1,2-oxazoles (including Hydrogenated) Patents (Class 548/240)
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Publication number: 20140243375Abstract: 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, orType: ApplicationFiled: September 28, 2012Publication date: August 28, 2014Applicant: Syngenta Participations AGInventors: Myriem El Qacemi, Jerome Yves Cassayre
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Publication number: 20140235869Abstract: 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: ApplicationFiled: August 24, 2012Publication date: August 21, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
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Publication number: 20140228577Abstract: 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: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jerome Yves CASSAYRE, Peter RENOLD, Myriem EL QACEMI, Thomas PITTERNA, Julie Clementine TOUEG
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Patent number: 8796464Abstract: A production method of an isoxazoline-substituted benzoic acid amide compound of Formula (1) where X is a halogen atom, C1-6 haloalkyl, etc., Y is a halogen atom, C1-6 alkyl, etc., R1 is a C1-6 haloalkyl, etc., R2 and R3 independently of each other are a hydrogen atom, C1-6 alkyl, etc., R4 is C1-6 alkyl, C1-6 haloalkyl, etc., R5 is a hydrogen atom, C1-6 alkyl, etc., m is an integer of 0 to 5, n is an integer of 0 to 4, including: reacting an isoxazoline-substituted benzene compound of Formula (3) where X, Y, R1, m, and n are the same as defined above, L is a chlorine atom, a bromine atom, —C(O)OH, —C(O)J, etc., J is a halogen atom, with a 2-aminoacetic acid amide compound of Formula (2) where R2, R3, R4, and R5 are the same as defined above, or a salt thereof; crystal forms and the production method thereof.Type: GrantFiled: February 1, 2013Date of Patent: August 5, 2014Assignee: Nissan Chemical Industries, Ltd.Inventors: Yuji Moriyama, Takashi Mizukoshi
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Publication number: 20140206606Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.Type: ApplicationFiled: August 24, 2012Publication date: July 24, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
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Publication number: 20140206633Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.Type: ApplicationFiled: February 3, 2011Publication date: July 24, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
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Publication number: 20140194376Abstract: 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; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).Type: ApplicationFiled: August 24, 2012Publication date: July 10, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
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Patent number: 8772295Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: GrantFiled: January 22, 2013Date of Patent: July 8, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 8765735Abstract: 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: GrantFiled: May 18, 2010Date of Patent: July 1, 2014Assignee: Infinity Pharmaceuticals, Inc.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
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Publication number: 20140179527Abstract: 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: ApplicationFiled: July 30, 2012Publication date: June 26, 2014Applicant: Bayer Intellectual Property GmbhInventors: Ralf Braun, Simon Dörner-Rieping, Arnim Köhn, Hartmut Ahrens, Stefan Lehr, Andreas Van Almsick, Isolde Häuser, Hansjörg Dietrich, Elmar Gatzweiler, Ines Heinemann, Christopher Hugh Rosinger
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Patent number: 8754053Abstract: 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 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: GrantFiled: February 17, 2011Date of Patent: June 17, 2014Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20140155617Abstract: 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: ApplicationFiled: September 30, 2013Publication date: June 5, 2014Applicant: E.I. du Pont de Nemours and CompanyInventor: Gary David Annis
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Patent number: 8735362Abstract: 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: GrantFiled: December 1, 2010Date of Patent: May 27, 2014Assignee: Syngenta Crop Protection, LLCInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Patent number: 8722673Abstract: The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: GrantFiled: December 22, 2009Date of Patent: May 13, 2014Assignee: BASF SEInventors: Karsten Koerber, Florian Kaiser, Matthias Pohlman, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Wolfgang von Deyn, Deborah L. Culberston, Cecille Ebuenga, Douglas D. Anspaugh, Franz-Josef Braun
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Publication number: 20140127165Abstract: 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: ApplicationFiled: January 6, 2014Publication date: May 8, 2014Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Patent number: 8710056Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein A is a substituted or unsubstituted isoxazole or isothiazole radical; V is C(Rv) or N; W is C(Rw) or N; with the proviso that either V or W is N; Rt, Ru, Rv, Rw are H, halogen, C1-C4-alkyl and the like; X1 is S, O or NR1a, wherein R1a is selected H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alkyl and the like.Type: GrantFiled: July 1, 2010Date of Patent: April 29, 2014Assignee: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
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Publication number: 20140113943Abstract: Disclosed are compounds of Formula 1, wherein R1 is halogen, C1-C2 haloalkyl or C1-C2 haloalkoxy; R2 is H, halogen or cyano; R3 is H, halogen or CF3; R4 is H, C2-C7 alkylcarbonyl or C2-C7 alkoxycarbonyl; and R5 is C1-C6 alkyl or C1-C6 haloalkyl, each substituted with one substituent independently selected from hydroxy, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylaminocarbonyl and C3-C9 halodialkylaminocarbonyl. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 15, 2013Publication date: April 24, 2014Inventors: George Philip Lahm, Jeffrey Keith Long, Ming Xu
