Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
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Patent number: 7799739Abstract: Novel biphenylcarboxamides of the formula (I) There is further provided a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 21, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 7799334Abstract: The present invention relates to pyrazolecarboxamides of the formula I in which the variables are as defined below: X is trifluoromethyl; R1 is F, Cl, Br, C1-C4-alkyl or C1-C4-haloalkyl; R2 is hydrogen, halogen or C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl or C3-C6-cycloalkyl; W is O or S; with the proviso that, if R3 is hydrogen and W is oxygen, a) R1 and R2 are not simultaneously methyl and F, respectively; b) R1 and R2 are not simultaneously trifluoromethyl and hydrogen or fluorine, respectively. to processes for preparing these compounds, to seeds and compositions comprising them and to methods for controlling harmful fungi.Type: GrantFiled: May 10, 2006Date of Patent: September 21, 2010Assignee: BASF AktiengesellschaftInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Wassilios Grammenos, Udo Hünger, Bernd Müller, Frank Schieweck, Anja Schwögler, Jan Klaas Lohmann, Joachim Rheinheimer, Jens Renner, Peter Schäfer
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Publication number: 20100234364Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 10, 2007Publication date: September 16, 2010Inventors: Arindrajit Basak, Jeff Jin, Jimmie Moore, Andrew M.K. Pennell, Sreenlvas Punna, Solomon Ungashe, Zheng Wei
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Patent number: 7795294Abstract: This invention is directed to a tetrahydro-2H-indazole pyrazole cannabinoid modulator compound of formula (I): or a form thereof, wherein p, R1, R2 and Ar are as herein described and * represents a chiral center, and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: February 13, 2007Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Fina Liotta, Huajun Lu, Michael P. Wachter, Mingde Xia
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Publication number: 20100216803Abstract: Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.Type: ApplicationFiled: March 25, 2008Publication date: August 26, 2010Applicant: Astellas Pharma Inc.Inventors: Tatsuya Zenkoh, Eisuke Nozawa, Keisuke Matsuura, Ryushi Seo
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Publication number: 20100204483Abstract: The present invention relates to a process for preparing hydrochloride-free 2-dihaloacyl-3-aminoacrylic esters by reacting acid fluorides with dialkylaminoacrylic acid derivatives.Type: ApplicationFiled: September 13, 2008Publication date: August 12, 2010Inventors: Sergii Pazenok, Norbert Lui
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Publication number: 20100197925Abstract: The present invention relates N-cycloalkyl-N-bicyclic-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group; T represents O, S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl group; X represents N or a CZ7 and Z2; Z3; L1 and L2 represent various substituents; their process of preparation; preparation intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: August 5, 2010Applicant: Bater SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Hadano Hiroyuki, Philippe Rinolfi, Jean-Pierre Vors
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Publication number: 20100197633Abstract: A compound of general formula (I): A process for preparing this compound. A compound of general formula (II) A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: October 4, 2006Publication date: August 5, 2010Applicant: BAYER CROPSCIENCE S.A.Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Patent number: 7767625Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: March 21, 2006Date of Patent: August 3, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Camilla Corsi, Josef Ehrenfreund, Clemens Lamberth, Hans Tobler
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Patent number: 7767827Abstract: Disclosed are pyrazole-1-carboxylate derivatives of the general formula (1), (wherein symbols are as defined in the specification), a process for the production thereof and processes for producing herbicidally active 3-aryloxypyrazole-1-carboxamide derivatives from the above compound and an intermediate therefor. According to this invention, there can be industrially advantageously produced 3-aryloxypyrazole-1-carboxamide derivatives that does not cause chemical damage on crops but exhibits excellent herbicidal activity against weeds that impair the growth of such crops.Type: GrantFiled: May 22, 2006Date of Patent: August 3, 2010Assignees: Kaken Pharmaceutical Co., Ltd., Sagami Chemical Research CenterInventors: Atsushi Uchida, Wakako Yokota, Kenji Hirai, Tomoyuki Yano
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Patent number: 7767706Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: February 25, 2008Date of Patent: August 3, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Patent number: 7767685Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g.Type: GrantFiled: June 25, 2007Date of Patent: August 3, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan Moorman, Mojgan Aghazadeh Tabrizi
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Publication number: 20100190779Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: July 31, 2008Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. Beaulieu, Paul J. Edwards, Martin Poirier, Jean Rancourt, Timothy A. Stammers
