1,2,4-triazoles (including Hydrogenated) Patents (Class 514/383)
  • Patent number: 10301287
    Abstract: The invention relates to solid forms of cenicriviroc mesylate, methods of their preparation, pharmaceutical compositions thereof and methods of their use.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: May 28, 2019
    Assignee: Tobira Therapeutics, Inc.
    Inventors: Pasit Phiasivongsa, Martin Ian Cooper, Emma Kay Sharp
  • Patent number: 10244755
    Abstract: Safeners for herbicides are suitable for increasing the microbicidal activity of fungicides.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: April 2, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Reiner Fischer, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Patent number: 10195194
    Abstract: A method of promoting remyelination in a subject in need thereof includes administering to the subject a therapeutically effective amount of at least one (1,3) Diazole compound, wherein the therapeutically effective amount is the amount effective to induce endogenous oligodendrocyte precursor cell (OPC) differentiation in the subject's central nervous system.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: February 5, 2019
    Assignee: Case Western Reserve University
    Inventors: Paul Tesar, Fadi J. Najm, Robert H. Miller
  • Patent number: 10188100
    Abstract: A matrix composition capable of forming an emulsion/micro-emulsion comprising an emulsifiable matrix, essentially free of alkyl pyrrolidone and alkoxylated alcohol, comprising: (i) a long chain substituted amide; (ii) a surface active agent; and (iii) optionally, an organic diluent.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: January 29, 2019
    Inventors: Kolazi S. Narayanan, Domingo Jon, Jayanti V. Patel
  • Patent number: 10183915
    Abstract: Disclosed are two axially chiral isomers and pharmaceutically available salts thereof, preparation method therefor, and pharmaceutical use of the two axially chiral isomers or pharmaceutical compositions thereof.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: January 22, 2019
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Jianfei Wang, Jing Zhang, Long Zhang, Yang Zhang, Jian Li, Shuhui Chen
  • Patent number: 10071971
    Abstract: The present invention relates to compounds of the formula I wherein the variables are defined in the description and claims, their preparation and uses thereof.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: September 11, 2018
    Assignee: BASF SE
    Inventors: Wassilios Grammenos, Ian Robert Craig, Nadege Boudet, Bernd Mueller, Jochen Dietz, Erica May Cambeis, Jan Klaas Lohmann, Thomas Grote, Egon Haden, Ana Escribano Cuesta
  • Patent number: 10071966
    Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: September 11, 2018
    Assignees: LUDWIG-MAXIMALIANS-UNIVERSITAT MUNCHEN, MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V.
    Inventors: Armin Giese, Uwe Bertsch, Hans Kretzschmar, Matthias Habeck, Thomas Hirschberger, Paul Tavan, Christian Griesinger, Andrei Leonov, Sergey Ryazanov, Petra Frick, Markus Geissen, Martin H. Groschup, Jens Wagner
  • Patent number: 10045968
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atom; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: August 14, 2018
    Assignee: TOBIRA THERAPEUTICS, INC.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
  • Patent number: 10028958
    Abstract: Methods, compounds and kits relating to treating cancer, reducing kinase inhibitor or resistance, and reducing or preventing diminished ectodomain shedding are described.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: July 24, 2018
    Assignee: Massachusetts Institute of Technology
    Inventors: Miles Aaron Miller, Madeleine Oudin, Aaron Samuel Meyer, Frank B. Gertler, Linda G. Griffith, Douglas A. Lauffenburger
  • Patent number: 10017679
    Abstract: The present invention relates to the field of reagents for oil and gas wells, and discloses a plugging agent for improving bearing capacity and a preparation method of the plugging agent, wherein, the plugging agent contains water, bridging granules, packing granules, and a cementing material, and, based on 100 parts by weight of water, the content of the bridging granules is 3-15 parts by weight, the content of the packing granules is 5-23 parts by weight, and the content of the cementing material is 4-11 parts by weight. The plugging agent in the present invention can improve the bearing capacity of the formation during well plugging, is applicable to shielded temporary plugging against serious leakage loss during extra-deep well drilling, has efficient and quick plugging performance, and is especially applicable to plugging against serious leakage loss in a formation where the well depth is greater than 3,000 m and conventional plugging agents can't attain a satisfactory plugging effect.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: July 10, 2018
    Assignee: Southwest Petroleum University
    Inventors: Pingya Luo, Dachuan Liang, Pingquan Wang, Mingyi Deng, Jinjun Huang, Yang Bai
  • Patent number: 9956205
    Abstract: Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: May 1, 2018
    Assignee: Ardea Biosciences, Inc.
