilayer by associating the lipid bilayer with a molecule that includes a moving component capable of moving (e.g., rotating) in response to an external stimulus; and exposing the molecule to an external stimulus before, during or after associating the molecule with the lipid bilayer. The exposing causes the moving component of the molecule to move and thereby open the lipid bilayer (e.g., by pore formation). The external stimuli may include an energy source, such as ultraviolet light. The opened lipid bilayer may be a component of cell membranes in vitro or in vivo. The opening of the lipid bilayer may allow for the passage of various materials (e.g., active agents, such as peptide-based drugs) through the lipid bilayer and into cells. Additional embodiments of the present disclosure pertain to the aforementioned molecules for opening lipid bilayers.
Type:
Grant
Filed:
July 14, 2017
Date of Patent:
October 26, 2021
Assignees:
WILLIAM MARSH RICE UNIVERSITY, DURHAM UNIVERSITY
Inventors:
James M. Tour, Robert Pal, Victor García-López, Lizanne Nilewski
Abstract: Provided herein are conjugates, compositions and methods for use in photoimmunotherapy, such as photoimmunotherapy induced by activation of a phthalocyanine dye conjugated to a targeting molecule that binds a protein on cell, for example, an IR700-antibody conjugate. In some embodiments, the phthalocyanine-dye conjugate can be activated by irradiation with near-infrared light. Features of the conjugates, compositions and methods, including the dose of the conjugate, provide various advantages, such as lower toxicity and/or improved efficacy. In some embodiments, also provided is a dual label phthalocyanine-dye conjugate in which the targeting molecule is conjugated to an additional fluorescent dye, which can be used for photoimmunotherapy while, for example, also exhibiting improved performance for imaging or detection. Also provided are therapeutic methods using the conjugates and compositions for treatment of diseases and conditions, including tumors or cancers.
Type:
Grant
Filed:
May 23, 2019
Date of Patent:
October 19, 2021
Assignee:
Rakuten Medical, Inc.
Inventors:
Merrill Biel, Roger Heim, Miguel Garcia-Guzman
Abstract: Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein L1 and L2 are each independently a covalent bond or a divalent linking group, R is a detectable label or therapeutic drug and B is an albumin binding moiety. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells using a compound of Formula (I).
Abstract: Berberine or its derivatives are used in the preparation of myocardial perfusion imaging agents It has been verified using in vitro investigations, in vivo biodistribution, and small animal PET dynamic imaging, etc., that 18F-labeled berberine derivatives can specifically accumulate in cardiomyocytes or heart tissues, and has good distribution properties of targetting heart muscle in living animals, together with high contrast values of heart v.s. peripheral tissue (liver, lung, blood, muscle, bone, etc.).
Abstract: An aqueous composition which is useful for producing coatings and capsule shells comprises a) dispersed particles of an esterified cellulose ether comprising (i) groups of the formula —C(O)—R—COOA or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein R is a divalent hydrocarbon group and A is hydrogen or a cation, and the total degree of ester substitution is more than 0.70, and b) an esterified cellulose ether comprising aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent hydrocarbon group, wherein I) the degree of neutralization of the groups —C(O)—R—COOH is not more than 0.4, II) the total degree of ester substitution is from 0.03 to 0.70, and III) the esterified cellulose ether b) has a solubility in water of at least 2.0 weight percent at 2° C.
Type:
Grant
Filed:
September 29, 2016
Date of Patent:
October 12, 2021
Assignee:
Nutrition & Biosciences USA 1, LLC
Inventors:
Oliver Petermann, Matthias Knarr, Meinolf Brackhagen
Abstract: A pharmaceutical tablet for use in administering one or more pharmaceutically active ingredients, comprising a polymer system, the one or more pharmaceutically active ingredients, a flavor, and a sweetener, wherein at least 20% by weight of the pharmaceutical tablet comprises substantially non-elastomeric polymer and less than 5% by weight of the pharmaceutical tablet comprises one or a combination of elastomeric polymers, and wherein the pharmaceutical tablet comprises at least 70% by weight of said polymer system comprising polyvinyl acetate (PVA) and less than 10% by weight of said polymer system comprising polymer having a molecular weight (Mw) greater than 50,000 g/mol.
Abstract: The present invention relates to a method of labelling biological molecules with 18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.
Type:
Grant
Filed:
January 22, 2013
Date of Patent:
October 5, 2021
Assignees:
GE Healthcare Limited, University of Southampton
Inventors:
Rajiv Bhalla, Sajinder Kaur Luthra, Gill Reid, I, William Levason
Abstract: The present invention provides a nanoparticle including at least one poly(vinyl alcohol) (PVA) having a molecular weight of from about 10 kDa to about 200 kDa, substituted with one or more moieties selected from: a therapeutic agent having a boronic acid moiety, wherein the therapeutic agent is covalently linked to the PVA via a boronate ester bond; a crosslinking group having a disulfide moiety, wherein the crosslinking group is covalently linked to the PVA, and a porphyrin, wherein the porphyrin is covalently linked to the PVA. Use of the nanoparticles for tumor detection and the treatment of diseases, including methods for photodynamic therapy and photothermal therapy, are also described.
Type:
Grant
Filed:
August 15, 2016
Date of Patent:
October 5, 2021
Assignee:
The Regents of the University of California
Inventors:
Kit S. Lam, Yuanpei Li, Kai Xiao, Caihong Feng
Abstract: Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.
Abstract: Described herein are Tz/TCO-based pretargeting strategies using an Al[18F]-NOTA-labeled tetrazine radioligand. This imaging strategy enables delineation of cancer at earlier time points compared to other imaging strategies and further decreases the radiation dose to healthy tissues compared to directly labeled antibodies. Al-based 18F imaging of small molecules, such as tetrazine, has not been previously achieved due to the decomposition of tetrazine during radiofluorination. Radiofluorination is advantageous over other radiolabeling methods because, in addition to having a shorter half-life, 18F is more readily available to produce and therefore integrated into hospital workflows.
Type:
Grant
Filed:
November 28, 2018
Date of Patent:
October 5, 2021
Assignee:
MEMORIAL SLOAN KETTERING CANCER CENTER
Inventors:
Brian Zeglis, Jason Lewis, Thomas Reiner, Jacob Lee Houghton, Jan-Philip Meyer, Christian Brand
Abstract: An automated radiopharmaceutical production and quality control system includes a particle accelerator, a radiopharmaceutical micro-synthesis subsystem, and quality control subsystem. The micro-accelerator of the improved biomarker generator is optimized for producing radioisotopes useful in synthesizing radiopharmaceuticals in quantities on the order of multiple unit doses, allowing for significant reductions in size, power requirements, and weight when compared to conventional radiopharmaceutical cyclotrons. The radiopharmaceutical micro-synthesis subsystem encompasses a small volume chemical synthesis system comprising a microreactor and/or a microfluidic chip and optimized for synthesizing the radiopharmaceutical in small quantities, allowing for significant reductions in processing time and in the quantity of radioisotope required. The automated quality control subsystem is used to test the composition and characteristics of the radiopharmaceutical to ensure that it is safe to inject.
Abstract: A breath test and a breath test method for diagnosing abnormal gastric emptying using a 13C labeled breath test meal by identifying the time of maximum excretion of 13CO2 in the breath samples. The test and test method include supplying a subject with the breath test meal, collecting a breath sample of the subject at a plurality of time points after the subject consumes the meal, generating measurements of 13CO2 excretion from the breath samples, identifying a time Tmax at which 13CO2 excretion is maximal, comparing Tmax to a cut-off value. The subject may be diagnosed as having delayed gastric emptying if Tmax is greater than the Tmax cut-off value.
Type:
Grant
Filed:
June 25, 2013
Date of Patent:
October 5, 2021
Assignee:
ADVANCED BREATH DIAGNOSTICS, LLC
Inventors:
Catherine Elizabeth Williams, Shane Anthony Crabtree
Abstract: The subject invention relates to novel micoparticulate and soluble forms of flavonoids, and their synthesis. The invention also includes novel formulations of such flavonoids. Further, the invention includes novel methods of manufacturing the flavonoid formulations. The invention also relates to a wide variety of applications of the flavonoid formulations.
Type:
Grant
Filed:
September 1, 2017
Date of Patent:
October 5, 2021
Assignee:
Vizuri Health Sciences Consumer Healthcare, Inc.