Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/329)
  • Patent number: 11760746
    Abstract: The present disclosure relates to methods and intermediates useful for preparing a compound of formula I. or a co-crystal, solvate, salt or combination thereof.
    Type: Grant
    Filed: June 16, 2021
    Date of Patent: September 19, 2023
    Assignee: Gilead Sciences, Inc.
    Inventors: Sachin Dhar, Alex Goldberg, Lars V. Heumann, Zilin Huang, Vinh Xuan Ngo, Trevor James Rainey, Dietrich P. Steinhuebel, Xianghong Wang, Scott Alan Wolckenhauer
  • Patent number: 11135209
    Abstract: Identified compounds demonstrate protein kinase inhibitory activity and inhibition of dependent cell signaling pathways, such as NOD2 cell signaling. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: October 5, 2021
    Assignees: University of Houston System, Trustees of Tufts College
    Inventors: Gregory Cuny, Chalada Suebsuwong, Alexei Degterev
  • Patent number: 11124532
    Abstract: The invention comprises novel chiral metal complex compounds of the formula wherein M, PR2, R3 and R4 are outlined in the description, its stereoisomers, in the form as a neutral complex or a complex cation with a suitable counter ion. The chiral metal complex compounds can be used in asymmetric reactions, particularly in asymmetric reductions of ketones, imines or oximes.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: September 21, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Matthias Beller, Marcel Garbe, Kathrin Junge, Michelangelo Scalone
  • Patent number: 10925865
    Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
    Type: Grant
    Filed: July 23, 2020
    Date of Patent: February 23, 2021
    Assignee: Nocion Therapeutics, Inc.
    Inventors: Bridget McCarthy Cole, James Lamond Ellis
  • Patent number: 10828287
    Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
    Type: Grant
    Filed: November 6, 2019
    Date of Patent: November 10, 2020
    Assignee: Nocion Therapeutics, Inc.
    Inventors: Bridget McCarthy Cole, James Lamond Ellis
  • Patent number: 9957251
    Abstract: The present invention provides a heterocyclic compound having a CDK8 and/or CDK19 inhibitory effect. The present invention provides a compound represented by formula (I) (in the formula, the symbols are as defined in the description) or a salt thereof.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: May 1, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takaharu Hirayama, Jun Fujimoto, Douglas Robert Cary, Masanori Okaniwa, Yasuhiro Hirata
  • Patent number: 9890122
    Abstract: The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: February 13, 2018
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Alessandro Falchi, Emilio Lutero, Emanuele Ferrari, Fausto Pivetti, Rocco Bussolati, Edoardo Mariani, Orsola Vecchi, Erhard Bappert, Caterina Ventrici
  • Patent number: 9783530
    Abstract: The present invention provides a compound of Formula I (The chemical formula should be inserted here.) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: October 10, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D. Edmondson, Zhuyan Guo, Eric Mertz, Anthony K. Ogawa, Sung-Sau So, Wanying Sun, Linda L. Brockunier, Amjad Ali, Rongze Kuang, Heping Wu
  • Patent number: 9556111
    Abstract: The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP185) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl)amine structure.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: January 31, 2017
    Assignee: UNIVERSITETET I OSLO
    Inventors: Kjetil Tasken, Birgitte Lygren, Ellen Ostensen, Jo Klaveness
  • Patent number: 9403753
    Abstract: A ruthenium bis(pyrazolyl)borate scaffold that enables cooperative reduction reactivity in which boron and ruthenium centers work in concert to effect selective nitrile reduction is provided. The pre-catalyst compound [?3-(1-pz)2HB(N?CHCH3)]Ru(cymene)+ TfO? (pz=pyrazolyl) was synthesized using readily-available materials through a straightforward route, thus making it an appealing catalyst for a number of reactions.
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: August 2, 2016
    Assignee: University of Southern California
    Inventors: Travis J. Williams, Zhiyao Lu
  • Patent number: 9328069
    Abstract: The present invention relates to a method for manufacturing an imine having no substituent group on the nitrogen by using, as a catalyst, a metal complex on an organic azide compound, and more specifically relates to a method in which a metal-complex catalyst is used to produce, from an organic azide having an alpha-hydrogen, an imine having no substituent group on the nitrogen via a continuous nitrogen removal and 1,2-hydrogen transfer reaction. The imine having no substituent group on the nitrogen manufactured by means of the method of the present invention can synthesize diverse coupling products comprising amine compounds by means of reactions with diverse nucleophiles.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: May 3, 2016
    Assignee: Postech Academy-Industry Foundation
    Inventors: Jai Wook Park, Young Ho Rhee, Jin Hee Lee, Jung Hoon Han, Sreya Gupta, Wook Jeong
  • Patent number: 9115081
    Abstract: Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: August 25, 2015
    Assignee: Cardiome Pharma Corp.
