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