Boron Or Spiro Containing Patents (Class 558/384)
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Patent number: 10112960Abstract: 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: GrantFiled: September 5, 2014Date of Patent: October 30, 2018Assignees: Dow AgroSciences LLC, The Board of Regents of the Michigan State UniversityInventors: Milton R. Smith, Robert E. Maleczka, Hao Li, Chathurika R. K. Jayasundara, Jossian Oppenheimer, Dmitrijs Sabasovs
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Patent number: 9175021Abstract: 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: GrantFiled: November 18, 2014Date of Patent: November 3, 2015Assignee: MERCK PATENT GMBHInventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
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Patent number: 8927757Abstract: 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: GrantFiled: January 12, 2011Date of Patent: January 6, 2015Assignee: Merck Patent GmbHInventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
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Patent number: 8921589Abstract: 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: GrantFiled: September 1, 2011Date of Patent: December 30, 2014Assignee: Merck Patent GmbHInventors: Kentaro Kawata, Nikolai Mykola Ignatyev, Michael Schulte, Hiroki Yoshizaki
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Patent number: 8901340Abstract: 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: GrantFiled: January 12, 2011Date of Patent: December 2, 2014Assignee: Merck Patent GmbHInventors: Hiromi Shinohara, Kentaro Kawata, Hiroki Yoshizaki, Peer Kirsch, Nikolai (Mykola) Ignatyev, William Robert Pitner, Michael Schulte, Jan Sprener, Maik Finze, Walter Frank
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Publication number: 20140312311Abstract: 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: ApplicationFiled: July 11, 2013Publication date: October 23, 2014Inventors: Chien-Tien CHEN, Wei-Shan CHAO, Hao-Wei LIU, Wei-Sheng SU
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Patent number: 8859800Abstract: 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: GrantFiled: July 6, 2012Date of Patent: October 14, 2014Assignee: Merck Patent GmbHInventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Jan Sprenger, Maik Finze, Walter Frank
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Publication number: 20140296223Abstract: 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: ApplicationFiled: August 31, 2012Publication date: October 2, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
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Patent number: 8835667Abstract: 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: GrantFiled: January 12, 2011Date of Patent: September 16, 2014Assignee: Merck Patent GmbHInventors: Hiromi Shinohara, Kentaro Kawata, Hiroki Yoshizaki, Peer Kirsch, Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
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Patent number: 8829201Abstract: 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: GrantFiled: July 6, 2012Date of Patent: September 9, 2014Assignee: Merck Patent GmbHInventors: Kentaro Kawata, Hiroki Yoshizaki, Hiromi Shinohara, Peer Kirsch, Nikolai (Mykola) Ignatyev, William-Robert Pitner, Emil Ferdinand Aust, Marlies Waterman
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Publication number: 20140155566Abstract: 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: ApplicationFiled: July 6, 2012Publication date: June 5, 2014Applicant: MERCK PATENT GMBHInventors: Nikolai (Mykola) Ignatyen, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Jan Sprenger, Maik Finze, Walter Frank
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Publication number: 20140107341Abstract: 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: ApplicationFiled: May 23, 2012Publication date: April 17, 2014Applicant: MERCK PATENT GMBHInventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Eduard Bernhardt, Vera Bernhardt-pitchougina, Helge Willner
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Patent number: 8653258Abstract: 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: GrantFiled: June 6, 2008Date of Patent: February 18, 2014Assignee: 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
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Publication number: 20140024635Abstract: 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: ApplicationFiled: September 25, 2013Publication date: January 23, 2014Applicant: The Trustees of The University Of PennsylvaniaInventors: WILLIAM F. DeGRADO, JUN WANG
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Publication number: 20130289050Abstract: 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: ApplicationFiled: March 4, 2013Publication date: October 31, 2013Applicants: VITAE PHARMACEUTICALS, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
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Publication number: 20130289000Abstract: 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: ApplicationFiled: June 24, 2013Publication date: October 31, 2013Inventors: Tsutomu Akama, Jacob J. Plattner
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Publication number: 20130244980Abstract: 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: ApplicationFiled: April 30, 2013Publication date: September 19, 2013Applicant: 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
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Patent number: 8436199Abstract: 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: GrantFiled: November 25, 2009Date of Patent: May 7, 2013Assignee: Merck Patent GmbHInventors: Maik Finze, Eduard Bernhardt, Helge Willner, Nikolai (Mykola) Ignatyev, Urs Welz-Biermann
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Publication number: 20120296096Abstract: 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: ApplicationFiled: January 12, 2011Publication date: November 22, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Hiromi Shinohara, Kentaro Kawata, Hiroki Yoshizaki, Peer Kirsch, Nikolai (Mykola) Ignatyev, William Robert Pitner, Michael Schulte, Jan Sprener, Maik Finze, Walter Frank
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Publication number: 20120289686Abstract: 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: ApplicationFiled: January 23, 2012Publication date: November 15, 2012Applicant: 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
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Publication number: 20120214765Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: ApplicationFiled: September 19, 2011Publication date: August 23, 2012Applicant: 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
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Publication number: 20120035132Abstract: Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed.Type: ApplicationFiled: January 27, 2011Publication date: February 9, 2012Applicant: Anacor Pharmaceuticals, Inc.Inventors: Kurt Jarnagin, Tsutomu Akama
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Publication number: 20120028957Abstract: 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: ApplicationFiled: August 1, 2010Publication date: February 2, 2012Inventors: William F. DeGrado, Jun Wang
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Publication number: 20120015933Abstract: 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: ApplicationFiled: September 29, 2011Publication date: January 19, 2012Applicant: SANOFI-AVENTISInventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
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Publication number: 20110207702Abstract: 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: ApplicationFiled: October 15, 2009Publication date: August 25, 2011Applicant: 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
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Publication number: 20110184175Abstract: 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: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Applicant: STELLA PHARMA CORPORATIONInventors: Mitsunori Kirihata, Tomoyuki Asano, Kohki Uehara, Yoshihide Hattori
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Publication number: 20110160366Abstract: 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: ApplicationFiled: December 10, 2010Publication date: June 30, 2011Applicant: CHEIL INDUSTRIES INC.Inventors: Woo Joong KIM, Seung Shik SHIN, Jin Hwan CHOI
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Publication number: 20110124877Abstract: 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: ApplicationFiled: August 24, 2009Publication date: May 26, 2011Applicant: KUREHA CORPORATIONInventors: Atsushi Ito, Takashi Shimokawara, Eiyu Imai, Yoichi Kanda, Nobuyuki Kusano, Masaru Mori, Rumi Suzuki
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Publication number: 20100254903Abstract: 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: ApplicationFiled: July 24, 2008Publication date: October 7, 2010Inventors: David Perrin, Richard Ting, Christopher Overall
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Publication number: 20100190748Abstract: 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: ApplicationFiled: July 21, 2009Publication date: July 29, 2010Applicant: 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
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Publication number: 20100137249Abstract: 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: ApplicationFiled: June 6, 2008Publication date: June 3, 2010Inventors: Binghe Wang, Nanting Ni, Junfeng Wang, Chung-Dar Lu, Han-Ting Chou, Minyong Li, Shilong Zheng, Yunfeng Cheng, Hanjing Peng
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Publication number: 20100069655Abstract: 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: ApplicationFiled: November 25, 2009Publication date: March 18, 2010Inventors: Maik FINZE, Eduard BERNHARDT, Helge WILLNER, Nikolai (Mykola) IGNATYEV, Urs WELZ-BIERMANN
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Publication number: 20090291917Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: ApplicationFiled: March 5, 2009Publication date: November 26, 2009Applicant: 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
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Publication number: 20090275523Abstract: 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: ApplicationFiled: November 25, 2008Publication date: November 5, 2009Applicant: SANOFI-AVENTISInventors: Manfred Schudok, Michael Wagner, Armin Bauer, Anna Kohlmann
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Publication number: 20080312451Abstract: 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: ApplicationFiled: September 20, 2006Publication date: December 18, 2008Applicant: KRKA, d.d. Novo mestoInventors: Miroslav Veverka, Martin Putala, Heinrich Brath, Silvo Zuppancic
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Patent number: 6562993Abstract: 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: GrantFiled: May 10, 2002Date of Patent: May 13, 2003Assignee: ISP Investments Inc.Inventors: Steven H. Bertz, Samuel T. D'Arcangelis, Ilya Makarovskiy, John J. Merianos
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Patent number: 6525036Abstract: 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: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Patent number: 5849958Abstract: 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: GrantFiled: March 17, 1997Date of Patent: December 15, 1998Assignee: American Cyanamid CompanyInventors: Keith D. Barnes, Yulin Hu
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Patent number: 5486622Abstract: 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: GrantFiled: April 5, 1995Date of Patent: January 23, 1996Assignee: Lonza Ltd.Inventor: Paul Hanselmann
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Patent number: 5470994Abstract: 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: GrantFiled: April 5, 1990Date of Patent: November 28, 1995Assignee: Eastman Kodak CompanyInventors: Franklin D. Saeva, David T. Breslin
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Patent number: 5401869Abstract: 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: GrantFiled: January 21, 1994Date of Patent: March 28, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Nikolaus Muller, Gerhard Marzolph, Bernhard Beitzke
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Patent number: 5384410Abstract: 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: GrantFiled: March 24, 1993Date of Patent: January 24, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Charles A. Kettner
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Patent number: 5248834Abstract: 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: GrantFiled: April 17, 1992Date of Patent: September 28, 1993Assignee: British Technology Group LimitedInventors: Michael Elliott, Norman F. Janes, Bhupinder P. S. Khambay, Ahmet Baydar
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Patent number: 5231205Abstract: 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: GrantFiled: September 23, 1991Date of Patent: July 27, 1993Assignee: Board of Regents of the University of NebraskaInventor: Reuben D. Rieke
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Patent number: 5166394Abstract: 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: GrantFiled: May 21, 1991Date of Patent: November 24, 1992Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breipohl, Wolfgang Konig
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Patent number: 5159100Abstract: 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: GrantFiled: December 13, 1991Date of Patent: October 27, 1992Assignee: Lonza Ltd.Inventor: Paul Hanselmann
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Patent number: 5095133Abstract: 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: GrantFiled: July 16, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Heinz U. Blank, Helmut Kraus
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Patent number: 4921632Abstract: 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: GrantFiled: August 19, 1988Date of Patent: May 1, 1990Assignees: NEC Corporation, Sanyo Chemical Industries, Ltd.Inventors: Toyokazu Nakamura, Yuzi Kato, Shohei Naemura, Chizuka Tani, Masahiro Satoh, Kunikiyo Yoshio, Hiroshi Kishiki, Hiroshi Hoshino
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Patent number: 4853151Abstract: 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: GrantFiled: August 11, 1987Date of Patent: August 1, 1989Assignee: Merck Patent Gesellschaft Mit Beschrankfter HaftungInventors: Fritz Vogtle, Wolfgang Calaminus
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Patent number: 4833263Abstract: 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: GrantFiled: January 13, 1988Date of Patent: May 23, 1989Assignee: Fuji Xerox Co., Ltd.Inventors: Yutaka Akasaki, Katsuhiro Sato, Hiroyuki Tanaka, Katsumi Nukada, Hidemi Sudo