    Inventors: Laszlo R. Treiber, Irina Zamansky, Jean-Luc Girardet
  • Patent number: 9943082
    Abstract: The present invention relates to novel mixtures, to processes for preparing these compounds, to compositions comprising these mixtures, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and for enhancing plant health.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: April 17, 2018
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Peter Dahmen, Heiko Rieck, Christophe DuBost
  • Patent number: 9861615
    Abstract: The present invention relates to methods and pharmaceutical compositions for the treatment of beta-thalassemias. In particular, the present invention relates to an XPO1 inhibitor for use in a method for treating beta-thalassemia in a subject in need thereof.
    Type: Grant
    Filed: November 28, 2014
    Date of Patent: January 9, 2018
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), Universite Paris Decartes, Assistance Publique-Hopitaux de Paris (APHP), Fondation Imagine, Centre National de la Recherche Scientifique (CNRS)
    Inventors: Olivier Hermine, Flavia Guillem, Jean-Benoit Arlet, Genevieve Courtois
  • Patent number: 9730439
    Abstract: A preformed concentrate, capable of forming emulsion/micro-emulsion upon dilution with water, for providing peripheral desiccating effect on leaves/crops comprising: (i) a water insoluble film forming polymer; (ii) a long chain substituted amide; and (iii) an oil soluble surfactant.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: August 15, 2017
    Assignee: ISP INVESTMENTS LLC
    Inventor: Kolazi S. Narayanan
  • Patent number: 9693997
    Abstract: The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: July 4, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Joseph Anthony Bilotta, Zhi Chen, Feng Chi, Elbert Chin, Qingjie Ding, Shawn David Erickson, Stephen Deems Gabriel, Nan Jiang, Buelent Kocer, Eric Mertz, Jean-Marc Plancher, Robert J. Weikert, Jing Zhang, Qiang Zhang
  • Patent number: 9655362
    Abstract: A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the following formula or its salt: wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2? is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2? is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2? and R2? optionally form a condensed ring containing an oxygen atom and (b) at least one other fungicide.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: May 23, 2017
    Assignee: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Hisaya Nishide, Shigeyuki Nishimura, Shigeru Mitani, Koji Minamida, Fumio Kanamori, Munekazu Ogawa, Shigehisa Kanbayashi, Toyoshi Tanimura, Koji Higuchi, Hidemasa Kominami, Tomohiro Okamoto, Akihiro Nishimura
  • Patent number: 9635856
    Abstract: The present invention provides a method for producing a co-crystal including thiophanate-methyl and a triazole-based compound such as tebuconazole and a method for producing an agricultural and horticultural chemical preparation using the co-crystal as a raw material. As one example, the agricultural and horticultural chemical preparation can be obtained by a method including the steps of obtaining a sol including a co-crystal by stirring a suspension including thiophanate-methyl, a triazole compound such as a tebuconazole, a surfactant, a defoaming agent and water at a mixing degree of 0.1-1.0 while holding the temperature of the suspension at 60° C.; and adding auxiliary components such as silica, calcium carbonate and the like to the sol.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: May 2, 2017
    Assignee: Nippon Soda Co., Ltd.
    Inventor: Satoru Yamamura
  • Patent number: 9603365
    Abstract: The present invention provides a method for producing a co-crystal including thiophanate-methyl and a triazole-based compound such as tebuconazole and a method for producing an agricultural and horticultural chemical preparation using the co-crystal as a raw material. As one example, the agricultural and horticultural chemical preparation can be obtained by a method including the steps of obtaining a sol including a co-crystal by stirring a suspension including thiophanate-methyl, a triazole compound such as a tebuconazole, a surfactant, a defoaming agent and water at a mixing degree of 0.1-1.0 while holding the temperature of the suspension at 60° C.; and adding auxiliary components such as silica, calcium carbonate and the like to the sol.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: March 28, 2017
    Assignee: Nippon Soda Co., Ltd.
