Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
  • Publication number: 20130245050
    Abstract: The present invention relates to the use of N-phenylethylpyrazole carboxamide derivatives or salts thereof for extended shelf life and storage stability of fruits and vegetables, to a method for extending shelf life or fruits and vegetables by applying N-phenylethylpyrazole carboxamide derivatives or salts thereof to the crops prior to the harvest of the fruits or vegetables.
    Type: Application
    Filed: August 15, 2011
    Publication date: September 19, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Heiko Rieck, Dominique Steiger, Peter Howard Davies, Sylvain Tafforeau, Lorianne Fought, George Hauley Musson, IV, Luk De Maeyer, Gilbert Labourdette, Helen Lachaise, Sebastian Hoffmann
  • Patent number: 8536215
    Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl or C1-C4haloalkyl; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4haloalkyl; R5 is hydrogen, halogen, C1-C4alkyl or C1-C4haloalkyl; G1 is a cyclohexenyl group which is mono- or polysubstituted by substituents selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, C3-C6cycloalkyl and phenyl; said cyclohexenyl group can form together with a C1-C4 alkylene group a bicyclic system which can be mono- or poly-substituted by substituents selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, C3-C6cycloalkyl and phenyl; are suitable for use as microbiocides.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: September 17, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Daniel Stierli, Harald Walter
  • Publication number: 20130237500
    Abstract: The present invention relates to novel (thio)carboxamides, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: November 14, 2011
    Publication date: September 12, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Juergen Benting, Philippe Desbordes, Stephanie Gary, Joerg Greul, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
  • Patent number: 8530461
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
  • Publication number: 20130231375
    Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: July 30, 2009
    Publication date: September 5, 2013
    Inventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
  • Patent number: 8524915
    Abstract: The invention relates to a process for the preparation of a compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III) reacting the halobenzyne of formula (III) so formed with (IV) wherein R1 and R2 are hydrogen or C1-C6alkyl; to (V), b) hydrogenating V in the presence of a metal catalyst to (VI), c) ozonising (VI) to (VII) d) converting (VII) in the presence of a phosphane and CCI4 or CHCI3 to (VIII) (VIII), and either e1) reacting VIII with NH3 in the presence of a catalyst to (IX) and f) reacting IX in the presence of a base with the compound of formula (X), to the compound of formula (I); or e2) reacting the compound of formula (VIII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with (Xa), to the compound of formula (I).
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: September 3, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Florian Schleth, Thomas Vettiger, Michael Rommel, Hans Tobler
  • Publication number: 20130225585
    Abstract: Disclosed is a pyrazole amide compound having fungicidal activity, with a structure shown by the general formula (I): Each of the substituents of the compound being defined as in the description. The compound of the present invention has fungicidal activity, and excellent prevention and controlling effects on diseases, such as cucumber downy mildew, corn rust, wheat powdery mildew, rice blast, etc., and in particular, a better prevention and controlling effect on cucumber downy mildew and corn rust. Also disclosed is a process for preparing the compound, a fungicidal composition containing the compound of general formula (I) and the use thereof in preventing and controlling disease in crops.
    Type: Application
    Filed: November 2, 2011
    Publication date: August 29, 2013
    Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATION
    Inventors: Changling Liu, Lizeng Wang, Zhinian Li, Xufeng Sun, Jie Lan, Lanhui Ren, Qiang Wu, Huiwei Chi
  • Publication number: 20130225833
    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 pyrazole-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: Application
    Filed: October 25, 2011
    Publication date: August 29, 2013
    Applicant: SOLVAY SA
    Inventor: Max Josef Braun
  • Patent number: 8519151
    Abstract: The invention relates to a process for the preparation of formula (I) which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III), wherein X is chloro or bromo; reacting the halobenzyne with a fulvene (IV), to a compound of formula (V) wherein X is chloro or bromo; b) hydrogenating V in the presence of a suitable metal catalyst to a compound of formula (VI) wherein X is chloro or bromo; and either c1) reacting the compound of formula VI with NH3 in the presence of a catalyst comprising palladium and at least one ligand to the compound of formula (VII); and d) reacting the compound of formula VII in the presence of a base with a compound of formula (VIII), to the compound of formula I; or c2 reacting the compound of formula (VI) in the presence of a copper catalyst and a ligand with the compound of formula (VIIIa), to the compound of formula (I).
