Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
  • Patent number: 10556867
    Abstract: The present invention relates to a novel process for preparing 3-fluoroalkyl-5-pyrazolecarboxylates from ketimines and oxalic acid derivatives which can be further transformed into 3-fluoroalkyl-5-pyrazolecarboxylic acids.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: February 11, 2020
    Assignees: BAYER CROPSCIENCE AKTIENGESELLSCHAFT, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Sergii Pazenok, Jean-Pierre Vors, Frédéric R. LeRoux, Etienne Schmitt
  • Patent number: 10246407
    Abstract: The present invention relates to a novel process for preparing substituted biphenylamides of the general formula (V) characterized in that anilides of the formula (II) in a solvent other than tetrahydrofuran, are reacted with an organoboron compound of the formula (III) in the presence of a catalyst system consisting of a ruthenium catalyst, an activator, an oxidizing agent and a metal triflate.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: April 2, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Thomas Himmler, Lars Rodefeld, Jonathan Hubrich, Lutz Ackermann
  • Patent number: 10125103
    Abstract: The present invention relates to a novel method for preparing 5-fluoro-1H-pyrazole-4-carbonyl fluorides by halogen exchange reaction of 5-chloro-1H-pyrazole-4-carbonyl chlorides with alkali metal fluorides, using non-polar solvents.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: November 13, 2018
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Sergii Pazenok, Hans Martin Thomas, Frank Volz
  • Patent number: 9926279
    Abstract: The present invention provides a process for the preparation of a compound of formula I: wherein R1 is C1-C4 haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 is methyl or ethyl; comprising reacting a compound of formula IV: wherein R1, R2 and R3 are as defined for the compound of formula I; with an alkylating agent in the presence of an amide.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: March 27, 2018
    Assignee: Syngenta Participations AG
    Inventors: Linhua Wang, Ritesh Bharat Sheth
  • Patent number: 9765033
    Abstract: The present invention describes a novel method for preparing 3,5-bis(fluoroalkyl)pyrazole derivatives.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: September 19, 2017
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Sergii Pazenok, Norbert Lui
  • Patent number: 9656964
    Abstract: The present invention relates to a process for the preparation of carboxamide derivatives of formula (I) R N O N N CF2H C H3F starting from 1-methyl-3-difluormethyl-.5-fluoro-1H-pyrazole-4-carbonyl halides in absence of an acid acceptor.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: May 23, 2017
    Inventors: Werner Lindner, Sergii Pazenok, Frank Volz
  • Patent number: 9656966
    Abstract: The present invention relates to a novel method for preparing 1-alkyl-3-difluoromethyl-5-fluor-1H-pyrazole-4-carbaldehydes or esters thereof of formula (I) by means of reductive dehalogenation, starting from 1-alkyl-3-chlorodifluoromethyl-5-fluoro-1H-pyrazole-4-carbaldehydes or esters thereof Formula (I)
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: May 23, 2017
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Norbert Lui, Sergii Pazenok
  • Patent number: 9617219
    Abstract: The present invention relates to solid forms of the fungicide of formula (I): compositions comprising the solid forms and methods of their use as fungicides.
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: April 11, 2017
    Assignee: Syngenta Participations AG
    Inventors: John Hone, Ian Kevin Jones, Neil George
  • Patent number: 9512081
    Abstract: The present invention relates to a novel process for preparing 3,5-bis(fluoroalkyl)pyrazole derivatives from ?,?-dihaloamines.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: December 6, 2016
    Assignees: BAYER CROPSCIENCE AKTIENGESELLSCHAFT, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Sergii Pazenok, Norbert Lui, Arnd Neeff, Winfried Etzel, Jean-Pierre Vors, Frederic R. Leroux, Gregory Landelle, Mark James Ford
  • Patent number: 9169233
    Abstract: The present invention relates to methods of initiating a reaction represented by scheme 1 wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: October 27, 2015
    Assignee: Syngenta Limited
    Inventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
  • Patent number: 9139507
    Abstract: The disclosure provides a process for the preparation of alkyl 3-difluoromethyl-1-methyl-1H-pyrazole-4-caboxylate and its analogs. The process includes a reaction workup method for Claisen condensation, wherein the enolate salt is acidified after removing remaining starting material and byproducts such as, ethanol and excessive ethyl acetate. The process also includes a method for completely drying alkyl difluoroacetoacetate and its analogs before use in the next step by reacting trialkyl orthoformate with the residual water. The process includes using Na2CO3 and/or K2CO3 to promote the ring-closure reaction to produce the alkyl 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylate. The process also includes effectively removing the regioisomer, alkyl 3-difluoromethyl-2-methyl-1H-pyrazole-4-caboxylate formed as a byproduct of the ring closure by a precipitation in a mixed solvent system and thereby eliminating the need for recrystallization of the final product.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: September 22, 2015
    Assignee: KINGCHEM LLC.
