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)
  • Patent number: 10538493
    Abstract: The present invention relates to a process to produce highly purified crystalline 1-(4-chlorophenyl)pyrazol-3-ol (I).
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: January 21, 2020
    Assignee: BASF SE
    Inventors: Volker Maywald, Roland Goetz, Daniel Saelinger, Timo Frassetto, Stefan Gropp
  • Patent number: 9035070
    Abstract: 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: Grant
    Filed: July 28, 2011
    Date of Patent: May 19, 2015
    Assignee: ESTEVE QUÍMICA, S.A.
    Inventors: Martí Bartra Sanmarti, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
  • Patent number: 9006280
    Abstract: 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: Grant
    Filed: November 18, 2009
    Date of Patent: April 14, 2015
    Assignees: Teikoku Pharma USA, Inc., Techno Guard Co., Ltd.
    Inventor: Kiichiro Nabeta
  • Patent number: 8859607
    Abstract: 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: Grant
    Filed: February 8, 2008
    Date of Patent: October 14, 2014
    Assignee: BASF SE
    Inventors: Rafel Israels, Heidi Emilia Saxell, Matthias Bratz, Marco Kuhns, Peter Erk
  • Patent number: 8816096
    Abstract: 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: Grant
    Filed: March 7, 2012
    Date of Patent: August 26, 2014
    Assignee: BASF SE
    Inventors: Alexander Korte, Michael Puhl, Tao Qu, Marco Coppola
  • Publication number: 20140162997
    Abstract: 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: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
  • Patent number: 8741809
    Abstract: 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: Grant
    Filed: October 9, 2009
    Date of Patent: June 3, 2014
    Assignee: BASF SE
    Inventors: Ulrike Troppmann, Wolfgang Meier, Guenter Oetter, Ulrich Steinbrenner, Tatjana Levy, Jurith Montag, Tanja Brunner, Reiner Weiler
  • Patent number: 8735321
    Abstract: 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: Grant
    Filed: May 6, 2009
    Date of Patent: May 27, 2014
    Assignee: BASF SE
    Inventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck
  • Patent number: 8686184
    Abstract: 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: Grant
    Filed: May 18, 2012
    Date of Patent: April 1, 2014
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20140057353
    Abstract: 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: Application
    Filed: December 1, 2011
    Publication date: February 27, 2014
    Applicants: REPROCELL INCORPORATED, NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Ayako Asai, Taito Nishino, Makiko Yui
  • Patent number: 8642780
    Abstract: 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: Grant
    Filed: March 17, 2011
    Date of Patent: February 4, 2014
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Bernd Mueller
  • Publication number: 20140024124
    Abstract: 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: Application
    Filed: February 16, 2012
    Publication date: January 23, 2014
    Applicants: NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY, CELLSEED INC.
    Inventors: Yasuro Shinohara, Yasuhiro Takegawa, Naoki Fujitani, Jun-ichi Furukawa, Hideaki Sakai
  • Publication number: 20130338373
    Abstract: 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: Application
    Filed: March 7, 2012
    Publication date: December 19, 2013
    Applicant: BASF SE
    Inventors: Alexander Korte, Michael Puhl, Tao Qu, Marco Coppola
  • Patent number: 8563748
    Abstract: 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: Grant
    Filed: September 20, 2011
    Date of Patent: October 22, 2013
    Assignee: BASF SE
    Inventors: Alexander Korte, Michael Puhl, Marco Coppola
  • Patent number: 8497381
    Abstract: 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: Grant
    Filed: February 25, 2009
    Date of Patent: July 30, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
  • Publication number: 20130184472
    Abstract: 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: Application
    Filed: July 28, 2011
    Publication date: July 18, 2013
    Applicant: ESTEVE QUIMICA, S.A.
    Inventors: Martí Bartra Sanmartí, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
  • Publication number: 20130178634
    Abstract: 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: Application
    Filed: September 20, 2011
    Publication date: July 11, 2013
    Applicant: BASF SE
    Inventors: Alexander Korte, Michael Puhl, Marco Coppola
  • Patent number: 8470867
    Abstract: 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: Grant
    Filed: February 9, 2010
    Date of Patent: June 25, 2013
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, Maria Montserrat Contijoch-Llobet
  • Patent number: 8367710
    Abstract: 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: Grant
    Filed: January 4, 2009
    Date of Patent: February 5, 2013
    Assignees: 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
  • Patent number: 8362271
    Abstract: 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: Grant
    Filed: September 3, 2010
    Date of Patent: January 29, 2013
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Gunter Lipowsky
  • Publication number: 20130005986
    Abstract: 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: Application
    Filed: March 17, 2011
    Publication date: January 3, 2013
    Applicant: BASF SE
    Inventors: Maximilian Dochnahl, Bernd Mueller
  • Patent number: 8329880
    Abstract: 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: Grant
    Filed: April 24, 2009
    Date of Patent: December 11, 2012
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Antoni Torrens Jover, Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent
  • Publication number: 20120308588
    Abstract: 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: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20120220463
    Abstract: 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: Application
    Filed: October 28, 2010
    Publication date: August 30, 2012
    Applicant: BASF SE
    Inventors: Heidi Emilia Saxell, Rafel Israels, Ansgar Schaefer, Matthias Bratz, Hans Wolfgang Hoeffken, Ingo Brode, Elisa Nauha, Maija Nissinen
  • Publication number: 20120165544
    Abstract: 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: Application
    Filed: September 3, 2010
    Publication date: June 28, 2012
    Applicant: BASF SE
    Inventors: Maximilian Dochnahl, Gunter Lipowsky
  • Patent number: 8168670
    Abstract: 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: Grant
    Filed: November 7, 2008
    Date of Patent: May 1, 2012
    Assignees: Teikoku Pharma USA, Inc., Techno Guard Co., Ltd.
