Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
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Publication number: 20140081030Abstract: 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: November 25, 2013Publication date: March 20, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Joerg Nico GREUL, Juergen BENTING, Peter DAHMEN, Ulrike WACHENDORFF-NEUMANN
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Publication number: 20140079806Abstract: The invention relates to the use of penflufen for protecting wood and wood-comprising materials against wood-destroying basidiomycetes.Type: ApplicationFiled: September 30, 2011Publication date: March 20, 2014Applicant: LANXESS Deutschland GmbHInventors: Bernd Koop, Martin Kugler, Thomas Jaetsch, Johannes Kaulen, Tanja Gerharz
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Patent number: 8673911Abstract: 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: GrantFiled: November 3, 2008Date of Patent: March 18, 2014Assignee: MethylGene Inc.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
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Publication number: 20140073783Abstract: 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: ApplicationFiled: July 8, 2013Publication date: March 13, 2014Applicant: THERAVANCE, INC.Inventors: Roland Gendron, Adam D. Hughes
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Publication number: 20140066466Abstract: 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: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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Publication number: 20140051680Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).Type: ApplicationFiled: February 28, 2012Publication date: February 20, 2014Applicant: REPLIGEN CORPORATIONInventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
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Patent number: 8653003Abstract: 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/eType: GrantFiled: January 2, 2012Date of Patent: February 18, 2014Assignee: Syngenta Participations AGInventors: Daniel Stierli, Harald Walter
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Patent number: 8653114Abstract: 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: GrantFiled: June 1, 2011Date of Patent: February 18, 2014Assignee: Bayer Intellectual Property GmbHInventors: Jörg Nico Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
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Publication number: 20140045906Abstract: 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: ApplicationFiled: August 7, 2013Publication date: February 13, 2014Inventors: Melissa Fleury, Adam D. Hughes
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Publication number: 20140045850Abstract: 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: ApplicationFiled: March 14, 2013Publication date: February 13, 2014Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20140045813Abstract: 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: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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
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Publication number: 20140046053Abstract: 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: ApplicationFiled: October 10, 2013Publication date: February 13, 2014Applicant: THERAVANCE, INC.Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Publication number: 20140038923Abstract: 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: ApplicationFiled: December 12, 2011Publication date: February 6, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Karen Wagner, Christophe Morisseau, Aaron Wecksler, Guodong Zhang
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Publication number: 20140039027Abstract: 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: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Andreas Görtz, Heiko Rieck, Hiroyuki Hadano
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Patent number: 8637678Abstract: 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: GrantFiled: December 16, 2009Date of Patent: January 28, 2014Assignee: Syngenta LimitedInventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
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Publication number: 20140024835Abstract: 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: September 24, 2013Publication date: January 23, 2014Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 8629288Abstract: 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: GrantFiled: February 12, 2009Date of Patent: January 14, 2014Assignee: Bayer Intellectual Property GmbHInventors: Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
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Publication number: 20140011997Abstract: 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: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: THERAVANCE, INC.Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
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Publication number: 20140011852Abstract: New aminoindanes amides are described, having general formula (I) the relative phytosanitary compositions and their use for the control of phytopathogenic fungi.Type: ApplicationFiled: December 19, 2011Publication date: January 9, 2014Applicant: STICHTING I-F PRODUCT COLLABORATIONInventors: Isabella Venturini, Matteo Santino Vazzola, Entela Sinani, Franco Pellacini, Lucio Filippini
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Patent number: 8618023Abstract: 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: GrantFiled: May 16, 2007Date of Patent: December 31, 2013Assignee: Syngenta Crop Protection, LLCInventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington
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Patent number: 8614214Abstract: 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: GrantFiled: November 2, 2011Date of Patent: December 24, 2013Assignee: Sinochem CorporationInventors: Changling Liu, Lizeng Wang, Zhinian Li, Xufeng Sun, Jie Lan, Lanhui Ren, Qiang Wu, Huiwei Chi
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Publication number: 20130338369Abstract: 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: ApplicationFiled: March 6, 2012Publication date: December 19, 2013Applicant: BASF SEInventors: Markus Heinrich, Gerald Pratsch
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Patent number: 8609866Abstract: 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: GrantFiled: December 17, 2010Date of Patent: December 17, 2013Assignee: ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20130330365Abstract: 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: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20130330366Abstract: 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: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20130331261Abstract: 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: ApplicationFiled: November 28, 2011Publication date: December 12, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Sebastian Hoffmann, Ruth Meissner, Pierre-Yves Coqueron, Philippe Desbordes