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: August 27, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Denis Gribkov, Remo Stohler, Thomas Vettiger, Michael Rommel
  • Patent number: 8519152
    Abstract: The invention relates to a process for the preparation of the compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula (X), reacting the halobenzyne of formula X so formed with cyclopentadiene to (III), b) reacting III in the presence of an inert solvent with an oxidant to (IV), c) reacting IV in the presence of a Lewis acid and a hydride source to (V), d) reacting V in the presence of an oxidizing agent, a base and an inert solvent to (VI), e) converting VI in the presence of a phosphane and CCl4 or CHCl3 to (VII), and either f1) reacting VII with NH3 in the presence of a catalyst to the compound of formula (VIII); and g) reacting VIII in the presence of a base with a compound of formula (IX), to the compound of formula (I); or f2) reacting the compound of formula (VII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with the compound
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: August 27, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Raphael Dumeunier, Florian Schleth, Thomas Vettiger, Michael Rommel, Stephan Trah
  • Patent number: 8513244
    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: May 18, 2012
    Date of Patent: August 20, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Adam D. Hughes
  • Publication number: 20130210883
    Abstract: The invention provides a compound of formula (I) as defined herein that is useful in the treatment and prevention of a disorder such as cachexia, stroke, atherosclerosis, coronary artery disease, or diabetes and disorders and conditions associated therewith. The invention also provides a method of screening for lipase inhibitors using a compound of formula (I) and determining its lipase inhibitory activity. activity.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Inventors: Johannes Grillari, Rolf Breinbauer, Martina Schweiger, Matthias Romauch, Robert Zimmermann, Nicole Mayer, Elisabeth Schraml, Klaus Fortschegger, Regina Grillari
  • Publication number: 20130210864
    Abstract: The present invention relates to N-benzyl heterocyclic carboxamides derivatives or their thiocarboxamides derivatives, their process of preparation, their use as fungicide, particularly in the form of compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 15, 2013
    Inventors: Jurgen Benting, Pierre Cristau, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hendrik Helmke
  • Patent number: 8507694
    Abstract: The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: August 13, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Denis Gribkov, Adrian Müller, Martin Lager, Fanny Giordano
  • Publication number: 20130204011
    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: Application
    Filed: February 5, 2013
    Publication date: August 8, 2013
    Applicant: WESTFAELISCHE WILHELMS UNIVERSITAET MUENSTER
    Inventor: Westfaelische Wilhelms Universitaet Muenster
  • Publication number: 20130203832
    Abstract: The present invention relates to novel solid forms of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-isopropyl-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide, such as crystal modifications and hydrates, compositions comprising these novel solid forms and to the use thereof in the control of disease infestation in cultivated plants.
    Type: Application
    Filed: February 19, 2008
    Publication date: August 8, 2013
    Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION, INC.
    Inventors: Paul Edward Bonnett, Neil George, Ian Kevin Jones, Shailesh Shah
  • Publication number: 20130197239
    Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: BAYER CROPSCIENCE AG
  • Publication number: 20130197240
    Abstract: Disclosed is a process for producing an aminoadamantane carbamate derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. A process for producing an acid addition salt of a compound represented by the Formula (II): or a solvate of the acid addition salt, wherein R1 and R2 are each independently hydrogen, substituted or unsubstituted alkyl or the like; R3 and R4 are each independently hydrogen, substituted or unsubstituted alkyl or the like; and R5 and R6 are each independently hydrogen, halogen, carboxy, nitro, substituted or unsubstituted alkyl or the like; which comprises separating an acid addition salt of a compound represented by the Formula (II) or a solvate of the acid addition salt by adding an acid to a mixture of syn isomer and anti isomer of a compound represented by the Formula (I): wherein R1, R2, R3, R4, R5, and R6 are as defined above, in the presence of a solvent.
