Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
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Publication number: 20130245050Abstract: 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: ApplicationFiled: August 15, 2011Publication date: September 19, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Heiko Rieck, Dominique Steiger, Peter Howard Davies, Sylvain Tafforeau, Lorianne Fought, George Hauley Musson, IV, Luk De Maeyer, Gilbert Labourdette, Helen Lachaise, Sebastian Hoffmann
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Patent number: 8536215Abstract: 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: GrantFiled: February 3, 2011Date of Patent: September 17, 2013Assignee: Syngenta Crop Protection LLCInventors: Daniel Stierli, Harald Walter
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Publication number: 20130237500Abstract: 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: ApplicationFiled: November 14, 2011Publication date: September 12, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Juergen Benting, Philippe Desbordes, Stephanie Gary, Joerg Greul, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
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Patent number: 8530461Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
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Publication number: 20130231375Abstract: 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: ApplicationFiled: July 30, 2009Publication date: September 5, 2013Inventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
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Patent number: 8524915Abstract: 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: GrantFiled: April 14, 2011Date of Patent: September 3, 2013Assignee: Syngenta Crop Protection LLCInventors: Florian Schleth, Thomas Vettiger, Michael Rommel, Hans Tobler
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Publication number: 20130225585Abstract: 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: ApplicationFiled: November 2, 2011Publication date: August 29, 2013Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATIONInventors: Changling Liu, Lizeng Wang, Zhinian Li, Xufeng Sun, Jie Lan, Lanhui Ren, Qiang Wu, Huiwei Chi
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Publication number: 20130225833Abstract: 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: ApplicationFiled: October 25, 2011Publication date: August 29, 2013Applicant: SOLVAY SAInventor: Max Josef Braun
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Patent number: 8519151Abstract: 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: GrantFiled: April 14, 2011Date of Patent: August 27, 2013Assignee: Syngenta Crop Protection LLCInventors: Denis Gribkov, Remo Stohler, Thomas Vettiger, Michael Rommel
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Patent number: 8519152Abstract: 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 compoundType: GrantFiled: April 14, 2011Date of Patent: August 27, 2013Assignee: Syngenta Crop Protection LLCInventors: Raphael Dumeunier, Florian Schleth, Thomas Vettiger, Michael Rommel, Stephan Trah
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Patent number: 8513244Abstract: 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: GrantFiled: May 18, 2012Date of Patent: August 20, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Adam D. Hughes
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Publication number: 20130210883Abstract: 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: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Inventors: Johannes Grillari, Rolf Breinbauer, Martina Schweiger, Matthias Romauch, Robert Zimmermann, Nicole Mayer, Elisabeth Schraml, Klaus Fortschegger, Regina Grillari
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Publication number: 20130210864Abstract: 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: ApplicationFiled: October 20, 2011Publication date: August 15, 2013Inventors: Jurgen Benting, Pierre Cristau, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hendrik Helmke
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Patent number: 8507694Abstract: 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: GrantFiled: July 7, 2010Date of Patent: August 13, 2013Assignee: Syngenta Crop Protection LLCInventors: Denis Gribkov, Adrian Müller, Martin Lager, Fanny Giordano
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Publication number: 20130204011Abstract: 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: ApplicationFiled: February 5, 2013Publication date: August 8, 2013Applicant: WESTFAELISCHE WILHELMS UNIVERSITAET MUENSTERInventor: Westfaelische Wilhelms Universitaet Muenster
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Publication number: 20130203832Abstract: 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: ApplicationFiled: February 19, 2008Publication date: August 8, 2013Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION, INC.Inventors: Paul Edward Bonnett, Neil George, Ian Kevin Jones, Shailesh Shah
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Publication number: 20130197239Abstract: 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: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: BAYER CROPSCIENCE AGInventor: BAYER CROPSCIENCE AG
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Publication number: 20130197240Abstract: 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: ApplicationFiled: August 8, 2011Publication date: August 1, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Yutaka Nishino, Hideki Shimizu, Takayuki Tsuritani, Natsuko Suzuki, Mutsumi Takaki, Tatsuya Kobayashi, Hideaki Sakamoto
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Patent number: 8492558Abstract: 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: GrantFiled: February 18, 2010Date of Patent: July 23, 2013Assignee: BASF SEInventors: Thomas Zierke, Volker Maywald, Sebastian Peer Smidt
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Publication number: 20130184279Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.Type: ApplicationFiled: December 18, 2012Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8481044Abstract: 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: GrantFiled: February 16, 2012Date of Patent: July 9, 2013Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Publication number: 20130172367Abstract: 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: ApplicationFiled: November 27, 2012Publication date: July 4, 2013Applicant: BAYER CROPSCIENCE AGInventor: Bayer CropScience AG
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Publication number: 20130165664Abstract: 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: ApplicationFiled: February 19, 2013Publication date: June 27, 2013Applicant: Bayer Intellectual Property GmbHInventor: Bayer Intellectual Property GmbH
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Publication number: 20130165492Abstract: 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: ApplicationFiled: December 21, 2012Publication date: June 27, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Publication number: 20130165443Abstract: 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: ApplicationFiled: August 23, 2012Publication date: June 27, 2013Inventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20130165666Abstract: 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: ApplicationFiled: December 19, 2012Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130150358Abstract: 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: ApplicationFiled: February 4, 2013Publication date: June 13, 2013Applicant: HMI MEDICAL INNOVATIONS, LLC.Inventor: HMI MEDICAL INNOVATIONS, LLC.
