Abstract: Described herein are crystalline forms of pharmaceutically acceptable salts of the lysyl oxidase-like 2 (LOXL2) inhibitor (3-(4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone. Also described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 inhibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.
Type:
Grant
Filed:
September 6, 2017
Date of Patent:
September 15, 2020
Assignee:
PHARMAKEA, INC.
Inventors:
David Lonergan, Kevin Ross Holme, Martin W. Rowbottom
Abstract: Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions which can be affected by potassium channel modulation. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels.
Type:
Grant
Filed:
June 2, 2017
Date of Patent:
September 15, 2020
Assignee:
Cadent Therapeutics, Inc.
Inventors:
Birgitte Langer Eriksen, Magnus Gustafsson, Charlotte Hougaard, Thomas Amos Jacobsen, Martin R. Jefson, Gregg F. Keaney, Jessica Klein, Janus Schreiber Larsen, John A. Lowe, III, John M. McCall, Dorte Strøbæk, Nadia Lybøl von Schoubye
Abstract: There is described a method of producing (?)-levoglucosenone, said method comprising, heating lignin to a temperature in excess of 150° C. for a time sufficient to convert a proportion of the lignin to (?)-evoglucosenone.
Type:
Grant
Filed:
April 20, 2016
Date of Patent:
September 15, 2020
Assignee:
UNIVERSITY OF YORK
Inventors:
James Hanley Clark, Mario De Bruyn, Vitaliy Lvovich Budarin
Abstract: The present invention discloses processes comprising a) reacting ethyl isonipecotate with 1-bromo-2-chloroethane in the presence of an organic base in a solvent to form ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof. Process step a) may be included in a process for preparing umeclidinium bromide that comprises further process steps: b) reacting ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (II) or a salt thereof with lithium diisopropylamide in a solvent to form ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III); c) reacting ethyl 1-azabicyclo[2.2.2]octane-4-carboxylate (III) with phenyl lithium in a solvent to form 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV); and d) reacting 1-azabicyclo[2.2.2]oct-4-yl(diphenyl)methanol (IV) with ((2-bromoethoxy)methyl) benzene in a solvent to form 4-[hydroxyl(diphenyl)methyl]-1-[2-(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide (I), umeclidinium bromide. A process comprising d) reacting 1-azabicyclo[2.2.
Type:
Grant
Filed:
November 10, 2017
Date of Patent:
September 1, 2020
Assignee:
Hovione Scientia Limited
Inventors:
Nuno Torres Lourenço, Luis Sobral, Rafael Antunes, Maria Santos, Margarida Espadinha
Abstract: The present invention relates to a new pharmaceutical composition containing a combination of 5-aminosalicylic acid and nicotinamide or related compounds. The combination is believed to beneficially influence the intestinal microbiota and/or reduce gastrointestinal inflammation. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.
Abstract: A composite polymeric material includes one or more repeating backbone units; one or more polarizable units incorporated into or connected to one or more of the one or more repeating backbone units; and one or more resistive tails connected to one or more of the repeating backbone units or to the one or more polarizable units as a side chain on the polarizable unit, on a hydrocarbon chain linking a polarizable unit to a backbone unit, or directly attached to a backbone unit. The composite polymeric material may be used to form a metadielectric, which may be sandwiched between to electrodes to form a metacapacitor.
Type:
Grant
Filed:
June 10, 2019
Date of Patent:
August 25, 2020
Assignee:
CAPACITOR SCIENCES INCORPORATED
Inventors:
Yan Li, Pavel Ivan Lazarev, Paul T. Furuta, Barry K. Sharp, Samuel Hein
Abstract: Methods for treating or relieving at least one symptom of urticarial disorders including chronic idiopathic urticaria, angioedema, and anaphylaxis, or a combination of these disorders in a mammal, including humans. The method comprises administering to the mammal a therapeutically effective amount of pramipexole, dexpramipexole or pharmaceutically acceptable salts thereof.
Abstract: This invention relates to deuterated analogs of etifoxine of Formula 1, solvates, prodrugs, and pharmaceutically acceptable salts thereof, as well as to methods for their preparation and use, and to pharmaceutical compositions. Briefly, this invention is generally directed to deuterated analogs of etifoxine as well as to methods for their preparation and use, and to pharmaceutical compositions containing the same.