    Inventor: Satoru Yamamura
  • Patent number: 9586970
    Abstract: The present invention relates to compounds of formula (I), wherein A, B, R1 and R2 are as defined herein before useful for the treatment of psychiatric disorders.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: March 7, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Alexander Flohr
  • Patent number: 9560847
    Abstract: A stable matrix emulsion concentrate of a biocide, e.g. 3-iodopropynyl-2-butyl carbamate (IPBC) and/or a triazole fungicide, and stable aqueous and/or organic solvent formulations thereof, i.e. dilutable in water and/or an organic solvent are provided, which are particularly useful for treating wood products to provide protection against microorganisms and insects.
    Type: Grant
    Filed: November 17, 2004
    Date of Patent: February 7, 2017
    Assignee: ISP INVESTMENTS LLC
    Inventors: Kolazi S. Narayanan, Xianbin Liu, Karen Winkowski, Jayanti Patel
  • Patent number: 9556143
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: December 1, 2014
    Date of Patent: January 31, 2017
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • Patent number: 9447082
    Abstract: The invention discloses optically active compounds of Formula (1a) or Formula (1b), wherein R1 and R2 are independently selected from the group consisting of hydrogen and a halogen selected from the group consisting of fluorine, chlorine, bromine, and iodine; and wherein (a) R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group having a linear or branched chain having 1 to 20 carbon atoms, or (b) R3 and R4 together form a cycloalkyl ring having 3 to 10 carbon atoms fused to the thiophene ring; and wherein R5 is CN or COOR?, where R? is methyl or ethyl. The compounds of Formula (1a) or Formula (1b) may be used in pharmaceutical compositions for treating fungal infections.
    Type: Grant
    Filed: April 29, 2014
    Date of Patent: September 20, 2016
    Assignees: FDC Limited, Council of Scientific Industrial Research
    Inventors: Hanumant Bapurao Borate, Sangeshwer Prabhakar Sawargave, Subhash Prataprao Chavan, Mohan Anand Chandavarkar, Ramakrishnan Ramacahndran Iyer, Amit Chandrakant Tawte, Deepali Damodar Rao
  • Patent number: 9370505
    Abstract: The invention relates to low-dose pharmaceutical compositions comprising the aromatase inhibitor 4,4?-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, as the active ingredient in a suitable carrier. The present invention also relates to a process for their preparation and to their use as therapeutic agents.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: June 21, 2016
    Assignee: Mereo BioPharma 2 Limited
    Inventors: Ann Taylor, Lloyd B. Klickstein, Jeewan Thakur
  • Patent number: 9295259
    Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkoxy-3-methyl-butyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 29, 2016
    Assignee: BASF SE
    Inventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
  • Patent number: 9283209
    Abstract: Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: March 15, 2016
    Assignee: NOVARTIS AG
    Inventors: Indrajit Ghosh, Jia-Ai Zhang
  • Patent number: 9265255
    Abstract: The present invention relates to novel active compound combinations which include of the insecticidally active compounds of the formula (I) in combination with fungicidally active compounds (II) and are highly suitable for controlling unwanted animal pests, such as insects, and unwanted phytopathogenic fungi.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: February 23, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Christian Funke, Heike Hungenberg, Rüdiger Fischer
  • Patent number: 9253983
    Abstract: In order to provide a compound that shows a strong effect on controlling a plant disease, a triazole compound of the present invention (i) is a compound in which —OH group, —R2 group, and CH2—Ar group are bonded in cis configuration with a cyclopentane, (ii) is (?)-enantiomer or (+) enantiomer, and (iii) is represented by Formula (I): (wherein R1 represents an alkyl group; R2 represents a haloalkyl group; and Ar represents a substituted/unsubstituted aromatic hydrocarbon group or a substituted/unsubstituted aromatic heterocyclic group.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: February 9, 2016
    Assignee: KUREHA CORPORATION
    Inventors: Taiji Miyake, Nobuyuki Araki, Toru Yamazaki
  • Patent number: 9205086
    Abstract: A pharmaceutical combination comprising an EGFR inhibitor and an Hsp90 inhibitor according to the following formulae (I) or (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof using pharmaceutical combinations disclosed herein.
