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.
Abstract: Disclosed herein are compounds of Formulae (I) and (II), methods of synthesizing compounds of Formulae (I) and (II), and methods of using compounds of Formulae (I) and (II) as an analgesic.
Type:
Grant
Filed:
September 15, 2015
Date of Patent:
June 4, 2019
Assignee:
Zeno Royalties & Milestones, LLC
Inventors:
Kevin Duane Bunker, Chuangxing Guo, Mark Charles Grier, Chad Daniel Hopkins, Joseph Robert Pinchman, Deborah Helen Slee, Qinhua Huang, Mehmet Kahraman
Abstract: Various prodrug compounds having the general structure: Active agent—(acid)-(linker)—SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.
Type:
Grant
Filed:
August 24, 2017
Date of Patent:
April 30, 2019
Assignee:
Evestra, Inc.
Inventors:
Klaus Nickisch, Bindu Santhamma, Gulzar Ahmed, Frederick Meece, Walter Elger, Ralf Wyrwa, Hareesh Nair
Abstract: The present invention relates to novel uses of C-19 steroid compounds, in particular C-19 steroids having an androsten-17-(OR4)-3-one structure for prophylactic and/or therapeutic uses, wherein R4 is hydrogen or an unsubstituted or substituted alkyl, aryl, acyl or any group leading to hydroxyl upon biological metabolization or chemical deprotection.
Abstract: The invention relates to fused piperidine amides useful as inhibitors of ion channels for the treatment of pain. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
July 8, 2014
Date of Patent:
March 19, 2019
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Michael Paul Deninno, Corey Anderson, Erica Lynn Conroy, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Sara Sabina Hadida-Ruah, Dennis James Hurley, Fabrice Jean Denis Pierre, Alina Silina, Johnny Uy, Jinglan Zhou
Abstract: The disclosure provides compounds, methods, and kits for diagnosis, detection, screening, and imaging of a disease condition (e.g., infection, cancer, tumor, neoplasia), in vitro, ex vivo, and/or in vivo. Certain embodiments include administering a cationic steroid antimicrobial (a “CSA” or “ceragenin”), the CSA including a steroidal backbone and a heterocyclic ring separated from the steroidal backbone by at least 4 atoms (and up to 24 atoms or more), to a subject having or at risk of having a disease condition in an amount effective to diagnose, detect, screen for or image the disease condition in the subject.
Abstract: The present invention provides an application of a dimethylamino micheliolide for preparing a pharmaceutical product for treating pulmonary fibrosis.
Type:
Grant
Filed:
January 28, 2016
Date of Patent:
March 5, 2019
Assignees:
Tianjin International Joint Academy of Biotechnology & Medicine, ACCENDATECH
Abstract: This invention offers an effective method of decreasing expression of apolipoprotein E and increasing expression of at least one of either LDL-receptor protein or AbcA1 protein including selecting mammalian cells expressing apoE and at least one of either LDL-receptor protein or AbcA1 protein, contacting the mammalian cell with an effective amount of a compound having general formula (I) or general formula (II) in an amount sufficient to decrease expression of the apoE and increase expression of at least one of the LDL-receptor protein or the AbcA1 protein in the mammalian cell.
Type:
Grant
Filed:
October 4, 2016
Date of Patent:
February 26, 2019
Assignees:
Mayo Foundation for Medical Education and Research, California State University, Fresno
Abstract: The current study established that treatment of diabetes using compound 1(2,4-dinitroanilino-benzoic acid), an anthranilic acid derivative, by restoring the functional activities of the pancreas via its insulinotropic action.
Type:
Grant
Filed:
August 22, 2017
Date of Patent:
January 22, 2019
Inventors:
Humera Jahan, Muhammad Iqbal Choudhary, Mehwish Manzoor, Khalid M. Khan, Atta-ur Rahman
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: The present invention concerns a spiroisoxazoline compound of general formula (I): in which m and n are 0 or 1, R1 represents, inter alia, an optionally substituted alkyl chain, in particular substituted with fluorine or with a cyclic group, and R2 is chosen from phenyl and optionally substituted benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the heterocycles having 5 or 6 vertices comprising at least one atom chosen from S, N and O. The present invention also concerns the use of this compound as a drug, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.
Type:
Grant
Filed:
December 20, 2013
Date of Patent:
January 8, 2019
Assignee:
Universite de Droit et de la Sante de Lille 2
Inventors:
Nicolas Willand, Benoit Deprez, Alain Baulard, Priscille Brodin, Matthieu Frederik Desroses, Laurence Agouridas-Dutot
Abstract: The present disclosure is generally directed to neuroactive substituted cyclopent[a]anthracenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
Abstract: Compounds of formula: in which R4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.
Type:
Grant
Filed:
August 8, 2017
Date of Patent:
December 11, 2018
Assignee:
Sloan-Kettering Institute for Cancer Research
Abstract: The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): (Formula (I)) (A) in combination with an aminoglycoside antibiotic for preventing or treating a bacterial infection in a subject; or (B) (a) for preventing or treating an infection caused by an electron transport-deficient bacteria in a subject; or (b) for the disinfection, sterilization and/or antisepsis of an object contaminated with an electron transport-deficient bacteria. There are provided compositions and kits using such compounds and inhibitors.
Type:
Grant
Filed:
December 23, 2014
Date of Patent:
November 27, 2018
Assignee:
Socpra Sciences et Genie S.E.C.
Inventors:
Éric Marsault, François Malouin, Félix Chagnon, Isabelle Guay, Simon Boulanger
Abstract: The present invention relates to methods of treating and/or preventing obesity comprising the administration of antioxidant inflammation modulators described herein, including for example bardoxolone methyl.
Abstract: The invention relates to a drug conjugate including a drug and a plant steroid. The drug conjugate may target the drug for intestinal cell delivery, and thus may be used to treat diseases, including intestinal diseases, or to affect intestinal metabolism. The invention therefore also relates to treating intestinal diseases and affecting intestinal metabolism with the drug conjugate.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
October 2, 2018
Assignee:
DAVIDSON LOPEZ LLC
Inventors:
Michael Davidson, John F. Arnett, Sadik Elshani, Roelof Rongen
Abstract: A tetrazolinone compound represented by formula (1) wherein E represents the following group E16; Y represents —O—CH2—; Q represents the following group Q46; R8 represents a C1-C6 alkyl group; R3, R30 and R31 are the same or different and represent a hydrogen atom; A represents a C6-C16 aryl group optionally having one or more atoms or groups selected from Group P1; R5 represents a C1-C3 alkyl group; and X represents an oxygen atom or a sulfur atom, has excellent control activity against pests.
Abstract: Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.
Type:
Grant
Filed:
March 22, 2016
Date of Patent:
August 21, 2018
Assignee:
Evestra, Inc.
Inventors:
Hareesh Nair, Bindu Santhamma, Klaus Nickisch
Abstract: Compositions and methods including Amodiaquine (AQ) or N-Desethy Amodiaquine (DEAQ) are provided for treating, inhibiting, or preventing cathepsin B dependent pathogens and toxins in a host cell or infected subject. Compositions and methods also include AQ or DEAQ in combination with an antibiotic for more effective clearance of the pathogen and/or toxins.
Type:
Grant
Filed:
October 23, 2015
Date of Patent:
August 7, 2018
Assignee:
Keck Graduate Institute of Applied Life Sciences
Inventors:
Mikhail Martchenko, Leeor Zilbermintz, William Leonardi