Abstract: A process for the preparation of 2,2,5,5-tetramethyltetrahydrofuran (TMTHF) includes contacting a TMTHF precursor with a solid catalyst, where the TMTHF precursor is 2,5-dimethylhexane-2,5-diol and/or 2,5-dimethyl-4-hexen-2-ol, and where the solid catalyst is a beta zeolite. TMTHF produced by the process may be used as a solvent.
Type:
Grant
Filed:
August 18, 2017
Date of Patent:
August 11, 2020
Assignee:
Nitto Belgium B.V.
Inventors:
Greet Bossaert, Charly Hoebers, Bart Forier, Fergal Byrne, Andrew John Hunt, Thomas James Farmer, James Hanley Clark
Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.
Type:
Grant
Filed:
August 3, 2016
Date of Patent:
August 11, 2020
Assignee:
Heptares Therapeutics Limited
Inventors:
Giles Albert Brown, Julie Cansfield, Mark Pickworth, Benjamin Gerald Tehan, Barry John Teobald
Abstract: Pharmaceuticals which are effective for treatment, prevention, and the like of cancer and have less side effects are disclosed. The antitumor agent of the present invention comprises as an effective ingredient at least one leukotriene inhibitor. Examples of the leukotriene inhibitor includes leukotriene production inhibitors and leukotriene receptor antagonists, and preferred specific examples of the leukotriene inhibitor include montelukast, zafirlukast, pranlukast, and zileuton; pharmaceutically acceptable salts of these compounds; and pharmaceutically acceptable solvates of these compounds and the salts. The leukotriene inhibitor can also be used as a relieving agent for pain accompanying a tumor(s), and as a stromal hyperplasia inhibitor.
Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Type:
Grant
Filed:
November 13, 2018
Date of Patent:
July 14, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, T. G. Murali Dhar, Hai-Yun Xiao, John L. Gilmore, Michael G. Yang, Zili Xiao, David Marcoux
Abstract: Disclosed herein are novel cannabionid receptor-2 (CB2) agonists and inverse agonists represented by Formula (I), and method of modulating the activity of CB2 by contacting the CB-2 receptor with a compound of Formula (I). Also, disclosed are methods for treating multiple myeloma or osteoporosis in a mammal in need thereof by modulating the activity of a cannabinoid receptor-2 (CB2).
Type:
Grant
Filed:
June 17, 2016
Date of Patent:
June 30, 2020
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Xiang-Qun Xie, Abdulrahman Almehizia, Peng Yang
Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.
Abstract: In a process for the epoxidation of an olefin with hydrogen peroxide in the presence of a solvent, where a mixture comprising olefin, an aqueous hydrogen peroxide solution and a solvent is continuously passed through a fixed bed of an epoxidation catalyst comprising a titanium zeolite, addition of a chelating agent to the aqueous hydrogen peroxide solution before mixing it with solvent reduces or prevents formation of deposits on the catalyst and blocking of orifices of a liquid distributor.
Type:
Grant
Filed:
January 6, 2017
Date of Patent:
June 9, 2020
Assignees:
EVONIK OPERATIONS GMBH, THYSSENKRUPP INDUSTRIAL SOLUTIONS AG
Inventors:
Franz Schmidt, Nico Dauth, Matthias Pascaly
Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.
Type:
Grant
Filed:
October 1, 2015
Date of Patent:
June 2, 2020
Assignee:
MERCK PATENT GMBH
Inventors:
Markus Klein, Oliver Schadt, Philipp Haselmayer, Mireille Krier
Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
August 2, 2018
Date of Patent:
June 2, 2020
Assignee:
Gilead Sciences, Inc.
Inventors:
Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
Abstract: The present disclosure relates to rotigotine behenate, methods for preparing the same and use of the same for treating diseases associated with dopamine receptor. The rotigotine behenate, the structure of which is shown below, is capable of reducing fluctuation in blood drug concentrations, improving the bioavailability of the drug in vivo, and achieving smooth and extended release of rotigotine.
Type:
Grant
Filed:
July 21, 2016
Date of Patent:
June 2, 2020
Assignee:
Shandong Luye Pharmaceutical Co., Ltd.
Inventors:
Mina Yang, Yongtao Jiang, Ying Meng, Tao Wang, Qian qian Xu, Xin Shao, Chunjie Sha