Abstract: Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.
Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
Type:
Grant
Filed:
September 20, 2019
Date of Patent:
April 13, 2021
Assignee:
Pfizer Inc.
Inventors:
Brian Stephen Gerstenberger, Andrew Christopher Flick, Vincent Michael Lombardo, James John Mousseau, Philippe Marcel Nuhant, Ralph Pelton Robinson, Jr., Mark Edward Schnute, Daniel Wei-Shung Kung, Daniel Copley Schmitt, Atli Thorarensen, John Isidro Trujillo, Rayomand Jal Unwalla, Huixian Wu
Abstract: The present invention relates to compounds of the general formula (I) in which Q, V, T, W, Y, X and A have the meanings given in the description—and to a process for preparation thereof and to the use thereof for controlling animal pests.
Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
Type:
Grant
Filed:
November 14, 2018
Date of Patent:
October 1, 2019
Assignee:
NOVIRA THERAPEUTICS, INC.
Inventors:
Ryan C. Clark, Yen Truong, Nicholas Stock, Jason Jacintho
Abstract: An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].
Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
Abstract: This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.
Type:
Grant
Filed:
July 29, 2015
Date of Patent:
January 31, 2017
Assignee:
The Brigham and Women's Hospital, Inc.
Inventors:
David Cohen, Neil Wagle, Gregory D. Cuny, Jun Xian, Marcie Glicksman, Ross L. Stein, Ekaterina Y. Shishova
Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
January 29, 2014
Date of Patent:
June 9, 2015
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
Abstract: Derivatives of pyridine of the formula wherein one of Y and A is CR and the other is N are kinase inhibitors useful in treating conditions associated with excess kinase activity.
Type:
Grant
Filed:
January 22, 2013
Date of Patent:
May 12, 2015
Assignee:
Gilead Sciences, Inc.
Inventors:
Christopher John Burns, Michael Francis Harte, James T. Palmer
Abstract: The present invention provides a compound of general formulae A useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof.
Type:
Grant
Filed:
February 25, 2014
Date of Patent:
April 14, 2015
Assignee:
Council of Scientific and Industrial Research
Inventors:
Ahmed Kamal, Mohammed Ashraf, Shaikh Faazil Bagwan, Yellamelli Valli Venkata Srikanth, Syed Mohammed Ali Hussaini, Adla Malla Reddy
Abstract: A fluorinated voltage sensitive dye has the structure wherein p is 0, 1, or 2; Xq? is an anionic counterion having a charge, q, that is 1 or 2; n is 1 or 2; R1 is an optionally substituted C1-C12, alkyl; R2 is hydrogen, and R3 is hydrogen or fluorine; or R2 and R3 collectively form a divalent —CH?CH—CH?CH— group; R4 and each occurrence of R5 are each independently hydrogen or fluorine; R6 is hydrogen or fluorine or trifluoromethyl; and each occurrence of R7 is independently C1-C6 alkyl; provided that the dye comprises at least one fluorine atom. The dye is particularly useful for monitoring the dynamics of action potentials in axons and/or dendrites.
Type:
Grant
Filed:
June 3, 2013
Date of Patent:
March 31, 2015
Assignee:
The University of Connecticut
Inventors:
Ping Yan, Corey D. Acker, Leslie M. Loew
Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.
Type:
Application
Filed:
November 13, 2012
Publication date:
February 19, 2015
Inventors:
William G. Cance, Ravindra K. Pandey, Elena V. Kurenova, Manivannan Ethirajan
Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
Abstract: The invention relates to 2-(4-Substituted phenylamino) polysubstituted pyridine compounds as inhibitors of non-nucleoside HIV reverse transcriptase, preparation methods and uses thereof. Specifically, the invention relates to compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description. The compounds of formula I of the invention are a type of anti-HIV active compounds having new backbone structure.
Type:
Grant
Filed:
September 28, 2009
Date of Patent:
January 13, 2015
Assignee:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
Inventors:
Lan Xie, Xingtao Tian, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
Type:
Grant
Filed:
July 30, 2010
Date of Patent:
October 21, 2014
Assignee:
Bayer Cropscience AG
Inventors:
Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
Type:
Grant
Filed:
December 18, 2012
Date of Patent:
October 14, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Armin Heckel, Andreas Blum, Dieter Hamprecht, Joerg Kley
Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:
Type:
Application
Filed:
March 25, 2014
Publication date:
October 2, 2014
Applicant:
Samsung Display Co., Ltd.
Inventors:
Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
Abstract: The present invention relates to functionalized fluoroalkylfluorophosphate salts, in particular as ionic liquids, to the preparation thereof and to the use thereof.
Type:
Grant
Filed:
August 30, 2011
Date of Patent:
September 30, 2014
Assignee:
Merck Patent GmbH
Inventors:
Berthold Theo Hoge, Anne Julia Bader, Nikolai Mykola Ignatyev, Michael Schulte, Wolfgang Hierse, Waldemar Wiebe, Helge Willner
Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
Type:
Grant
Filed:
December 7, 2012
Date of Patent:
September 30, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer
Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
Type:
Grant
Filed:
January 7, 2013
Date of Patent:
September 23, 2014
Assignee:
The Trustees of the University of Pennsylvania
Abstract: Provided herein are methods for selectively detecting an alkyne-presenting molecule in a sample and related detection reagents, compositions, methods and systems.
Type:
Application
Filed:
March 7, 2014
Publication date:
September 18, 2014
Applicant:
LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
Type:
Grant
Filed:
December 7, 2012
Date of Patent:
August 5, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.
Type:
Application
Filed:
June 15, 2012
Publication date:
July 31, 2014
Applicants:
SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATION
Abstract: A compound of Formula I, Formula IA, Formula IB, or Formula II, or an acid or base addition salt thereof, and use of these compounds as antioxidants. In one embodiment, a compound of Formula II, wherein each of X, Y, and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1, and R2 are each bonded to a carbon atom in their own respective aryl ring.
Type:
Application
Filed:
June 4, 2012
Publication date:
July 24, 2014
Applicants:
UNIVERSITA DI BOLOGNA, Queen's University at Kingston
Inventors:
Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I or II or a stereoisomer, tautomer, racemic, metabolite, pro- or pre-drug, salt, hydrate, or solvate thereof, wherein Ar, Cy, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
Type:
Grant
Filed:
December 29, 2011
Date of Patent:
July 22, 2014
Assignee:
The Regents of the University of California
Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
Type:
Grant
Filed:
May 13, 2011
Date of Patent:
June 17, 2014
Assignee:
Array BioPharma Inc.
Inventors:
Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, David A. Mareska, Steven Armen Boyd
Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.
Type:
Grant
Filed:
December 28, 2012
Date of Patent:
June 17, 2014
Assignee:
Dow AgroSciences, LLC.
Inventors:
Jossian Oppenheimer, Mark V. M. Emonds, Christopher W. Derstine, Robert C. Clouse
Abstract: The present disclosure provides for method of treatment and/or prevention of disease states that require cystine for maintenance or progression of the disease state. In addition, methods for screening and identifying novel therapeutic agents useful in the treatment of such disease states are described. In one embodiment, the disease state is a cancer, such as, but not limited to, glioma. In this embodiment, methods for the treatment and prevention of glioma by inhibiting cystine uptake or decreasing intracellular cystine concentrations are provided. The present disclosure teaches that glioma cells are dependent on system Xc for cystine uptake. Pharmacological inhibition of system Xc causes a rapid depletion of intracellular glutathione, resulting in decreased cell growth. In contrast, non-malignant astrocytes and cortical neurons remain viable in the presence of Xc inhibitors and continue to take up cystine via alternate amino acid transporters.
Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
Type:
Grant
Filed:
March 5, 2013
Date of Patent:
May 27, 2014
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Juan-Miguel Jimenez, Philip Collier, Jeremy Green, Gregory Henkel, Michael Liu, Timothy Neuberger
Abstract: An amine-based compound and an organic light-emitting diode including the amine-based compound are provided. The amine-based compound may be used between a pair of electrodes of an organic light-emitting diode. For example, the amine-based compound may be used in an emission layer and/or between the emission layer and an anode (for example, in a hole injection layer, a hole transport layer, a functional layer having a hole injection ability and a hole transport ability). Accordingly, an organic light-emitting diode including a first electrode, a second electrode facing the first electrode, and an organic layer that is interposed between the first electrode and the second electrode, and includes the amine-based compound is provided.
Type:
Application
Filed:
March 13, 2013
Publication date:
May 22, 2014
Inventors:
Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
Abstract: This invention discloses and claims a series of polycyclic monomers and polymers useful in the production of optical waveguides. The polymers of the invention comprise one or more repeating units represented by the formula (IV): Wherein m, X, R1 and R2 are as defined herein. The films formed from the polymers of this invention exhibit significant changes in refractive index (greater than or equal to 0.5%) after exposure to suitable actinic or thermal energy thereby having superior optical transmission performance, which is of importance for modern optical applications such as wave guiding and optical data storage.
Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
June 20, 2013
Date of Patent:
April 15, 2014
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
Abstract: The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Type:
Grant
Filed:
May 6, 2010
Date of Patent:
April 15, 2014
Assignee:
Aniona APS
Inventors:
Dan Peters, Elsebet Østergaard Nielsen, Karin Sandager Nielsen, Gordon Munro
Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
Abstract: Monosubstituted oxalic acid derivatives of the general formula (I) [A]+[O—C(O)—C(O)—O—X???(I) Wherein the meaning is for [A]+ a cation made from an organic moiety A having a formally positively charged heteroatom selected from the group consisting of nitrogen, phosphorus and sulfur X is a C1 to C30 organic residue and wherein the following compounds (I) are disclaimed: Tetramethylammonium monomethyloxalate Methyltri(alkyl)ammonium monomethyloxalate Trimethyl(1-hydroxyethyl)ammonium monomethyloxalate Methyltriethylammonium monomethyloxalate Tetraethylammonium monomethyloxalate n-Propyltriethylammonium mono-n-propyloxalate n-Butyltriethylammonium mono-n-butyloxalate Benzyltriethylammonium monobenzyloxalate cyclohexyldimethylammonium monomethyloxalate Dimethyl-phenylammonium monomethyloxalate.
Type:
Application
Filed:
October 9, 2013
Publication date:
April 10, 2014
Applicant:
BASF SE
Inventors:
Klemens Massonne, Joerg Sundermeyer, Axel Braam
Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
Type:
Grant
Filed:
August 8, 2011
Date of Patent:
March 25, 2014
Assignee:
Rempex Pharmaceuticals, Inc.
Inventors:
Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
Type:
Grant
Filed:
November 22, 2010
Date of Patent:
March 11, 2014
Assignee:
Dow AgroSciences, LLC.
Inventors:
Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein each of W, Q, R1, R2, R3, R4, R5, m, and n is as defined herein, pharmaceutically acceptable compositions thereof, and methods of using the same.
Type:
Grant
Filed:
March 22, 2010
Date of Patent:
March 11, 2014
Assignee:
The Johns Hopkins University
Inventors:
Jun O. Liu, Yunzhao Ren, Fan Pan, Curtis R. Chong, Reinhold Penner, Jonathan R. Behr
Abstract: The invention relates to bis(perfluoroalkyl)phosphinous acids, bis(perfluoroalkyl)thiophosphinous acids and derivatives, the synthesis thereof and the use thereof, in particular for the synthesis of air-stable metal complexes for catalytic processes.
Type:
Grant
Filed:
July 10, 2009
Date of Patent:
February 11, 2014
Assignee:
Merck Patent GmbH
Inventors:
Berthold Hoge, Anne Julia Bader, Boris Kurscheid, Nikolai (Mykola) Ignatyev, Emil Ferdinand Aust
Abstract: The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-?,?,?-trifluoro-2,6-di-nitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.
Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
Type:
Application
Filed:
December 28, 2012
Publication date:
February 6, 2014
Applicant:
Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
Inventor:
Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthmas.
Type:
Grant
Filed:
July 10, 2012
Date of Patent:
December 31, 2013
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Sarah Dunham, Adam D. Hughes, Craig Husfeld, Eric L. Stangeland
Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
Type:
Application
Filed:
March 7, 2013
Publication date:
December 12, 2013
Applicant:
THE UNIVERSITY OF HOUSTON SYSTEM
Inventors:
T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.