Halogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/345)
  • Patent number: 11312672
    Abstract: The invention relates to process for the manufacture or preparation of fluorinated benzene, in particular monofluorobenzene, in a vapor-phase fluorination process. The process of the invention, for example, can comprise a batch or continuous manufacture or preparation of fluorinated benzene, in particular monofluorobenzene, using hydrogen fluoride (HF) in gas phase as fluorination gas. Also, in this process of the invention, for example, fluorination catalysts are involved.
    Type: Grant
    Filed: July 8, 2020
    Date of Patent: April 26, 2022
    Inventors: Changyue Zhou, Yong Wang
  • Patent number: 10882824
    Abstract: The present invention relates to a method for purifying a compound represented by the formula (I), the method including treating a mixture containing the compound represented by the formula (I) and a compound represented by the formula (II) with an aqueous solution of a basic compound. where, in the formula (I), R1 represents a hydrogen atom or a chlorine atom; in the formula (II), R2, R3 and R4 are the same or different from each other and represent a hydrogen, a chlorine atom or a fluorine atom independently, at least one of R3 and R4 represent a chlorine atom or a fluorine atom, and, in the case where R3 represents a chlorine atom, R4 represents a chlorine atom or a fluorine atom.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: January 5, 2021
    Assignee: ISHIHARA SANGYO KAISHA, LTD.
    Inventor: Hiroshi Yoshizawa
  • Patent number: 10851060
    Abstract: The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. The preparation process comprises the following steps: enabling pyridine and chlorine gas to continuously experience chlorination reaction under irradiation of ultraviolet light by using pyridine and chlorine gas as starting materials and using trifluoromethyl chlorobenzene as a solvent, and cooling a chlorination reaction product and the solvent to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through liquid phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: December 1, 2020
    Assignee: Zhejiang Avilive Chemical Co., Ltd.
    Inventors: Huiyue Li, Keqiang Jin, Jiaquan Zhu
  • Patent number: 10577326
    Abstract: The present invention relates to a method for preparing 2-chloro-6-trichloromethylpyridine with product purity greater than or equal to 99.0% by using trifluoromethyl chlorobenzene as a solvent for reaction between 2-methylpyridine with chlorine gas, in which 2-methylpyridine and chlorine gas are used as starting materials, trifluoromethyl chlorobenzene is used as a solvent, 2-methylpyridine is prepared into a liquid raw material by using the solvent trifluoromethyl chlorobenzene, and the liquid raw material is continuously fed to perform liquid phase photochlorination reaction at temperature of 160-240° C. under irradiation of ultraviolet light to obtain 2-chloro-6-trichloromethylpyridine solution.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: March 3, 2020
    Assignee: Zhejiang Avilive Chemical, Co., Ltd.
    Inventors: Huiyue Li, Keqiang Jin, Jiaquan Zhu
  • Patent number: 10442766
    Abstract: The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% through gas phase photochlorination of pyridine by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. Gasified pyridine and heated chlorine gas are enabled to continuously experience chlorination reaction under irradiation of ultraviolet light by using gasified pyridine and heated chlorine gas as starting materials and using heated trifluoromethyl chlorobenzene as a solvent, and a gas phase reaction product and the solvent are cooled to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through gas phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: October 15, 2019
    Assignee: Zhejiang Avilive Chemical Co., Ltd.