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Publication number: 20140107149Abstract: 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: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: Eli Lilly and CompanyInventors: Zengyun AN, Liang CHEN, Shuhui CHEN, Jean Marie DEFAUW, Scott Dale HOLMSTROM, Ping HU, Chongzhi TANG, William Hunter WHITE, Wentao WU, Yang ZHANG
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Publication number: 20140107161Abstract: The present invention provides compounds of formula (I) wherein R1, R2, 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: ApplicationFiled: May 12, 2012Publication date: April 17, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
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Publication number: 20140100108Abstract: 3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.Type: ApplicationFiled: March 26, 2012Publication date: April 10, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht, Jeffrey Martin Hills, Philippe Rinolfi, Heinz KEHNE
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Patent number: 8686014Abstract: 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 sail 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: GrantFiled: July 24, 2009Date of Patent: April 1, 2014Assignee: Syngenta LimitedInventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Thomas Pitterna
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Publication number: 20140080877Abstract: A compound of formula (I): wherein A1, A2, A3, A4, 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 them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: November 25, 2013Publication date: March 20, 2014Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Renold, Werner Zambach, Peter Maienfisch, Michel Muehlebach
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Patent number: 8673951Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.Type: GrantFiled: January 20, 2011Date of Patent: March 18, 2014Assignee: Nissan Chemical Industries, Ltd.Inventors: Takeshi Mita, Yuki Furukawa, Ken-ichi Toyama, Manabu Yaosaka, Eitatsu Ikeda, Yoshihide Masuzawa, Mitsuaki Komoda
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Patent number: 8648081Abstract: 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: GrantFiled: May 8, 2012Date of Patent: February 11, 2014Assignee: Eli Lilly and CompanyInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Publication number: 20140038821Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Patent number: 8637496Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.Type: GrantFiled: June 2, 2008Date of Patent: January 28, 2014Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
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Patent number: 8633134Abstract: The invention relates to substituted amidine 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 amidine compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such substituted amidine compounds. The substituted amidine compounds of the present invention are defined by the following formula I: wherein A1 to A4, B1 to B3, R1 to R3, (R4)p, (R5)q, X and Y are defined as in the description.Type: GrantFiled: December 14, 2009Date of Patent: January 21, 2014Assignee: BASF SEInventors: Florian Kaiser, Karsten Koerber, Matthias Pohlman, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Wolfgang von Deyn, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Cecille Ebuenga
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Publication number: 20140011758Abstract: This invention recites isoxazoline substituted derivatives of Formula (1) stereoisomers thereof, geometric isomers thereof, veterinarily acceptable salts 5 thereof, compositions thereof, and their use as a parasiticide in animals. The variables A, W, R 1a, R 1b, R 1c, R 2, R 3, R 5, and n are as described herein.Type: ApplicationFiled: March 8, 2012Publication date: January 9, 2014Inventors: Valerie A. Vaillancourt, John A. Wendt, Graham M. Kyne, Sanjay Menon
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Patent number: 8623896Abstract: A compound of formula (I), wherein A1, A2, A3, A4, 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 them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: GrantFiled: December 16, 2008Date of Patent: January 7, 2014Assignee: Syngenta Crop Protection, LLCInventors: Peter Renold, Werner Zambach, Peter Maienfisch, Michel Muehlebach
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Patent number: 8623875Abstract: 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: GrantFiled: June 10, 2008Date of Patent: January 7, 2014Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Ty Wagerle, Ming Xu
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Patent number: 8618147Abstract: Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.Type: GrantFiled: January 28, 2013Date of Patent: December 31, 2013Assignee: The Feinstein Institute for Medical ResearchInventor: Yousef Al-Abed
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Publication number: 20130345221Abstract: 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: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: NOVARTIS AGInventors: Noëlle Gauvry, Steve Nanchen
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Patent number: 8609858Abstract: The present invention relates to novel spiro derivatives of parthenin prepared by the dipolar cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nitrile imide, ozone, azomethine imides, azomethine ylides etc. with exocyclic double bond of C ring (?-methylene-?-butyrolactone). Representative compounds have been screened for their anticancer activity against different cancer cell lines. ICs0 value of these analogues varies between 4.3 ?M to 93 ?M. A mechanistic correlation of their anticancer activity has been described. The results of the cytotoxicity test of the compounds studies indicated that the ?,?-unsaturated ketonic moiety in parthenin plays an important role in the maintenance of the high level of cytotoxicity.Type: GrantFiled: March 5, 2009Date of Patent: December 17, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Mahabalarao Sampath Kumar Halmuthur, Ajit Kumar Saxena, Subhash Chandra Taneja, Shashank Kumar Singh, Vijay Kumar Sethi, Naveed Ahmed Qazi, Sanghapal Damodhar Sawant, Mahendhar Reddy Doma, Abid Hussain Banday, Monika Verma, Ghularn Nabi Qazi