    Type: Application
    Filed: August 8, 2011
    Publication date: August 1, 2013
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Yutaka Nishino, Hideki Shimizu, Takayuki Tsuritani, Natsuko Suzuki, Mutsumi Takaki, Tatsuya Kobayashi, Hideaki Sakamoto
  • Patent number: 8492558
    Abstract: The present invention relates to a process for preparing 2-aminobiphenyls of the formula I in which n is 0, 1, 2 or 3, R1 is hydrogen, cyano or fluorine, and each R2 is independently selected from cyano, fluorine, C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-alkoxy, C1-C4-fluoroalkoxy, C1-C4-alkylthio and C1-C4-fluoroalkylthio. The invention also relates to a process for preparing pyrazolecarboxamides of such 2-aminobiphenyls.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: July 23, 2013
    Assignee: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Sebastian Peer Smidt
  • Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8481044
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-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: Grant
    Filed: February 16, 2012
    Date of Patent: July 9, 2013
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20130172367
    Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Application
    Filed: November 27, 2012
    Publication date: July 4, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: Bayer CropScience AG
  • Publication number: 20130165664
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoro-1-alkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.
    Type: Application
    Filed: February 19, 2013
    Publication date: June 27, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventor: Bayer Intellectual Property GmbH
  • Publication number: 20130165492
    Abstract: The present invention provides a compound, that is wherein Y, W, Z, R1, R2, R4, R5 and R6 are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.
    Type: Application
    Filed: December 21, 2012
    Publication date: June 27, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130165443
    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: Application
    Filed: August 23, 2012
    Publication date: June 27, 2013
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20130165666
    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: Application
    Filed: December 19, 2012
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130150358
    Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
    Type: Application
    Filed: February 4, 2013
    Publication date: June 13, 2013
    Applicant: HMI MEDICAL INNOVATIONS, LLC.
    Inventor: HMI MEDICAL INNOVATIONS, LLC.
  • Publication number: 20130143940
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 31, 2011
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
  • Patent number: 8450499
    Abstract: The invention relates to a process for the preparation of formula (I), which process comprises a) reacting the compound (II), with cyclopentadiene to (III); b) reacting this compound in the presence of an oxidant to the compound of formula (IV); c) hydrogenating this compound in the presence of a metal catalyst and an inert solvent under hydrogen atmosphere to the compound of formula (V); d) reacting this compound in the presence of a Brönsted acid followed by a reducing agent to the compound of formula (VI); e) reacting VI with a compound (VII), in the presence of a base to a compound of formula (VIII); f) converting the compound of formula VIII in the presence of an oxidizing agent to the compound of formula (IX); and g) reacting the compound of formula IX in the presence of triphenylphosphane/carbon tetrachloride or riphenylphosphane/bromotrichloromethane to the compound of formula I.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: May 28, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Raphael Dumeunier, Hans Tobler
  • Patent number: 8449890
    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: Grant
    Filed: February 16, 2012
    Date of Patent: May 28, 2013
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20130131321
    Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a
    Type: Application
    Filed: August 3, 2011
    Publication date: May 23, 2013
    Applicant: GRAFFINITY PHARMACEUTICALS GMBH
    Inventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
  • Publication number: 20130131119
    Abstract: The present invention relates to fungicidal N-[(het)arylethyl)] pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, 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: Application
    Filed: June 1, 2011
    Publication date: May 23, 2013
    Inventors: Jurgen Benting, Christoph Braun, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Thomas Knobloch, Ruth Meissner, Ulrike Wachendorf-Neumann, Lothar Willms
  • Publication number: 20130131124
    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: Application
    Filed: June 1, 2011
    Publication date: May 23, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Publication number: 20130123322
    Abstract: The present invention relates to fungicidal benzocycloalkene carboxamides or their thiocarboxamide derivatives of formula (I), 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: Application
    Filed: July 19, 2011
    Publication date: May 16, 2013
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Ulrike Wachendorff-neumann
  • Publication number: 20130123510
    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: Application
    Filed: July 22, 2011
    Publication date: May 16, 2013
    Applicant: SOLVAY SA
    Inventors: Max Josef Braun, Janis Jaunzems
  • Patent number: 8440854
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Melean Visnick
  • Patent number: 8436037
    Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula III wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: May 7, 2013
    Assignee: Syngenta Limited
    Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi, Fanny Giordano, Martin Zeller, Gottfried Seifert, Shailesh Shah, Neil George, Ian Jones, Paul Bonnett
  • Patent number: 8436191
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 7, 2013
    Assignee: Bayer CropScience AG
    Inventors: Sergii Pazenok, Norbert Lui, Marc Kosten, Guenter Bartels
  • Publication number: 20130109863
    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: Application
    Filed: December 17, 2012
    Publication date: May 2, 2013
    Applicant: Janssen Pharmaceutica N.V.
    Inventor: Janssen Pharmaceutica N.V.
  • Patent number: 8431718
    Abstract: The present invention relates to a novel process for the preparation of 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl halides and the intermediates occurring in this process, ethyl 5-chloro-1-methyl-3-difluoromethyl-1H-pyrazole-4-carboxylate and ethyl 5-fluoro-1-methyl-3-difluoromethyl-1H-pyrazole-4-carboxylate.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: April 30, 2013
    Assignee: Bayer CropScience AG
    Inventors: Sergii Pazenok, Norbert Lui, Stephanie Gary
  • Patent number: 8431609
    Abstract: A process for preparation of Pyrazole derivatives adapted for one pot reaction involving the use of a pyclizing agent and involving the step of amidation in the presence of a catalyst. The steps for isolation and purification of found Pyrazole derivatives are also disclosed.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: April 30, 2013
    Inventors: Darmesh Mahendrabhai Shah, Guruprasad Wader
  • Publication number: 20130102790
    Abstract: The present invention relates to N-cycloalkyl-N-bicyclicmethylene-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group, T represents O or S, Z1 represents a C3-C7-cycloalkyl group, X represents N or a CZ7 and Y1, Y2, Z2, Z3, L1 and L2 represent various substituents. Their process of preparation, the preparation of intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions are also disclosed.
    Type: Application
    Filed: December 13, 2012
    Publication date: April 25, 2013
    Inventors: Jurgen BENTING, Peter DAHMEN, Philippe DESBORDES, Stephanie GARY, Pierre GENIX, Benoit HARTMANN
  • Publication number: 20130101684
    Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.
    Type: Application
    Filed: April 15, 2011
    Publication date: April 25, 2013
    Applicant: Chromocell Corporation
    Inventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
  • Patent number: 8426471
    Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, and R4 are as defined herein.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: April 23, 2013
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Publication number: 20130096162
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Publication number: 20130096174
    Abstract: A plant disease control composition comprising a carboxamide compound represented by formula (I) whose enantiomer ratio R form/S form of the carboxamide compound is 80/20 or more has an excellent plant disease controlling activity.
    Type: Application
    Filed: June 20, 2011
    Publication date: April 18, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuichi Matsuzaki, Hiroshi Sakaguchi
  • Publication number: 20130090479
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.
    Type: Application
    Filed: July 3, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Philip Collier
  • Patent number: 8415274
    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: September 28, 2004
    Date of Patent: April 9, 2013
    Assignee: Bayer CropScience AG
    Inventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
  • Patent number: 8410157
    Abstract: The present invention relates to N-cycloalkyl-benzyl-thiocarboxamide or N-cycloalkyl-benzyl-N-substituted-carboximidamide amide derivatives of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl; T represents S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl and Z2; Z3, X and n represent various substituents; their process of preparation; their use as fungicide active agents, 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: July 31, 2008
    Date of Patent: April 2, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Jean-Pierre Vors
  • Publication number: 20130079302
    Abstract: The present invention relates to fungicidal N-[(het)arylalkyl)]pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, 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: Application
    Filed: June 1, 2011
    Publication date: March 28, 2013
    Inventors: Jurgen Benting, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Ruth Meissner, Ulrike Wachendorff-Neumann