    Type: Grant
    Filed: April 19, 2011
    Date of Patent: December 8, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Ronald K. Blackman, Kevin Paul Foley, David Proia
  • Patent number: 9179677
    Abstract: A fungicidal mixture comprising (1) 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxy-propyl]-2,4-dihydro-[1,2,4]-triazole-3-thione (prothioconazole) of the formula I or a salt or adduct thereof and at least one further fungicide or a salt or adduct thereof selected from the group consisting of (2) fenpropimorph of the formula II and (3) tridemorph of the formula III n=10, 11, 12 (60-70%) or 13 and (4) fenpropidin of the formula IV in a synergistically effective amount is described.
    Type: Grant
    Filed: February 26, 2003
    Date of Patent: November 10, 2015
    Assignee: BASF AKTIENGESELLSCHAFT
    Inventors: Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, V. James Spadafora, Thomas Christen
  • Patent number: 9175009
    Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: November 3, 2015
    Assignee: GENENTECH, INC.
    Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
  • Patent number: 9108933
    Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating c-Met associated cancers, in a subject in need thereof.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: August 18, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Zhenjian Du, Kevin Paul Foley
  • Patent number: 9090569
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: October 23, 2009
    Date of Patent: July 28, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
  • Publication number: 20150148308
    Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Tatsuya Suzuki, Atsushi Iwata, Yoshihiko Nokura
  • Patent number: 9040570
    Abstract: Provided are methods of treating or preventing a fungal infection in a subject. The methods comprise selecting a subject with or at risk of developing a fungal infection and administering to the subject a therapeutically effective amount of toremifene and fluconazole or derivatives thereof.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: May 26, 2015
    Assignee: University of Rochester
    Inventor: Damian J. Krysan
  • Publication number: 20150133509
    Abstract: The present invention provides a tree trunk injection agent whereby pathogenic fungi and/or pests in trees can be effectively controlled merely by a short-time application in a low chemical dose, and a method for controlling tree diseases using the tree trunk injection agent. According to one embodiment of the present invention, the tree trunk injection agent is obtained by adding, to an aqueous solution of an insecticidal component such as acetamiprid, a hardly soluble fungicidal component such as thiophanate-methyl so as to suspend the hardly soluble fungicidal component, wherein a particle size based on 50% volume of the fungicidal component is 4 ?m or less, or adding thereto at least one fungicidal component selected from a group consisting of triflumizole and metconazole.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 14, 2015
    Applicant: NIPPON SODA CO., LTD.
    Inventors: Takahiro Maekawa, Yasuhiro Omori
  • Publication number: 20150133500
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20150126363
    Abstract: The present invention provides a composition comprising a pesticide and a copolymer, which contains in polymerized form acrylic acid and/or methacrylic acid (monomer A); a mono C12-C22 alkyl terminated poly(C2-6 alkylene glycol)(meth)acrylate (monomer B); and a C1-C8 alkyl(meth)acrylate (monomer C). Further on, it provides a process for preparing said composition by contacting the pesticide and the copolymer; a method for controlling phytopathogenic fungi and/or unwanted plant growth and/or unwanted insect or mite infestation and/or for regulating the growth of plants, wherein said composition is caused to act on the respective pests, their habitat or the plants to be protected from the respective pest, to the soil and/or to unwanted plants and/or the crop plants and/or their habitat; and a plant propagation material comprising said composition.
    Type: Application
    Filed: March 22, 2013
    Publication date: May 7, 2015
    Inventors: Murat Mertoglu, Ann-Kathrin Marguerre, Vandana Kurkal-Siebert, Son Nguyen-Kim
  • Publication number: 20150126467
    Abstract: The disclosure relates to use of alginate oligomers to enhance the effects of antifungal agents. The invention provides a method to improve the efficacy of an antifungal agent against a fungus, said method comprising using said antifungal agent together with an alginate oligomer. The fungus may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antifungal agent in treating a subject infected, suspected to be infected, or at risk of infection, with a fungus. In another aspect the method can be used to combat fungal contamination of a site e.g., for disinfection and cleaning purposes.
