Abstract: Compounds of formula (IIc); wherein X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different; Y1, Y2, Y3 and Y4 independently from each other are N or CR9 wherein R9 may be same or different and wherein up to 3 of the group Y1, Y2, Y3 and Y4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.
Abstract: HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound; and determining the activity of the HDAC protein.
Type:
Grant
Filed:
January 5, 2017
Date of Patent:
August 28, 2018
Assignees:
President and Fellows of Harvard College, Dana-Farber Cance Institute, Inc.
Abstract: Combinations of (3?)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) with acidic substances such as citric acid, ascorbic acid, methyl-4-hydroxy benzoate, saccharin, vanillic acid, adipic acid, maleic acid, malic acid, tartaric acid are useful as pharmaceutical preparations and show improved properties such as aqueous solubility and dissolution kinetics, especially in the form of cocrystals or their combination with a suitable acid.
Type:
Grant
Filed:
December 9, 2014
Date of Patent:
August 14, 2018
Assignee:
BASF SE
Inventors:
Tiziana Chiodo, Beate Salvador, Marcus Vossen, Andreas Hafner, Tobias Hintermann, Martin Szelagiewicz, Fritz Blatter, Martin Viertelhaus, Walter Weishaar
Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
Type:
Grant
Filed:
December 11, 2015
Date of Patent:
August 14, 2018
Assignee:
GALAPAGOS NV
Inventors:
Frédéric Gilbert Labéguère, Gregory John Robert Newsome, Luke Jonathan Alvey, Laurent Raymond Maurice Sanière, Stephen Robert Fletcher
Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising an acid labile proton pump inhibitor and a buffering agent and to use of such compositions in treating nocturnal acid breakthrough.
Type:
Grant
Filed:
January 15, 2016
Date of Patent:
August 14, 2018
Assignee:
THE CURATORS OF THE UNIVERSITY OF MISSOURI
Abstract: The present invention relates to the treatment of peptic ulcers. In particular, the present invention provides methods and compositions for the treatment of peptic ulcers. In addition, the present invention provides a method of reducing gastric acid secretion in a subject.
Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.
Type:
Grant
Filed:
November 30, 2016
Date of Patent:
August 7, 2018
Assignee:
Emory University
Inventors:
Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
Abstract: A method is provided for treating an individual for a cellular proliferative disorder, including administering to the individual in need of such treatment a therapeutically effective amount of the compound pterostilbene wherein UDP-glucuronosyltransferase (UGT) activity is increased. In an embodiment, 12-HETE levels can be reduced by administration of pterostilbene.
Type:
Grant
Filed:
September 22, 2014
Date of Patent:
August 7, 2018
Assignees:
ChromaDex Inc., The Regents of the Unviersity of California
Abstract: The present invention is drawn to a pharmaceutical composition comprising racecadotril, at least one surfactant and a lipid. The pharmaceutical composition is useful in treating diarrhea.
Abstract: Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4?-(morpholinomethyl)-[1,1?-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.
Abstract: The subject of the present invention is the use of aminaphtone for the preparation of a medicament for treating arteriophaties, in particular arteriophaties of a degenerative inflammatory type. Preferably, said medicament is formulated for oral administration.
Abstract: Candidate compounds for specific inhibition of Rpn11 are represented by Formula 1a where each of R2, R3, R4, R5, R6, and R7 is independently selected from hydrogen (H), substituted and unsubstituted alkyl groups, carboxyl groups, or substituted and unsubstituted carboxyamides.
Type:
Grant
Filed:
August 17, 2016
Date of Patent:
June 26, 2018
Assignees:
California Institute of Technology, The Regents of the University of California
Inventors:
Raymond J. Deshaies, Jing Li, Seth Cohen, Christian Perez, Yuyong Ma
Abstract: Provided are methods of treating skin with at least two alternating treatment modalities to improve the health and/or diminish signs of aging. Some methods according to the present invention may comprise topically applying at least two separate compositions, in a sequential, rotating, or alternating fashion to overcome adaptation, tolerance, or sensitization phenomena.
Type:
Grant
Filed:
January 26, 2017
Date of Patent:
May 15, 2018
Assignee:
Avon Products, Inc.
Inventors:
Uma Santhanam, Jolanta Idkowiak-Baldys, Daniel Thorn Leeson, Anthony David Gonzalez, Glen Thomas Anderson
Abstract: Disclosed are methods, compounds, and compositions useful for increasing autophagy and promoting longevity. The methods, compounds, and compositions relate to urolithins and urolithin precursors and use thereof. Certain urolithins are represented by Formula I, while certain urolithin precursors are represented by Formula IV. The urolithin may be urolithin A, urolithin B, urolithin C, or urolithin D. The urolithin precursor may be ellagic acid or an ellagitannin. The methods include in vivo, ex vivo, and in vitro uses of the compounds and compositions.
Type:
Grant
Filed:
March 10, 2015
Date of Patent:
May 8, 2018
Assignee:
Amazentis SA
Inventors:
Christopher L. Rinsch, William Blanco-Bose, Bernard Schneider, Laurent Mouchiroud, Dongryeol Ryu, Penelope Andreux, Johan Auwerx
Abstract: Disclosed are compounds of the formula (I) and (II) which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.
Type:
Grant
Filed:
November 20, 2014
Date of Patent:
May 8, 2018
Assignees:
The United States of America, as represented by the Secretary, Department of Health and Human Services, Saint Louis University
Inventors:
Kenneth A. Jacobson, Dilip K. Tosh, Daniela Salvemini
Abstract: A pharmacological composition for the treatment of bacterial and protozoal infections in a patient. The preferred pharmacological composition comprises a pharmaceutical carrier and an active composition selected from the group consisting of: a) an amount of sodium oxalate and an amount of oxalic acid, b) an amount of sodium citrate and an amount of citric acid, or c) mixtures of a) and b). The amounts and weight ratios of a) the sodium oxalate and oxalic acid, and b) the sodium citrate and citric acid in the active composition are such as to produce a safe and effective pharmacological composition. Sodium salts of other carboxylic acids may be used. The invention also relates to the method of using the pharmacological composition for the safe and effective treatment of bacterial infections, protozoal infections and dermatological diseases.
Abstract: The invention relates to (S)-acyl-4?-phosphopantetheine derivatives, methods of their synthesis, and related medical uses of such compounds. Preferred medical uses relate to the treatment of neurodegenerative diseases, such as PKAN.
Type:
Grant
Filed:
October 29, 2014
Date of Patent:
May 8, 2018
Assignees:
ACIES BIO D.O.O., RIJKSUNIVERSITEIT GRONINGEN, ACADEMISCH ZIEKENHUIS GRONINGEN
Inventors:
Branko Jenko, Gregor Kosec, Hrvoje Petkovic, Ajda Podgorsek Berke, Jerca Pahor, Alen Cusak, Oda Cornelia Maria Sibon, Balaji Srinivasan
Abstract: The invention comprises a method of treating polycystic kidney disease (PKD) in a mammal, such as a human or feline (e.g., Persian cat), comprising administering a therapeutically effective amount of the compound of formula to the mammal. Also provided are uses of the compound for preparation of a medicament for treating PKD and the above compound and compositions comprising it for treating PKD.
Type:
Grant
Filed:
May 18, 2016
Date of Patent:
May 1, 2018
Assignee:
SYMPHONY EVOLUTION, INC.
Inventors:
Philip Frost, William W. N. Liao, Eric K. Rowinsky
Abstract: The present invention is directed to a method of treating a subject with autism spectrum disorder by administering an acetylaminopropane sulfonate.
Type:
Grant
Filed:
June 24, 2016
Date of Patent:
May 1, 2018
Assignee:
Indiana University Research and Technology Corporation
Abstract: Described are compositions that may be orally administered that comprise a bioreversible derivative of hydroxy N-substituted-2-aminotetralin or an enantiomer or salt or prodrug thereof, and a pharmaceutically acceptable carrier suitable for oral administration in the amount present, wherein the composition is orally bioavailable when administered to a subject. The bioreversible derivative has an intrinsic lipophilicity C log P value of about 7 to about 11.5. A method comprises oral administering such composition to a human subject in need of hydroxy N-substituted-2-aminotetralin therapy.
Type:
Grant
Filed:
July 21, 2014
Date of Patent:
May 1, 2018
Assignee:
SPRIASO LLC
Inventors:
William I. Higuchi, Firoozeh Aminian Patel