Chalcogen Bonded Directly To Ring Carbon Of The Diazole Ring Patents (Class 548/366.1)
  • Patent number: 11927868
    Abstract: Electro-optic (EO) devices having an EO polymer core comprising a first host polymer and a first nonlinear optical chromophore (NLOC); and a cladding comprising a second host polymer and a second NLOC, and methods of preparing the same; wherein the first NLOC has a first bridge covalently bonded to an electron-accepting group and an electron-donating group; wherein the second NLOC has a second bridge covalently bonded to an electron-accepting group and an electron-donating group; and wherein the second bridge is less conjugated than the first bridge such that the cladding has an index of refraction that is less than that of the EO polymer core, and wherein the second NLOC is present in the second host polymer in a concentration such that the cladding has a conductivity equal to or greater than at least 10% of the conductivity of the EO polymer core at a poling temperature.
    Type: Grant
    Filed: January 9, 2023
    Date of Patent: March 12, 2024
    Assignee: Lightwave Logic, Inc.
    Inventors: Youngwoo Yi, Cory Steven Pecinovsky, Michael Stephen Lebby, Richard Anthony Becker
  • Patent number: 11731961
    Abstract: Compounds of Formula (I), racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions containing the compounds, racemates, enantiomers, diastereomers thereof are disclosed. These compounds have GPR40 agonist activity and are capable of modulating blood glucose levels and glucose-dependent insulin secretion mechanism, and, thus, exhibit excellent glucose lowering efficacy without the risk of hypoglycemia. These compounds could be used in preventing and/or treating type 2 diabetes through adequate control of blood glucose.
    Type: Grant
    Filed: November 10, 2021
    Date of Patent: August 22, 2023
    Assignee: ILDONG PHARMACEUTICAL CO., LTD.
    Inventors: Jae-Hoon Kang, Hong-Sub Lee, Kyung-Mi An, Chang-Hee Hong, Hyun-Jung Kwak, Shuo-Lin Cui, Hyo-Jung Song
  • Patent number: 11639345
    Abstract: The present invention provides novel inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.
    Type: Grant
    Filed: July 1, 2020
    Date of Patent: May 2, 2023
    Assignee: MIGAL—GALILEE RESEARCH INSTITUTE LTD.
    Inventors: Itai Bloch, Elad Cohen, Rachel Amir, Maayan Gal
  • Patent number: 9932312
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-methyl-3-difluoromethyl-1H-pyrazole-4-carbaldehyde, a useful intermediate in the manufacture of fungicides.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: April 3, 2018
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Norbert Lui, Sergii Pazenok
  • Patent number: 9012478
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 21, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 8957102
    Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: February 17, 2015
    Assignee: Neopharm Co., Ltd.
    Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
  • Patent number: 8937185
    Abstract: Provided are improved processes for the preparation of 1-aryl pyrazole compounds of formula (I) and (IB): which are substituted at the 5-position of the pyrazole ring with a carbon-linked functional group. The process described are efficient and scalable and do not utilize hazardous sulfenyl halide reagents.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: January 20, 2015
    Assignee: Merial Limited
    Inventors: Charles Q Meng, Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Xinxi Zhan, Jean Robert Labrosse, Michel Mulhauser
  • Patent number: 8933246
    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 a pyrazole 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: January 10, 2013
    Date of Patent: January 13, 2015
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Gunter Lipowsky
  • Patent number: 8921407
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: December 30, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
  • Publication number: 20140288074
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, fungicides: wherein Q1, R1, R1a, R2, R3 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: March 21, 2014
    Publication date: September 25, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: ANDREW EDMUND TAGGI, Jeffrey Keith Long, Moumita Kar
  • Patent number: 8802713
    Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: August 12, 2014
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Satoru Ohata, Katsuya Kato, Keiji Toriyabe, Yoshihiro Ito, Ryuji Hamaguchi, Yuki Nakano
  • Patent number: 8765971
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: July 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Sergii Pazenok, Norbert Lui, Marc Kosten, Guenter Bartels
  • Publication number: 20140171469
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: June 19, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • 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: 8673901
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: March 18, 2014
    Assignee: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Patent number: 8658686
    Abstract: Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: February 25, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Taito Nishino, Katsuaki Miyaji, Shunsuke Iwamoto, Takumi Mikashima, Koichiro Saruhashi, Yo Kishikawa
  • Patent number: 8642626
    Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: February 4, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
  • 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
  • Patent number: 8586594
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: November 19, 2013
    Assignee: AbbVie Inc.
    Inventors: Andrew J. Souers, Ju Gao, Todd M. Hansen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
  • Publication number: 20130253204
    Abstract: Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6, R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.