    Inventors: Bertrand M. C. Plouvier, Doug Ta Hung Chou, Grace Jung, Lewis Siu Leung Choi, Tao Sheng, Anthony G. M. Barrett, Marco S. Passafaro, Martin Kurz, Daniel Moeckli, Pirmin Ulmann, Alfred Hedinger
  • Publication number: 20150141653
    Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Inventors: Yasushi SHIBATA, Tsutomu IMAGAWA
  • Patent number: 9035065
    Abstract: The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treating depression by administering the ethanamine compound.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: May 19, 2015
    Assignee: AstraZeneca AB
    Inventors: Michael Balestra, Peter Bernstein, Glen E. Ernst, William Frietze, John McCauley, David Nugiel, Lihong Shen
  • Publication number: 20150133510
    Abstract: The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP185) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl)amine structure.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Applicant: Universitetet I Oslo
    Inventors: Kjetil Tasken, Birgitte Lygren, Ellen Ostensen, Jo Klaveness
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 8980890
    Abstract: The invention relates to compounds and methods for treating cell proliferation disorders.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: March 17, 2015
    Assignee: Kinex Pharmaceuticals, LLC
    Inventor: David G. Hangauer, Jr.
  • Patent number: 8946463
    Abstract: The present invention relates to a chemocatalytic liquid-phase process for the direct one-stage amination of alcohols to primary amines by means of ammonia in high yields using a catalyst system containing at least one transition metal compound and a xantphos ligand.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Evonik Degussa GmbH
    Inventors: Florian Klasovsky, Thomas Tacke, Jan Christoph Pfeffer, Thomas Haas, Matthias Beller, Andreas Martin, Jens Deutsch, Angela Koeckritz, Sebastian Imm, Juergen Haberland
  • Patent number: 8937055
    Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: January 20, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
  • Patent number: 8916569
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: December 23, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140364586
    Abstract: Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.
    Type: Application
    Filed: June 26, 2014
    Publication date: December 11, 2014
    Inventors: Andrew Graham WATTS, Terrence Kantner, Amanda Barbara MacKenzie
  • Patent number: 8906946
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: December 9, 2014
    Assignee: Dompe' S.p.A.
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Publication number: 20140348753
    Abstract: The development of a series of fluorescent materials including heterocycle-functionalized luminogens with aggregation-induced/enhanced emission (AIE/AEE), long wavelength emission, and high solid state fluorescence quantum efficiency is contemplated. The described fluorescent materials are promising candidates in selective luminescence-based chemosensor for Hg2+ or ATP, fluorescent staining for mitochondria in living cells with high photostability, stimuli-responsive luminescent materials, and materials for optical waveguides. In addition, these heterocycle-functionalized luminogens are particularly useful as fluorescent labels for biopolymers such as peptides, antibodies, or nucleic acids, making them useful as AIE-active biocompatible probes for clinical cancer imaging and diagnostics.
    Type: Application
    Filed: May 24, 2013
    Publication date: November 27, 2014
    Inventors: Benzhong TANG, Wing Yip LAM, Na ZHAO, Min LI, Bin LIU, Haibin SHI, Dan DING
  • Patent number: 8895589
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: November 25, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20140335019
    Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
  • Patent number: 8883180
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8884022
    Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: November 11, 2014
    Assignee: North Carolina State University
    Inventors: Christian Melander, Steven A. Rogers
  • Publication number: 20140323724
    Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid.
    Type: Application
    Filed: July 11, 2014
    Publication date: October 30, 2014
    Inventors: Yasushi SHIBATA, Tsutomu IMAGAWA
  • Patent number: 8871934
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: October 28, 2014
    Assignee: Japan Tobacco Inc.
    Inventors: Takahisa Motomura, Hironobu Nagamori, Koichi Suzawa, Hirotsugu Ito, Toru Morita, Satoru Kobayashi, Hisashi Shinkai
  • Publication number: 20140316080
    Abstract: The present invention relates to hardeners for epoxy resins, which contain secondary amino groups having pyridinyl groups. They harden surprisingly quickly together with epoxy resins even under cold and humid conditions and without producing blushing to give films with a high degree of hardness, the highest degrees of hardness being obtained with a surprisingly low amount of hardener required. They are especially suitable for low-emission coatings with high resistance requirements.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 23, 2014
    Inventors: Andreas Kramer, Edis Kasemi
  • Patent number: 8859778
    Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: October 14, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Elisabetta Armani, Maurizio Delcanale
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Publication number: 20140288306
    Abstract: The present invention provides novel ruthenium based catalysts, and a process for preparing amines, by reacting a primary alcohol and ammonia in the presence of such catalysts, to generate the amine and water. According to the process of the invention, primary alcohols react directly with ammonia to produce primary amines and water in high yields and high turnover numbers. This reaction is catalyzed by novel ruthenium complexes, which are preferably composed of quinolinyl or acridinyl based pincer ligands.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventors: David Milstein, Chidambaram Gunanathan
  • Patent number: 8841460
    Abstract: A compound, or a salt thereof, having the formula wherein Y is n is 1 or 2; each R is independently H, alkyl, substituted alkyl, a polyether moiety, carboxyl, substituted carboxyl, carbamate, substituted carbonate, carbonyloxy, alkoxy, substituted alkoxy, haloalkyl, halogen, nitro, amino, aryloxy, cyano, hydroxyl, or sulfonyl; R1 is H, lower alkyl or aralkyl; R2 is selected from H, acyl, aralkyl, phosphonyl, —SO2R3; —C(O)R5; —C(O)OR7 or —C(O)NR9R10; R3; R5; R7; R9 and R10 independently are selected from H, lower alkyl, aralkyl or aryl; and R20 is selected from alkyl, substituted alkyl, a polyether moiety, carboxyl, substituted carboxyl, carbamate, substituted carbonate, carbonyloxy, alkoxy, substituted alkoxy, haloalkyl, halogen, nitro, amino, aryloxy, cyano, hydroxyl, or sulfonyl.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 23, 2014
    Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of the University of Oregon
    Inventors: Darren W. Johnson, Calden Carroll, Michael M. Haley, Jeff Engle
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 8796175
    Abstract: The invention relates to the use of at least one compound selected from the class of the sulphoximines for enhancing plants' intrinsic defenses and/or for improving plant growth and/or for enhancing the resistance of plants to plant diseases which are caused by fungi, bacteria, viruses, MLOs (mycoplasma-like organisms) and/or RLOs (rickettsia-like organisms), and/or for enhancing the resistance of plants to abiotic stress factors.