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Patent number: 8609706Abstract: The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.Type: GrantFiled: May 15, 2012Date of Patent: December 17, 2013Assignee: Infinity Discovery, Inc.Inventors: Alfredo C. Castro, Kristopher M. Depew, Michael J. Grogan, Charles W. Johannes, Edward B. Holson, Brian T. Hopkins, Gregg F. Keaney, Nii O. Koney, Tao Liu, David A. Mann, Marta Nevalainen, Stephane Peluso, Lawrence Blas Perez, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20130324538Abstract: 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 warm-blooded animals.Type: ApplicationFiled: February 9, 2012Publication date: December 5, 2013Inventors: Noëlle Gauvry, Steve Nanchen
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Patent number: 8598087Abstract: Disclosed is a solid form of 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide (Compound 1). Also disclosed are compositions containing a solid form of Compound 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a solid form of Compound 1 or a composition containing a solid form of Compound 1.Type: GrantFiled: May 19, 2011Date of Patent: December 3, 2013Assignee: E. I. du Pont de Nemours and CompanyInventor: Martin James Currie
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Patent number: 8598367Abstract: The present invention offers compounds or their salts expressed by formula (I) (in the formula, X indicates an alkyl group, or the like; Y indicates an alkyl group; Z indicates a respectively independent nitro group, or the like; n indicates any integer from 0 to 3; A indicates carbon atom, or the like, and hydrogen atom is bonded thereto in the case where the carbon atom is not substituted with Z; D indicates oxygen atom, or the like; W indicates hydrogen atom, or the like; R1 and R2 indicate respectively independent hydrogen atoms, or the like; R1 and R2 may be bonded, and may form a heterocycle together with the nitrogen atom between R1 and R2).Type: GrantFiled: January 25, 2013Date of Patent: December 3, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Jyun Iwata, Masahiro Kawaguchi
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Patent number: 8598366Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: GrantFiled: July 26, 2012Date of Patent: December 3, 2013Assignee: Synta Pharmaceuticals CorporationInventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
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Patent number: 8592418Abstract: The present 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: GrantFiled: June 11, 2011Date of Patent: November 26, 2013Assignee: Novartis AGInventors: Steve Nanchen, Noelle Gauvry, Thomas Goebel
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Patent number: 8563474Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.Type: GrantFiled: July 6, 2009Date of Patent: October 22, 2013Assignee: BASF SEInventors: Karsten Koerber, Florian Kaiser, Juergen Langewald
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Patent number: 8552040Abstract: Methods of use and pharmaceutical compositions for a genus of low molecular weight compounds comprising optionally substituted isoxazoline ring systems that act as inhibitors of MIF (macrophage migration inhibitory factor) are disclosed. Specifically, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatoid arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).Type: GrantFiled: April 14, 2011Date of Patent: October 8, 2013Assignee: CPSI Stockholder TrustInventor: Yousef Al-Abed
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Patent number: 8546357Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds.Type: GrantFiled: November 16, 2012Date of Patent: October 1, 2013Assignees: Eli Lilly and Company, Anacor Pharmaceuticals, Inc.Inventors: Tsutomu Akama, Terry William Balko, Jean Marie Defauw, Jacob J. Plattner, William Hunter White, Joseph Raymond Winkle, Yong-Kang Zhang, Yasheen Zhou
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Patent number: 8546389Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: GrantFiled: October 20, 2011Date of Patent: October 1, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Publication number: 20130245072Abstract: 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: ApplicationFiled: May 10, 2013Publication date: September 19, 2013Applicant: SYNGENTA CORP PROTECTION LLCInventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
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Patent number: 8530461Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
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Publication number: 20130225826Abstract: 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: ApplicationFiled: October 31, 2011Publication date: August 29, 2013Applicant: BASF SEInventors: Karsten Koerber, Markus Kordes, Michael Rack, Wolfgang Von Deyn, Florian Kaiser
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Publication number: 20130225586Abstract: The present invention provides a compound having Formula I or II: wherein B, R, X, Ar, and Y are defined herein, pharmaceutically acceptable salts thereof and pharmaceutically acceptable prodrugs thereof. The present invention also provides methods of making and using the compound.Type: ApplicationFiled: September 25, 2012Publication date: August 29, 2013Applicant: CPSI STOCKHOLDER TRUSTInventor: CPSI Stockholder Trust
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Publication number: 20130217736Abstract: Disclosed are compounds of Formula 1, wherein R1 is halogen, C1-C2 haloalkyl or C1-C2 haloalkoxy; R2 is H, halogen or cyano; R3 is H, halogen or CF3; R4 is H, C2-C7 alkylcarbonyl or C2-C7 alkoxycarbonyl; and R5 is C1-C6 alkyl or C1-C6 haloalkyl, each substituted with one substituent independently selected from hydroxy, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylaminocarbonyl and C3-C9 halodialkylaminocarbonyl. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Inventor: E. I. Du Pont de Nemours and Company
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Publication number: 20130217699Abstract: 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: ApplicationFiled: May 8, 2012Publication date: August 22, 2013Applicant: ELI LILLY AND COMPANYInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Patent number: 8513431Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: GrantFiled: July 9, 2012Date of Patent: August 20, 2013Assignee: E.I. du Pont de Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith