Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
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Patent number: 7919632Abstract: The present invention relates to a novel process for preparing known fungicidally active 1,3-dimethyl-5-fluoro-1H-pyrazole-4-carboxamides from the corresponding acid fluoride and aniline derivatives in the absence of an acid acceptor.Type: GrantFiled: June 7, 2006Date of Patent: April 5, 2011Assignee: Bayer Cropscience AGInventors: Arnd Neeff, Sergiy Pazenok
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Publication number: 20110077251Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2010Publication date: March 31, 2011Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
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Publication number: 20110071291Abstract: A hydrazide compound represented by the formula (1): (wherein R1, R2, R3, R4, A1, A2, J, Q and n are defined in the specification) has excellent pesticidal activity.Type: ApplicationFiled: November 19, 2010Publication date: March 24, 2011Inventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
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Patent number: 7910606Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: September 18, 2009Date of Patent: March 22, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David William Will, Hans Matter
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Patent number: 7906656Abstract: 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: GrantFiled: February 5, 2010Date of Patent: March 15, 2011Assignee: 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: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Publication number: 20110060022Abstract: 4-[4-(2-Adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid and pharmaceutically-acceptable salts thereof and a particular crystalline form of the Agent (Form 1); their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: November 5, 2008Publication date: March 10, 2011Applicant: ASTRAZENECA ABInventors: Martin Packer, James Stewart Scott, Andrew Stocker, Paul Robert Owen Whittamore
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Publication number: 20110054183Abstract: A process for preparing arylcarboxamides of the formula (I) where Ar =a mono- to trisubstituted phenyl, pyridyl or pyrazolyl ring, where the substituents are selected from halogen, Ci-C4-alkyl and C1-C4-haloalkyl; M =thienyl or phenyl, which may bear a halogen substituent; Q =direct bond, cyclopropylene, fused bicycio[2.2.1]heptane or bicyclo[2.2.1]heptene ring; R1 =hydrogen, halogen, C1-C6-alkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, mono- to trisubstituted phenyl, where the substituents are selected from halogen and trifluoromethylthio, or cyclopropyl; by reacting an acid chloride of the formula (II) with an arylamine (III) in a suitable nonaqueous solvent, wherein, in the absence of an auxiliary base, a) the acid chloride (II) is initially charged, b) a pressure of from 0 to 700 mbar is established, c) the arylamine (III) is metered in in an approximately stoichiometric amount and d) the product of value is isolated.Type: ApplicationFiled: May 6, 2009Publication date: March 3, 2011Inventors: Wolfgang Reichert, Christopher Koradin, Sebastian Peer Smidt, Volker Maywald, Bernd Wolf, Michael Rack, Thomas Zierke, Michael Keil
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Publication number: 20110046371Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.Type: ApplicationFiled: April 30, 2009Publication date: February 24, 2011Applicant: BASF SEInventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
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Patent number: 7893098Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5;Type: GrantFiled: September 25, 2009Date of Patent: February 22, 2011Assignee: Sepracor Inc.Inventors: Q. Kevin Fang, Seth Hopkins, Michele Heffernan, Milan Chytil
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Publication number: 20110040096Abstract: The present invention relates to a process for preparing 2-(aminomethylidene)-4,4-dihalo-3-oxobutyric esters of the formula (I), wherein R1, R2, R3 are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl, and/or R2 together with R3 and the nitrogen atom to which the two radicals are attached are a heterocyclic radical, in which a corresponding 3-aminoacrylic ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or alkaline earth metal fluoride; and the further conversion of halogen-substituted 2-(aminomethylidene)-3-oxobutyric esters of the formula (I) to halomethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.Type: ApplicationFiled: April 30, 2009Publication date: February 17, 2011Applicant: BASF SEInventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
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Publication number: 20110034495Abstract: A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.Type: ApplicationFiled: November 22, 2006Publication date: February 10, 2011Applicant: INTERMUNE, INC.Inventors: Scott D. Seiwert, Karl Kossen, Vladimir Serebryany
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Publication number: 20110034516Abstract: The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: December 12, 2008Publication date: February 10, 2011Applicant: ACTELIONInventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Heinz Fretz, Corinna Grisostomi, Xavier Leroy, Julien Pothier, Sylvia Richard-Bildstein
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Publication number: 20110028735Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives with hydrazines in the presence of carbonyl compounds.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Applicant: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui, Arnd Neeff
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Publication number: 20110028729Abstract: The present invention relates to a process for preparing 1-aryl-substituted pyrazoles, comprising the reaction of alkoxy enones and enamino ketones with arylhydrazine derivatives to give 1-aryl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-aryl-substituted trihalomethylpyrazoles, and the further processing thereof.Type: ApplicationFiled: July 23, 2010Publication date: February 3, 2011Applicant: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui
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Publication number: 20110028529Abstract: New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: March 5, 2010Publication date: February 3, 2011Applicant: AstraZeneca ABInventor: Gary Peter TOMKINSON
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Publication number: 20110028530Abstract: New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: March 5, 2010Publication date: February 3, 2011Applicant: AstraZeneca ABInventor: Gary Peter TOMKINSON