    Type: Grant
    Filed: August 17, 2009
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Wolfgang Thielert, Heike Hungenberg
  • Patent number: 8785649
    Abstract: An object of the present invention is to provide a novel fungicide having an excellent fungicidal activity. The compound used as the fungicide of the present invention is an ethynylphenylamidine compound or a salt thereof, the compound being represented by Formula (1): wherein R1 and R2 are each hydrogen or C1-12 alkyl, or R1 and R2 may be bonded together to form C1-7 alkylene; R3 is hydrogen or C1-4 alkylthio; R4, R5, R6, and R7 are each hydrogen, halogen, etc.; and R8 is hydrogen, C1-20 alkyl, C3-8 cycloalkyl, C1-4 haloalkyl, phenyl, a heterocyclic group, or —(CH2)n-Si(R9)(R10)(R11) wherein R9, R10, and R11 are each C1-6 alkyl, and n is an integer of 0 or 1.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: July 22, 2014
    Assignee: Otsuka Agritechno Co., Ltd.
    Inventors: Satoru Masumoto, Hitoshi Mutsutani, Sachi Kimura
  • Publication number: 20140179878
    Abstract: A polyimide including a structure shown as Formula II is provided, wherein X is halogen, A1 is selected from one of Formula 1 to Formula 18, and n is from 2 to 500,
    Type: Application
    Filed: December 25, 2012
    Publication date: June 26, 2014
    Applicant: TAIWAN TEXTILE RESEARCH INSTITUTE
    Inventors: Der-Jang Liaw, Wen-Hsiang Chen, Ying-Chi Huang, Bo-Cheng Tao
  • Patent number: 8742124
    Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: June 3, 2014
    Assignee: AstraZeneca AB
    Inventors: Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
  • Publication number: 20140138632
    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
  • Patent number: 8722895
    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: April 9, 2013
    Date of Patent: May 13, 2014
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Richard M. Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Patent number: 8722896
    Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: May 13, 2014
    Assignee: The Regents of the University of California
    Inventors: Qun-Yong Zhou, Jia-Da Li, Qi Huang
  • Patent number: 8648204
    Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: February 11, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Elisabetta Armani, Maurizio Delcanale
  • Publication number: 20140039181
    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
  • Publication number: 20140031398
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Application
    Filed: January 27, 2012
    Publication date: January 30, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Patent number: 8637674
    Abstract: The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: January 28, 2014
    Assignee: EWHA University-Industry Collaboration Foundation
    Inventors: Yun Soo Bae, Jee Hyun Lee, Mi Sun Seo, Soo Young Lee, Sun Choi, Kee In Lee, Hye Rin Bin
  • Patent number: 8637673
    Abstract: Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are hydrogenated to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A, R1 and R2 radicals are each as defined in the description:
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Norbert Lui, Stefan Antons
  • Patent number: 8623942
    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.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
  • Publication number: 20130331580
    Abstract: The present invention relates to a chemocatalytic liquid-phase process for the direct one-stage amination of alcohols to primary amines by means of ammonia in high yields using a catalyst system containing at least one transition metal compound and a xantphos ligand.
    Type: Application
    Filed: December 14, 2011
    Publication date: December 12, 2013
    Applicant: EVONIK DEGUSSA GmbH
    Inventors: Florian Klasovsky, Thomas Tacke, Jan Christoph Pfeffer, Thomas Haas, Matthias Beller, Andreas Martin, Jens Deutsch, Angela Koeckritz, Sebastian Imm, Juergen Haberland
  • Publication number: 20130330762
    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: Application
    Filed: June 3, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF CONNECTICUT
    Inventors: Ping Yan, Corey D. Acker, Leslie M. Loew