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Publication number: 20100184994Abstract: The present invention relates to a process for preparing 3-difluoromethyl-substituted pyrazole compounds of the formula (I) in which R1 is H, halogen, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, phenyl, naphthyl, hetaryl, cyano, —C(?O)—OR1a, —C(?O)—NR1bR1c, —C(?O)—SR1d or —C(?S)—SR1e; R2 is H, C1-C4-alkyl, benzyl or phenyl; R3 is H, halogen, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C8-cycloalkoxy, C2-C8-alkenyloxy, C1-C8-alkylthio, C1-C8-haloalkylthio, C3-C8-cyclo-alkylthio or C2-C8-alkenylthio; compounds of the formula (II.a) or (II.b), in which R1 and R3 each have one of the definitions given above; R4 is halogen, —OR4a, —SR4a, —O—SO2—R4a or an —NR4bR4c group; R5 and R6 are each C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, benzyl or phenyl, or, together with the nitrogen atom to which they are bonded, are a 3- to 8-membered heterocycle; Lewis acid adducts of compounds of the formula (II.b); the use of compounds of the formula (II.a) or (II.Type: ApplicationFiled: June 13, 2008Publication date: July 22, 2010Applicant: BASF SEInventors: Markus Nett, Thomas Grote, Jan Klaas Lohmann, Jochen Dietz, Sebastian Peer Smidt, Michael Rack, Thomas Zierke
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Publication number: 20100173966Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 6, 2008Publication date: July 8, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, Harald Walter, Hans Tobler
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Publication number: 20100174093Abstract: A process for the production of a compound of formula (I), which comprises a) reacting a compound of formula (II), wherein R1 and R2 are both independently C1-C6 alkyl, with methylhydrazine in the presence of water and a water-immiscible organic solvent being inert in saponification reactions, to form a compound of formula (III) wherein R1 is as defined for formula (II) and b) saponifying that compound in situ leading to the formation of the compound of formula (I) by b1) adding a base to form the anion of the compound of formula (I) and then adding an; acid to form the compound of formula (I); or b2) adding an acid to form the compound of formula (I).Type: ApplicationFiled: May 13, 2008Publication date: July 8, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Fanny Giordano, Thomas Vettiger, Juerg Gustav Wiss
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Publication number: 20100174094Abstract: The present invention relates to a process for preparing N-substituted (3-dihalomethylpyrazol-4-yl)carboxamides of the formula (I) in which R1 is optionally substituted phenyl or C3-C7-cycloalkyl, R1a is hydrogen or fluorine, or R1a together with R1 is optionally substituted C3-C5-alkanediyl or C5-C7-cycloalkanediyl, R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C4-alkoxy-C1-C2-alkyl, X is F or Cl and n is 0, 1, 2 or 3; which comprises A) providing a compound of the formula (II) in which X is F or Cl, Y is Cl or Br and R2 has one of the meanings given above and B) reacting a compound of the formula (II) with carbon monoxide and a compound of the formula (III) in which R1, R1a and n have one of the meanings given above; in the presence of a palladium catalyst; to intermediates used for the preparation according to the process according to the invention, and also to processes for their preparation.Type: ApplicationFiled: May 30, 2008Publication date: July 8, 2010Applicant: BASF SEInventors: Thomas Zierke, Joachim Rheinheimer, Michael Rack, Sebastian Peer Smidt, Ansgar Gereon Altenhoff, Joachim Schmidt-Leithoff, Nina Challand
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Publication number: 20100160377Abstract: The invention relates to derivatives of pyrazole 3,5-carboxylates, of general formula (I): in which R1, R2, R3, R4, R5, X, Y, V, W and n are as defined herein. The invention also relates to salts of these compounds as well as hydrates or of solvates, enantiomers, diastereoisomers and mixtures thereof. Also disclosed are the methods of preparation and application in therapeutics of compounds of formula (I).Type: ApplicationFiled: December 24, 2009Publication date: June 24, 2010Applicant: SANOFI-AVENTISInventors: Yann FORICHER, Martin SMRCINA, Viviane VAN DORSSELAER, Fabienne WEBER
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Publication number: 20100152266Abstract: This invention relates to novel intermediates used in the preparation of iodopyrazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, and to the preparation of such intermediates.Type: ApplicationFiled: February 5, 2010Publication date: June 17, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Publication number: 20100144817Abstract: The present invention relates to N-cycloalkyl-benzyl-thiocarboxamide or N-cycloalkyl-benzyl-N-substituted-carboximidamide amide derivatives of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl; T represents S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl and Z2; Z3, X and n represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors
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Publication number: 20100144785Abstract: The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3 and B represents an aromatic, 6-membered, fused, (hetero)aryl; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch
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Patent number: 7732375Abstract: The invention relates to novel hexylcarboxanilides of the formula (I) in which L, R1, R3 and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: October 12, 2004Date of Patent: June 8, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Olaf Gebauer, Jörg Nico Greul, Benoit Hartmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Publication number: 20100137394Abstract: The invention provides inhibitors of Wnt signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein R1 to R7 and Z are as defined herein.Type: ApplicationFiled: April 29, 2008Publication date: June 3, 2010Applicants: Grenentech, Inc., Curis, Inc.Inventors: Shirley Ann Brunton, Janet L. Gunzner, Tom Coulter, John H.A Stibbard, James C. Marsters, JR.
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Publication number: 20100137291Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: ApplicationFiled: December 11, 2009Publication date: June 3, 2010Inventors: Richard A. EARL, Maiko EZAWA, Xinqin FANG, David S. GARVEY, Ricky D. GASTON, Subhash P. KHANAPURE, L. Gordon LETTS, Chia-En LIN, Ramani R. RANATUNGA, Stewart K. RICHARDSON, Joseph D. SCHROEDER, Cheri A. STEVENSON, Shiow-Jyi WEY
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Patent number: 7728019Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: December 1, 2003Date of Patent: June 1, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Patent number: 7728029Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: March 14, 2007Date of Patent: June 1, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Kevin William Anderson, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Jr., Kevin Richard Guertin, Nancy-Ellen Haynes, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Lida Qi, Pamela Loreen Rossman, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Qiang Zhang
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Publication number: 20100130358Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: ApplicationFiled: November 29, 2007Publication date: May 27, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Michel Muehlebach, Gerald Wayne Craig
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Patent number: 7723371Abstract: The invention relates to a fungicidally active compound of the general Formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R3, R4 and R5; R1 and R2 are independently H, halo, C1-4 alkyl or C1-4 haloalkyl; and R3, R4 and R5 are each, independently, H, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 haloalkoxy, provided that at least one of R3, R4 and R5 is not H; to the preparation of these compounds, to novel intermediates used in their preparation, to agrochemical compositions which comprise at least one of the novel compounds as an active ingredient, to the preparation of the compositions and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestations of plants by phytopathogenic microorganisms, especially fungi.Type: GrantFiled: November 13, 2006Date of Patent: May 25, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Camilla Corsi, Josef Ehrenfreund, Hans Tobler
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Patent number: 7714144Abstract: The present invention relates to a novel process for preparing known 5-fluoro-1,3-dialkyl-1H-pyrazole-4-carbonyl fluorides which can be used as starting materials for active fungicidal ingredients by a halex reaction.Type: GrantFiled: September 5, 2006Date of Patent: May 11, 2010Assignee: Bayer CropScience AGInventors: Arnd Neeff, Sergiy Pazenok
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Patent number: 7705160Abstract: This invention relates to a method for preparing a 3-halo-4,5-dihydro-1H-pyrazole compound of Formula I comprising contacting with HX1 a different 4,5-dihydro-1H-pyrazole compound of Formula II wherein X1 is halogen and L, R, k and X2 are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein X1, R3, R6, R7, R8a, R8b and n are as defined in the disclosure.Type: GrantFiled: December 21, 2007Date of Patent: April 27, 2010Assignee: E.I. du Pont de Nemours and CompanyInventor: Gary David Annis
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Publication number: 20100099568Abstract: The present invention relates to heteroaroyl-substituted serinamides of the formula (I) in which the variables A and R1 to R6 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of the compositions comprising these compounds for controlling unwanted plants.Type: ApplicationFiled: January 10, 2008Publication date: April 22, 2010Applicant: BASF SEInventors: Matthias Witschel, Dschun Song, Eike Hupe, Trevor William Newton, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt
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Publication number: 20100093707Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji NAKAMURA, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100087494Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: February 21, 2008Publication date: April 8, 2010Inventors: Pierre-Yves Coqueron, Rudiger Fischer, Oliver Gaertzen, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Klaus Kunz, Darren Mansfield, Amos Mattes, Oswald Ort, Philippe Desbordes
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Patent number: 7687531Abstract: This invention relates to novel iodopyrazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, to a plurality of processes for preparing these compounds and to their use for controlling unwanted microorganisms. This invention further relates to novel intermediates and their preparation.Type: GrantFiled: May 12, 2004Date of Patent: March 30, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Publication number: 20100074863Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 17, 2009Publication date: March 25, 2010Inventors: Yat Sun Or, Ce Wang, Xiaowen Peng, Lu Ying, Yao-Ling Qiu
