Benzene Ring Is Bonded Directly To Ring Nitrogen Of The Diazole Ring (e.g., 1-phenyl-3-methyl-5-pyrazolone; Antipyrine, Etc.) Patents (Class 548/371.1)
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Patent number: 10538493Abstract: The present invention relates to a process to produce highly purified crystalline 1-(4-chlorophenyl)pyrazol-3-ol (I).Type: GrantFiled: November 9, 2017Date of Patent: January 21, 2020Assignee: BASF SEInventors: Volker Maywald, Roland Goetz, Daniel Saelinger, Timo Frassetto, Stefan Gropp
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Patent number: 9035070Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: GrantFiled: July 28, 2011Date of Patent: May 19, 2015Assignee: ESTEVE QUÍMICA, S.A.Inventors: Martí Bartra Sanmarti, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
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Patent number: 9006280Abstract: Pyrazolone derivative formulations are provided. The formulations include a pyrazolone derivative active agent, e.g., edaravone, and an amphiphilic solubilizing agent. Also provided are methods of making and using the subject formulations.Type: GrantFiled: November 18, 2009Date of Patent: April 14, 2015Assignees: Teikoku Pharma USA, Inc., Techno Guard Co., Ltd.Inventor: Kiichiro Nabeta
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Patent number: 8859607Abstract: The present invention relates to crystalline complexes comprising at least one agriculturally active organic compound A having at least one functional moiety which is capable as serving as a hydrogen acceptor in a hydrogen bond and thiophanate-methyl.Type: GrantFiled: February 8, 2008Date of Patent: October 14, 2014Assignee: BASF SEInventors: Rafel Israels, Heidi Emilia Saxell, Matthias Bratz, Marco Kuhns, Peter Erk
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Patent number: 8816096Abstract: The present invention relates to a process for the preparation of 2-[[[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]phenyl]-hydroxylamine from the correspondingly substituted nitrobenzene compound.Type: GrantFiled: March 7, 2012Date of Patent: August 26, 2014Assignee: BASF SEInventors: Alexander Korte, Michael Puhl, Tao Qu, Marco Coppola
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Publication number: 20140162997Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: June 12, 2014Applicant: Janssen Pharmaceutica NVInventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
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Patent number: 8741809Abstract: The present invention relates to a novel liquid formulation for crop protection which comprises a) pyraclostrobin; b) at least one organic solvent S1 with a water solubility of less than 2 g/l at 20° C.; c) at least one organic solvent S2 with a water solubility of at least 2 g/l at 20° C., where S2 comprises at least one solvent S2.1 with a water solubility of more than 200 g/l at 20° C. and optionally at least one solvent S2.2 with a water solubility of 2 to 200 g/l at 20° C.; d) at least one anionic surface-active substance SA1; e) at least one nonionic surface-active substance SA2; and f) water. The invention also relates to the use of the crop protection formulation for treatment of plants and seed, and to corresponding methods.Type: GrantFiled: October 9, 2009Date of Patent: June 3, 2014Assignee: BASF SEInventors: Ulrike Troppmann, Wolfgang Meier, Guenter Oetter, Ulrich Steinbrenner, Tatjana Levy, Jurith Montag, Tanja Brunner, Reiner Weiler
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Process for the production of particles comprising active agrochemical ingredients in amorphous form
Patent number: 8735321Abstract: An object of the present invention is a process for the preparation of particles which comprise two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is the use of an agrochemical active ingredient for inhibiting the crystallization of another agrochemical active ingredient in a preparation process for particles which comprise the two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is particles which comprise two agrochemical active ingredients in amorphous form. The use in plant protection is also described.Type: GrantFiled: May 6, 2009Date of Patent: May 27, 2014Assignee: BASF SEInventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck -
Patent number: 8686184Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: May 18, 2012Date of Patent: April 1, 2014Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20140057353Abstract: An expanding agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful as a therapy for various hematopoietic diseases and useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy is provided. A method of producing hematopoietic stem cells and/or hematopoietic progenitor cells, which comprises expanding hematopoietic stem cells by culturing hematopoietic stem cells ex vivo in the presence of a compound represented by the formula following (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof (wherein R1 to R8 are as defined in the description).Type: ApplicationFiled: December 1, 2011Publication date: February 27, 2014Applicants: REPROCELL INCORPORATED, NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Ayako Asai, Taito Nishino, Makiko Yui
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Patent number: 8642780Abstract: The present invention relates to N-carbomethoxy-N-methoxy-(2-chloromethyl)-aniline compounds of the formula I, wherein: n is 0, 1, 2 or 3, each R1 is independently selected from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy. The invention also relates to processes and intermediates for preparing such compounds of formula I. The invention furthermore relates to processes for preparing 2-(pyrazol-3?-yloxymethylene)-anilides in which compounds of formula I are applied as precursors.Type: GrantFiled: March 17, 2011Date of Patent: February 4, 2014Assignee: BASF SEInventors: Maximilian Dochnahl, Bernd Mueller
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Publication number: 20140024124Abstract: A glycoprotein and/or a glycopeptide which are a test substance is heated in the presence of a pyrazolone derivative, an isoxazolone derivative, a hydantoin derivative, a rhodanine derivative, a maleimide derivative, or the like under a basic condition to cleave and label a post-translational modification group for analysis, thereby enabling analysis of a post-translational modification of a serine residue and/or a threonine residue.Type: ApplicationFiled: February 16, 2012Publication date: January 23, 2014Applicants: NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY, CELLSEED INC.Inventors: Yasuro Shinohara, Yasuhiro Takegawa, Naoki Fujitani, Jun-ichi Furukawa, Hideaki Sakai
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Publication number: 20130338373Abstract: The present invention relates to a process for the preparation of 2-[[[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl] phenyl]-hydroxylamine from the correspondingly substituted nitrobenzene compound.Type: ApplicationFiled: March 7, 2012Publication date: December 19, 2013Applicant: BASF SEInventors: Alexander Korte, Michael Puhl, Tao Qu, Marco Coppola
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Patent number: 8563748Abstract: The present invention relates to a process for the preparation of a ring-substituted N-phenylhydroxylamine by reduction of the correspondingly substituted nitrobenzene compound, wherein the reduction is carried out by reacting the substituted nitrobenzene compound with hydrazine in the presence of a ruthenium catalyst.Type: GrantFiled: September 20, 2011Date of Patent: October 22, 2013Assignee: BASF SEInventors: Alexander Korte, Michael Puhl, Marco Coppola
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Patent number: 8497381Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: February 25, 2009Date of Patent: July 30, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Publication number: 20130184472Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: ApplicationFiled: July 28, 2011Publication date: July 18, 2013Applicant: ESTEVE QUIMICA, S.A.Inventors: Martí Bartra Sanmartí, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
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Publication number: 20130178634Abstract: The present invention relates to a process for the preparation of a ring-substituted N-phenylhydroxylamine by reduction of the correspondingly substituted nitrobenzene compound, wherein the reduction is carried out by reacting the substituted nitrobenzene compound with hydrazine in the presence of a ruthenium catalyst.Type: ApplicationFiled: September 20, 2011Publication date: July 11, 2013Applicant: BASF SEInventors: Alexander Korte, Michael Puhl, Marco Coppola
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Patent number: 8470867Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: GrantFiled: February 9, 2010Date of Patent: June 25, 2013Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, Maria Montserrat Contijoch-Llobet
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Patent number: 8367710Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: GrantFiled: January 4, 2009Date of Patent: February 5, 2013Assignees: Jiangsu Hengrui Medicine Co. Ltd., Shanghai Hengrui Pharmaceutical Co. Ltd.Inventors: Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fei, Shenglan Wang, Li Wang
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Patent number: 8362271Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with apyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.Type: GrantFiled: September 3, 2010Date of Patent: January 29, 2013Assignee: BASF SEInventors: Maximilian Dochnahl, Gunter Lipowsky
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Publication number: 20130005986Abstract: The present invention relates to N-carbomethoxy-N-methoxy-(2-chloromethyl)-aniline compounds of the formula I, wherein: n is 0, 1, 2 or 3, each R1 is independently selected from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy. The invention also relates to processes and intermediates for preparing such compounds of formula I. The invention furthermore relates to processes for preparing 2-(pyrazol-3?-yloxymethylene)-anilides in which compounds of formula I are applied as precursors.Type: ApplicationFiled: March 17, 2011Publication date: January 3, 2013Applicant: BASF SEInventors: Maximilian Dochnahl, Bernd Mueller
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Patent number: 8329880Abstract: The invention relates to a process for preparing naphthalen-2-yl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: GrantFiled: April 24, 2009Date of Patent: December 11, 2012Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Antoni Torrens Jover, Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent
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Publication number: 20120308588Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120220463Abstract: The present invention relates to crystalline complexes of 4-hydroxy benzoic acid and selected pesticides. It also relates to agriculturally useful compositions of the complexes.Type: ApplicationFiled: October 28, 2010Publication date: August 30, 2012Applicant: BASF SEInventors: Heidi Emilia Saxell, Rafel Israels, Ansgar Schaefer, Matthias Bratz, Hans Wolfgang Hoeffken, Ingo Brode, Elisa Nauha, Maija Nissinen
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Publication number: 20120165544Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with apyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.Type: ApplicationFiled: September 3, 2010Publication date: June 28, 2012Applicant: BASF SEInventors: Maximilian Dochnahl, Gunter Lipowsky
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Patent number: 8168670Abstract: Pyrazolone derivative emulsion formulations are provided. The emulsion formulations include a pyrazolone derivative active agent, e.g., Edaravone, oil, water and an emulsifier. Also provided are methods of making and using the subject emulsion formulations.Type: GrantFiled: November 7, 2008Date of Patent: May 1, 2012Assignees: Teikoku Pharma USA, Inc., Techno Guard Co., Ltd.Inventor: Kiichiro Nabeta
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Patent number: 8163757Abstract: The present invention relates to compounds of formula (IA) or (IB) or pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: September 2, 2010Date of Patent: April 24, 2012Assignee: MediGene AGInventor: Ian Richard Matthews
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Publication number: 20120059163Abstract: In one aspect, the present invention provides a hyperpolarizable organic chromophore. The chromophore is a nonlinear optically active compound that includes a ?-donor conjugated to a ?-acceptor through a ?-electron conjugated bridge. In other aspects of the invention, donor structures and acceptor structures are provided. In another aspect of the invention, a chromophore-containing polymer is provided. In one embodiment, the chromophore is physically incorporated into the polymer to provide a composite. In another embodiment, the chromophore is covalently bonded to the polymer, either as a side chain polymer or through crosslinking into the polymer. In other aspects, the present invention also provides a method for making the chromophore, a method for making the chromophore-containing polymer, and methods for using the chromophore and chromophore-containing polymer.Type: ApplicationFiled: November 7, 2011Publication date: March 8, 2012Applicant: Optimer Photonics, Inc.Inventors: Vincent D. McGinniss, Steven M. Risser, Elizabeth Drotleff, Edward Jiang, Kevin B. Spahr
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Publication number: 20110071282Abstract: The invention relates to a process for preparing naphthalen-2-yl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: ApplicationFiled: April 24, 2009Publication date: March 24, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Antoni Torrens Jover, Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent
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Publication number: 20110065634Abstract: The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Inventors: William J. Greenlee, Andrew Stamford, Michael W. Miller, Duane Eugene DeMong
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Patent number: 7868185Abstract: The present invention relates to small molecule protein tyrosine phosphatase inhibitors, especially Shp-2 inhibitors, of formula (I) and/or (II), and to pharmaceutical compositions comprising them. The invention is also directed to the use of said compounds for the treatment of phosphatase-mediated diseases, especially cancer and metastasis. The invention further concerns a method for treating a proliferative disease, a genetic disorder, an autoimmune disease, an angiogenic disorder or cancer in a patient in need of such treatment, comprising administering to said patient a therapeutically effective amount of at least one compound of formula (I) and/or (II).Type: GrantFiled: June 1, 2006Date of Patent: January 11, 2011Assignees: Max-Delbruck-Centrum fur Molekulare Medizin, Forschungsverbund Berlin E, V.Inventors: Klaus Hellmuth, Walter Birchmeier, Joerg Rademann, Stefanie Grosskopf
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Publication number: 20100331342Abstract: Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1 and R2 independently represent H, or C1-C6 alkyl; R3 represents H; F; Cl; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or CI; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O)NR6R7, —NR7C(?O)R6, —NHC(?O)NR7R6 or —NHC(?S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may be interrupted by one or more —O—, —S— or —N(R8)— radicals wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —CF3;—OH; —SH; —NR8R8 wherein eType: ApplicationFiled: September 2, 2010Publication date: December 30, 2010Applicant: Medigene LimitedInventor: Ian Richard Matthews
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Publication number: 20100324091Abstract: A pyrazolone derivative represented by formula (I) below: wherein R1 to R3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis.Type: ApplicationFiled: June 23, 2008Publication date: December 23, 2010Applicant: Kowa Company, Ltd.Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
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Publication number: 20100316601Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: ApplicationFiled: January 4, 2009Publication date: December 16, 2010Inventors: Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fel, Shenglan Wang, Li Wang
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Publication number: 20100150899Abstract: The present invention relates to new pyrazolinone scavengers of free radicals, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113543Abstract: The present invention relates to crystalline complexes comprising at least one agriculturally active organic compound A having at least one functional moiety which is capable as serving as a hydrogen acceptor in a hydrogen bond and thiophanate-methyl.Type: ApplicationFiled: February 8, 2008Publication date: May 6, 2010Applicant: BASF SEInventors: Rafel Israels, Heidi Emilia Saxell, Matthias Bratz, Marco Kuhns, Peter Erk
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Patent number: 7652057Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: August 29, 2006Date of Patent: January 26, 2010Assignee: Hoffman-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V Mayweg, Werner Neidhart
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Publication number: 20090281102Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, U1, U2, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 1, 2009Publication date: November 12, 2009Applicant: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7456315Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: February 26, 2004Date of Patent: November 25, 2008Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20080269293Abstract: This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.Type: ApplicationFiled: August 22, 2007Publication date: October 30, 2008Inventors: Liguo Chi, Chulho Choi, Andrew G. Geyer, Robert M. Kennedy, Jeffery A. Pfefferkorn, Roy T. Winters
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Publication number: 20080119458Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor: wherein the variables are described in the specification.Type: ApplicationFiled: October 5, 2007Publication date: May 22, 2008Applicant: WyethInventors: William Ronald Solvibile, Ji-ln Kim, Marla Jean Williams, Jonathan Laird Gross, Albert Jean Robichaud
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Patent number: 7202367Abstract: The present invention concerns a process for arylating or vinylating or alkynating a nucleophilic compound. More particularly, the invention concerns arylating nitrogen-containing organic derivatives. The arylating or vinylating or alkynating process of the invention consists of reacting a nucleophilic compound with a compound carrying a leaving group and is characterized in that the reaction is carried out in the presence of an effective quantity of a catalyst based on a metallic element M selected from groups (VIII), (Ib) and (IIb) of the periodic table and at least one ligand comprising at least one imine function and at least one supplemental nitrogen atom as the chelating atoms.Type: GrantFiled: May 31, 2002Date of Patent: April 10, 2007Assignee: Rhodia ChimieInventors: Pascal Philippe Cellier, Henri-Jean Cristau, Jean-Francis Spindler, Marc Taillefer
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Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
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Patent number: 6864373Abstract: A process is provided for preparing a celecoxib-crystallization inhibitor composite wherein at least a detectable amount of celecoxib is in amorphous form. Also provided are compositions prepared according to such a process. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.Type: GrantFiled: May 8, 2003Date of Patent: March 8, 2005Assignee: Pharmacia CorporationInventors: Hong Zhuang, Ping Gao
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Patent number: 6838458Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: January 4, 2005Assignee: Pfizer, Inc.Inventor: Subas M. Sakya
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Publication number: 20040030151Abstract: A process is provided for preparing a celecoxib-crystallization inhibitor composite wherein at least a detectable amount of celecoxib is in amorphous form. Also provided are compositions prepared according to such a process. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.Type: ApplicationFiled: May 8, 2003Publication date: February 12, 2004Inventors: Hong Zhuang, Ping Gao
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Patent number: 6689805Abstract: A pyrazole-3-one derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: wherein: R1 and R2 each independently represent C1-C3 alkyl, aryl, or substituted aryl; R3 represents amino or methyl; R4 and R5 each independently represent hydrogen, C1-C3 alkyl, halogen, methyl substituted with halogen, C1-C3 alkoxy, cyano, or nitro; or a non-toxic salt thereof.Type: GrantFiled: June 13, 2003Date of Patent: February 10, 2004Assignee: CJ Corp.Inventors: Il Hwan Cho, Ji Young Noh, Sang Wook Park, Hyung Chul Ryu, Jee Woong Lim, Jong Hoon Kim, Myeong Yun Chae, Dal Hyun Kim, Sung Hak Jung, Hyun Jung Park, Young Hoon Kim, In Ki Min
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Publication number: 20030165561Abstract: The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.Type: ApplicationFiled: November 1, 2002Publication date: September 4, 2003Inventors: Rajinder Singh, Dane Goff, Henry Lu, Sarkiz D. Issakani, Thomas Sun
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Patent number: 6562856Abstract: The invention relates to novel pyrazolyl benzyl ethers, to a process for their preparation and to their use for controlling harmful organisms.Type: GrantFiled: June 14, 2002Date of Patent: May 13, 2003Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Bernd-Wieland Krüger, Fritz Maurer, Martin Vaupel, Astrid Mauler-Machnik, Ulrike Wachendorff-Neumann, Gerd Hänssler, Karl-Heinz Kuck, Christoph Erdelen, Peter Lösel
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Patent number: 6322775Abstract: The present invention relates to novel cosmetic compositions, in particular for coloring the skin and/or the hair, comprising, in a cosmetically acceptable support, at least one 4,5-pyrazolinedione. The invention also relates to novel 4,5-pyrazolinediones, to processes for their preparation and to their uses in the cosmetics field.Type: GrantFiled: January 6, 1999Date of Patent: November 27, 2001Assignee: L'Oreal S.A.Inventors: Gérard Malle, Laurent Vidal