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Patent number: 7879897Abstract: The invention relates to 5-sub-stituted-oxyalkylaminopyrazole derivatives of the formula or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests including arthropods and helminths.Type: GrantFiled: August 21, 2004Date of Patent: February 1, 2011Assignee: Merial LimitedInventors: David Teh-Wei Chou, Stefan Schnatterer, Werner Knauf, Karl Seeger
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Patent number: 7879761Abstract: The present invention relates to heteroaroyl-substituted serineamides 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: GrantFiled: March 29, 2006Date of Patent: February 1, 2011Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Rack, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt
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Patent number: 7879760Abstract: This invention relates to novel isopentylcarboxanilides 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: February 1, 2011Assignee: 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: 20110021538Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.Type: ApplicationFiled: April 1, 2009Publication date: January 27, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
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Publication number: 20110021540Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: January 27, 2011Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria Ek, Jorg Holenz, Martin H. Johansson, Annika Kers, Katja Narhi, Gunnar Nordvall, Liselotte Ohberg, Daniel Sohn, Jenny Viklund, Stefan Von Berg
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Publication number: 20110015406Abstract: A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl group or an acyl group, or together represent an atomic group that forms a 5- or 6-membered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl group; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.Type: ApplicationFiled: March 11, 2009Publication date: January 20, 2011Applicant: Mitsui Chemicals Agro, Inc.Inventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
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Patent number: 7872146Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.Type: GrantFiled: May 6, 2006Date of Patent: January 18, 2011Assignee: Bayer CropScience AGInventors: Thierry Eynard, Cécile Franc
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Publication number: 20110009457Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.Type: ApplicationFiled: December 9, 2008Publication date: January 13, 2011Applicant: BAYER CROPSCIENCE AGInventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
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Publication number: 20110009642Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.Type: ApplicationFiled: February 12, 2009Publication date: January 13, 2011Applicant: Bayer Cropscience AGInventor: Sergii Pazenok
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Publication number: 20110009409Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 2, 2010Publication date: January 13, 2011Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
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Publication number: 20110004002Abstract: A process for preparing alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrates (VI) where R is methyl or ethyl, from crude reaction mixtures of alkyl 4,4-difluoroacetoacetates (I) by a) reacting where M is a sodium or potassium ion, and without additional solvent to form an enolate (V) b) releasing the corresponding alkyl 4,4-difluoroacetoacetate (I) from the enolate (V) by means of acid, c) removing the salt formed from cation M and acid anion as a solid and d) converting (I), without isolation from the crude reaction mixture, to the alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrate (VI), and the use of (VI) for preparing 1-methyl-3-difluoromethyl-pyrazol-3-ylcarboxyates VIIType: ApplicationFiled: February 27, 2009Publication date: January 6, 2011Applicant: BASF SEInventors: Volker Maywald, Sebastian Peer Smidt, Bernd Wolf, Christopher Koradin, Thomas Zierke, Michael Rack, Michael Keil
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Publication number: 20110003999Abstract: The present invention relates to a process for preparing substituted biphenylanilides of the formula I which comprises reacting a compound of formula II in the presence of a base and of a palladium catalyst selected from the group of: a) palladium-triarylpliosphine or -trialkylphosphine complex with palladium in the zero oxidation state, b) salt of palladium in the presence of triarylphospine or trialkylphosphine as a complex ligand or c) metallic palladium, optionally applied to support, in the presence of triarylphosphine or trialkylphosphine, in a solvent, with a diphenylborinic acid according to formula (III)Type: ApplicationFiled: February 17, 2009Publication date: January 6, 2011Applicant: Bayer CropScience AGInventor: Michael DOCKNER
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Publication number: 20110003998Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; X is Br or Cl; and R5, R6, R7 and R8 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 4 wherein R11, R12, R13 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.Type: ApplicationFiled: March 4, 2009Publication date: January 6, 2011Inventor: Donald J. Dumas
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Patent number: 7863460Abstract: In a process for producing 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylate (3) by a reaction of 2-alkoxymethylenefluoroacylacetate (1) and hydrazine (2), the reaction is conducted in the presence of a base and water, to produce 1-substituted-3-fluoroalkylpyrazole-4-carboxylate (3) with high selectivity and yield. This novel process enables to produce 1-substituted-3-fluoroalkylpyrazole-4-carboxylate (3), which is useful as an intermediate for pharmaceuticals and agrochemicals, with high selectivity and yield by simple and safe operations.Type: GrantFiled: February 23, 2006Date of Patent: January 4, 2011Assignees: Sagami Chemical Research Center, Japan Finechem Company, Inc.Inventors: Hidenori Aihara, Wakako Yokota, Tetsu Yamakawa, Kenji Hirai
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Publication number: 20100331302Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 8, 2010Publication date: December 30, 2010Applicant: Chemocentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20100324071Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Yan Shi, Peter T. W. Cheng, Ying Wang, Denis E. Ryono