    Inventors: Zheqing Wang, Angang Wang, Yongcan Wang, Zhenwei Li
  • Patent number: 9051272
    Abstract: The invention relates to a process for the preparation of a compound of formula (I), wherein R1, R2 and R3 are as defined in claim 1, which process comprises a) adding a compound of formula (II), in the presence of an inert organic solvent to a mixture comprising an organic nitrite of formula (III) (R4—O—N?O (III)), wherein R4 is C1-C8alkyl, a compound of formula (IV), and an inert organic solvent; b) reacting the resulting compound of formula (V), with H2N—O—CH3 to the compound of formula (VII), c) reducing the compound of formula (VII) to the compound of formula (VIII), d) and reacting the compound of formula VIII with a compound of formula (IX), in which R* is halogen, hydroxy or C1-6 alkoxy, to the compound of formula (I).
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: June 9, 2015
    Assignee: Syngenta Participations AG
    Inventors: Daniel Stierli, Harald Walter, Michael Rommel, Reinhard Georg Hanreich, Martin Zeller, Thomas Vettiger, Tomas Smejkal
  • Patent number: 9040709
    Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Markus Jachmann, Takayuki Wakamatsu, Mitsuharu Anryu
  • Publication number: 20150141247
    Abstract: The present invention relates to novel 1-methyl-3-dihalogenomehtyl-5-halogenopyrazole(thio)biphenyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: May 21, 2015
    Inventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
  • Patent number: 9035071
    Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: May 19, 2015
    Assignee: Allergan, Inc.
    Inventors: Jussi J. Kangasmetsa, William R. Carling, Jose L. Martos, David F. Woodward, Jenny W. Wang
  • Publication number: 20150133658
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 15, 2014
    Publication date: May 14, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20150126748
    Abstract: The present invention relates to a novel method for preparing 1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful precursor for the preparation of fungicides, by means of reductive dehalogenation, starting from N-alkyl-3-haloalkyl-5-halopyrazolecarbaldehyde.
    Type: Application
    Filed: May 10, 2013
    Publication date: May 7, 2015
    Inventors: Sergii Pazenok, Norbert Lui, Thomas Norbert Mueller
  • Publication number: 20150119571
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20150119241
    Abstract: The present invention relates to novel 1-methyl-3-dihalogenomethyl-5-halogenopyrazole(thio)indanyl carbox-amides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Inventors: Pierre-Yves Coqueron, Simon Maechling, Mazen Es-Sayed, Pierre Wasnaire, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stéphane Brunet, Hélène Lachaise, Pierre Genix
  • Publication number: 20150119375
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
  • Publication number: 20150119242
    Abstract: The present invention relates to novel pyrazole(thio)tetrahydronaphthyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Simon Maechling, Mazen Es-Sayed, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
  • Publication number: 20150119243
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: Simon Maechling, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise, Pierre Genix
  • Patent number: 9018241
    Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: April 28, 2015
    Assignee: Janssen Pharmaceutica, NV
    Inventors: John R. Carson, James J. McNally
  • Patent number: 9012657
    Abstract: A method for producing a pyrazole compound of the general formula (5) includes reacting a 2-acyl-3-aminoacrylic acid ester of the general formula (1) with a hydrazine of the general formula (4) in the presence of a base where R1, R2, R3 and R4 each independently represent an alkyl group wherein R5 represents an alkyl group or an aryl group wherein R1, R4 and R5 have the same meanings as above. It is possible by this production method to produce the 1,3-disubstituted pyrazol-4-carboxylic acid ester at a high yield and selectivity and with less discoloration.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: April 21, 2015
    Assignee: Central Glass Company, Limited
    Inventors: Masamune Okamoto, Hideaki Imura, Naoto Takada
  • Publication number: 20150105252
    Abstract: Disclosed is a method for controlling the growth of undesired vegetation comprising contacting the vegetation or its environment with a herbicidally effective amount of a compound of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, R1, Q and J are as defined in the disclosure. Also disclosed is a method wherein the compound of Formula 1 (i.e. in a herbicidally effective amount) is comprised in a herbicidal composition further comprising at least one component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are compound of Formula 1 (including all stereoisomers), including N-oxides and salts thereof, their use as herbicides wherein A, R1, Q and J are as defined in the disclosure.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 16, 2015
    Inventor: THOMAS MARTIN STEVENSON
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 9006143
    Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
  • Publication number: 20150099766
    Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
  • Patent number: 8999956
    Abstract: The present invention relates to fungicidal N-[(het)arylalkyl)]pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogs, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: April 7, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jurgen Benting, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Ruth Meissner, Ulrike Wachendorff-Neumann
  • Patent number: 8993556
    Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: March 31, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
  • Patent number: 8993752
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: March 31, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Roland Gendron, Adam D. Hughes
  • Patent number: 8987318
    Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: March 24, 2015
    Assignee: Alexar Therapeutics, Inc.
