1,2-oxazoles (including Hydrogenated) Patents (Class 548/240)
  • Patent number: 10550111
    Abstract: The present invention relates to herbicide. Specifically to a kind of uracil compounds containing isoxazoline ring and the uses thereof. The present invention compounds have very good herbicidal activity, can effectively control weeds, such as Echinochloa crusgalli, Setaria viridis, Cyperus difformis, Juncellus serotinus, Digitaria sangunalis, Arthraxon hispidus, Abutilon theophrasti, Zinnia elegans, Amaranthus retrofluxes, Portulaca oleracea, Xanthium sibiricum, Solanum nigrum, Cassia tora, Hibiscus trionum, Glycine soja, an so on. They can effectively control weeds even at lower doses. The present invention compounds also safe to wheats, corns and rices, and can used as herbicides in agriculture fields.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: February 4, 2020
    Assignee: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD.
    Inventors: Changling Liu, Jichun Yang, Hongjuan Ma, Qiao Wu, Dongliang Cui, Kecheng Yan, Miao Li
  • Patent number: 10287279
    Abstract: A systematic screening has revealed a family of compounds that exhibit inhibitory effects on 12/15-lipoxygenase. Accordingly, the present invention relates to the use of these compounds for the inhibition of 12/15-lipoxygenase and for the treatment of a condition involving 12/15-lipoxygenase. Exemplary conditions include, but are not limited to, stroke, periventricular leukomalacia, cardiac arrest with resuscitation, atherosclerosis, Parkinson's disease, Alzheimer's disease, and breast cancer.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: May 14, 2019
    Assignees: THE CHILDREN'S HOSPITAL CORPORATION, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services
    Inventors: Klaus Joachin Van Leyen, Theodore R. Holman, David J. Maloney, Ajit Jadhav, Anton Simeonov, Ganesha Rai
  • Patent number: 10160731
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.
    Type: Grant
    Filed: April 5, 2018
    Date of Patent: December 25, 2018
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Patent number: 9834523
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: December 5, 2017
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Patent number: 9744148
    Abstract: The present invention relates to methods for inhibiting the activity of human kallikrein 7 (KLK7) (also known as serine protease stratum corneum chymotryptic enzyme, SCCE). The invention further relates to the use of KLK7 inhibitors of Formula I for the treatment and prevention of diseases, more specifically for the treatment and prevention of skin diseases. The invention also provides new compounds demonstrated to be inhibitors of KLK7.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: August 29, 2017
    Assignee: SIXERA Pharma AB
    Inventor: Marcel Linschoten
  • Patent number: 9593126
    Abstract: The invention recites an improved process for preparing spirocyclic isoxazoline derivatives of Formula (1) wherein “*”, R1a, R1b, and R1c are as described herein.
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: March 14, 2017
    Assignee: Zoetis Services LLC
    Inventors: Sean D. W. Greenwood, Timothy L. Stuk
  • Patent number: 9315468
    Abstract: Methods that include latent 1,3-dipole-functional compounds are disclosed herein. The latent 1,3-dipole-functional compound (e.g., an oxime) can be used to form an active 1,3-dipole-functional compound (e.g., a nitrile oxide) that can be used to react with a cyclic alkyne in a dipolar cycloaddition reaction.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: April 19, 2016
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Geert-Jan Boons, Frederic Friscourt, Petr A. Ledin, Ngalle Eric Mbua
  • Patent number: 9085541
    Abstract: The present invention relates to a process for producing aromatic carbonyl compounds of formula I and aromatic imine compounds of formula III comprising the step of reacting a (hetero)aromatic halogen or sulfonate compound II wherein the variables are as defined in the claims and description, with a mixture of carbon monoxide and hydrogen in the presence of a transition metal complex catalyst. The invention also relates to specific compounds III, to compositions comprising them and to their use for combating invertebrate pests.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: July 21, 2015
    Assignee: BASF SE
    Inventors: Karsten Koerber, Florian Kaiser, Christian Rein, Joachim Schmidt-Leithoff, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Juergen Langewald
  • Patent number: 9034820
    Abstract: The invention generally relates to compositions and methods of their use. More specifically, the invention relates to the use of a compound in modulating erythropoiesis in a subject by mediating the activity and/or quantity of a member present in the LPA3-mediated signaling pathway, such as lysophosphatidic acid receptor subtype 3 (LPA3).
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: May 19, 2015
    Inventor: Hsinyu Lee
  • Patent number: 9029409
    Abstract: The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: May 12, 2015
    Assignee: AbbVie Inc.
    Inventors: David J. Calderwood, Eric C. Breinlinger, Steven L. Swann, Venkata Srikanth Chitty, Subramanya Seetharama Shastry Hosahalli, Subhendu Mukherjee, Siva Sanjeeva Rao Thunuguntla
  • Publication number: 20150126371
    Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 7, 2015
    Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
  • Publication number: 20150126523
    Abstract: The present invention relates to novel and inventive isoxazoline of formula (I) and salts thereof: wherein variables D1, D2, D3, D4, D5, R1, B1, B2, B3, R2, R3, R4, R5, R6, Y, Z, L, a and b are described herein are as defined in the description. The invention also relates to parasiticidal and pesticidal compositions comprising the isoxazoline compounds of formula (I), processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: MERIAL LIMITED
    Inventor: Charles Q. Meng
  • Publication number: 20150119375
    Abstract: 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: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Bayer Cropscience AG
    Inventors: 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
  • Patent number: 9006447
    Abstract: The present invention relates to a method for preparing 4-chloro-, 4-bromo- or 4-iodobenzaldehyde oximes and phenyl-substituted isoxazoline compounds prepared from these oximes.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: April 14, 2015
    Assignee: BASF SE
    Inventors: Karsten Koerber, Markus Kordes, Michael Rack, Wolfgang Von Deyn, Florian Kaiser
  • Publication number: 20150098928
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 9, 2015
    Applicant: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Ty Wagerle, Ming Xu
  • Publication number: 20150099738
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Application
    Filed: June 30, 2014
    Publication date: April 9, 2015
    Inventors: Mark L. BEHNKE, Alfredo C. CASTRO, Lawrence K. CHAN, Catherine A. EVANS, Louis GRENIER, Michael J. GROGAN, Yves LEBLANC, Tao LIU, Stephane PELUSO, Daniel A. SNYDER, Thomas T. TIBBITTS
  • Patent number: 8999889
    Abstract: The invention relates to substituted ketonic isoxazoline compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted ketonic isoxazoline compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such substituted ketonic isoxazoline compounds. The substituted ketonic isoxazoline compounds of the present invention are defined by the following formula I: wherein A1 to A4, R1 to R3, (R4)p, (R5)q, X and (G)m are defined as in the description.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: April 7, 2015
    Assignee: BASF SE
    Inventors: Karsten Koerber, Florian Kaiser, Wolfgang von Deyn, Steffen Gross, Joachim Dickhaut, Prashant Deshmukh, Nina Gertrud Bandur, Arun Narine, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun
  • Publication number: 20150087519
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of formula I and their use as herbicides, The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 16, 2013
    Publication date: March 26, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20150072993
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Zengyun AN, Liang CHEN, Shuhui CHEN, Jean Marie DEFAUW, Scott Dale HOLMSTROM, Ping HU, Chongzhi TANG, William Hunter WHITE, Wentao WU, Yang ZHANG
  • Publication number: 20150065724
    Abstract: The present invention is directed to novel synthetic methods for preparing a compound of Structural Formula (I): wherein R is —H or a hydroxyl protecting group. Also included are synthetic intermediates described herein.
    Type: Application
    Filed: September 3, 2014
    Publication date: March 5, 2015
    Applicant: AbbVie Inc.
    Inventors: Yi-Yin Ku, Yu-Ming Pu, Hao Yang, Alan Christesen
  • Patent number: 8952175
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: February 10, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Manabu Yaosaka, Tomohisa Utsunomiya, Yuji Moriyama, Tomohiro Matsumoto, Kazutaka Matoba
  • Publication number: 20150031537
    Abstract: There are described 4-nitro-substituted N-(tetrazol-5-yl)-, N-(triazol-5-yl)- and N-(1,3,4-oxadiazol-2-yl)arylcarboxamides of the general formula (I) as herbicides. In this formula (I), X, Y and W are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A is N and CY.
    Type: Application
    Filed: February 18, 2013
    Publication date: January 29, 2015
    Inventors: Simon Dörner-Rieping, Ralf Braun, Arnin Köhn, Hartmut Ahrens, Stefan Lehr, Hansjörg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20150005507
    Abstract: A method for manufacturing a crystal and a crystal of (S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide and a method for manufacturing the crystal. It is elucidated that (S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide that has a crystalline polymorph.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 1, 2015
    Inventors: Kazutaka MATOBA, Takeshi MITA, Kotatsu MATSUBARA, Takahiro KAGAMI, Kunimitsu NAKAHIRA, Masaki KOBAYASHI, Hotaka IMANAKA, Rika MIYACHI, Masashi OHNO
  • Publication number: 20140371464
    Abstract: The invention recites a chiral process for the synthesis of isoxazoline azetidine phenyl substituted derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, processes for making, and their use as a parasiticide in an animal.
    Type: Application
    Filed: January 29, 2013
    Publication date: December 18, 2014
    Inventors: Denis Billen, Sean David William Greenwood, Timothy Lee Stuk
  • Publication number: 20140371068
    Abstract: N-(1,2,5-Oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- or N-(triazol-5-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), R, V, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical. W is CY or N.
    Type: Application
    Filed: December 10, 2012
    Publication date: December 18, 2014
    Inventors: Armin Koehn, Stefan Lehr, Ralf Braun, Simon Doerner-Rieping, Hartmut Ahrens, Hansjoerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler
  • Publication number: 20140371240
    Abstract: 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: Application
    Filed: December 17, 2012
    Publication date: December 18, 2014
    Inventors: Michael Maue, Tobias Kapferer, Friedrich August Muehlthau, Olga Malsam
  • Patent number: 8901119
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 2, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Publication number: 20140350261
    Abstract: There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an ?,?-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
    Type: Application
    Filed: November 8, 2012
    Publication date: November 27, 2014
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Ken-ichi Toyama, Yuji Moriyama, Kazutaka Matoba, Manabu Yaosaka, Eitatsu Ikeda
  • Publication number: 20140350061
    Abstract: A compound of formula (I): where A1, A2, A3, A4, A5, A6, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: February 24, 2014
    Publication date: November 27, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Peter RENOLD, Jerome Yves CASSAYRE, Myriem EL QACEMI, Thomas PITTERNA
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Patent number: 8889710
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: November 18, 2014
    Assignee: Eli Lilly and Company
    Inventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
  • Patent number: 8883809
    Abstract: The present invention provides a compound of general formulae 3a-i to 6a-i, 7a-i to 10a-i, 12a-i to 15a-i, 16a-i to 19a-i, 21a-i to 24a-i, 25a-i to 28a-i, 30a-i to 33a-i, 34a-i to 37a-i and 39a-i to 42a-i, 43a-i to 46a-i useful as potential antitumour agents against human cancer cell lines and a process for the preparation thereof.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: November 11, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Earla V. Bharathi, Jonnala S. Reddy, Dudekula Dastagiri, Arutla Viswanath
  • Patent number: 8859592
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: October 14, 2014
    Assignee: Syngenta Corp Protection LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • Patent number: 8853410
    Abstract: The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) which are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I) wherein R1 to R5, R8 and R9 are described as in the description. The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: October 7, 2014
    Assignee: BASF SE
    Inventors: Michael Rack, Karsten Koerber, Florian Kaiser
  • Publication number: 20140288105
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, OSCAR MIGUEL MORADEI
  • Publication number: 20140275186
    Abstract: This invention relates to novel 4,5-dihydroisoxazoles and 4,5-dihydro[1,2,4]-oxadiazoles of formula (I), to their use as androgenic or antiandrogenic agents or androgen receptor modulators, and to methods of their preparation.
    Type: Application
    Filed: October 17, 2012
    Publication date: September 18, 2014
    Inventors: Juha Pulkkinen, Pekka Poutiainen, Tuomas Oravilahti, Jorma Palvimo, Mikael Perakyla, Reino Laatikainen, Tarja Ihalainen
  • Publication number: 20140275079
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Patent number: 8835653
    Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: August 18, 2010
    Date of Patent: September 16, 2014
    Assignee: Sanofi
    Inventors: Markus Follmann, Volkmar Wehner, Jean-Michel Altenburger, Gilbert Lassalle, Jean-Pascal Herault
  • Publication number: 20140256553
    Abstract: Provided are an ortho-substituted phenylisoxazoline-based compound with 2,6-difluorobenzyloxymethyl represented by Formula 1, or a racemate or enantiomer thereof, a herbicide including the ortho-substituted phenylisoxazoline-based compound, or the racemate or enantiomer thereof as an active ingredient, and a method of selectively controlling grass weed comprising treating with the ortho-substituted phenylisoxazoline-based compound, or the racemate or enantiomer thereof before or after the grass weed emerges.
