Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
  • Publication number: 20140081030
    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: November 25, 2013
    Publication date: March 20, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Joerg Nico GREUL, Juergen BENTING, Peter DAHMEN, Ulrike WACHENDORFF-NEUMANN
  • Publication number: 20140079806
    Abstract: The invention relates to the use of penflufen for protecting wood and wood-comprising materials against wood-destroying basidiomycetes.
    Type: Application
    Filed: September 30, 2011
    Publication date: March 20, 2014
    Applicant: LANXESS Deutschland GmbH
    Inventors: Bernd Koop, Martin Kugler, Thomas Jaetsch, Johannes Kaulen, Tanja Gerharz
  • Patent number: 8673911
    Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: March 18, 2014
    Assignee: MethylGene Inc.
    Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
  • Publication number: 20140073783
    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: Application
    Filed: July 8, 2013
    Publication date: March 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Adam D. Hughes
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 8653003
    Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; R5 is hydrogen, halogen or C1-C4alkyl; R6 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkynyl; R7 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkynyl, C3-C6cycloalkyl-C3-C6alkynyl, C1-C6haloalkyl, C1-C6haloalkoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R5 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl, C3-C6alkynyl, amino, C1-C6alkylcarbonylamino, C1-C6alkoxycarbonylamino or C3-C6cycloalkylcarbonylamino; R9 is hydrogen, halogen, C1-C6alkyl, C1-C6alkoxy, C2-C6alkenyl, C3-C6alkynyl, C3-C6cycloalkyl-C3-C6alkynyl, halophenoxy, halophenyl, C1-C6haloalkyl, C1-C6haloalkoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R10 is hydrogen, halogen, C1-C4alkyl, C1-C6alkoxy, C2-C6alkenyl or C3-C6alkynyl; X is CH2, O or S; n is 0, 1 or 2; and agronomically acceptable salts/isomers/structural isomers/stereoisomers/diastereoisomers/e
    Type: Grant
    Filed: January 2, 2012
    Date of Patent: February 18, 2014
    Assignee: Syngenta Participations AG
    Inventors: Daniel Stierli, Harald Walter
  • Patent number: 8653114
    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: June 1, 2011
    Date of Patent: February 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Publication number: 20140045906
    Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds 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: August 7, 2013
    Publication date: February 13, 2014
    Inventors: Melissa Fleury, Adam D. Hughes
  • Publication number: 20140045850
    Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 13, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Publication number: 20140045813
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
  • Publication number: 20140046053
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: October 10, 2013
    Publication date: February 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140038923
    Abstract: The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay.
    Type: Application
    Filed: December 12, 2011
    Publication date: February 6, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Karen Wagner, Christophe Morisseau, Aaron Wecksler, Guodong Zhang
  • Publication number: 20140039027
    Abstract: The present invention relates to a method for controlling Asian soybean rust (ASR) of a conventionally bred ASR-tolerant, Stem canker resistant and/or Frog-eye leaf spot resistant soybean variety comprising the application of a succinate dehydrogenase inhibitor (SDHI) fungicide to said plant, plant propagation material, or at its locus of growth.
    Type: Application
    Filed: February 13, 2012
    Publication date: February 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Andreas Görtz, Heiko Rieck, Hiroyuki Hadano
  • Patent number: 8637678
    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 16, 2009
    Date of Patent: January 28, 2014
    Assignee: Syngenta Limited
    Inventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
  • Publication number: 20140024835
    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: September 24, 2013
    Publication date: January 23, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 8629288
    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: Grant
    Filed: February 12, 2009
    Date of Patent: January 14, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Publication number: 20140011852
    Abstract: New aminoindanes amides are described, having general formula (I) the relative phytosanitary compositions and their use for the control of phytopathogenic fungi.
