Boron Or Spiro Containing Patents (Class 558/384)
  • Patent number: 10112960
    Abstract: Methods for the selective borylation of arenes, including arenes substituted with an electron-withdrawing group (e.g., 1-chloro-3-fluoro-2-substituted benzenes) are provided. The methods can be used, in some embodiments, to efficiently and regioselectively prepare borylated arenes without the need for expensive cryogenic reaction conditions.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: October 30, 2018
    Assignees: Dow AgroSciences LLC, The Board of Regents of the Michigan State University
    Inventors: Milton R. Smith, Robert E. Maleczka, Hao Li, Chathurika R. K. Jayasundara, Jossian Oppenheimer, Dmitrijs Sabasovs
  • Patent number: 9175021
    Abstract: The invention relates to a process for the preparation of salts having perfluoroalkyltricyano- or perfluoroalkylcyanofluoroborate anions, ((per)fluoro)phenyltricyano- or ((per)fluoro)phenylcyanofluoroborate anions, phenyltricyanoborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms or phenylcyanofluoroborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms, by reaction of alkali metal trifluoroperfluoroalkylborate with trialkylsilyl cyanide and a subsequent salt-exchange reaction or by direct reaction of an organic trifluoroperfluoroalkyl borate with trialkylsilyl cyanide.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: November 3, 2015
    Assignee: MERCK PATENT GMBH
    Inventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
  • Patent number: 8927757
    Abstract: The invention relates to a process for the preparation of salts having perfluoroalkyltricyano- or perfluoroalkylcyanofluoroborate anions, ((per)fluoro)phenyltricyano- or ((per)fluoro)phenylcyanofluoroborate anions, phenyltricyanoborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4C atoms or phenylcyanofluoroborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4C atoms, by reaction of alkali metal trifluoroperfluoroalkylborate with trialkylsilyl cyanide and a subsequent salt-exchange reaction or by direct reaction of an organic trifluoroperfluoroalkyl borate with trialkylsilyl cyanide.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: January 6, 2015
    Assignee: Merck Patent GmbH
    Inventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
  • Patent number: 8921589
    Abstract: The present invention relates to electrolyte formulations comprising at least one imidazolium fluorotricyanoborate or pyrrolidinium fluorotricyanoborate and their use in an electrochemical and/or optoelectronic device such as a photovoltaic cell, a light emitting device, an electrochromic or photo-electrochromic device, an electrochemical sensor and/or biosensor, preferably their use in a dye or quantum dot sensitized solar cell.
    Type: Grant
    Filed: September 1, 2011
    Date of Patent: December 30, 2014
    Assignee: Merck Patent GmbH
    Inventors: Kentaro Kawata, Nikolai Mykola Ignatyev, Michael Schulte, Hiroki Yoshizaki
  • Patent number: 8901340
    Abstract: The present invention relates to compounds containing perfluoroalkyl-cyano-alkoxy-borate anions or perfluoroalkyl-cyano-alkoxy-fluoro-borate anions, ((per)fluoro)phenyl-cyano-alkoxy-borate anions or ((per)fluoro)phenyl-cyano-alkoxy-fluoro-borate anions or phenyl-cyano-alkoxy-borate anions which are monosubstituted or disubstituted with perfluoroalkyl groups having 1 to 4 C atoms or phenyl-cyano-alkoxy-fluoro-borate anions which are monosubstituted or disubstituted with perfluoroalkyl groups having 1 to 4 C atoms, the preparation thereof and the use thereof, in particular as part of electrolyte formulations for dye sensitized solar cells.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: December 2, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hiromi Shinohara, Kentaro Kawata, Hiroki Yoshizaki, Peer Kirsch, Nikolai (Mykola) Ignatyev, William Robert Pitner, Michael Schulte, Jan Sprener, Maik Finze, Walter Frank
  • Publication number: 20140312311
    Abstract: An optoelectronic materials for OLED is represented by formula (I): wherein R1 is selected from a group consisting of formulas (II)-(VI): wherein R2 and R3 are identical and selected from a group consisting of formula (VII) and formula (VIII): The optoelectronic materials possesses superior luminescent performance and thermal stability and is suitable to be a new type of ambipolar materials for OLED elements.