    Inventor: Raju Mohan
  • Patent number: 8987470
    Abstract: A process for the manufacture of pyrazole-4-carboxamides, in particular, of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxamides which are useful as pharmaceuticals and agrochemicals. The carboxamides are prepared from the corresponding pyzole-4-carboxylic acid esters and appropriate amine in the presence of a base. The reaction is performed in a reaction medium which is essentially free of water; alternatively, the base is used in an amount equal to or greater than 0.25 equivalents per mole of amine.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: March 24, 2015
    Assignee: Solvay SA
    Inventor: Max Josef Braun
  • Patent number: 8981116
    Abstract: A process for the manufacture of an ester or the respective free acid of a 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acid of formula (I), wherein in such formula (I), Y is H, F or an alkyl group having from 1 to 12 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group or an aryl group; R1 is H or an organic residue; R2 is H or an organic residue. Such process comprises submitting a compound of formula (II) to a reduction reaction, wherein in such formula (II), Y is the same as defined for formula (I); X is Cl, Br or I; R1? is H or an organic residue; and R2? is H or an organic residue.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: March 17, 2015
    Assignee: Solvay SA
    Inventors: Max Josef Braun, Janis Jaunzems
  • Publication number: 20150057318
    Abstract: The invention relates to the use of succinate dehydrogenase SDH inhibitors (SDHIs), in particular bixafen, penflufen or fluopyram for controlling wood diseases in grape, to a method for treating plants or plant parts for controlling wood diseases in grape and to a method for controlling wood diseases in grape plants and plant parts, and in plants which grow from the seedlings, grafts and cuttings, by treating them with SDHIs.
    Type: Application
    Filed: February 19, 2013
    Publication date: February 26, 2015
    Applicants: BAYER CROPSCIENCE AG, BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Lucien Meunier, Gilbert Labourdette, Helene Lachaise
  • Publication number: 20150045372
    Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Patent number: 8946231
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20150018562
    Abstract: The invention relates to a process for the preparation of a compound of formula (I), wherein R1, R2 and R3 are as defined in claim 1, which process comprises a) adding a compound of formula (II), in the presence of an inert organic solvent to a mixture comprising an organic nitrite of formula (III) (R4—O—N?O (III)), wherein R4 is C1-C8 alkyl, a compound of formula (IV), and an inert organic solvent; b) reacting the resulting compound of formula (V), with H2N—O—CH3 to the compound of formula (VII), c) reducing the compound of formula (VII) to the compound of formula (VIII), d) and reacting the compound of formula VIII with a compound of formula (IX), in which R* is halogen, hydroxy or C1-6 alkoxy, to the compound of formula (I).
    Type: Application
    Filed: February 26, 2013
    Publication date: January 15, 2015
    Inventors: Daniel Stierli, Harald Walter, Michael Rommel, Reinhard Georg Hanreich, Martin Zeller, Thomas Vettiger, Tomas Smejkal
  • Publication number: 20150011779
    Abstract: The present invention relates to novel 3,5-bis(fluoroalkyl)pyrazole-4-carboxylic acid derivatives and to a process for preparing 3,5-bis(fluoroalkyl)pyrazole-4-carboxylic acid derivatives and 3,5-bis(fluoroalkyl)pyrazoles.
    Type: Application
    Filed: January 31, 2013
    Publication date: January 8, 2015
    Inventors: Sergii Pazenok, Norbert Lui, Jean-Pierre Vors, Frederic R. Leroux, Florence Giornal
  • Publication number: 20150005320
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 1, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Publication number: 20150005503
    Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
    Type: Application
    Filed: September 16, 2014
    Publication date: January 1, 2015
    Inventors: SIGRIDUR SOLEY KRISTJANSDOTTIR, RAFAEL SHAPIRO, MATTHEW RICHARD OBERHOLZER
  • Publication number: 20150005345
    Abstract: The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 1, 2015
    Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
  • Publication number: 20150005293
    Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: September 9, 2014
    Publication date: January 1, 2015
    Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
  • Patent number: 8921575
    Abstract: The present invention relates to O-CYCLOPROPYLCYCLOHEXYL-CARBOXANILIDES derivatives of formula (I); their process of preparation, their use as fungicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: December 30, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Joerg Nico Greul, Juergen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Publication number: 20140378474
    Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
  • Publication number: 20140378461
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
  • Publication number: 20140371240
    Abstract: The invention relates to compounds of the general formulae (I) and (II) in which the radicals A1, A2, A3, A4, M1, M2, M3, Q, R1, T, W1 and W2 have the meaning given in the description and to the use of the compounds for controlling animal pests. The invention furthermore relates to processes and intermediates for preparing the compounds of formula (I).
    Type: Application
    Filed: December 17, 2012
    Publication date: December 18, 2014
    Inventors: Michael Maue, Tobias Kapferer, Friedrich August Muehlthau, Olga Malsam
  • Patent number: 8912342
    Abstract: A method of synthesizing Pyrazoles by means of the oxidative conversion of Enamines with suitable N-containing carboxylic acid derivatives in the presence of copper ions and 2-picolinic acid derivatives is provided.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: December 16, 2014
    Assignee: Westfälische Wilhelms Universität Münster
    Inventors: Frank Glorius, Mamta Suri
  • Publication number: 20140364622
    Abstract: The present invention relates to a process for the enantioselective preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ((1S,4R)-9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide of formula Ib.
    Type: Application
    Filed: February 13, 2013
    Publication date: December 11, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventor: Tomas Smejkal