    Type: Application
    Filed: September 14, 2012
    Publication date: May 7, 2015
    Applicant: AlgiIPharma AS
    Inventors: Edvar Onsøyen, Arne Dessen, David William Thomas, Katja Etel Hill, Hàvard Sletta, Anne Tøndervik, Geir Klinkenberg, Rolf Myrvold
  • Publication number: 20150126499
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20150126436
    Abstract: The present invention provides a method of treatment of Scedosporium spp.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: BIODIEM LIMITED
    Inventors: Julie Phillips, Tania Sorrell, Sharon Chen
  • Publication number: 20150126569
    Abstract: A quaternary fungicide mixture for controlling diseases of turfgrass and/or ornamentals.
    Type: Application
    Filed: August 13, 2014
    Publication date: May 7, 2015
    Inventors: Allan S. LAS, Jerry L. CORBETT, Paul R. MOORE
  • Patent number: 9023483
    Abstract: The present invention provides a method of protecting wood or other celiulosic material from decay by copper-tolerant fungi, and wood preservative formulations for use in the same. The wood preservative formulations comprise a biocidal metal compound, a 1,2,4-triazole and a didecyl quaternary ammonium cation. Didecyldimethyl quaternary ammonium compounds are particularly preferred.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: May 5, 2015
    Assignee: Arch Timber Protection Limited
    Inventors: Craig Andrew Mars, David Grindon Cantrell, Kevin Hughes, Andrew Stewart Hughes
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20150112116
    Abstract: Provided herein are methods comprising providing a tyrosine derivative and a solid particulate material (and, optionally, melanin) and applying force to said tyrosine derivative and said solid particulate material for a time and under conditions effective to impregnate at least one of said tyrosine derivative and said solid particulate material with the other of said tyrosine derivative and said solid particulate material. The invention also provides compositions comprising at least one of a tyrosine derivative impregnated with a solid particulate material and a solid particulate material impregnated with a tyrosine derivative.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 23, 2015
    Inventor: STEVEN HOFFMAN
  • Publication number: 20150111893
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
  • Publication number: 20150110773
    Abstract: Methods and kits for GPP-targeting, e.g., for the treatment of oncogenic Kras-associated cancers, and methods for determining the efficacy of those methods are provided.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 23, 2015
    Inventors: Alec C. Kimmelman, Jaekyoung Son, Lewis Cantley, Costas A. Lyssiotis
  • Patent number: 9012489
    Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: April 21, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Barbara Bertani, Marco Ferrara, Iain Lingard, Rocco Mazzaferro, Holger Rosenbrock
  • Publication number: 20150105437
    Abstract: A process for the preparation of random radical copolymers which comprises a) at least one olefinically unsaturated sulfonic acid of the formula (I), where n is 0 to 10; X is O or NR5; R1 is hydrogen or methyl; R2, R3 independently of one another are hydrogen or C1- to C6-alkyl and R5 is hydrogen, alkyl, aryl, alkylaryl, arylalkyl, alkoxyalkyl, aryloxyalkyl, alkoxyaryl, hydroxyalkyl, (di)alkylaminoalkyl, (di)alkylaminoaryl, (di)arylaminoalkyl, alkylarylaminoalkyl or alkylarylaminoaryl, it being possible for the aryl radicals to be monosubstituted or polysubstituted, salts thereof or mixtures of acid and salts and b) at least two structurally different olefinically unsaturated monomers of the formula (II), where Y is O or NR7; R5 is hydrogen or methyl; R6 is alkyl, hydroxyalkyl, (di)alkylaminoalkyl or (di)alkylaminoaryl and R7 is hydrogen, alkyl, aryl, alkylaryl, arylalkyl, alkoxyalkyl, aryloxyalkyl, alkoxyaryl, hydroxyalkyl, (di)alkylaminoalkyl, (di)alkylaminoaryl, (di)arylaminoalkyl, alkyl
    Type: Application
    Filed: October 21, 2014
    Publication date: April 16, 2015
    Inventors: Holger TUERK, Cedric DIELEMAN, Hans-Guenter BOHRMANN, Sebastian KOLTZENBURG