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Publication number: 20100069646Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylates of the formula I in which R1 is C1-C8-alkyl, C3-C8-cycloalkyl, C1-C4-alkoxy-C1-C4-alkyl, etc.; and R2 is hydrogen, C1-C4-alkyl, benzyl or phenyl, wherein a) a compound of the general formula II in which X is fluorine, chlorine or bromine, R1 has one of the meanings given above and R4 is C1-C8-alkyl, C3-C8-cycloalkyl, C2-C8-alkenyl, benzyl or phenyl, is reacted with a silane compound of the general formula R3nSiCl(4-n) in which n is 1, 2 or 3 and the substituents R3 are independently of one another selected from the group consisting of C1-C8-alkyl and phenyl and with a metal selected from the metals of groups 1, 2, 3, 4 and 12 of the Periodic Table of the Elements having a redox potential of less than ?0.7 V, based on a normal hydrogen electrode (at 25° C. and 101.Type: ApplicationFiled: November 2, 2007Publication date: March 18, 2010Applicant: BASF SEInventors: Martin Sukopp, Michael Rack, Sebastian Peer Smidt, Sandra Löhr, Michael Keil, Jochen Dietz, Joachim Rheinheimer, Thomas Grote, Thomas Zierke, Jan Klaas Lohmann
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Patent number: 7678924Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 is C1-C4haloalkyl; R2 is C1-C6alkyl and R3 is methyl or ethyl, by reaction of compounds of formula II wherein the substituents are as defined for formula I, with compounds of formula III wherein R3 is as defined for formula I and n is 0 or 1.Type: GrantFiled: October 19, 2005Date of Patent: March 16, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Camilla Corsi, Josef Ehrenfreund, Clemens Lamberth, Hans Tobler
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Publication number: 20100056786Abstract: The present invention relates to a novel process for preparing known fungicidally active alkylanilides from 2-alkylhaloaromatics and heterocyclylamides.Type: ApplicationFiled: July 12, 2007Publication date: March 4, 2010Applicant: Bayer CropScience AGInventor: Alexander Straub
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Publication number: 20100056758Abstract: The invention relates to the use of a selective inhibitor of CB2 receptor expression and/or for the manufacture of a medicament indented for the treatment and/or the prevention of obesity and obesity-related disorders.Type: ApplicationFiled: April 4, 2008Publication date: March 4, 2010Inventors: Vanessa Deveaux, Fatima Teixeira Clerc, Syivie Manin, Sophie Lotersztajn, Ariane Mallat, Jeanne Tran-Van-Nhieu
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100041899Abstract: The present invention relates to a process for preparing substituted pyrazolyl chlorides by chlorinating aldehydes of the formula (II) under free-radical conditions.Type: ApplicationFiled: January 9, 2008Publication date: February 18, 2010Applicant: Bayer Crop Science AGInventors: Norbert Lui, Jens-Dietmar Heinrich, Alexander Straub, Thomas Wollner, James Mark Ford
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Patent number: 7659408Abstract: Pyrazole carboxamides of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.Type: GrantFiled: August 3, 2004Date of Patent: February 9, 2010Assignee: Merck Sharp & Dhome Corp.Inventors: Ying-Duo Gao, Xin Gu, Nancy J. Kevin, Sherman T. Waddell
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Publication number: 20100029478Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: ApplicationFiled: June 6, 2007Publication date: February 4, 2010Inventors: Bernd Alig, Rüdiger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Görgens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
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Publication number: 20100029950Abstract: This invention provides compounds of Formula I, methods for their preparation and use for preparing compounds of Formula II wherein R1, R2, R3, R5, R6, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R7, R8, R9 and n are as defined in the disclosure. This invention also pertains to certain compounds of Formula 4 and 6 used to prepare compounds of Formula I. wherein R1, R2, R5, X and n are as defined in the disclosure.Type: ApplicationFiled: October 13, 2009Publication date: February 4, 2010Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Gary David Annis, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 7655680Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.Type: GrantFiled: May 16, 2005Date of Patent: February 2, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Isao Takemura, Kenji Watanabe, Kunio Oshima, Nobuaki Ito, Junpei Haruta, Hidetaka Hiyama, Masatoshi Chihiro, Hideki Kawasome, Yoko Sakamoto, Hironobu Ishiyama, Takumi Sumida, Kazuhiko Fujita, Hideki Kitagaki
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Publication number: 20100022780Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with at least one compound of Formula 3 in the presence of a solvent comprising one or more organic solvents selected from ethers and nitrites and a catalytically effective amount of a palladium complex comprising at least one tertiary phosphine ligand of Formula 4 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; M1 is an alkali metal; and R5, R6 and R7 are defined in the disclosure; provided that when R2 is Cl, then X is Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the aforedescribed method.Type: ApplicationFiled: December 5, 2007Publication date: January 28, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Joerg Bruening, Albert Loren Casalnuovo, Vladimir Grushin
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Publication number: 20100022611Abstract: The present invention pertains to cannabinoid (CB) receptor neutral antagonists, and especially CB1 neutral antagonists, and including, for example, certain 1,5-di-aryl-pyrazole compounds.Type: ApplicationFiled: February 7, 2008Publication date: January 28, 2010Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEENInventors: Iain Robert Greig, Ruth Alexandra Ross, Roger Guy Pertwee