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Publication number: 20130143940Abstract: 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: ApplicationFiled: August 31, 2011Publication date: June 6, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
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Patent number: 8450499Abstract: 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: GrantFiled: April 14, 2011Date of Patent: May 28, 2013Assignee: Syngenta Crop Protection LLCInventors: Raphael Dumeunier, Hans Tobler
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Patent number: 8449890Abstract: 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: GrantFiled: February 16, 2012Date of Patent: May 28, 2013Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
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Publication number: 20130131321Abstract: 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; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
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Publication number: 20130131119Abstract: 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: ApplicationFiled: June 1, 2011Publication date: May 23, 2013Inventors: 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
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Publication number: 20130131124Abstract: 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: ApplicationFiled: June 1, 2011Publication date: May 23, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
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Publication number: 20130123322Abstract: 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: ApplicationFiled: July 19, 2011Publication date: May 16, 2013Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Ulrike Wachendorff-neumann
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Publication number: 20130123510Abstract: 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: ApplicationFiled: July 22, 2011Publication date: May 16, 2013Applicant: SOLVAY SAInventors: Max Josef Braun, Janis Jaunzems
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Patent number: 8440854Abstract: 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: GrantFiled: January 23, 2012Date of Patent: May 14, 2013Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Melean Visnick
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Patent number: 8436037Abstract: 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: GrantFiled: August 5, 2011Date of Patent: May 7, 2013Assignee: Syngenta LimitedInventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi, Fanny Giordano, Martin Zeller, Gottfried Seifert, Shailesh Shah, Neil George, Ian Jones, Paul Bonnett
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Patent number: 8436191Abstract: 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: GrantFiled: November 19, 2010Date of Patent: May 7, 2013Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui, Marc Kosten, Guenter Bartels
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Publication number: 20130109863Abstract: 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: ApplicationFiled: December 17, 2012Publication date: May 2, 2013Applicant: Janssen Pharmaceutica N.V.Inventor: Janssen Pharmaceutica N.V.
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Patent number: 8431718Abstract: 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: GrantFiled: April 22, 2011Date of Patent: April 30, 2013Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui, Stephanie Gary
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Patent number: 8431609Abstract: 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: GrantFiled: April 30, 2007Date of Patent: April 30, 2013Inventors: Darmesh Mahendrabhai Shah, Guruprasad Wader
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Publication number: 20130102790Abstract: 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: ApplicationFiled: December 13, 2012Publication date: April 25, 2013Inventors: Jurgen BENTING, Peter DAHMEN, Philippe DESBORDES, Stephanie GARY, Pierre GENIX, Benoit HARTMANN
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Publication number: 20130101684Abstract: 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: ApplicationFiled: April 15, 2011Publication date: April 25, 2013Applicant: Chromocell CorporationInventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
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Patent number: 8426471Abstract: 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: GrantFiled: July 13, 2012Date of Patent: April 23, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Publication number: 20130096162Abstract: 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: ApplicationFiled: December 3, 2012Publication date: April 18, 2013Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20130096174Abstract: 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: ApplicationFiled: June 20, 2011Publication date: April 18, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuichi Matsuzaki, Hiroshi Sakaguchi
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Publication number: 20130090479Abstract: 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: ApplicationFiled: July 3, 2012Publication date: April 11, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Philip Collier
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Patent number: 8415274Abstract: 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: GrantFiled: September 28, 2004Date of Patent: April 9, 2013Assignee: Bayer CropScience AGInventors: Ulrike Wachendorff-Neumann, Peter Dahmen, Ralf Dunkel, Hans-Ludwig Elbe, Anne Suty-Heinze, Heiko Rieck
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Patent number: 8410157Abstract: 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: GrantFiled: July 31, 2008Date of Patent: April 2, 2013Assignee: Bayer Cropscience AGInventors: Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Jean-Pierre Vors
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Publication number: 20130079302Abstract: 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: ApplicationFiled: June 1, 2011Publication date: March 28, 2013Inventors: Jurgen Benting, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Ruth Meissner, Ulrike Wachendorff-Neumann