    Inventors: Huiyue Li, Keqiang Jin, Jiaquan Zhu
  • Patent number: 10442765
    Abstract: The present invention relates to a novel process for producing of 2,3-dichloro-5-(trichloromethyl)pyridine by using PCl5 as chlorinating agent at elevated temperature and pressure.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: October 15, 2019
    Assignee: Cheminova A/S
    Inventor: Casper Stoubeak Andersen
  • Patent number: 9850208
    Abstract: Processes for the preparation of 2-chloro-5-methylpyridine are described.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: December 26, 2017
    Assignee: Vertellus Holdings LLC
    Inventors: Ramiah Murugan, Martin Grendze
  • Patent number: 9701635
    Abstract: The present invention provides compositions and methods for the selective C—H fluorination of nitrogen-containing heteroarenes with AgF2, which has previously been considered too reactive for practical, selective C—H fluorination. Fluorinated heteroarenes are prevalent in numerous pharmaceuticals, agrochemicals and materials. However, the reactions used to introduce fluorine into these molecules require pre-functionalized substrates or the use of F2 gas. The present invention provides a mild and general method for the C—H fluorination of nitrogen-containing heteroarene compounds to 2-fluoro-heteroarenes with commercially available AgF2. In various embodiments, these reactions occur at ambient temperature within one hour and occur with exclusive selectivity for fluorination at the 2-position. Exemplary reaction conditions are effective for fluorinating diazine heteroarenes to form a single fluorinated isomer.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: July 11, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: John Hartwig, Patrick Fier
  • Patent number: 9556177
    Abstract: The present disclosure provides compounds having Formula II-vi-a: wherein Cy1, Cy2, and A? are defined as set forth in the specification. These compounds are synthetic intermediates used to prepare inhibitors of Raf protein kinase.
    Type: Grant
    Filed: July 28, 2014
    Date of Patent: January 31, 2017
    Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Weirong Chen, Benjamin Lane, Hairuo Peng
  • Patent number: 9193683
    Abstract: Processes for manufacturing dihalopyridines without the use of copper salts are described. Additional processes for manufacturing dihalopyridines from niacinamide are described.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: November 24, 2015
    Assignee: Vertellus Specialties Inc.
    Inventor: Ramiah Murugan
  • Patent number: 9040572
    Abstract: This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: May 26, 2015
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: In Woo Kim, Ji Duck Kim, Hong Chul Yoon, Hee Kyoon Yoon, Byung Goo Lee, Joon Hwan Lee, Young Mook Lim, Soo Jin Choi
  • Publication number: 20150038722
    Abstract: An organic compound represented by General Formula (G100) is provided. A novel liquid crystal composition containing the organic compound is provided.
    Type: Application
    Filed: July 21, 2014
    Publication date: February 5, 2015
    Inventors: Momoko KATO, Yasuhiro NIIKURA, Makoto IKENAGA, Manabu KOBAYASHI, Tetsuji ISHITANI
  • Patent number: 8889685
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8883180
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20140275539
    Abstract: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Ground Fluor Pharmaceuticals, Inc.
    Inventor: Stephen G. DiMagno
  • Patent number: 8835409
    Abstract: 3-Alkenyl-6-halo-4-aminopicolinic acids and their derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: September 16, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer, Thomas L. Siddall
  • Patent number: 8809332
    Abstract: Besylate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: August 19, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8809377
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: August 19, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
  • Publication number: 20140220125
    Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: July 12, 2012
    Publication date: August 7, 2014
    Applicant: NOVARTIS AG
    Inventors: Wolfgang Marterer, Mahavir Prashad, Edwin Bernard Villhauer, Liladhar Murlidhar Waykole, James Anthony Vivelo, Bertrand Sutter, Jean-Claude Bianchi, Raeann Wu, Denis Har, Piotr H. Karpinski, Massimo Pignone, Doris Stingelin, Eckart Buerger
  • Patent number: 8785650
    Abstract: 3-substituted-6-trifluoromethyl pyridines are useful synthetic intermediates in the preparation of the N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines, which are useful in forming potent insecticides. Methods of forming such 3-substituted-6-trifluoromethyl pyridines are disclosed. Also disclosed are methods of using 6-trichloromethyl halogenated pyridines to form 3-substituted-6-trifluoromethyl pyridines are disclosed.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 22, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Ronald Ross, Jr., James M. Renga, Douglas Bland, Gary Roth, Alexander P. Fung, Clark S. Davis
  • Patent number: 8742127
    Abstract: [Problem] The present invention provides an industrially advantageous production method of a 6-halogeno-3-arylpyridine derivative in which cryogenic condition is not required, production step is short, and an isomer difficult to be separated is not produced as a by-product, [Solution] A production method of a 6-halogeno-3-arylpyridine derivative represented by the general formula (III) comprising: the first step reacting a 2,5-dihalogenopyridine derivative represented by the general formula (I) with a magnesiation reagent; and the second step reacting the product obtained from the above-described first step, in the presence of a palladium compound, with a halogenoaryl derivative represented by the general formula (II).
