Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
Type:
Grant
Filed:
August 14, 2013
Date of Patent:
November 8, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Kenneth J. Barr, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Dongshan Zhang, Brian M. Andresen, Neville J. Anthony, Blair T. Lapointe, Nunzio Sciammetta
Abstract: A chromene compound having a short fading half period, especially, a short fading half period even at a low temperature in a general-purpose polymer solid matrix. The chromene compound is represented by the following formula (1). wherein R1 is a hydroxyl group or the like, R2 and R3 are each an aryl group or the like, C* is a spiro carbon atom, a spiro ring A represented by the following formula is a saturated hydrocarbon ring having 4 to 12 ring member carbon atoms or the like, and at least one ring member carbon atom constituting the ring A is a group represented by the following formula (4), and X is a divalent group such as arylene group, wherein R7 and R8 are each a cycloalkyl group or the like.
Abstract: Disclosed herein are methods for the treatment of pediatric otic diseases or conditions with antimicrobial agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).
Type:
Grant
Filed:
August 26, 2014
Date of Patent:
November 8, 2016
Assignee:
OTONOMY, INC.
Inventors:
Fabrice Piu, Qiang Ye, Luis A. Dellamary, Carl Lebel
Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
Type:
Grant
Filed:
October 8, 2012
Date of Patent:
November 8, 2016
Assignees:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN, WAYNE STATE UNIVERSITY
Inventors:
Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.
Type:
Grant
Filed:
October 8, 2013
Date of Patent:
November 1, 2016
Assignee:
MEDIVATION TECHNOLOGIES, INC.
Inventors:
David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
Abstract: The present invention provides compounds of Formula III and Formula VI, and processes for their preparation. The present invention further provides use of the compounds of Formula III and Formula VI for the preparation of tofacitinib or isomers or a mixture of isomers or salts thereof.
Type:
Grant
Filed:
December 17, 2013
Date of Patent:
November 1, 2016
Assignee:
SUN PHARMACEUTICAL INDUSTRIES LIMITED
Inventors:
Mohammed Salman Hashmi, Yoginder Pal Sachdeva, Chandra Has Khanduri
Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.
Type:
Grant
Filed:
September 29, 2014
Date of Patent:
October 25, 2016
Assignee:
The Regents of the University of California
Inventors:
Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
Type:
Grant
Filed:
March 21, 2013
Date of Patent:
October 25, 2016
Assignee:
Rutgers, The State University of New Jersey
Inventors:
Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
Abstract: The present invention relates to compositions and methods of using free radical scavengers with reduced 1O2 generation. In certain embodiments, these compositions and methods of use relate to fullerene-derived ketolactams and fullerene-derived ketolactam derivatives, fullerene derivatives, and/or fullerenes. In yet other embodiments, the invention relates to cosmetic or dermatological compositions comprising said free radical scavengers with reduced 1O2 generation.
Type:
Grant
Filed:
November 11, 2013
Date of Patent:
October 25, 2016
Assignee:
Solenne BV
Inventors:
David F. Kronholm, Alexander B. Sieval, Jan C. Hummelen
Abstract: The invention concerns diallylisoidide in a first aspect, and in a related aspect concerns an improved method for making the diallyl ether derivatives of anhydrohexitols generally, whether isosorbide, isomannide, isoidide or a mixture of two or all three of these, whereby these derivatives may be produced efficiently up to quantitative yields.
Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
Type:
Grant
Filed:
February 21, 2013
Date of Patent:
October 4, 2016
Assignee:
SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
Inventors:
Anthony B. Pinkerton, Russell Dahl, Nicholas D. P. Cosford, Jose Luis Millan
Abstract: A process for producing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) including salts and hydrates thereof of general formula (I) from the respective cyclen. The process involves the use of cationic- and anionic exchange resins and solvent treatments to remove the organic and inorganic contaminants. Any cations present in the raw DOTA or other contaminants resulting from the reaction of cyclen are largely reduced in early stages of the process allowing to obtain good yields of DOTA in a purified grade and in an easier and reliable way. The process is useful for the production of DOTA, of macrocyclic compounds including metal ions complexes thereof and of compositions including the macrocyclic compounds that can be used as contrast agents for magnetic resonance imaging.
Type:
Grant
Filed:
January 22, 2014
Date of Patent:
October 4, 2016
Assignee:
AGFA HEALTHCARE NV
Inventors:
Diederik Buffel, Rakesh Ganorkar, Jennifer Burt, Xavier Boi
Abstract: A new method for the synthesis of L-Glutamyl-?-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
October 4, 2016
Assignee:
BTG INTERNATIONAL LIMITED
Inventors:
James Alan Kerschen, Alexander James Bridges, Milind D. Choubal, Sean Mark Dalziel, Thomas Elliott Jacks, Andrew S. Thompson, James Robert Zeller
Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
Type:
Grant
Filed:
November 13, 2013
Date of Patent:
October 4, 2016
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Romyr Dominique, Francisco Javier Lopez-Tapia, Eric Mertz, Sung-Sau So
Abstract: This disclosure features fungicidal combinations that include a paraffinic oil and an emulsifier. The combinations can further include one or more of the following: pigments, silicone surfactants, anti-settling agents, conventional fungicides such as demethylation inhibitors (DMI) and quinone outside inhibitors (Qol) and water. The fungicidal combinations are used for controlling infection of a crop plant by a fungal pathogen.
Abstract: A process for the preparation of the calcium complex of 10-(2, 3-Dihydroxy-1-(hydroxymethyl)propyl)-1,4,7,10-tetraazacyclodecane-4,7-triacetic acid, also known as Calcobutrol, starting from the pure gadolinium complex (Gadobutrol) is disclosed. Also disclosed is Calcobutrol with a hitherto unknown level of purity.
Abstract: The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.
Abstract: The invention relates to pyridinone derivatives of general formula (I) as inhibitors of tissue transglutaminase, to methods for producing the pyridinone derivatives, to pharmaceutical compositions containing said pyridinone derivatives and to their use for the prophylaxis and treatment of diseases associated with tissue transglutaminase.
Type:
Grant
Filed:
July 12, 2013
Date of Patent:
September 6, 2016
Assignee:
ZEDIRA GMBH
Inventors:
Christian Buchold, Uwe Gerlach, Martin Hils, Ralf Pasternack, Johannes Weber
Abstract: The invention relates to solid dispersions of poorly water soluble compounds, in particular Compound A as disclosed herein, formed by solvent co-precipitation or spray drying, resulting in improved bioavailability, safety and tolerability of said compounds.
Type:
Grant
Filed:
January 21, 2014
Date of Patent:
August 30, 2016
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
Steve Lomuscio, Hua Ma, Michael Allen Matchett, Harpreet K. Sandhu, Navnit Hargovindas Shah, Yu-E Zhang