    Type: Application
    Filed: May 18, 2012
    Publication date: September 11, 2014
    Applicants: MOGHU RESEARCH CENTER LTD., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Kwan Ko, Gyu Hwan Yon, Jae Wook Ryu, Dong Wan Koo, Jun Ho Nam, Sung Wan Pyo, Jae Min Hwang, Suk Jin Koo, Ki Hwan Hwang, Dong Guk Lee, Man Seok Jeon, Nam Gyu Cho, Sung Hun Kim, Jong Su Lim, Kun Hoe Chung
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140249316
    Abstract: The present invention relates to compounds formula (I): wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined herein; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 13, 2014
    Publication date: September 4, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Patent number: 8822517
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: September 2, 2014
    Assignee: Adamed SP. Z O.O.
    Inventors: Marcin Kolaczkowski, Piotr Kowalski, Jolanta Jaśkowska, Monika Marcinkowska, Katarzyna Mitka, Adam Bucki, Anna Wesolowska, Maciej Pawlowski
  • Patent number: 8822502
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A1?, A2?, A3?, A4?, A5?, A6?, G1, R1, R2, R3, R4, R5a and R5b are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I) or compounds of formula (I?), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising compounds of formula (I) or compounds of formula (I?), and to methods of using compounds of formula (I) or compounds of formula (I?) to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 2, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Vladimir Bobosik, Peter Renold, Jérôme Yves Cassayre, Pierre Joseph Marcel Jung
  • Patent number: 8822378
    Abstract: N-(Tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and use thereof as herbicides N-(Tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), X, Y, Z and R represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B represent N and CY.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: September 2, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ralf Braun, Simon Dörner-Rieping, Arnim Köhn, Hartmut Ahrens, Stefan Lehr, Andreas Van Almsick, Isolde Häuser-Hahn, Hansjörg Dietrich, Elmar Gatzweiler, Ines Heinemann, Christopher Hugh Rosinger
  • Patent number: 8822466
    Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Noëlle Gauvry, Steve Nanchen
  • Publication number: 20140243375
    Abstract: The present invention provides compounds of formula I wherein G1 is oxygen; R1 is hydrogen; R2 is group P L is a bond, methylene or ethylene; R3 is hydrogen; R4 is independently hydrogen, cyano, cyano-C1-C8alkyl, C1-C8alkyl, C1-C8haloalkyl, C3-C8cycloalkyl, C3-C8-cycloalkyl where one carbon atom is replaced by O, S, S(O) or SO2, or C3-Cgcycloalkyl-C1-C8alkyl, C3-C8cycloalkyl-C1-C8alkyl where one carbon atom in the cycloalkyl group is replaced by O, S, S(O) or SO2, or C3-C8cycloalkyl-C1-C8haloalkyl, C1-C8hydroxyalkyl, C1-C8alkoxy-C1-C8alkyl, C2-C8alkenyl, C2-C8haloalkenyl, C2-C8alkynyl, C2-C8haloalkynyl, phenyl, phenyl substituted by one to three R6, phenyl-C1-C4alkyl, phenyl-C1-C4alkyl wherein the phenyl moiety is substituted by one to three R6, 5-6 membered heteroaryl-C1-C4alkyl or 5-6 membered heteroaryl-C1-C4alkyl wherein the heteroaryl moiety is substituted by one to three R6, or C1-C4alkyl-(C1-C4alkyl-O—N?)C—CH2—; each R6 is independently halogen, cyano, nitro, C1-C8alkyl, C1-C8haloalkyl, C1-C8alkoxy, or
    Type: Application
    Filed: September 28, 2012
    Publication date: August 28, 2014
    Applicant: Syngenta Participations AG
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre
  • Publication number: 20140235869
    Abstract: The present invention relates to processes for the preparation of thietane derivatives of the formula (IA) and thietane derivatives of the formula (IB) wherein R1, R2, A1, A2, A3, A4, B, and n are as defined in the claims. The invention also relates to intermediates useful in the processes, as well as the compounds of formula (IA) and (IB) and their use as pesticides.
    Type: Application
    Filed: August 24, 2012
    Publication date: August 21, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140228577
    Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves CASSAYRE, Peter RENOLD, Myriem EL QACEMI, Thomas PITTERNA, Julie Clementine TOUEG