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Publication number: 20100292273Abstract: Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*.Type: ApplicationFiled: December 8, 2008Publication date: November 18, 2010Applicant: 7TM PHARMA A/SInventors: Jean Marie Receveur, Emelie Bjurling, Anthony Murray, Thomas Hoegberg, Peter Aadal Nielsen, Jean-Michel Linget, Pia Karina Noerregaard, Dorthe Almholt
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Publication number: 20100286144Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.Type: ApplicationFiled: July 21, 2010Publication date: November 11, 2010Inventors: Yoko TAKAHASHI, Ryu Nagata, Kantaro Ushiroda
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Publication number: 20100286221Abstract: The present invention relates to N-cycloalkyl-benzyl-amide derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions:Type: ApplicationFiled: November 15, 2006Publication date: November 11, 2010Inventors: Darren Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Stephanie Gary, Stephane Carbonne, Ralf Dunkel, Arounarith Tuch, Jean-Pierre Vors
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Publication number: 20100280251Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further 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 method disclosed above.Type: ApplicationFiled: December 18, 2007Publication date: November 4, 2010Applicant: E.I. Du Pont De Nemours and CompanyInventors: Joerg Bruening, Gary David Annis, Martin James Currie, Donald J. Dumas, Rafael Shapiro
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Patent number: 7820708Abstract: Novel carboxamides of the formula (I) The present application also relates to 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: October 26, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste
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Patent number: 7820830Abstract: The present invention relates to a novel process for the preparation of a compound of general formula (I): wherein R1 is H or C1-4 alkyl and R2 is difluoromethyl or trifluoromethyl, which comprises reacting a compound of general formula (II): wherein R1 has the meaning given above and X is chloro or bromo, with a compound of general formula (III): wherein R2 has the meaning given above, in the presence of a base, a palladium catalyst and a ferrocenyl biphoshine ligand of the Josiphos type, the reaction being carried out in an ether solvent at a reflux temperature of at least 100° C.Type: GrantFiled: November 13, 2006Date of Patent: October 26, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Camilla Corsi, Josef Ehrenfreund, Hans Tobler
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Publication number: 20100267741Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas Ia, Ib, IIa, and IIb) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: April 19, 2010Publication date: October 21, 2010Inventors: Stephen David Penrose, Kevin James Doyle
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Publication number: 20100267687Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: ApplicationFiled: November 13, 2008Publication date: October 21, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio Nakamura, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Patent number: 7812040Abstract: This invention is directed to a compound of the formula Ia or Ib, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-iType: GrantFiled: June 12, 2006Date of Patent: October 12, 2010Assignee: Pfizer Inc.Inventor: Travis T Wager
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Publication number: 20100255996Abstract: The present invention relates to a new crystalline form of 3-(Difluormethyl)-1-methyl-N-(3?,4?,5?-trifluor[1,1?-biphenyl]-2-yl)-1H-pyrazol-4-carboxamide. The invention also relates to processes for the production of this crystalline form and formulations for plant protection which contain the crystalline form of 3-(Difluormethyl)-1-methyl-N -(3?,4?,5?-trifluor[1,1?-biphenyl]-2-yl)-1H-pyrazol-4-carboxamide.Type: ApplicationFiled: July 7, 2008Publication date: October 7, 2010Applicant: BASF SEInventors: Heidi Emilia Saxell, Jochen Dietz, Sebastian Peer SMIDT, Cedric Dieleman
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Publication number: 20100256390Abstract: The present invention relates to novel processes for the production of compounds of formula (I) wherein Hal and Hal? are independently Cl or F, and R1 is H, Cl or F.Type: ApplicationFiled: June 16, 2008Publication date: October 7, 2010Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Martin Charles Bowden, Brian David Gott, David Anthony Jackson
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Publication number: 20100249091Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally subsType: ApplicationFiled: September 17, 2009Publication date: September 30, 2010Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Publication number: 20100249123Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.Type: ApplicationFiled: March 19, 2008Publication date: September 30, 2010Applicant: ADDEX PHARMA SAInventors: Beatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
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Publication number: 20100247435Abstract: The present invention provides a method for determination of neural activity in a sample. The method of the invention is useful for the determination of neural activity in both in vivo and in vitro samples and is particularly useful in providing diagnostic information in subjects suspected to have a neurological condition that leads to disturbed neurological signalling. Also provided by the invention are compounds suitable for use in the method of the invention, and a pharmaceutical composition useful for carrying out the method of the invention.Type: ApplicationFiled: June 12, 2008Publication date: September 30, 2010Inventor: Erik Arstad
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Publication number: 20100240907Abstract: The present invention relates to novel processes for the production of compounds of formula (I) wherein Hal and Hal? are independently selected from Cl and F, and R1 is selected from Cl, F and H.Type: ApplicationFiled: June 16, 2008Publication date: September 23, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Martin Charles Bowden, Brian David Gott, David Anthony Jackson, Lacob Gutsu
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Publication number: 20100240659Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: , its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.Type: ApplicationFiled: May 7, 2008Publication date: September 23, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani