Abstract: Described herein are compositions and compounds having one or more aziridinyl groups, and methods of making the same. The compounds can also have one or more nitrogen atoms that each can be positively charged. The composition and compounds can inactivate one or more nucleic acid molecules (e.g. a DNA and/or a RNA from a pathogen) in a sample. The sample can comprise a blood or blood product (e.g., donated blood). The compositions and compounds can inactivate any nucleic acid present in a blood or blood product, thereby making the blood or blood product safe for use (e.g., in a transfusion).
Abstract: Propargyl-functionalized macrocyclic compounds can include non-aggregating compounds having at least one phthalocyanine (Pc), azaphthalocyanine (AzaPc), or naphthalocyanine (Nc) unit. The compounds can be metal-free or metal-complexed. The metal-complexed compounds can include zinc (II), for example. The compounds can include multiple propargyl moieties at different sites, e.g., peripheral or non-peripheral sites, as described herein. Exemplary compounds include an azaphthalocyanine complex (AzaPc1) and phthalocyanine complexes (Pc2-Pc5). The compounds may provide efficient solubility in aqueous and/or organic solvents, optimal physicochemical properties, improved photo-sensitizability, significant tumor specificity, and electron transfer tunability. The compounds can provide suitable non-aggregated molecular scaffolds for construction of numerous macrocycle derivatives via different organic transformation methodologies, e.g., Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC).
Type:
Grant
Filed:
October 2, 2018
Date of Patent:
July 28, 2020
Assignee:
Kuwait University
Inventors:
Saad A. Makhseed, Ali A. Husain, Asaithampi Ganesan, Mahmut Durmus
Abstract: A pharmaceutical composition for tranquilizing cardiomyocytes present in heart muscle in a subject diagnosed with a cardiac overload disease comprises a therapeutically effective amount of a Vitamin D5 compound and a pharmaceutically acceptable excipient. A method for treating or preventing heart failure in a subject diagnosed as having heart failure or being at risk for heart failure, comprises administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a Vitamin D5 compound and a pharmaceutically acceptable excipient.
Type:
Grant
Filed:
February 21, 2008
Date of Patent:
July 21, 2020
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Abstract: The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): There are provided compositions and kits using such compounds and inhibitors.
Type:
Grant
Filed:
September 20, 2018
Date of Patent:
July 21, 2020
Assignee:
SOCPRA SCIENCES ET GÉNIE S.E.C.
Inventors:
Éric Marsault, François Malouin, Félix Chagnon, Isabelle Guay, Simon Boulanger
Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
Type:
Grant
Filed:
April 4, 2018
Date of Patent:
July 21, 2020
Assignee:
Emory University
Inventors:
Christopher MacNevin, Donald G. Stein, Dennis C. Liotta, Iqbal Sayeed, David B. Guthrie, Mark A. Lockwood, Michael G. Natchus
Abstract: An isolated or synthesized compound of Formula I and salts thereof are provided. A compound isolated from Actinomadura and having a chemical formula of C38H60O12 is also provided. Compositions including the compounds and methods of using the compounds to treat bacterial infections including gram positive infections such as C. difficile are also disclosed.
Type:
Grant
Filed:
October 28, 2015
Date of Patent:
May 26, 2020
Assignee:
WISCONSIN ALUMNI RESEARCH FOUNDATION
Inventors:
Timothy Scott Bugni, Thomas Philip Wyche, Douglas R. Braun, Jeffrey S. Piotrowski, Nasia Safdar
Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
Type:
Grant
Filed:
June 13, 2018
Date of Patent:
May 19, 2020
Assignee:
CELGENE QUANTICEL RESEARCH, INC.
Inventors:
Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
Abstract: Suggested is a antimicrobial agent An antimicrobial composition comprising (a) at least one acetophenone derivative of formula (I) in which R1 stands for hydrogen or methyl, and R2 stands for hydrogen, hydroxyl or a —OCH3 group, or a cosmetically or pharmaceutically acceptable salt thereof, and (b) at least one second antimicrobial agent.
Type:
Grant
Filed:
March 6, 2014
Date of Patent:
May 5, 2020
Assignee:
Symrise AG
Inventors:
Manuel Pesaro, Bernd Hölscher, Gerhard Schmaus, Antje Köhler
Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
Abstract: Methods of treating, reducing, or preventing a disease or symptom relating to a disease such as oral mucositis, gingivitis, periodontitis, gastric mucositis, inflammatory fibrosis, gastritis, colitis, ileitis, Crohn's disease, chronic inflammatory intestinal disease, inflammatory bowel syndrome, chronic inflammatory bowel disease, celiac disease, ulcerative colitis, a gastric ulcer, a peptic ulcer, a buccal ulcer, a nasopharyngeal ulcer, an esophageal ulcer, a duodenal ulcer, a gastrointestinal ulcer, an autoimmune disorder, inflammation associated with cancer, cancer treatment, or radiation, and/or pain that include: identifying a patient in need of treatment; and administering a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA), or a pharmaceutically acceptable salt thereof. Kits comprising such compositions and instructions on such methods are also contemplated herein.
Abstract: The invention pertains to ligands that bind to CD81 and that inhibit or block Plasmodium attachment to CD81, compositions and methods for preventing, inhibiting or treating infection by Plasmodium and ligands that target a Plasmodium binding site on CD81 and methods of making and using them. A series of ligand binding sites on the large extracellular loop of the open conformation of CD81 have been identified. Several important sites were located in regions identified by mutational studies to be the site of Plasmodium binding. Ligands that recognize these sites were identified. Linking together two or three ligands that bind with low or moderate affinities to different structurally unique sites on a target protein were used to generate small molecule ligand conjugates that exhibit very high affinities to their CD81 targets. Hybrid ligand molecules were also designed using fragment-based drug design methods to generate analogs of the ligands that bind more tightly to the protein than the parent compounds.
Abstract: Disclosed is a method of treatment or prevention of frailty in an elderly patient, particularly having an age of 60 or older. The method provides the concomitant parenteral administration of a combination of an anabolic steroid and a vitamin D compound. A preferred combination comprises nandrolone decanoate and cholecalciferol (vitamin D3). The invention, in a further preference, provides a booster therapy to support frail elderly that have undergone hospitalization or surgery to retain independence and regain their regular physical and mental activities.
Type:
Grant
Filed:
August 23, 2010
Date of Patent:
January 28, 2020
Assignee:
Organext Research B.V.
Inventors:
Marjanna Prins, Helenius Jan Kloosterboer
Abstract: Rhein analogues that exhibit anti-proliferative activity, particular against cancer cells, are described herein. In some embodiments, the compounds contain a flat or planar ring system. Such rings system by facilitate non-covalent binding of the compounds to the DNA complex, such as by intercalation. In some embodiment, the compounds contain a flat or planar ring system as described above and one or more substituents which are alkylating moieties, electrophilic groups or Michael acceptors or groups which contain one or more alkylating moieties, electrophilic groups and/or Michael acceptors. The compounds described herein can also contain one more functional groups to improve the solubility of the compounds.
Type:
Grant
Filed:
July 10, 2013
Date of Patent:
January 28, 2020
Assignees:
Georgia State University Research Foundation, Inc., Emory University, Children's Healthcare of Atlanta, Inc.
Abstract: Various embodiments of this invention are directed to pharmaceutical compositions and methods for treating diseases, including focal segmental glomerulosclerosis or pulmonary arterial hypertension. The compositions of such embodiments include activated fatty acids such as alkyl substituted fatty acids, keto fatty acids and nitro fatty acids. The methods of various embodiments include administering an effective amount of 10-nitro-9(E)-octadec-9-enoic acid to treat such diseases.
Abstract: A pharmaceutical composition of 3-(1-{3-[5-(1-Methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile or a pharmaceutically acceptable salt and/or solvate thereof in combination with N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxy-anilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide.
Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
Type:
Grant
Filed:
February 15, 2017
Date of Patent:
December 10, 2019
Assignee:
REATA PHARMACEUTICALS, INC.
Inventors:
Christopher F. Bender, Xin Jiang, Eric Anderson, Melean Visnick
Abstract: The invention described herein pertains to anticancer therapeutic agents that exhibit preferential cytotoxicity to malignant cells that express a cancer specific isoform of proliferating cell nuclear antigen (caPCNA) compared to cytotoxicity to comparable non-malignant cells, pharmaceutical compositions comprising the agents, and their use in cancer therapy.
Abstract: The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.
Type:
Grant
Filed:
August 15, 2014
Date of Patent:
September 24, 2019
Assignee:
Memorial Sloan-Kettering Cancer Center
Inventors:
Gabriela Chiosis, Pengrong Yan, Pallav Patel, Hardik J. Patel, Tony Taldone, Chenghua Yang, Weilin Sun, Stefan O. Ochiana
Abstract: The present invention provides a method of treating one or more sodium channel related diseases or disorders in an individual, including related symptoms. The method comprises administering to the individual a tetrahydropyridine derivative in an amount effective to treat sodium channel related diseases or disorders in individuals. These compounds are generally categorized as Ritalin related compounds. The present invention also provides compounds for use in the treatment of and also for use in the manufacture of a medicament for the treatment of sodium channel related diseases or disorders in an individual. A method is further provided for the preparation and isolation of the derivatives of the compound of the present invention.