    Inventor: Kiichiro Nabeta
  • Patent number: 8163757
    Abstract: The present invention relates to compounds of formula (IA) or (IB) or pharmaceutically or veterinarily acceptable salt thereof:
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: April 24, 2012
    Assignee: MediGene AG
    Inventor: Ian Richard Matthews
  • Publication number: 20120059163
    Abstract: 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: Application
    Filed: November 7, 2011
    Publication date: March 8, 2012
    Applicant: Optimer Photonics, Inc.
    Inventors: Vincent D. McGinniss, Steven M. Risser, Elizabeth Drotleff, Edward Jiang, Kevin B. Spahr
  • Publication number: 20110071282
    Abstract: 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: Application
    Filed: April 24, 2009
    Publication date: March 24, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Antoni Torrens Jover, Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent
  • Publication number: 20110065634
    Abstract: 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: Application
    Filed: May 13, 2009
    Publication date: March 17, 2011
    Inventors: William J. Greenlee, Andrew Stamford, Michael W. Miller, Duane Eugene DeMong
  • Patent number: 7868185
    Abstract: 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: Grant
    Filed: June 1, 2006
    Date of Patent: January 11, 2011
    Assignees: Max-Delbruck-Centrum fur Molekulare Medizin, Forschungsverbund Berlin E, V.
    Inventors: Klaus Hellmuth, Walter Birchmeier, Joerg Rademann, Stefanie Grosskopf
  • Publication number: 20100331342
    Abstract: 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 e
    Type: Application
    Filed: September 2, 2010
    Publication date: December 30, 2010
    Applicant: Medigene Limited
    Inventor: Ian Richard Matthews
  • Publication number: 20100324091
    Abstract: 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: Application
    Filed: June 23, 2008
    Publication date: December 23, 2010
    Applicant: Kowa Company, Ltd.
    Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
  • Publication number: 20100316601
    Abstract: 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: Application
    Filed: January 4, 2009
    Publication date: December 16, 2010
    Inventors: Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fel, Shenglan Wang, Li Wang
  • Publication number: 20100150899
    Abstract: The present invention relates to new pyrazolinone scavengers of free radicals, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 10, 2009
    Publication date: June 17, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100113543
    Abstract: 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: Application
    Filed: February 8, 2008
    Publication date: May 6, 2010
    Applicant: BASF SE
    Inventors: Rafel Israels, Heidi Emilia Saxell, Matthias Bratz, Marco Kuhns, Peter Erk
  • Patent number: 7652057
    Abstract: 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: Grant
    Filed: August 29, 2006
    Date of Patent: January 26, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V Mayweg, Werner Neidhart
  • Publication number: 20090281102
    Abstract: 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: Application
    Filed: May 1, 2009
    Publication date: November 12, 2009
    Applicant: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7456315
    Abstract: 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: Grant
    Filed: February 26, 2004
    Date of Patent: November 25, 2008
    Assignee: Intrexon Corporation
    Inventors: Robert Eugene Hormann, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20080269293
    Abstract: 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: Application
    Filed: August 22, 2007
    Publication date: October 30, 2008
    Inventors: Liguo Chi, Chulho Choi, Andrew G. Geyer, Robert M. Kennedy, Jeffery A. Pfefferkorn, Roy T. Winters
  • Publication number: 20080119458
    Abstract: 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: Application
    Filed: October 5, 2007
    Publication date: May 22, 2008
    Applicant: Wyeth
    Inventors: William Ronald Solvibile, Ji-ln Kim, Marla Jean Williams, Jonathan Laird Gross, Albert Jean Robichaud
  • Patent number: 7202367
    Abstract: 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: Grant
    Filed: May 31, 2002
    Date of Patent: April 10, 2007
    Assignee: Rhodia Chimie
    Inventors: Pascal Philippe Cellier, Henri-Jean Cristau, Jean-Francis Spindler, Marc Taillefer
  • Patent number: 7037880
    Abstract: 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: Grant
    Filed: August 8, 2002
    Date of Patent: May 2, 2006
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Patent number: 6864373
    Abstract: 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: Grant
    Filed: May 8, 2003
    Date of Patent: March 8, 2005
    Assignee: Pharmacia Corporation
    Inventors: Hong Zhuang, Ping Gao
  • Patent number: 6838458
    Abstract: 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: Grant
    Filed: November 1, 2002
    Date of Patent: January 4, 2005
    Assignee: Pfizer, Inc.
    Inventor: Subas M. Sakya
  • Publication number: 20040030151
    Abstract: 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: Application
    Filed: May 8, 2003
    Publication date: February 12, 2004
    Inventors: Hong Zhuang, Ping Gao
  • Patent number: 6689805
    Abstract: 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: Grant
    Filed: June 13, 2003
    Date of Patent: February 10, 2004
    Assignee: 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
  • Publication number: 20030165561
    Abstract: 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: Application
    Filed: November 1, 2002
    Publication date: September 4, 2003
    Inventors: Rajinder Singh, Dane Goff, Henry Lu, Sarkiz D. Issakani, Thomas Sun
  • Patent number: 6562856
    Abstract: The invention relates to novel pyrazolyl benzyl ethers, to a process for their preparation and to their use for controlling harmful organisms.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: May 13, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: 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
  • Patent number: 6322775
    Abstract: 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: Grant
    Filed: January 6, 1999
    Date of Patent: November 27, 2001
    Assignee: L'Oreal S.A.
    Inventors: Gérard Malle, Laurent Vidal