    Type: Application
    Filed: December 19, 2011
    Publication date: January 9, 2014
    Applicant: STICHTING I-F PRODUCT COLLABORATION
    Inventors: Isabella Venturini, Matteo Santino Vazzola, Entela Sinani, Franco Pellacini, Lucio Filippini
  • Patent number: 8618023
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides. Formula (I), wherein X is oxygen or sulfur; A is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, or a phenyl ring; the heterocyclic ring or the phenyl being substituted by the groups R6, R7 and R8; R6, R7 and R8 are each, independently, hydrogen, halogen, cyano, nitro, C1-4 alky, C1-4 halogenalkyl, C1-4 halogenalkoxy, C1-4 alkoxy(C1-4)alkyl or C1-4halogenalkoxy(C1-4)alkyl, provided that at least one of R6, R7 and R8 is not hydrogen; B is a phenyl, naphthyl or quinolinyl group, which is substituted by one or more substituents R9.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: December 31, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington
  • Patent number: 8614214
    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: Grant
    Filed: November 2, 2011
    Date of Patent: December 24, 2013
    Assignee: Sinochem Corporation
    Inventors: Changling Liu, Lizeng Wang, Zhinian Li, Xufeng Sun, Jie Lan, Lanhui Ren, Qiang Wu, Huiwei Chi
  • Publication number: 20130338369
    Abstract: The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
    Type: Application
    Filed: March 6, 2012
    Publication date: December 19, 2013
    Applicant: BASF SE
    Inventors: Markus Heinrich, Gerald Pratsch
  • Patent number: 8609866
    Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: December 17, 2013
    Assignee: ActiveSite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Publication number: 20130330365
    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: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130330366
    Abstract: In one aspect, the invention relates to compounds having the formula XII: 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: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130331261
    Abstract: The present invention relates to the novel use of pyrazole carboxylic acid amides, compositions comprising these compounds and their use in methods for the reduction of mycotoxin contamination in plants.
    Type: Application
    Filed: November 28, 2011
    Publication date: December 12, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Sebastian Hoffmann, Ruth Meissner, Pierre-Yves Coqueron, Philippe Desbordes
  • Patent number: 8598222
    Abstract: The present invention relates to a process for preparing 1,3-substituted pyrazole compounds of the formula I in which X is especially a CX1X2X3 group in which X1, X2 and X3 are each independently especially hydrogen, fluorine or chlorine, R1 is C1-C4-alkyl or cyclopropyl, and R2 is hydrogen, CN or a CO2R2a group in which R2a is especially C1-C6-alkyl, comprising the following steps: i) reacting a compound of the formula II with a hydrazone of the formula III where the variables X and R2 in formula II are each as defined for formula I, Y is oxygen, an NRy1 group or an [NRy2Ry3]+Z? group, R3 is OR3a or an NR3bR3c group, and where the variable R1 in formula III is as defined for formula I, R4 and R5 are each independently hydrogen, C1-C6-alkyl, optionally substituted phenyl, where at least one of the R4 and R5 radicals is different from hydrogen, and where R4 and R5 together with the carbon atom to which they are bonded may also be a 5- to 10-membered saturated carbocycle; ii) treating the reac
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: December 3, 2013
    Assignee: BASF SE
    Inventors: Bernd Wolf, Volker Maywald, Michael Keil, Christopher Koradin, Michael Rack, Thomas Zierke, Martin Sukopp
  • Patent number: 8592605
    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: Grant
    Filed: March 14, 2013
    Date of Patent: November 26, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
  • Patent number: 8592578
    Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: November 26, 2013
    Assignee: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
  • Publication number: 20130310567
    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: January 27, 2012
    Publication date: November 21, 2013
    Applicant: EI DU PONT DE NEMOURS AND COMPANY
    Inventors: Sigridur Soley Kristjansdottir, Rafael Shapiro, Matthew Richard Oberholzer
  • Publication number: 20130310592
    Abstract: The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1 H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide by acylating the oxime oxygen of the compound of formula (VIII), in the presence of a solvent and an acylating agent of formula (XI) R 1C(X)—CI (XI); wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(?CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; and a) if R1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (XIIa) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R1 is C1-C6alkoxy, CH3—C(?CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6al
    Type: Application
    Filed: January 25, 2012
    Publication date: November 21, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Miroslav Terinek, Dominik Faber, Stefan Koenig
  • Patent number: 8586536
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: December 14, 2011
    Date of Patent: November 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Patent number: 8586753
    Abstract: The present invention relates to a process for the preparation of 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives comprising the reaction of substituted 1,3-dioxolanes and 1,4-dioxanes with alkyl- or arylhydrazines to give 1-alkyl- or 1-aryl-substituted dihydro-1H-pyrazoles, and their further reaction to give 1-alkyl- or 1-aryl-substituted 5-pyrazolecarboxylic acid derivatives, which can be used as valuable intermediates for producing insecticidally effective anthranilamides.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Bayer CropScience AG
    Inventors: Sergii Pazenok, Norbert Lui, Igor Gerus
  • Patent number: 8580835
    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: Grant
    Filed: February 19, 2008
    Date of Patent: November 12, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Paul Edward Bonnett, Neil George, Ian Kevin Jones, Shailesh Shah
  • Patent number: 8580971
    Abstract: New pyrazolylcarboxanilides of the formula (I) in which R and R1 have the meanings given in the description, a plurality of processes for the preparation of these substances and their use for controlling undesired microorganisms, and novel intermediates and their preparation.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: November 12, 2013
    Assignee: Bayer CropScience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Thomas Seitz, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Patent number: 8580836
    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: Grant
    Filed: June 20, 2011
    Date of Patent: November 12, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yuichi Matsuzaki, Hiroshi Sakaguchi
  • Publication number: 20130296383
    Abstract: The present invention relates to decahydro-1,4-methanonaphthalen carboxamide derivatives of formula (Ia) or (Ib); 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: November 14, 2011
    Publication date: November 7, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Publication number: 20130296269
    Abstract: The present invention relates to novel 5-halogenopyrazole(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: November 7, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Benting, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Jörg Greul, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 8575362
    Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: November 5, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, Jr., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
  • Publication number: 20130289025
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 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: March 20, 2013
    Publication date: October 31, 2013
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8569376
    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) and/or (V): 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, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: October 29, 2013
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Publication number: 20130281505
    Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; R5 is hydrogen, halogen or C1-C4alkyl; R6 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkynyl; R7 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkynyl, C3-C6cycloalkyl-C3-C6alkynyl, C1-C6haloalkyl, C1-C6haloalkoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R5 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl, C3-C6alkynyl, amino, C1-C6alkylcarbonylamino, C1-C6alkoxycarbonylamino or C3-C6cycloalkylcarbonylamino; R9 is hydrogen, halogen, C1-C6alkyl, C1-C6alkoxy, C2-C6alkenyl, C3-C6alkynyl, C3-C6cycloalkyl-C3-C6alkynyl, halophenoxy, halophenyl, C1-C6haloalkyl, C1-C6haloalkoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R10 is hydrogen, halogen, C1-C4alkyl, C1-C6alkoxy, C2-C6alkenyl or C3-C6alkynyl; X is CH2, O or S; n is 0, 1 or 2; and agronomically acceptable salts/isomers/structural isomers/stereoisomers/diastereoisomers/e
    Type: Application
    Filed: January 2, 2012
    Publication date: October 24, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Daniel Stierli, Harald Walter
  • Patent number: 8563747
    Abstract: The invention provides a process for the preparation of a compound of formula (I) in particular, wherein a compound of formula (II) is reacted with a dialkylsulphate. R1 is C1-C4haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 is methyl or ethyl.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: October 22, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Linhua Wang, Jefferson Thomas Ebert
  • Publication number: 20130274481
    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: Application
    Filed: August 3, 2011
    Publication date: October 17, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Linhua Wang, Ritesh Bharat Sheth
  • Patent number: 8558006
    Abstract: The present invention relates to processes for the preparation of a compound of formula (I) comprising reacting a compound of formula (IV) with a compound of formula III or (IIIA) in the presence of an acid; wherein R1 is C1-C4 haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; R3 is methyl or ethyl; R4 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and n is 0 or 1.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: October 15, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Linhua Wang, Ritesh Bharat Sheth, Maren Fuerst
  • Publication number: 20130264519
    Abstract: Metal extractants of 2-hydroxyphenyldiazole compounds according to Formula (2): and tautomers and salts thereof, are disclosed, wherein substituents R5, R7, R9, and R10 are as defined herein.
    Type: Application
    Filed: May 29, 2013
    Publication date: October 10, 2013
    Inventors: John Campbell, Ronald Matthys Swart, Lucy Emeleus, Susan Owens
  • Patent number: 8552050
    Abstract: The invention described herein features methods, compositions, and kits for the use of activators of PKM2 for the treatment, prevention, or amelioration of diseases related to PKM2 function, including, e.g., cancer, diabetes, atherosclerosis, restenosis, obesity, autoimmune disorders, and proliferative disorders.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: October 8, 2013
    Assignee: Beth Israel Deaconess Medical Center
    Inventors: Lewis C. Cantley, Matthew G. Vander Heiden, Heather R. Christofk
  • Patent number: 8552049
    Abstract: Compounds of Formula (I) wherein R1 is C1-C4alkyl or C1-C4 haloalkyl; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; R5 is hydrogen, halogen, C1-C4alkyl or C1-C4halogenalkyl; R6 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; R7 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkinyl, C3-C6cycloalkyl-C3-C6alkinyl, halophenoxy, halophenyi, C1-C6haloalkyl, C1-C6haloakoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R8 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; with the provisio that at least one of R6, R7 and R8 is different from hydrogen; n is 0 or 1, are suitable for use as microbriocides.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: October 8, 2013
    Assignee: Syngenta Corp Protection, LLC
    Inventors: Daniel Stierli, Harald Walter
  • Publication number: 20130261158
    Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogues, their process of 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. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Application
    Filed: July 30, 2009
    Publication date: October 3, 2013
    Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Publication number: 20130245041
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and 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: Application
    Filed: November 26, 2012
    Publication date: September 19, 2013
    Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson