Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Type:
Grant
Filed:
June 7, 2012
Date of Patent:
November 24, 2015
Assignee:
AUTIFONY THERAPEUTICS LIMITED
Inventors:
Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
Abstract: Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof.
Type:
Grant
Filed:
July 22, 2011
Date of Patent:
November 17, 2015
Assignees:
The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino
Inventors:
Daniele Piomelli, Jason R. Clapper, Guillermo Moreno-Sanz, Andrea Duranti, Giovanna Guiducci, Marco Mor, Giorgio Tarzia
Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
Type:
Grant
Filed:
February 10, 2014
Date of Patent:
November 10, 2015
Assignee:
TEVA PHARMACEUTICAL INDUSTRIES LTD.
Inventors:
E. Itzhak Lerner, Moshe Flashner-Barak, Erwin v. Achthoven, Hans Keegstra, Ruud Smit
Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
Type:
Grant
Filed:
December 29, 2010
Date of Patent:
November 10, 2015
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the macrolides, the carboxylates or other classes, and which are highly suitable for controlling animal pests such as insects and undesired acarids.
Type:
Grant
Filed:
September 13, 2008
Date of Patent:
November 3, 2015
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
December 1, 2011
Date of Patent:
September 22, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Dean Boyall, Guy Brenchley, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
Abstract: The present invention relates to a method for the production of a formulation that is stable to oxidation and that is based on paracetamol in an aqueous solvent, comprising the steps of (i) dissolving paracetamol in an aqueous solvent comprising an isotonic agent that is sodium chloride and a buffer agent that is sodium citrate, having a temperature between 65° C. and 95° C. and having pH between 5.0 and 6.0 in a reaction vessel, (ii) replacing the remaining air in the vessel by an inert gas, such as nitrogen, and cooling the solution so formed to a temperature below 38° C., (iii) adding cysteine hydrochloride to the solution without mechanical agitation, and (iv) closing the reaction vessel and mechanically agitating the solution in a nitrogen atmosphere. The further relates to a formulation prepared according to the method.
Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
Abstract: The present specification discloses compositions comprising at least one therapeutic compound capable of modulating androgen production and methods and uses for treating a disorder associated with androgen production using such compositions and/or compounds.
Type:
Grant
Filed:
September 26, 2013
Date of Patent:
July 7, 2015
Assignee:
Tangent Reprofilling Limited
Inventors:
Suzanne Dilly, Gregory Stoloff, Paul Taylor
Abstract: The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.
Type:
Grant
Filed:
March 29, 2011
Date of Patent:
June 23, 2015
Assignee:
Novartis AG
Inventors:
Charles Meyers, Michael H. Serrano-Wu, Tom Thuren
Abstract: The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use.
Type:
Grant
Filed:
June 24, 2011
Date of Patent:
June 16, 2015
Assignee:
LEO PHARMA A/S
Inventors:
Soren Ebdrup, Kim Troensegaard Nielsen, Tanja Maria Greve
Abstract: A composition for increasing the bioavailability of an active pharmaceutical ingredient (“API”) in humans and animals, comprising a first water soluble surfactant having a cloud point greater than about 37° C., a second water soluble surfactant having a cloud point greater than about 37° C., wherein a mixture of the first surfactant and the second surfactant comprises a cloud point less than about 37° C.
Abstract: Psoriasis is treated by application of a composition containing a nitrone spin trap such as ?-phenyl t-butyl nitrone (PBN) and derivatives thereof. Preferred compositions and method of treatments further comprise at least one adjunctive ingredient including fatty acid esters of ascorbic acid such as ascorbyl palmitate and ascorbyl stearate, and polyenylphosphatidylcholine.
Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
September 18, 2013
Date of Patent:
May 12, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Dean Boyall, Guy Brenchley, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
Abstract: The disclosure relates to a pharmaceutical composition for oral administration, containing, as active principle, a benzofuran derivative having antiarrhythmic activity, in particular dronedarone and the pharmaceutically acceptable salts thereof, and at least one lipid carrier, said pharmaceutical composition being intended to be used in unit dosage form of the capsule type, in particular with a hard shell. This pharmaceutical composition and the dosage form comprising such a composition aim to limit the meal time effect following oral administration in humans. The lipid carrier allows: the solubilization of the active principle of the invention; and the shielding thereof from the negative effects of pH in the intestinal tract, thereby allowing same to be spared from the meal effect to a significant extent.
Type:
Grant
Filed:
May 6, 2013
Date of Patent:
April 28, 2015
Assignee:
Sanofi
Inventors:
Bernard Abramovici, Stephane Beilles, Sandra Chambonnet, Jean-Claude Gautier
Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.
Type:
Grant
Filed:
August 22, 2011
Date of Patent:
April 7, 2015
Assignee:
The University of British Columbia
Inventors:
Xiaoxia Wang, Labros George Meimetis, Matthew Bruce Nodwell, Raymond Andersen
Abstract: Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
Type:
Grant
Filed:
September 27, 2012
Date of Patent:
March 24, 2015
Assignee:
Janssen Pharmaceutica NV
Inventors:
Margery Connelly, Christopher M. Flores, Mark J. Macielag
Abstract: The present invention is directed to a rhenium complex of general Formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X is Se; Y is NH, O or S or is a methylene group; Z is halogen; m=0, 1, or 2 and p=0, 1, or 2, provided that m and p are both different from zero when Y is NH, O or S; n=3; R? is a phenyl group or a group of general Formula —(CH2)q—COOH wherein q=1 or 2, a pharmaceutical composition comprising a therapeutically effective amount of at least one of such rhenium complex where X is additionally S or Te, a method for preparing said rhenium complex and a method for treating a proliferative growth related-disorder using a therapeutically effective amount of at least one of said rhenium complex where X is additionally S or Te. Also claimed is the use of compounds of formula (II) in the preparation of compounds of formula (I).
Type:
Grant
Filed:
June 1, 2011
Date of Patent:
March 24, 2015
Assignees:
Societe de Coordination de Recherches Therapeutiques, Universite Paris-Sud 11, Centre National de la Recherche Scientifique
Inventors:
Philippe Collery, Jean D'Angelo, Georges Morgant