    Type: Application
    Filed: December 1, 2011
    Publication date: September 26, 2013
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Taito Nishino, Katsuaki Miyaji, Shunsuke Iwamoto, Takumi Mikashima, Koichiro Saruhashi, Yo Kishikawa
  • Patent number: 8476458
    Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: July 2, 2013
    Assignees: The Wistar Institute, The John Hopkins University
    Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
  • Publication number: 20130165664
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoro-1-alkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.
    Type: Application
    Filed: February 19, 2013
    Publication date: June 27, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventor: Bayer Intellectual Property GmbH
  • Patent number: 8455664
    Abstract: The present invention relates to a process for preparing 1-alkyl-3-difluoromethyl-5-hydroxypyrazoles, which are valuable intermediates for the production of fungicides.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: June 4, 2013
    Assignee: Bayer CropScience AG
    Inventors: Sergii Pazenok, Michael Müller, Norbert Lui
  • Publication number: 20130131352
    Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I 5 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 a pyrazole 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: January 10, 2013
    Publication date: May 23, 2013
    Applicant: BASF SE
    Inventor: BASF SE
  • Publication number: 20130123500
    Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
    Type: Application
    Filed: July 29, 2011
    Publication date: May 16, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
  • Patent number: 8440839
    Abstract: The present invention provides: dinitropyrazole derivatives of formula (I) in which: R?NO2, NH2, NF2, NHOH, OH or NHNH2 and R??H when R?NH2, NF2, NHOH, OH or NHNH2 or R??H, NH2 or a linear or branched C1-C4 alkyl group, optionally substituted by at least one hydroxy and/or one fluoro group, when R?NO2; other than 4-amino-3,5-dinitropyrazole; and also the salts of said derivatives of formula (I) in which R??H; the preparation of said derivatives and of their salts; and energetic compositions comprising at least one of said derivatives and/or at least one salt of such a derivative.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: May 14, 2013
    Assignees: Herakles, Eurenco
    Inventor: Gregoire Herve
  • Patent number: 8436191
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 7, 2013
    Assignee: Bayer CropScience AG
    Inventors: Sergii Pazenok, Norbert Lui, Marc Kosten, Guenter Bartels
  • Publication number: 20130072536
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Application
    Filed: November 13, 2012
    Publication date: March 21, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventor: SYNTA PHARMACEUTICALS CORP.
  • Publication number: 20130053386
    Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 5, 2010
    Publication date: February 28, 2013
    Inventors: William Colby Brown, Richard W. Heidebrecht, Jason Brubaker, Christian Fischer, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
  • Publication number: 20120264925
    Abstract: A process for preparing pyrazole-glycoside derivatives of the general Formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C1-C8)-alkyl, where one, more than one or all hydrogen(s) may be replaced by fluorine; X (C1-C3)-alkylene, (C2-C3)-alkenylene.
    Type: Application
    Filed: August 26, 2010
    Publication date: October 18, 2012
    Applicant: SANOFI
    Inventors: Michael Podeschwa, David Rigal, Kai Rossen, Bernhard Otto, Hermut Wehlan, Theodor Andreas Wollmann, Bernd Becker, Berndt Kulitzscher, Alexander Schaefer
  • Patent number: 8273784
    Abstract: The present invention provides: dinitropyrazole derivatives of formula (I) in which: R?NO2, NH2, NF2, NHOH, OH or NHNH2 and R??H when R?NH2, NF2, NHOH, OH or NHNH2 or R??H, NH2 or a linear or branched C1-C4 alkyl group, optionally substituted by at least one hydroxy and/or one fluoro group, when R?NO2; other than 4-amino-3,5-dinitropyrazole; and also the salts of said derivatives of formula (I) in which R??H; the preparation of said derivatives and of their salts; and energetic compositions comprising at least one of said derivatives and/or at least one salt of such a derivative.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: September 25, 2012
    Assignees: Herakles, Eurenco
    Inventor: Gregoire Herve
  • Publication number: 20120238581
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.
    Type: Application
    Filed: May 31, 2012
    Publication date: September 20, 2012
    Inventors: Andrew J. Souers, Ju Gao, Todd M. Hasen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
  • 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: 8202878
    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, a pharmaceutical composition of formula (I), and related methods for treating or preventing metabolic diseases or conditions.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: June 19, 2012
    Assignee: Abbott Laboratories
    Inventors: Andrew J. Souers, Ju Gao, Todd M. Hansen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
  • Publication number: 20110319430
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O)m, NR4, CR15R16, C(?O) or C(?S); and R1, R1a, R2, R4, R15, R16 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: March 3, 2010
    Publication date: December 29, 2011
    Applicant: E.I. Du pont Nemours and Company
    Inventors: Jeffrey Keith Long, Wonpyo Hong, Andrew Edmund Taggi
  • Publication number: 20110288304
    Abstract: The present invention relates to a process for preparing 1-alkyl-3-difluoromethyl-5-hydroxypyrazoles, which are valuable intermediates for the production of fungicides.
    Type: Application
    Filed: May 19, 2011
    Publication date: November 24, 2011
    Applicant: Bayer CropScience AG
    Inventors: Sergii PAZENOK, Michael Müller, Norbert Lui
  • Patent number: 8063044
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: August 25, 2008
    Date of Patent: November 22, 2011
    Assignee: Pfizer Inc.
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 8063067
    Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: November 22, 2011
    Assignee: Merck Patent GmbH
    Inventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
  • Patent number: 8030498
    Abstract: A benzoylpyrazole compound represented by the formula (I) or its salt, useful as herbicides and intermediates thereof.
    Type: Grant
    Filed: December 13, 2006
    Date of Patent: October 4, 2011
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Hiroshi Shimoharada, Masamitsu Tsukamoto, Masahiko Ikeguchi, Hiroshi Kikugawa, Makiko Sano, Yoshinori Kitahara, Hidemasa Kominami, Tatsuya Okita
  • Publication number: 20110224413
    Abstract: Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives and pyrazole intermediates of the same. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes and intermediates for preparing the same.
    Type: Application
    Filed: November 19, 2009
    Publication date: September 15, 2011
    Inventors: Michael Tolar Martin, Michael S. McClure, Vassil Elitzin
  • Publication number: 20110207940
    Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.
    Type: Application
    Filed: November 19, 2010
    Publication date: August 25, 2011
    Applicant: Bayer CropScience AG
    Inventors: Sergii Pazenok, Norbert Lui, Marc Kosten, Guenter Bartels
  • Patent number: 7988740
    Abstract: The invention relates to colorant compositions for the oxidative dyeing of keratin fibers comprising radical scavengers in the dyeing composition. The invention also relates to methods for reducing color formation outside of the keratin fiber during oxidative dyeing comprising using such compositions.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: August 2, 2011
    Assignee: The Procter & Gamble Company
    Inventors: Guiru Zhang, Bryan Patrick Murphy, Jennifer Mary Marsh, Richard Marc Dahlgren
  • Patent number: 7985266
    Abstract: The invention relates to colorant compositions for the oxidative dyeing of keratin fibers comprising an inhibiting system of radical scavengers and chelants in the dyeing composition. The invention also relates to methods for reducing color formation outside of the keratin fiber during oxidative dyeing comprising using such colorant compositions.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: July 26, 2011
    Assignee: The Procter & Gamble Company
    Inventors: Guiru Zhang, Bryan Patrick Murphy, Jennifer Mary Marsh, Richard Marc Dahlgren
  • Publication number: 20110166343
    Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].
    Type: Application
    Filed: March 14, 2011
    Publication date: July 7, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
  • Publication number: 20110070297
    Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
    Type: Application
    Filed: December 1, 2010
    Publication date: March 24, 2011
    Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
  • Publication number: 20110045101
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is Q2 or R1; X is N, CR2 or CQ3; Y is N or CR3; Z is N or CR4; and Q1, Q2, Q3, R1 R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: May 7, 2009
    Publication date: February 24, 2011
    Applicant: E.I. Du Pont De Nemours and Company
    Inventors: Thomas Paul Selby, James Francis Bereznak, John Joseph Bisaha, Amy X. Ding, Mary Ann Hanagan, Jeffrey Keith Long, Andrew Edmund Taggi, Vijayagopal Gopalsamuthiram
  • Patent number: 7872038
    Abstract: The invention relates to 1-(2,4,6-trisubstituted-phenyl)-5-amino-4-substituted-pyrazole derivatives of formula (I) 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: Grant
    Filed: February 25, 2005
    Date of Patent: January 18, 2011
    Assignee: Merial Limited
    Inventors: Stefan Schnatterer, David Teh-Wei Chou, Werner Knauf, Daniela Jans, Karl Seeger
  • Patent number: 7863310
    Abstract: The present invention provides kinase inhibitors of Formula I:
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: January 4, 2011
    Assignee: Eli Lilly and Company
    Inventors: Rosanne Bonjouklian, Robert Dean Dally, Alfonso de Dios, Mirian Filadelfa del Prado Catalina, Carmen Dominguez-Fernandez, Carlos Jaramillo Aguado, Beatriz Lopez de Uralde-Garmendia, Timothy Alan Shepherd
  • 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: 20100210704
    Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.
    Type: Application
    Filed: October 17, 2008
    Publication date: August 19, 2010
    Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.
    Inventors: Satoru Ohata, Katsuya Kato, Keiji Toriyabe, Yoshihiro Ito, Ryuji Hamaguchi, Yuki Nakano