Abstract: The present invention relates to compounds useful as inhibitors of the PAR-2 signaling pathway. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of GPCRs in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such GPCRs; and the comparative evaluation of new inhibitors of the PAR-2 signaling pathway. The compounds of this invention have formula I: wherein the variables are as defined herein.
Abstract: The invention relates to a new administration form for the oral application of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate and the pharmacologically acceptable salts thereof.
Abstract: In one aspect, the invention relates methods for inhibiting or preventing muscle atrophy or increasing muscle mass by providing to a subject in need thereof an effective amount of ursolic acid, a derivative thereof, or an analog of the ursane scaffold. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
May 19, 2011
Date of Patent:
January 2, 2018
Assignees:
UNIVERSITY OF IOWA RESEARCH FOUNDATION, THE UNITED STATES OF AMERICA AS REPRESENTED BY VETERANS AFFAIRS
Inventors:
Christopher M. Adams, Steven D. Kunkel, Manish Suneja, Michael Welsh
Abstract: Methods for synthesizing amooranin (25-hydroxy-3-oxoolean-12-en-28-oic acid (AMR) and/or amooranin analogs, including amooranin methyl ester (AMR-Me), by using oleanolic acid in an oxidation process, and therapeutic uses thereof are described.
Abstract: The present invention relates to a novel pseudoceramide derivative, a pharmaceutically acceptable salt thereof or a solvate thereof, and a pharmaceutical or cosmetic composition containing the same as an active ingredient. The novel pseudoceramide derivative of the present invention is expected to be very useful for treating or preventing skin diseases by activating cannabinoid receptors. In addition, the novel pseudoceramide derivative, the pharmaceutically acceptable salt thereof or the solvate thereof, of the present invention, has a simple synthesis process compared with a known cannabinoid receptor antagonist so as to reduce processing time and curtail material costs, and thus is economical, and has advantages such as easy emulsification during the formulation of cosmetic products or medical supplies.
Type:
Grant
Filed:
September 1, 2014
Date of Patent:
October 24, 2017
Assignee:
NEOPHARM CO., LTD.
Inventors:
Se Kyoo Jeong, Bong-Woo Kim, Jeong Eun Jeon, Bu-Mahn Park
Abstract: The present invention relates to novel anthranilamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q, Y and n are each as defined in the description—, to the use thereof as insecticides and acaricides for control of animal pests, and to several processes for preparation thereof.
Type:
Grant
Filed:
July 8, 2011
Date of Patent:
October 17, 2017
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Rüdiger Fischer, Ernst Rudolf Gesing, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Arnd Voerste, Ulrich Gorgens
Abstract: Antimicrobial compositions comprising a terpenoid in combination with an antimicrobial agent are provided. In addition, uses of such compositions in various applications involving preventing, combating or treating microbial infections, or preventing microbial growth or establishment are provided.
Type:
Grant
Filed:
September 10, 2010
Date of Patent:
August 29, 2017
Assignee:
UNIVERSITY OF SURREY
Inventors:
Franciscus Antonius Anna Maria De Leij, Mina Kalantarzadeh, Dulcie Mulholland, Tony Hutchings
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:
July 11, 2014
Date of Patent:
August 29, 2017
Assignee:
Evestra, Inc.
Inventors:
Klaus Nickisch, Bindu Santhamma, Gulzar Ahmed, Frederick Meece, Walter Elger, Ralf Wyrwa, Hareesh Nair
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:
May 19, 2014
Date of Patent:
August 8, 2017
Assignee:
Sloan-Kettering Institute for Cancer Research
Abstract: The invention generally relates to methods and compounds for treating proliferative disorders, viral infections, or both. In some embodiments, the invention provides an anticancer or antiviral compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating a proliferative disorder or a viral infection including administering an anticancer or antiviral compound that binds to a thromboxane receptor, has preferential binding for either TPalpha (TP?) or TPbeta (TP?) receptor subtype.
Type:
Grant
Filed:
April 17, 2013
Date of Patent:
August 1, 2017
Assignee:
UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN
Abstract: [Problem] To provide a novel pharmaceutical composition which contains a medically active component and which can suppress delays in the release of said component due to gelling. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1), or a salt thereof, a cellulosic excipient, and a salting-out agent.
Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids 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.
Type:
Grant
Filed:
December 18, 2013
Date of Patent:
June 13, 2017
Assignees:
Washington University, Sage Therapeutics, Inc.
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit Hedgehog signaling. Also described herein are methods for using such Hedgehog signaling inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of Hedgehog signaling.
Abstract: The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
Type:
Grant
Filed:
August 27, 2010
Date of Patent:
April 18, 2017
Assignee:
Tetraphase Pharmaceuticals, Inc.
Inventors:
Yonghong Deng, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Jingye Zhou, Joyce A. Sutcliffe, Magnus P. Ronn
Abstract: The present invention provides compositions and methods for use in the treatment of hyperproliferative dermal diseases. Specifically, the present invention teaches pharmaceutical compositions for topical administration consisting essentially of a vitamin D metabolite, calcipotriol, and nicotinamide, which are particularly effective in treating and in the maintenance therapy of psoriasis and other related dermal disorders and diseases.
Type:
Grant
Filed:
September 30, 2015
Date of Patent:
March 28, 2017
Assignee:
Dermipsor Ltd.
Inventors:
Avikam Harel, Zeev Even-Chen, Olga Bloch
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:
September 10, 2013
Date of Patent:
March 14, 2017
Assignee:
REATA PHARMACEUTICALS, INC.
Inventors:
Christopher F. Bender, Xin Jiang, Eric Anderson, Melean Visnick
Abstract: An object of the present invention is to develop a method of enhancing the cognitive ability of a brain to fundamentally cure a disease. It has been found out that, by using a medicament for treating or preventing a disease including a combination of a major tranquilizer, and vitamin C or a salt thereof and, if necessary, drip infusion, an antidepressant and an iron agent, the cognitive ability of a brain is enhanced, thus, an arbitrary disease including various cancers can be treated. The present invention also provides a method for treating or preventing a disease including a step of administering a major tranquilizer, and vitamin C or a salt thereof to a subject suffering from the disease.
Abstract: The invention relates to compositions for use in animal models of neurodegenerative disease and methods therefor. More particularly, the invention relates to the use of neurotoxic sterol glycosides or neurotoxic glycolipids, or combinations thereof, in animal models of neurodegenerative disease. Neurotoxicity-modulating chromenols can also be used in these animal models in combination with the neurotoxic sterol glycosides or neurotoxic glycolipids, or combinations thereof.
Type:
Grant
Filed:
October 30, 2009
Date of Patent:
February 21, 2017
Assignee:
NEURODYN, INC.
Inventors:
Christopher Ariel Shaw, Denis George Kay
Abstract: An aromatic compound represented by formula (1): wherein R1 and R2 each independently represents a halogen atom, a C1-C4 alkyl group, or a C1-C4 haloalkyl group; m and n each independently represents an integer of 0 to 4; R3 and R4 each represents a hydrogen atom; Y represents formula: —OC(?X)ZR5 or —SC(?X)ZR5; R5 represents a C1-C3 alkyl group optionally having one or more halogen atoms; Z represents a sulfur atom, NR8, or a direct bond; R8 represents a C1-C3 alkyl group or a hydrogen atom; Q represents a pyrazolyl group optionally having a substituent; and W and X each independently represents an oxygen atom or a sulfur atom, has excellent control activity against pests.