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Patent number: 8598222Abstract: 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 reacType: GrantFiled: May 4, 2009Date of Patent: December 3, 2013Assignee: BASF SEInventors: Bernd Wolf, Volker Maywald, Michael Keil, Christopher Koradin, Michael Rack, Thomas Zierke, Martin Sukopp
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Patent number: 8592605Abstract: 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: GrantFiled: March 14, 2013Date of Patent: November 26, 2013Assignee: Bayer Intellectual Property GmbHInventors: Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
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Patent number: 8592578Abstract: 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: GrantFiled: October 17, 2012Date of Patent: November 26, 2013Assignee: BASF SEInventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
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Publication number: 20130310567Abstract: 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: ApplicationFiled: January 27, 2012Publication date: November 21, 2013Applicant: EI DU PONT DE NEMOURS AND COMPANYInventors: Sigridur Soley Kristjansdottir, Rafael Shapiro, Matthew Richard Oberholzer
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Publication number: 20130310592Abstract: 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-C6alType: ApplicationFiled: January 25, 2012Publication date: November 21, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Miroslav Terinek, Dominik Faber, Stefan Koenig
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Patent number: 8586536Abstract: 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: GrantFiled: December 14, 2011Date of Patent: November 19, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Patent number: 8586753Abstract: 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: GrantFiled: December 15, 2010Date of Patent: November 19, 2013Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui, Igor Gerus
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Patent number: 8580835Abstract: 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: GrantFiled: February 19, 2008Date of Patent: November 12, 2013Assignee: Syngenta Crop Protection, LLCInventors: Paul Edward Bonnett, Neil George, Ian Kevin Jones, Shailesh Shah
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Patent number: 8580971Abstract: 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: GrantFiled: February 21, 2006Date of Patent: November 12, 2013Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Thomas Seitz, Peter Dahmen, Ulrike Wachendorff-Neumann
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Patent number: 8580836Abstract: 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: GrantFiled: June 20, 2011Date of Patent: November 12, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Yuichi Matsuzaki, Hiroshi Sakaguchi
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Publication number: 20130296383Abstract: 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: ApplicationFiled: November 14, 2011Publication date: November 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jörg Greul, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann
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Publication number: 20130296269Abstract: 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: ApplicationFiled: November 14, 2011Publication date: November 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: 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
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Patent number: 8575362Abstract: 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: GrantFiled: June 15, 2011Date of Patent: November 5, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, Jr., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
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Publication number: 20130289025Abstract: 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: ApplicationFiled: March 20, 2013Publication date: October 31, 2013Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8569376Abstract: 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: GrantFiled: March 1, 2013Date of Patent: October 29, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Publication number: 20130281505Abstract: 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/eType: ApplicationFiled: January 2, 2012Publication date: October 24, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Daniel Stierli, Harald Walter
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Patent number: 8563747Abstract: 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: GrantFiled: July 27, 2010Date of Patent: October 22, 2013Assignee: Syngenta Crop Protection, LLCInventors: Linhua Wang, Jefferson Thomas Ebert
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Publication number: 20130274481Abstract: 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: ApplicationFiled: August 3, 2011Publication date: October 17, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Linhua Wang, Ritesh Bharat Sheth
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Patent number: 8558006Abstract: 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: GrantFiled: July 27, 2010Date of Patent: October 15, 2013Assignee: Syngenta Crop Protection, LLCInventors: Linhua Wang, Ritesh Bharat Sheth, Maren Fuerst
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Publication number: 20130264519Abstract: 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: ApplicationFiled: May 29, 2013Publication date: October 10, 2013Inventors: John Campbell, Ronald Matthys Swart, Lucy Emeleus, Susan Owens
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Patent number: 8552050Abstract: 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: GrantFiled: August 18, 2008Date of Patent: October 8, 2013Assignee: Beth Israel Deaconess Medical CenterInventors: Lewis C. Cantley, Matthew G. Vander Heiden, Heather R. Christofk
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Patent number: 8552049Abstract: 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: GrantFiled: May 12, 2011Date of Patent: October 8, 2013Assignee: Syngenta Corp Protection, LLCInventors: Daniel Stierli, Harald Walter
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Publication number: 20130261158Abstract: 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: ApplicationFiled: July 30, 2009Publication date: October 3, 2013Inventors: 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
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Publication number: 20130245041Abstract: 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: ApplicationFiled: November 26, 2012Publication date: September 19, 2013Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson