Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
Type:
Grant
Filed:
March 12, 2019
Date of Patent:
March 2, 2021
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Jae U. Jeong, Deepak Bandyopadhyay, Patrick M. Eidam, Philip Anthony Harris, Jianxing Kang, Bryan Wayne King, Ami Lakdawala Shah, Lara Kathryn Leister, Attiq Rahman, Joshi M. Ramanjulu, Clark A. Sehon, Robert Singhaus, Jr., Daohua Zhang
Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
Type:
Grant
Filed:
July 24, 2019
Date of Patent:
March 2, 2021
Assignee:
SIGA TECHNOLOGIES INC.
Inventors:
Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
Type:
Grant
Filed:
July 9, 2019
Date of Patent:
February 16, 2021
Assignee:
Vernalis (R&D) Ltd.
Inventors:
Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
Abstract: The invention is a method of treating a subject with primary progressive or secondary progressive multiple sclerosis. The method comprises administering an effect amount of Cis-N-cyclohexyl-N-ethyl-3-(3-chloro-4-cyclohexylphenyl)prop-2-enylamine or a pharmaceutically acceptable salt thereof to the subject.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
February 16, 2021
Assignee:
Case Western Reserve University
Inventors:
Paul Tesar, Drew Adams, Steven B. Landau
Abstract: Use of pycnidione, epolone A, and epolone B as anti-dandruff actives either alone or in combination in anti-dandruff compositions, particularly shampoos and conditioners. The actives are particularly effective against Malassezia yeasts and Malassezia furfur. A method of obtaining pycnidione, epolone A, and epolone B from culturing of Neosetophoma samarorum is also described.
Type:
Grant
Filed:
June 8, 2016
Date of Patent:
January 26, 2021
Inventors:
Russell Greig Kerr, David Patrick Overy, Fabrice Berrué
Abstract: A method for increasing bacteria belonging to the genus Akkermansia in an intestinal bacterial flora, comprising the step of ingesting a composition containing astaxanthin.
Type:
Grant
Filed:
April 6, 2018
Date of Patent:
January 19, 2021
Assignees:
Fuji Chemical Industries Co., Ltd., Kyoto Prefectural Public University Corporation
Inventors:
Yuji Naito, Kazuhiro Kamada, Kumi Tominaga
Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
Type:
Grant
Filed:
April 8, 2019
Date of Patent:
January 12, 2021
Assignee:
Heptares Therapeutics Limited
Inventors:
John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
Abstract: Formulations, methods of manufacturing, methods of stabilizing, kits, and uses as medicament are provided, for example for the treatment of pain. The formulations can comprise gabapentin optionally combined with at least one non-opioid pain drug in an aqueous carrier. The pharmaceutical formulation can have a pH of about 2.0 to about 10.0. The at least one non-opioid pain drug can be acetaminophen. The components can be included in any amount suitable for purposes of obtaining properties desirable for an injectable infusion, for example an intravenous infusion.
Type:
Grant
Filed:
April 7, 2017
Date of Patent:
December 29, 2020
Assignee:
Nevakar Inc.
Inventors:
Varun Khurana, Vivek Yadav, Jack Martin Lipman, Tao Zhang, Iouri V. Ilitchev, Tushar Hingorani, Kumaresh Soppimath, Navneet Puri
Abstract: It is an object of the present invention to provide a novel therapeutic agent and method for treating amyotrophic diseases, and more specifically a therapeutic agent and method for treating neurogenic amyotrophic disorders such as amyotrophic lateral sclerosis (ALS) and myogenic amyotrophic disorders such as sarcopenia or disuse muscle atrophy. Provided is a therapeutic agent for amyotrophic diseases that comprises one or more compounds selected from the group consisting of compounds represented by the formula (I), the formula (II) and the formula (III), and pharmaceutically acceptable salts of the compounds when R3 represents OH.
Abstract: The invention provides compositions and methods that are effective to improve NO production in vivo and/or to increase NO levels in blood. Such compositions and methods are useful to improve sexual function in males and females.
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, Y and R2 are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
June 4, 2018
Date of Patent:
December 1, 2020
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Patrizio Mattei, Daniel Hunziker, Patrick Di Giorgio, Jerome Hert, Markus Rudolph, Lisha Wang
Abstract: The present invention provides a method of treating symptoms associated with Androgen Deprivation Therapy comprising administering to a patient in need of such treatment an effective amount of a compound of Formula I: or a pharmaceutically acceptable salt thereof.
Abstract: The ketogenic diet (KD) has therapeutic implications in many disease states. It was hypothesized ketone precursor supplementation would elevate blood ketone levels to therapeutic ranges (2-7 mM) without need for dietary restriction. The effects of ketogenic agents were tested on blood glucose, ketones, and lipids with a 28-day dose escalation study in male Sprague-Dawley rats: R,S-1,3-Butandiol (BD), acetoacetate ketone ester (KE), and control (H2O) (n?8). Days 1-28, rats received a daily 5 g/kg intragastric gavage, based on previous toxicology studies. Once weekly, whole blood samples (10 ?l) were acquired for analysis of glucose and ?HB at 0, 0.5, 1, 4, 8, and 12 hours after test substance administration, or until ?HB returned to baseline. At day 1 and 28, 10 ?L of whole blood were collected to measure triglycerides, total cholesterol, and HDL concentration. Significant elevation of blood ketone was observed with a significant inverse relationship with blood glucose for the duration of the experiment.
Abstract: Provided is a stable pharmaceutical composition for oral administration comprising 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide (hereinafter referred to as compound A) or a pharmaceutically acceptable salt thereof, wherein the generation of related substances during storage is inhibited. In the stable pharmaceutical composition for oral administration, the proportion of crystals of compound A or a pharmaceutically acceptable salt thereof is 60% or more with respect to the total amount of compound A or a pharmaceutically acceptable salt thereof.
Abstract: The invention provides a method of inhibiting the conversion of carnitine to trimethylamine (TMA) and lowering TMAO in an individual comprising administering to the individual one or more compositions comprising a compound set forth in Formula (I): Wherein the compound is administered in an amount effective to inhibit conversion of carnitine to TMA in the individual.
Type:
Grant
Filed:
December 1, 2016
Date of Patent:
September 29, 2020
Assignees:
The Procter & Gamble Company, The Cleveland Clinic Foundation
Inventors:
Stanley Leon Hazen, Jose Carlos Garcia-Garcia, George Franklin Gerberick, John August Wos, David Thomas Stanton, Thomas Alfred Inglin, Michael Reilly, Angela Jane Deutsch, Jodie Michele Reed, David Blair Cody
Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.
Type:
Grant
Filed:
August 17, 2018
Date of Patent:
September 22, 2020
Assignees:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, FRIEDRICH-ALEXANDER-UNIVERSITÄT, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Inventors:
Brian K. Shoichet, Anat Levit, Aashish Manglik, Brian Kobilka, Peter Gmeiner, Harald Hübner, Daniela Gisela Dengler
Abstract: The invention provides one or more methods of inhibiting the conversion of choline to trimethylamine (TMA) and lowering TMAO in an individual comprising administering to the individual one or more compositions comprising a compound set forth in Formula (I): wherein the compound is administered in an amount effective to inhibit formation of trimethylamine (TMA) from choline in the individual.
Type:
Grant
Filed:
December 1, 2016
Date of Patent:
September 22, 2020
Assignees:
The Procter & Gamble Company, The Cleveland Clinic Foundation
Inventors:
Stanley Leon Hazen, Jose Carlos Garcia-Garcia, George Franklin Gerberick, John August Wos, David Thomas Stanton, Thomas Alfred Inglin, Michael Reilly, Angela Jane Deutsch, Jodie Michele Reed, David Blair Cody
Abstract: This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.
Type:
Grant
Filed:
May 2, 2016
Date of Patent:
September 15, 2020
Assignees:
GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC., EMORY UNIVERSITY
Inventors:
Binghe Wang, Erwin Van Meir, Jalisa Holmes Ferguson, Stefan Kaluz, Xingyue Ji