Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
Type:
Grant
Filed:
April 4, 2018
Date of Patent:
February 12, 2019
Assignee:
AbbVie Inc.
Inventors:
Jayanthy Jayanth, Patrick J. Marroum, Peter T. Mayer, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Ben Klünder
Abstract: Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R1, R2, R3, R5, R6, A, and Z, are defined herein.
Abstract: The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient.
Type:
Grant
Filed:
October 6, 2015
Date of Patent:
January 29, 2019
Assignees:
HELMHOLTZ-ZENTRUM FÜR INFEKTIONSFORSCHUNG GMBH, MEDIZINISCHE HOCHSCHULE HANNOVER
Abstract: Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula; wherein X is OH, C1-C6 alkoxyl; Y and Z are independently selected from a C1-C6 alkyl, C1-C6 alkoxyl, halogen, mi-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.
Abstract: Methods for the safe administration of imidazole or imidazolium compounds such as zoledronic acid, and conditions that may be treated by these methods, are described herein.
Abstract: The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
Type:
Grant
Filed:
April 25, 2017
Date of Patent:
January 8, 2019
Assignee:
Intercept Pharmaceuticals, Inc.
Inventors:
André Steiner, Heidi Waenerlund Poulsen, Emilie Jolibois, Melissa Rewolinski, Ralf Gross, Emma Sharp, Fiona Dubas-Fisher, Alex Eberlin
Abstract: Imipridones selectively modulate Class A G protein-coupled receptors (GPCRs), such as the D2-like subfamily of dopamine receptors, and are useful for treating conditions and disorders in need of such modulation, such as cancers. Specifically, the cancer is a midline glioma, a cancer having a histone H3 mutation, or both. In addition, methods of identifying whether a subject having these conditions, is likely to be responsive to a treatment regimen, such as imipridone administration, are provided. Furthermore, methods of assessing the effectiveness of a treatment regimen, such as imipridone administration, monitoring, or providing a prognosis for a subject with these condition are also provided.
Type:
Grant
Filed:
April 8, 2018
Date of Patent:
January 8, 2019
Assignee:
Oncoceutics, Inc.
Inventors:
Joshua E. Allen, Martin Stogniew, Varun Vijay Prabhu
Abstract: The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
Type:
Grant
Filed:
November 20, 2015
Date of Patent:
December 18, 2018
Assignee:
Intercept Pharmaceuticals, Inc.
Inventors:
André Steiner, Heidi Waenerlund Poulsen, Emilie Jolibois, Melissa Rewolinski, Ralf Gross, Emma Sharp, Fiona Dubas-Fisher, Alex Eberlin
Abstract: Compositions and methods are provided that are useful in the treatment of inflammatory bowel disease (IBD) patients. The Compositions and methods are suitable in the prevention or postponement of a relapse in inflammatory bowel disease patients.
Type:
Grant
Filed:
January 22, 2016
Date of Patent:
November 27, 2018
Assignee:
Nestec S.A.
Inventors:
Stephanie Blum-Sperisen, Magali Faure, Denis Breuille, Emil Chuang
Abstract: A method of treating or preventing multiple sclerosis includes administering a therapeutically effective amount of a cyclohexane derivative represented by Formula (I): wherein A is a substituent represented by Formula (IIa) or (IIb): R1 and R2 are each independently a hydrogen atom, chlorine atom, C1-C3 haloalkyl, C1-C4 alkyl, C1-C4 alkoxy, or cyano; R3 is a hydrogen atom or chlorine atom; R4 is a fluorine atom, hydroxymethyl, or hydroxyl; R5 and R6 are each independently a hydrogen atom, fluorine atom, C1-C3 haloalkyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, C1-C4 alkoxy, hydroxyl, or C2-C5 alkylcarbonyloxy, or optionally together form oxo; R7 and R8 are each independently a hydrogen atom or fluorine atom; Y is an oxygen atom or sulfur atom; and Z is a nitrogen atom or methine or a pharmaceutically acceptable salt thereof to a mammal.
Abstract: Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are provided.
Abstract: The application provides methods of treating or reducing thrombocytopenia, leukopenia, anemia, or neutropenia in a patient in need thereof, comprising the step of administering an effective amount of a compound selected from Compounds 1-6, disclosed herein.
Type:
Grant
Filed:
September 14, 2017
Date of Patent:
October 30, 2018
Assignee:
GILEAD SCIENCES, INC.
Inventors:
Esteban M. Abella, Julie A. Di Paolo, Kathleen S. Keegan, Antonio Mario Querido Marcondes, Yang Pan, Arati V. Rao
Abstract: Polymerization inhibitor compositions are provided. The polymerization inhibitor compositions may include at least one hydroxylamine of a nitroxide and at least one phenylenediamine. Methods of inhibiting the unwanted polymerization of monomers are also provided. The methods include adding the presently disclosed polymerization inhibitor compositions to a fluid containing the monomers. The monomers may be ethylenically unsaturated monomers, such as acrylic acid, methacrylic acid, acrylonitrile, methacrylonitrile, acrolein, methacrolein, acrylate, methacrylate, acrylamide, methacrylamide, vinyl acetate, butadiene, ethylene, propylene, and styrene.
Abstract: Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided.
Abstract: This disclosure relates to methods administering various compounds in conjunction with dextromethorphan to a human being. Dosage forms, drug delivery systems, and methods related to dextromethorphan or dextrorphan and bupropion, hydroxybupropion, erythrohydroxybupropion, threohydroxybupropion, or a metabolite or prodrug of any of these compounds are also disclosed.
Abstract: A method for treating a symptom of a neurodegenerative condition. The method includes topically administering a composition that contains a sex steroid or a cannabinoid or a mixture of both to the forehead, to an area of the outer ear of the subject not including the ear canal, or to both of these anatomical locations. The symptom treatable by the method is a motor symptom or a non-motor symptom.
Abstract: The present invention describes novel and improved dosage forms containing fluticasone propionate for the treatment of conditions associated with inflammation of the esophagus.
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
Type:
Grant
Filed:
November 20, 2015
Date of Patent:
August 14, 2018
Assignee:
Intercept Pharmaceuticals, Inc.
Inventors:
André Steiner, Heidi Waenerlund Poulsen, Emilie Jolibois, Melissa Rewolinski, Ralf Gross, Emma Sharp, Fiona Dubas-Fisher, Alex Eberlin