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: June 3, 2014
    Assignee: Kuraray Co., Ltd.
    Inventors: Nobusuke Kashiki, Toshiki Mori, Katsuji Ujita
  • Patent number: 8691997
    Abstract: The present invention provides processes for producing 2-chloro-3-trifluoromethylpyridine which is useful as an intermediate for medicines and agrochemicals, at a high production rate in a high yield. Specifically, the present invention relates to a process for producing 2-chloro-3-trifluoromethylpyridine or a salt thereof comprising allowing 3-trifluoromethylpyridine N-oxide to react with a chlorinating agent; and also relates to a process for producing 2-chloro-3-trifluoromethylpyridine or a salt thereof comprising oxidizing 3-trifluoromethylpyridine to produce 3-trifluoromethylpyridine N-oxide and subsequently allowing the obtained 3-trifluoromethylpyridine N-oxide to react with a chlorinating agent.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: April 8, 2014
    Assignee: Ishihara Sangyo Kaisha, Ltd
    Inventor: Fumihiro Fukui
  • Patent number: 8653110
    Abstract: Disclosed are novel active compound combinations comprising at least one substituted enaminocarbonyl compound and azadirachtin, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids. Methods of controlling insects and acarids are also disclosed.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: February 18, 2014
    Assignee: Bayer CropScience AG
    Inventors: Michael Kilian, Margit Doth
  • Publication number: 20130338361
    Abstract: Provided by the present invention is a novel method for obtaining an 18F-labelled compound wherein said compound comprises an 18F-labelled pyridyl ring. The method of the invention is advantageous over the prior art methods as it provides these compounds in higher radiochemical yields than have been possible with previous methods. Also provided by the present invention is an 18F-labelled synthon useful in the method of the invention.
    Type: Application
    Filed: March 1, 2012
    Publication date: December 19, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Helen May Betts, Imtiaz Khan, Edward George Robins
  • Patent number: 8557933
    Abstract: Alternate methods for preparing functionalized pyridyl-amine products from pyridinyl starting materials are provided herein. These alternately-prepared functionalized pyridyl-amines can be used as ligands or ligand precursors in catalytic compositions, e.g., in oligomerization reactions. Methods for such reactions are also provided herein.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: October 15, 2013
    Assignee: ExxonMobil Chemical Patents Inc.
    Inventors: John Robert Hagadorn, Timothy Marlow Boller, Steven Douglas Brown, Gary Michael Diamond, Keith Anthony Hall, James Martin Longmire, Lily Joy Ackerman, Susan Jessica Schofer, Eric Lee Kuiokalani Dias, Andrew Cottone, III, Carl Edgar Whittle
  • Publication number: 20130261310
    Abstract: 3-substituted-6-trifluoromethyl pyridines are useful synthetic intermediates in the preparation of the N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines, which are useful in forming potent insecticides. Methods of forming such 3-substituted-6-trifluoromethyl pyridines are disclosed. Also disclosed are methods of using 6-trichloromethyl halogenated pyridines to form 3-substituted-6-trifluoromethyl pyridines are disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 3, 2013
    Inventors: RONALD ROSS, JR., JAMES RENGA, DOUGLAS C. BLAND, GARY A. ROTH, ALEXANDER P. FUNG, CLARK S. DAVIS
  • Patent number: 8541416
    Abstract: L-malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl) carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: September 24, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8530666
    Abstract: The present invention relates to a process for the production of trifluoromethylated unsubstituted or substituted aryl or heteroaryl compounds which comprises reacting an unsubstituted or substituted aryl or heteroaryl halide with a trifluoroacetate of formula (I) or (II), wherein R1 is hydrogen or a C1-C5 alkyl group and M an alkali metal or an ammonium ion, in the presence of and an anorganic halogenide salt or a trifluoroacetacid salt as activator compound and a catalytic combination of a copper salt with a monodentate, bidentate or tridentate aromatic or aliphatic amine or pyridine ligand.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: September 10, 2013
    Assignee: SALTIGO GmbH
    Inventors: Alain Cotté, Matthias Gotta, Matthias Beller, Thomas Schareina, Alexander Zapf, Xiao-Feng Wu
  • Publication number: 20130211093
    Abstract: Disclosed herein is a cost effective and environmentally friendly process to prepare 1-hydroxy-6-substituted pyridones from 2,6-dichloropyridine.
    Type: Application
    Filed: February 8, 2013
    Publication date: August 15, 2013
    Applicant: ARCH CHEMICALS, INC.
    Inventor: Arch Chemicals, Inc.
  • Patent number: 8497268
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful to provide blood levels of eszopiclone that are independent of fasting state.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: July 30, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8497267
    Abstract: Besylate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: July 30, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8445686
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: May 21, 2013
    Assignee: AbbVie Inc.
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Mueller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steve Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Publication number: 20130123506
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Application
    Filed: December 17, 2012
    Publication date: May 16, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: BAYER CROPSCIENCE AG
  • Patent number: 8431577
    Abstract: The present invention discloses a crystalline form of S-zopiclone (Formula I) having a powder X-Ray diffraction spectrum excited by Cu-Ka radiation with characteristic peaks expressed in terms of 2? at about 11.08°, about 12.38°, about 15.86°, about 17.88°, about 19. 98° and about 20.58°; a DSC thermogram with a peak at about 207.7° C. and an infrared absorption spectrum (IR) with characteristic peaks at about 3078 cm?1, about 2942˜2838 cm?1, about 2790 cm?1, about 1716 cm?1, about 1463 cm?1, about 1372 cm?1 and about 757 cm?1. The present invention also discloses a method for preparing the crystalline form of eszopiclone, its pharmaceutical composition and its use in preparing a medicament for treating sleep disorders.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 30, 2013
    Assignee: Tianjin Tasly Group Co., Ltd.
    Inventors: Guocheng Wang, Xueyu Xu
  • Publication number: 20130096312
    Abstract: The present invention relates to a process for preparing 4-hydroxypyridines of formula I wherein R1, R2, R3 and R4 have the meanings defined in the description.
    Type: Application
    Filed: June 20, 2011
    Publication date: April 18, 2013
    Applicant: BASF SE
    Inventors: Volker Maywald, Frederik Menges, Uwe Josef Vogelbacher, Michael Rack, Michael Keil, Wassilios Grammenos, Marianna Vrettou-Schultes, Jan Klaas Lohmann, Bernd Mueller, Thorsten Jabs
  • Patent number: 8404855
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: March 26, 2013
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Rolf Pontzen, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Thomas Müller, Christian Arnold, Erich Sanwald
  • Publication number: 20130023661
    Abstract: The present invention relates to the use of compounds of the formula (I) as fluorinating reagents, to a process for the fluorination of organic compounds by reaction thereof with compounds of the formula (I), and to compounds of the formula (I).
    Type: Application
    Filed: March 7, 2011
    Publication date: January 24, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Nikolai (Mykola) Ignatyev, Aleksandra Atatrah, Peter Barthen, Walter Frank
  • Publication number: 20120316341
    Abstract: Methods for fluorinating organic compounds are described herein.
    Type: Application
    Filed: April 11, 2012
    Publication date: December 13, 2012
    Inventors: Tobias Ritter, Pingping Tang
  • Patent number: 8309723
    Abstract: Present invention relates to an improved process for the preparation of Zopiclone and its enantiomerically enriched isomer (Eszopiclone). 6-(5-Chloropyridin-2-yl)-5-hydroxy-7-oxo-5,6-dihydropyrrolo[3,4-b]pyrazine is reacted with 1-chloro-carbonyl-4-methylpiperazine in the presence of alkali earth metal carbonates, hydroxides or oxides in a solvent medium to give Zopiclone. It is reacted with optically active acid in a mixture of water and water miscible organic solvent followed by work up to give Eszopiclone. The present invention also relates to process for the conversion of (R) or (S) Zopiclone to 6-(5-chloropyrid-2-yl)-5-hydroxy-7-oxo-5,6-dihydro-pyrrolo-[3,4-b]-pyrazine of the intermediate which can be converted to racemic Zopiclone.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: November 13, 2012
    Assignee: Mylan Laboratories Ltd.
    Inventors: Om Dutt Tyagi, Tushar Kumar Srivastava, Vellanki Siva Ram Prasad, Dnyandev Ragho Rane, Bandi Naga Durga Rao, Daggula Srinivas Reddy
  • Patent number: 8293918
    Abstract: Disclosed herein an improved process for producing 2,3-dihalopyridine with high purity at industrial scale with minimum effluent.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 23, 2012
    Assignee: Jubilant Organosys Limited
    Inventors: Gelebith H. Modi, Anil Kumar Tyagi, Ashutosh Agarwal, Hem Chandra, Nikhilesh Chandra Bhardwaj, Pradeep Kumar Verma
  • Publication number: 20120259125
    Abstract: The present invention provides processes for producing 2-chloro-3-trifluoromethylpyridine which is useful as an intermediate for medicines and agrochemicals, at a high production rate in a high yield. Specifically, the present invention relates to a process for producing 2-chloro-3-trifluoromethylpyridine or a salt thereof comprising allowing 3-trifluoromethylpyridine N-oxide to react with a chlorinating agent; and also relates to a process for producing 2-chloro-3-trifluoromethylpyridine or a salt thereof comprising oxidizing 3-trifluoromethylpyridine to produce 3-trifluoromethylpyridine N-oxide and subsequently allowing the obtained 3-trifluoromethylpyridine N-oxide to react with a chlorinating agent.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 11, 2012
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventor: Fumihiro Fukui
  • Publication number: 20120252789
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Dirk Wienke
  • Patent number: 8269005
    Abstract: L-malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: September 18, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas
  • Publication number: 20120208809
    Abstract: The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c?]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers an
    Type: Application
    Filed: November 30, 2009
    Publication date: August 16, 2012
    Applicant: SANOFI
    Inventors: Didier Babin, Olivier Bedel, Thierry Gouyon, Serge Mignani, David Papin
  • Patent number: 8212047
    Abstract: Alternate methods for preparing functionalized pyridyl-amine products from pyridinyl starting materials are provided herein. In addition, these alternately-prepared functionalized pyridyl-amines can be used as ligands or ligand precursors in catalytic compositions, e.g. for use in alkene oligomerization reactions.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: July 3, 2012
    Assignee: Exxonmobil Chemical Patents Inc.
    Inventors: John Robert Hagadorn, Timothy Marlow Boller, Steven Douglas Brown, Gary Michael Diamond, Keith Anthony Hall, James Martin Longmire, Lily Joy Ackerman, Susan Jessica Schofer, Eric Lee Kuiokalani Dias, Andrew Cottone, III, Carl Edgar Whittle
  • Patent number: 8212036
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: July 3, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas
  • Publication number: 20120101278
    Abstract: A process for producing a biaryl compound, characterized by reacting an arylhydrazine compound, hydrogen peroxide and an aryl compound. When the reaction is conducted in the presence of a given metal or a compound of the metal or in the presence of a metal oxide obtained by reacting the given metal or a compound of the metal with hydrogen peroxide, then the yield of the biaryl compound is improved.
    Type: Application
    Filed: December 27, 2011
    Publication date: April 26, 2012
    Inventor: KOJI HAGIYA
  • Patent number: 8106211
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: January 31, 2012
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Rolf Pontzen, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Thomas Müller, Christian Arnold, Erich Sanwald
  • Patent number: 8106212
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: January 31, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Beck, Olga Malsam, Ralf Nauen, Ulrich Görgens, Thomas Müller, Christian Arnold, Erich Sanwald
  • Patent number: 8084615
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: December 27, 2011
    Assignees: University of Washington, Novartis Vaccines and Diagnostics, Inc.
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar