Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
Type:
Grant
Filed:
October 1, 2013
Date of Patent:
April 4, 2017
Assignee:
Gilead Sciences, Inc.
Inventors:
Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-·dihydrochloride with acrylonitrile to provide 1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazol-3-amine, by oxidizing to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
Type:
Grant
Filed:
September 9, 2015
Date of Patent:
April 4, 2017
Assignee:
Dow AgroSciences LLC
Inventors:
Qiang Yang, Beth Lorsbach, Xiaoyong Li, Gary Roth, David E. Podhorez
Abstract: A vinca alkaloid compound that is substituted at the 20?-position with a urea or thiourea group is disclosed. The urea's proximal nitrogen atom bonded to the 20?-position carbon atom is secondary, whereas the distal nitrogen atom can be unsubstituted only when the compound contains an optionally present 10?-fluoro substituent, and is otherwise preferably mono- or di-substituted. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using a compound.
Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.
Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Type:
Grant
Filed:
May 3, 2012
Date of Patent:
March 28, 2017
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia
Abstract: Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.
Abstract: New compounds of the general formula Xm-G-CLn are described as well as methods for their production and use in the analysis, detection and purification of target molecules. These constitute multivalent chelator-compounds with an affinity-tag binding to metal-chelator-complexes which can selectively modify and/or immobilize target molecules by a multitude of probes or functional units.
Type:
Grant
Filed:
July 26, 2005
Date of Patent:
March 28, 2017
Assignee:
JOHANN WOLFGANG GOETHE-UNIVERSITAT FRANKFURT AM MAIN
Inventors:
Jacob Piehler, Robert Tampe, Suman Lata
Abstract: The present invention relates to a method for preparing the pyripyropene compound of the formula (I) which method comprises the following steps: i) subjecting a pyripyropene compound of formula Pyripyropene A to an alkaline hydrolysis to yield a 1,7,11 -trideacetylpyripyropene A, ii) reacting 1,7,11-trideacetylpyripyropene A obtained in step i) with cyclopropane carbonyl chloride to yield a raw product containing the pyripyropene compound of formula (I); iii) subjecting the raw product of step ii) to crystallization to yield a crystalline pyripyropene compound of formula (I) and a mother liquor; and iv) recycling the mother liquor or a pyripyropene compound containing fraction thereof to the alkaline hydrolysis of step i).
Type:
Grant
Filed:
January 15, 2014
Date of Patent:
March 21, 2017
Assignee:
BASF SE
Inventors:
Melanie Bonnekessel, Wolfgang Reichert, Ralf Hoock, Thomas Kaeding, Christopher Koradin, Andreas Pletsch, Manfred Ehresmann, Hartwig Schroeder
Abstract: The present invention provides a novel and improved process for the production of the production of hindered anilines containing perfluoroalky groups in good yield any by using close to stoichiometric amounts of acylating agent.
Type:
Grant
Filed:
April 1, 2014
Date of Patent:
March 21, 2017
Assignee:
Syngenta Participations AG
Inventors:
Helmars Smits, Thomas Pitterna, Ottmar Franz Hueter, Andrew Edmunds, Andre Stoller, Pierre Joseph Marcel Jung
Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Type:
Grant
Filed:
September 15, 2015
Date of Patent:
March 21, 2017
Assignee:
Akebia Therapeutics, Inc.
Inventors:
Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
Abstract: The present invention provides a method for synthesizing Milbemycin oxime. The method comprises the following steps. (1) Oxidizing reaction: oxidizing Milbemycin, using hypochlorite or chlorite as oxidizers and piperidine nitrogen oxygen free radicals as the catalyst and halide as the catalyst promoter. The oxidation reaction is conducted in a dichloromethane solvent for 0.5-4 hours at ?5-15° C. to produce the intermediate product Milbemycin ketone. (2) Oximation reaction: reacting the Milbemycin ketone with a hydroxylamine hydrochloride oximation agent in a 1,4-dioxane reaction solvent for 10-16 hours at 25-35° C. to obtain Milbemycin oxime. The method provided by the present invention realized the industrial production of Milbemycin oxime for the first time domestically. Moreover, the yield of the prepared product is higher than competing products both at home and abroad.
Abstract: An agrochemical solid formulation contains fenpyrazamine and an acid component. The formulation has no problem of emission of odor and has excellent storage stability. A mixture of 1 g of the agrochemical solid formulation and 99 g of ion exchange water has a pH at 25° C. of 8 or less.
Abstract: The present invention concerns particular fluorenes, the use of the compound in an electronic device, and an electronic device containing at least one of these compounds. The present invention further concerns a method for producing the compound and a formulation and composition containing one or more of the compounds.
Type:
Grant
Filed:
June 27, 2013
Date of Patent:
March 14, 2017
Assignee:
Merck Patent GmbH
Inventors:
Teresa Mujica-Fernaud, Elvira Montenegro, Amir Hossain Parham, Arne Buesing, Frank Voges
Abstract: The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
March 14, 2017
Assignee:
AICURIS ANTI-INFECTIVE CURES GMBH
Inventors:
Wilfried Schwab, Alexander Birkmann, Kerstin Paulus, Kurt Vogtli, Dieter Haag, Stephan Maas, Kristian Ruepp
Abstract: Disclosed are methods for synthesizing an ester or a carboxylic acid from an organic alcohol. To form the ester one reacts, in the presence of oxygen gas, the alcohol with methanol or ethanol. This reaction occurs in the presence of a catalyst comprising palladium and a co-catalyst comprising bismuth, tellurium, lead, cerium, titanium, zinc and/or niobium (most preferably at least bismuth and tellurium). Alternatively that catalyst can be used to generate an acid from that alcohol, when water is also added to the reaction mix.
Type:
Grant
Filed:
May 1, 2015
Date of Patent:
March 14, 2017
Assignee:
WISCONSIN ALUMNI RESEARCH FOUNDATION
Inventors:
Shannon S. Stahl, Adam B. Powell, Thatcher W. Root, David S. Mannel, Maaz S. Ahmed
Abstract: This invention relates to novel (±)1-(Dimethylamino)ethyl substituted 6H-benzo[c]chromen-6-one compounds which are useful as pharmaceutical compositions.