    Type: Application
    Filed: July 11, 2013
    Publication date: October 23, 2014
    Inventors: Chien-Tien CHEN, Wei-Shan CHAO, Hao-Wei LIU, Wei-Sheng SU
  • Patent number: 8859800
    Abstract: The invention relates to new compounds containing alkyl-alkoxy-cyano-borate anions, their preparation and their use, in particular as part of electrolyte formulations for electrochemical or optoelectronic devices.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: October 14, 2014
    Assignee: Merck Patent GmbH
    Inventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Jan Sprenger, Maik Finze, Walter Frank
  • Publication number: 20140296223
    Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Patent number: 8835667
    Abstract: The present invention relates to electrolyte formulations comprising at least one compound of formula (I) Ma+[B(Rf)(CN)x(F)y]a— (I) in which Ma+ is an inorganic or organic cation, Rf denotes straight-chain or branched perfluoroalkyl groups having 1 to 4 C atoms, C6F5, C6H5, partially fluorinated phenyl or phenyl which is monosubstituted or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms, a is 1 or 2, x is 1, 2 or 3, y is 0, 1 or 2 and x+y is 3 and their use in an electrochemical and/or optoelectronic device such as a photovoltaic cell, a capacitor, a light emitting device, an electrochromic or photo-electrochromic device, an electrochemical sensor and/or biosensor, preferably their use in a dye or quantum dot sensitized solar cell.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: September 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hiromi Shinohara, Kentaro Kawata, Hiroki Yoshizaki, Peer Kirsch, Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
  • Patent number: 8829201
    Abstract: The present invention relates to electrolyte formulations comprising at least one imidazolium difluorodicyanoborate or pyrrolidinium difluorodicyanoborate and their use in an electrochemical and/or optoelectronic device such as a photovoltaic cell, a light emitting device, an electrochromic or photo-electrochromic device, an electrochemical sensor and/or biosensor, preferably their use in a dye or quantum dot-sensitized solar cell.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: September 9, 2014
    Assignee: Merck Patent GmbH
    Inventors: Kentaro Kawata, Hiroki Yoshizaki, Hiromi Shinohara, Peer Kirsch, Nikolai (Mykola) Ignatyev, William-Robert Pitner, Emil Ferdinand Aust, Marlies Waterman
  • Publication number: 20140155566
    Abstract: The invention relates to new compounds containing alkyl/alkenyl-cyano-borate or alkyl/alkenyl-cyano-fluoroborate anions, their preparation and their use, in particular as part of electrolyte formulations for electrochemical or optoelectronic devices.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Nikolai (Mykola) Ignatyen, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Jan Sprenger, Maik Finze, Walter Frank
  • Publication number: 20140107341
    Abstract: The present invention relates to compounds containing hydrido-tricyano-borate anions, their preparation and their use, in particular as part of electrolyte formulations for electrochemical or optoelectronic devices.
    Type: Application
    Filed: May 23, 2012
    Publication date: April 17, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Eduard Bernhardt, Vera Bernhardt-pitchougina, Helge Willner
  • Patent number: 8653258
    Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: February 18, 2014
    Assignee: Georgia State University Research Foundation, Inc.
    Inventors: Binghe Wang, Nanting Ni, Junfeng Wang, Chung-Dar Lu, Han-Ting Chou, Minyong Li, Shilong Zheng, Yunfeng Cheng, Hanjing Peng
  • Publication number: 20140024635
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 23, 2014
    Applicant: The Trustees of The University Of Pennsylvania
    Inventors: WILLIAM F. DeGRADO, JUN WANG
  • Publication number: 20130289000
    Abstract: This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Application
    Filed: June 24, 2013
    Publication date: October 31, 2013
    Inventors: Tsutomu Akama, Jacob J. Plattner
  • Publication number: 20130289050
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Application
    Filed: March 4, 2013
    Publication date: October 31, 2013
    Applicants: VITAE PHARMACEUTICALS, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
  • Publication number: 20130244980
    Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
    Type: Application
    Filed: April 30, 2013
    Publication date: September 19, 2013
    Applicant: ANACOR PHARMACEUTICALS, INC.
    Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M Hold, James J. Leyden, Kirk R. Maples, Jacob J. Plaitner, Virginia Sanders, Yong-Kang Zhang
  • Patent number: 8436199
    Abstract: The invention relates to boron-containing acids of the general formula (I) [B(RF)4-x-y(CN)xFy]?H+ (I), where x=0, 1, 2, 3 or 4, y=0, 1, 2 or 3 x+y?4, and in which the ligands RF may be identical or different and RF stands for a perfluorinated or partially fluorinated C1-12-alkyl group and where the CN group is bonded to the B atom via the C atom, and complexes thereof with a solvent, to salts comprising a cation and the anion of a selection of the acids according to the invention, and to processes for the preparation of the salts.
    Type: Grant
    Filed: November 25, 2009
    Date of Patent: May 7, 2013
    Assignee: Merck Patent GmbH
    Inventors: Maik Finze, Eduard Bernhardt, Helge Willner, Nikolai (Mykola) Ignatyev, Urs Welz-Biermann
  • Publication number: 20120296096
    Abstract: The present invention relates to compounds containing perfluoroalkyl-cyano-alkoxy-borate anions or perfluoroalkyl-cyano-alkoxy-fluoro-borate anions, ((per)fluoro)phenyl-cyano-alkoxy-borate anions or ((per)fluoro)phenyl-cyano-alkoxy-fluoro-borate anions or phenyl-cyano-alkoxy-borate anions which are monosubstituted or disubstituted with perfluoroalkyl groups having 1 to 4 C atoms or phenyl-cyano-alkoxy-fluoro-borate anions which are monosubstituted or disubstituted with perfluoroalkyl groups having 1 to 4 C atoms, the preparation thereof and the use thereof, in particular as part of electrolyte formulations for dye sensitized solar cells.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 22, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Hiromi Shinohara, Kentaro Kawata, Hiroki Yoshizaki, Peer Kirsch, Nikolai (Mykola) Ignatyev, William Robert Pitner, Michael Schulte, Jan Sprener, Maik Finze, Walter Frank
  • Publication number: 20120289686
    Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
    Type: Application
    Filed: January 23, 2012
    Publication date: November 15, 2012
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. Baker, Tsutomu Akama, Michael Richard Kevin Alley, Stephen J. Benkovic, Michael DiPierro, Vincent S. Hernandez, Karin M. Hold, Isaac Kennedy, Igor Likhotvorik, Weimin Mao, Kirk R. Maples, Jacob J. Plattner, Fernando Rock, Virginia Sanders, Aaron M. Stemphoski, George Petros Yiannikouros, Siead Zagar, Yong-Kang Zhang, Huchen Zhou
  • Publication number: 20120214765
    Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
    Type: Application
    Filed: September 19, 2011
    Publication date: August 23, 2012
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
  • Publication number: 20120035132
    Abstract: Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed.
    Type: Application
    Filed: January 27, 2011
    Publication date: February 9, 2012
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Kurt Jarnagin, Tsutomu Akama
  • Publication number: 20120028957
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 1, 2010
    Publication date: February 2, 2012
    Inventors: William F. DeGrado, Jun Wang
  • Publication number: 20120015933
    Abstract: The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.
    Type: Application
    Filed: September 29, 2011
    Publication date: January 19, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
  • Publication number: 20110207702
    Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Application
    Filed: October 15, 2009
    Publication date: August 25, 2011
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Robert Jacobs, Matthew Orr, Stephen Wring, Daitao Chen, Huchen Zhou, Dazhong Ding, Yiqing Feng, Long Yi, Vincent S. Hernandez, Yong-Kang Zhang, Jacob J. Plattner
  • Publication number: 20110184175
    Abstract: Disclosed is a method for producing a BSH derivative, which comprises a step of addition-reacting BSH with an ?,?-unsaturated nitrile compound in the presence of a base. Various BSH derivatives obtained by the method are also disclosed.
    Type: Application
    Filed: July 23, 2009
    Publication date: July 28, 2011
    Applicant: STELLA PHARMA CORPORATION
    Inventors: Mitsunori Kirihata, Tomoyuki Asano, Kohki Uehara, Yoshihide Hattori
  • Publication number: 20110160366
    Abstract: The present invention provides a phosphonate based compound represented by the following Chemical Formula 1 and a flameproof thermoplastic resin composition comprising (A) a thermoplastic resin and (B) a phosphonate based compound represented by the following Chemical Formula 1. The flameproof thermoplastic resin composition can exhibit good flame retardancy and impact strength. Further, the composition does not include a halogenated flame retardant and thus can provide environmental and safety benefits. wherein R1 and R2 are each independently C1-C4 alkylene and X is a cyano group.
    Type: Application
    Filed: December 10, 2010
    Publication date: June 30, 2011
    Applicant: CHEIL INDUSTRIES INC.
    Inventors: Woo Joong KIM, Seung Shik SHIN, Jin Hwan CHOI
  • Publication number: 20110124877
    Abstract: To provide a novel 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative, a method for producing the same, and an agro-horticultural agent and an industrial material protecting agent containing as an active ingredient the abovementioned 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative. To be a 5-benzyl-4-azolylmethyl-4-spiro[2.4]heptanol derivative represented by Formula (I): wherein X denotes a halogen atom, a C1-C5 alkyl group, a C1-C5 haloalkyl group, a C1-C5 alkoxy group, a C1-C5haloalkoxy group, a phenyl group, a cyano group or a nitro group; n denotes an integer of 0 to 5; when n is not less than 2, Xs may be the same or different; R1, R2, R3, R4 each independently denotes a hydrogen atom, a halogen atom or a C1-C5 alkyl group; and A denotes a nitrogen atom or a methyne group.
    Type: Application
    Filed: August 24, 2009
    Publication date: May 26, 2011
    Applicant: KUREHA CORPORATION
    Inventors: Atsushi Ito, Takashi Shimokawara, Eiyu Imai, Yoichi Kanda, Nobuyuki Kusano, Masaru Mori, Rumi Suzuki
  • Publication number: 20100254903
    Abstract: Substituted aryl-boron compounds comprising at least one 18F atom, as illustrated by the formula (I), where at least one of Y1 or Y2 is 18F and A1 is a substituted aromatic ring, with G1-5 being, independently, C or N, and where the substitutents of the aromatic ring or polycyclic moiety (other than boron) comprise at least one electron-withdrawing group (EWG), providing that sigma total (?total) for all substituents on the aromatic ring or polycyclic moiety except B is about 0.06 or more when said at least one EWG is positioned ortho to B, or about 0.2 or more when no EWG is positioned ortho to B. The compounds include neutral (N=1) and ionic borate (N=2) embodiments. The compounds are useful as positron emission tomography (PET) imaging agents.
    Type: Application
    Filed: July 24, 2008
    Publication date: October 7, 2010
    Inventors: David Perrin, Richard Ting, Christopher Overall
  • Publication number: 20100190748
    Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
    Type: Application
    Filed: July 21, 2009
    Publication date: July 29, 2010
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk R. Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
  • Publication number: 20100137249
    Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.
    Type: Application
    Filed: June 6, 2008
    Publication date: June 3, 2010
    Inventors: Binghe Wang, Nanting Ni, Junfeng Wang, Chung-Dar Lu, Han-Ting Chou, Minyong Li, Shilong Zheng, Yunfeng Cheng, Hanjing Peng
  • Publication number: 20100069655
    Abstract: The invention relates to boron-containing acids of the general formula (I) [B(RF)4-x-y(CN)xFy]?H+ (I), where x=0, 1, 2, 3 or 4, y=0, 1, 2 or 3 x+y?4, and in which the ligands RF may be identical or different and RF stands for a perfluorinated or partially fluorinated C1-12-alkyl group and where the CN group is bonded to the B atom via the C atom, and complexes thereof with a solvent, to salts comprising a cation and the anion of a selection of the acids according to the invention, and to processes for the preparation of the salts.
    Type: Application
    Filed: November 25, 2009
    Publication date: March 18, 2010
    Inventors: Maik FINZE, Eduard BERNHARDT, Helge WILLNER, Nikolai (Mykola) IGNATYEV, Urs WELZ-BIERMANN
  • Publication number: 20090291917
    Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
    Type: Application
    Filed: March 5, 2009
    Publication date: November 26, 2009
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
  • Publication number: 20090275523
    Abstract: The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.
    Type: Application
    Filed: November 25, 2008
    Publication date: November 5, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Manfred Schudok, Michael Wagner, Armin Bauer, Anna Kohlmann
  • Publication number: 20080312451
    Abstract: The invention provides a process for the preparation of a sartan derivative of formula (I) (formula as filed in paper form) (I) wherein the substituents have the meaning indicated in the description, or a pharmaceutically acceptable salt thereof, comprising reacting 2-cyanophenylboronic acid or a derivative thereof with a p-halobenzyl-1H-imidazole derivative of formula (VI), (formula as filed in paper form) (VI) wherein (part of formula as filed in paper form), X, Y, R1 and R2 are as defined above, and Z is I, Br or Cl, in the presence of a transition metal catalyst and an inorganic or organic base.
    Type: Application
    Filed: September 20, 2006
    Publication date: December 18, 2008
    Applicant: KRKA, d.d. Novo mesto
    Inventors: Miroslav Veverka, Martin Putala, Heinrich Brath, Silvo Zuppancic
  • Patent number: 6562993
    Abstract: The invention relates to preservative compounds having the formula: where: X and Y are H or Br, with at least one of X and Y being Br; R is H or CH3; and n=1-8; and mixtures thereof.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: May 13, 2003
    Assignee: ISP Investments Inc.
    Inventors: Steven H. Bertz, Samuel T. D'Arcangelis, Ilya Makarovskiy, John J. Merianos
  • Patent number: 6525036
    Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.
    Type: Grant
    Filed: January 5, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
  • Patent number: 5849958
    Abstract: Pesticidal 1,4-diaryl-2-fluoro-2-butene compounds having the structural formula I ##STR1## and compositions and methods comprising those compounds for the control of insect and acarid pests.
    Type: Grant
    Filed: March 17, 1997
    Date of Patent: December 15, 1998
    Assignee: American Cyanamid Company
    Inventors: Keith D. Barnes, Yulin Hu
  • Patent number: 5486622
    Abstract: 5-Oxaspiro[2.4]heptan-6-one: ##STR1## is obtained from [3-(hydroxymethyl)oxetan-3-yl]acetonitrile by reaction with hydrogen bromide and then cyclizing the intermediate product 4,4-bis(bromomethyl)dihydro-2-furanone with zinc. 5-Oxaspiro[2.4]heptan-6-one is an intermediate product for the production of leukotriene antagonists.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: January 23, 1996
    Assignee: Lonza Ltd.
    Inventor: Paul Hanselmann
  • Patent number: 5470994
    Abstract: Sulfonium and oxysulfonium salts, useful as photoinitiators, have directly attached to the sulfur atom thereof:at least one aromatic or heterocyclic aromatic substituent containing at least 14 aromatic atoms and having a removable positive hydrogen ion, said substituent exhibiting a higher energy occupied molecular orbital than at least one other substituent directly attached to said sulfur atom;and at least one substituent comprising an electron withdrawing group and exhibiting a lower energy unoccupied molecular orbital than at least one other substituent directly attached to said sulfur atom;said salt being capable, upon exposure to visible radiation, of undergoing irreversible intramolecular rearrangement to form a Bronsted acid comprising the anion of said salt and said removable positive hydrogen ion.
    Type: Grant
    Filed: April 5, 1990
    Date of Patent: November 28, 1995
    Assignee: Eastman Kodak Company
    Inventors: Franklin D. Saeva, David T. Breslin
  • Patent number: 5401869
    Abstract: Aminomethylene compounds of the formula ##STR1## may advantageously be prepared by reacting C--H-acidic compounds of the formula ##STR2## with formamide acetals of the formula ##STR3## in which the radicals R.sup.1 to R.sup.6 have the meaning given in the description,if the process is carried out in the presence of a secondary amine of the formula ##STR4## in which R.sup.7 and R.sup.8 have the meaning given in the description.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: March 28, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
  • Patent number: 5384410
    Abstract: A method for the removal of ester protecting groups from .alpha.-amino boronic acid is disclosed for the preparation of compounds of formula (II) belowR.sup.1 -X.sub.n -NHCH (R.sup.2)-B(OH).sub.
    Type: Grant
    Filed: March 24, 1993
    Date of Patent: January 24, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Charles A. Kettner
  • Patent number: 5248834
    Abstract: Pesticidal compounds of formula II: R.sub.A CR.sub.3 .dbd.CR.sub.4 CHDR.sub.Bin which formula:R.sub.A represents a group ArCR.sub.1 R.sub.2 - in which Ar represents a phenyl or naphthyl group optionally substituted by one or more halogen, alkoxy, haloalkoxy, methylenedioxy, C.sub.1 -C.sub.6 alkyl or haloalkyl groups;R.sub.1 and R.sub.2 together with the carbon to which they are attached represent a C.sub.3 -C.sub.6 cycloalkyl group optionally substituted by one or more halogen atoms or C.sub.1 -C.sub.6 alkyl groups.R.sub.3 and R.sub.4 which may be identical or differ, represent hydrogen halogen or C.sub.1 -C.sub.6 alkyl groups andR.sub.B represents the residue of an alcohol R.sub.B CHDOH in which D is hydrogen or cyano and of which the [1R, cis] 2,2-dimethyl-3-(2,2-dibromovinyl) cyclopropane carboxylic ester is significantly insecticidal,the configuration of R.sub.A and CHDR.sub.
    Type: Grant
    Filed: April 17, 1992
    Date of Patent: September 28, 1993
    Assignee: British Technology Group Limited
    Inventors: Michael Elliott, Norman F. Janes, Bhupinder P. S. Khambay, Ahmet Baydar
  • Patent number: 5231205
    Abstract: The magnesium complexes of cyclic hydrocarbons, such as 1,2-dimethylenecycloalkanes, are readily prepared in high yields using highly reactive magnesium. Reactions of these (2-butene-1,4-diyl)magnesium reagents with electrophiles such as dibromoalkanes, alkylditosylates, or bromoalkylnitriles serve as a convenient method for synthesizing spirocyclic systems. Significantly, spirocarbocycles prepared by thisThe present invention was made with Government support under Contract No. GM35153 awarded by the National Institute of Health. The Government has certain rights in the invention.
    Type: Grant
    Filed: September 23, 1991
    Date of Patent: July 27, 1993
    Assignee: Board of Regents of the University of Nebraska
    Inventor: Reuben D. Rieke
  • Patent number: 5166394
    Abstract: Novel compounds of the formula I ##STR1## in which X is an anion, and a process for the preparation thereof, are described. Compounds of the formula I are used as coupling reagents in peptide synthesis.
    Type: Grant
    Filed: May 21, 1991
    Date of Patent: November 24, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Breipohl, Wolfgang Konig
  • Patent number: 5159100
    Abstract: A process for the production of cyclopropanenitrile derivatives. A diol of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, branched or unbranched, or a C.sub.1 -C.sub.6 alkenyl group, branched or unbranched, or wherein R.sub.1 and R.sub.2 together is a C.sub.4 -C.sub.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: October 27, 1992
    Assignee: Lonza Ltd.
    Inventor: Paul Hanselmann
  • Patent number: 5095133
    Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of alkoxides of the formulaM.sup.1 OR.sup.10 (IV)where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.10, X.sup.- and M.sup.1 have the meaning mentioned in the description.
    Type: Grant
    Filed: July 16, 1990
    Date of Patent: March 10, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz U. Blank, Helmut Kraus
  • Patent number: 4921632
    Abstract: Liquid Crystal compounds represented by the following formula are disclosed. ##STR1## wherein R and R' are independently selected from alkyl groups containing 1.about.20 carbon atoms; X is --O--, --O--CO--O-- or direct bond; A.sub.1 and A.sub.2 are independently cyclic groups (such as phenylene and biphenylene), said cyclic groups may be substituted with 1.about.4 fluorine, chlorine or bromine atoms, or 1 or 2 substituent groups selected from the group consisting of cyano, nitro and trifluoromethyl groups; Y is --CO--O--, --O--CO--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --N.dbd.N--, --CH.sub.2 S--, --SCH.sub.2 -- or direct bond; and * represents asymmetric atom providing optical activity.
    Type: Grant
    Filed: August 19, 1988
    Date of Patent: May 1, 1990
    Assignees: NEC Corporation, Sanyo Chemical Industries, Ltd.
    Inventors: Toyokazu Nakamura, Yuzi Kato, Shohei Naemura, Chizuka Tani, Masahiro Satoh, Kunikiyo Yoshio, Hiroshi Kishiki, Hiroshi Hoshino
  • Patent number: 4853151
    Abstract: Dispirotetradecanes of the formula I ##STR1## wherein R.sup.1 and R.sup.2 are each independently of each other alkyl containing 1 to 12 carbon atoms wherein one or more non-adjacent CH.sub.2 groups may also be replaced by --O--, --CO--, --CO--O--, --O--CO--, --O--COO-- and/or --CH.dbd.CH-- (trans), one of the radicals R.sup.1 and R.sup.2 also being H, F, Cl, Br, I, CN, NO.sub.2, NCS,A.sup.1 and A.sup.2 are each independently of each other trans-1,4-cyclohexylene wherein one or two non-adjacent CH.sub.2 groups may be replaced by --O-- and/or --S--, or 1,4-phenylene wherein one or more CH groups may also be replaced by N, with it also being possible optionally for A.sup.1 and A.sup.2 to be substituted laterally or axially by F, Cl, CN, CH.sub.3,Z.sup.1 and Z.sup.2 are each independently of each other --C--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 -- or a single bond,m and n are each 0, 1 or 2,(m+n) 0, 1 or 2,X.sup.1, X.sup.2, X.sup.3 and X.sup.
    Type: Grant
    Filed: August 11, 1987
    Date of Patent: August 1, 1989
    Assignee: Merck Patent Gesellschaft Mit Beschrankfter Haftung
    Inventors: Fritz Vogtle, Wolfgang Calaminus
  • Patent number: 4833263
    Abstract: An electron-accepting compound represented by the formula (I): ##STR1## wherein R represents a hydrogen atom or --B(Mes).sub.2 and Mes represents a mesityl group.A method for preparing an electron-accepting compound represented by the above-described formula (I), which comprises condensing a benzophenone derivative represented by the following formula (II) with malononitride, ##STR2## wherein R and Mes have the same meanings as defined for the formula (I).
    Type: Grant
    Filed: January 13, 1988
    Date of Patent: May 23, 1989
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Yutaka Akasaki, Katsuhiro Sato, Hiroyuki Tanaka, Katsumi Nukada, Hidemi Sudo