Plural Nitrogens In The Six-membered Hetero Ring Patents (Class 544/66)
  • Patent number: 11884639
    Abstract: A field of asymmetric catalytic synthesis, and in particular a preparation method for a high optical indoxacarb intermediate includes reacting 5-chloro-2-methoxycarbonyl-1-indanone ester (or indanone ester for short) with an oxidizing agent in the presence of a chiral Zr-salen polymer to obtain an indoxacarb intermediate (2S)-5-chloro-2,3-dihydro-2-hydroxy-1-oxo-1H-indole-2-carboxylic acid methyl ester. The yield is stabilized between 86% and 90%, and the S-enantiomer content is up to 99%. Such catalyst can replace catalysts such as cinchonine, and greatly increase the content of the effective S-enantiomer of the indoxacarb, so that the content of the hydroxyl intermediate S-enantiomer of the indoxacarb is raised from 75% to 99% or more. In addition, the chiral Zr-salen polymer catalyst is recycled without retreatment, and can be recycled at least 5 times or more, greatly reducing the production cost and laying a foundation for the industrial production of high quality indoxacarb.
    Type: Grant
    Filed: April 25, 2019
    Date of Patent: January 30, 2024
    Assignee: SHANDONG JINGBO AGROCHEMICALS TECHNOLOGY CO., LTD.
    Inventors: Zhongyang Wang, Daoquan Cheng, Tingchao Pang, Ping Wang, Jiancheng Liu, Renping Han, Lianyou Yu, Nengchun Wei
  • Patent number: 9453007
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: September 27, 2016
    Assignees: ABBVIE INC., ABBOTT PRODUCTS GMBH
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
  • Publication number: 20150031691
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 29, 2015
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Publication number: 20140303154
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: June 19, 2014
    Publication date: October 9, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Publication number: 20140275525
    Abstract: The invention relates to a method for modifying isocyanates using catalysts having a water content not exceeding 1,000 ppm.
    Type: Application
    Filed: November 27, 2012
    Publication date: September 18, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Frank Richter, Martin Brahm
  • Publication number: 20140221362
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
  • Publication number: 20140221203
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip LAHM, Renee Marie LETT, Brenton Todd SMITH, Benjamin Kenneth SMITH, Clarice Anne TYLER
  • Patent number: 8796265
    Abstract: An anti-infection solution including (i) from 10% to 30% by weight with respect to the total volume of the solution of at least one compound of Formula (I): wherein: X represents a hydrogen or halogen atom or a hydroxy function, R1 represents: a 1-piperazinyl radical, which may be substituted in position 4 by a methyl, acetyl or 4-aminobenzyl group; a morpholino radical: a 1-pyrrolidinyl radical substituted in position 3 by a chlorine atom or by an amino, aminomethyl, (methylamino) methyl, (ethylamino) methyl or methoxy group; a 1-imidazolyl radical that can be substituted in position 4 by the methyl group, or a 1-piperidyl radical substituted in position 4 by a hydroxy or methoxy group, and R2 represents an alkyl radical, linear, branched or ring, including 1 to 10 carbon atoms, or at least one of its pharmaceutically acceptable salts, (ii) benzyl alcohol as a stabilizing agent, and at least one stabilizing agent, and (iii) at least one solubilization agent selected from the group consisting of carbolic
    Type: Grant
    Filed: January 24, 2007
    Date of Patent: August 5, 2014
    Assignee: SA Vetoquinol
    Inventor: Marinette Moreau
  • Publication number: 20140179691
    Abstract: Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.
    Type: Application
    Filed: March 29, 2012
    Publication date: June 26, 2014
    Applicant: LEGOCHEM BIOSCIENCES, INC.
    Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Sun Young Kim, Hong Bum Lee, Hyang Sook Lee, Kyuman Oh, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim, Hye Jin Heo
  • Patent number: 8685964
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: April 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
  • Patent number: 8673900
    Abstract: In many embodiments, the present invention provides novel heterocyclic compounds which are modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Jun Qin, Xiaoxiang Liu, Hongmei Li, Wei Zhou, Anandan Palani, Xiaohong Zhu, Monica L. Vicarel, Mihirbaran Mandal, Zhong-Yue Sun, Chad E. Bennett, Troy Michael McCracken, Gioconda V. Gallo
  • Publication number: 20140038919
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: February 6, 2014
    Applicant: AbbVie Inc.
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
  • Patent number: 8637667
    Abstract: Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: January 28, 2014
    Assignee: Legochem Bioscience Ltd.
    Inventors: Young Lag Cho, Jong Un Cho, Sung Yoon Baek, Ho Young Song, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Publication number: 20130331384
    Abstract: The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.
    Type: Application
    Filed: February 14, 2012
    Publication date: December 12, 2013
    Applicant: The Regents of the University of California
    Inventors: Richard L. Gallo, Teruaki Nakatsuji
  • Publication number: 20130267482
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Application
    Filed: June 3, 2013
    Publication date: October 10, 2013
    Inventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
  • Publication number: 20130230506
    Abstract: The present invention relates to a bioactive agent capable of increasing the intracellular concentration and/or activity of Hsp70 for use in the treatment of a lysosomal storage disease which arise from a defect in an enzyme whose activity is not directly associated with the presence of lysosomal BMP as a co-factor; such as glycogen storage diseases, gangliosidoses, neuronal ceroid lipofuscinoses, cerebrotendinous cholesterosis, Wolman's disease, cholesteryl ester storage disease, disorders of glycosaminoglycan metabolism, mucopolysaccharidoses, disorders of glycoprotein metabolism, mucolipidoses, aspartylglucosaminuria, fucosidosis, mannosidoses, and sialidosis type II.
    Type: Application
    Filed: November 22, 2011
    Publication date: September 5, 2013
    Applicant: ORPHAZYME APS
    Inventors: Thomas Kirkegaard Jensen, Anders Morkeberg Hinsby
  • Publication number: 20130210805
    Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
    Type: Application
    Filed: October 6, 2011
    Publication date: August 15, 2013
    Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
  • Patent number: 8486934
    Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: July 16, 2013
    Assignee: Bayer CropScience AG
    Inventors: Bernd-Wieland Krüger, Achim Hense, Bernd Alig, Rüdiger Fischer, Christian Funke, Ernst Rudolf Gesing, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold, Peter Lümmen, Erich Sanwald
  • Patent number: 8450485
    Abstract: Novel benzoxazole derivatives are provided to reduce driving voltage of light-emitting elements, and to reduce power consumption of light-emitting elements, light-emitting devices, and electronic devices. A benzoxazole derivative represented by the general formula (G1) is provided. Since the benzoxazole derivative represented by the general formula (G1) has an electron-injecting property, the benzoxazole derivative can be suitably used for light-emitting elements, light-emitting devices, and electronic devices.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Hiroko Nomura, Takahiro Ushikubo, Satoshi Seo
  • Patent number: 8426403
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: April 23, 2013
    Inventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Brian A. McKittrick, John W. Clader, Mark D. McBriar, Anandan Palani
  • Patent number: 8350025
    Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: January 8, 2013
    Assignee: Syngenta Limited
    Inventors: Gillan Beveridge, Ewan Campbell Boyd, Jack Hugh Vass, Alan John Whitton
  • Publication number: 20120245158
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I.
    Type: Application
    Filed: June 15, 2010
    Publication date: September 27, 2012
    Inventors: Xianhai Huang, Zhaoning Zhu, William J. Greenlee, Anandan Palani, Robert G. Aslanian
  • Publication number: 20120227545
    Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.
    Type: Application
    Filed: July 21, 2010
    Publication date: September 13, 2012
    Applicant: ANGLO OPERATIONS LIMITED
    Inventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
  • Patent number: 8242112
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: August 14, 2012
    Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Patent number: 8242113
    Abstract: Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: August 14, 2012
    Assignee: Legochem Biosciences, Inc.
    Inventors: Young Lag Cho, Sang Eun Chae, Sung Yoon Baek, Yeon Ok Kim, Seong Jin Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Patent number: 8178525
    Abstract: Disclosed are novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions containing the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: May 15, 2012
    Assignee: Legochem Bioscience Ltd.
    Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Publication number: 20120108808
    Abstract: Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.
    Type: Application
    Filed: July 7, 2010
    Publication date: May 3, 2012
    Applicant: LEGOCHEM BIOSCIENCE LTD.
    Inventors: Young Lag Cho, Jong Un Cho, Sung Yoon Baek, Ho Young Song, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Publication number: 20120107328
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Application
    Filed: November 3, 2008
    Publication date: May 3, 2012
    Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
  • Publication number: 20120058891
    Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.
    Type: Application
    Filed: November 9, 2011
    Publication date: March 8, 2012
    Applicant: Bayer CropScience AG
    Inventors: Bernd-Wieland Krüger, Achim Hense, Bernd Alig, Rüdiger Fischer, Christian Funke, Ernst Rudolf Gesing, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold, Peter Lümmen, Erich Sanwald
  • Publication number: 20120022054
    Abstract: The present invention concerns novel substituted aryl derivatives, their process of preparation and their use for inhibiting virus replication and for treating viral diseases or disorders such as HIV and/or HCV infection.
    Type: Application
    Filed: December 10, 2009
    Publication date: January 26, 2012
    Applicant: LABORATOIRE BIODIM
    Inventors: Richard Benarous, Sabine Barbey-Treve, Jean-Marc Paris, Sebastien Berrut, Clarisse Berlioz-Torrent, Stephane Emiliani
  • Patent number: 8084603
    Abstract: The present invention relates to naphthalenetetracarboxylic acid derivates, to a process for their preparation and to their use, especially as an n-type semiconductor.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: December 27, 2011
    Assignee: BASF Aktiengesellschaft
    Inventor: Martin Koenemann
  • Publication number: 20110306593
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
    Type: Application
    Filed: November 11, 2009
    Publication date: December 15, 2011
    Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
  • Patent number: 8071590
    Abstract: A subject of the invention is the compounds of formula (I): wherein R1, R2, R3, R?3, R4, R?4, R5, R6 and R7 are as described in the application, in the form of enantiomers or mixtures, as well as their salts with acids and bases, their preparation and their application as anti-bacterials, in both human and veterinary medicine.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: December 6, 2011
    Assignee: Vetoquinol SA
    Inventors: Sandrine Ropp, Christophe Morice, Bruno Giethlen, Paola Ciapetti, Florence Chery-Mozziconacci, Camille G. Wermuth, Francoise Leblanc, Marc Schneider
  • Publication number: 20110294756
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 12, 2009
    Publication date: December 1, 2011
    Inventors: Zhaoning Zhu, William J., Xianhai Huang, Jun Qin, XIaoxiang Liu, Hongmei Li, Wei Zhou, Anandan Palani, Xiaohong Zhu, Monica L. Vicarel, Mihirbaran Mandal, Zhong-Yue Sun, Chad E. Bennett, Troy Michael McCracken, Gioconda V. Gallo
  • Publication number: 20110275802
    Abstract: The present invention relates to a process for modifying diisocyanates for preparing polyisocyanates, where the diisocyanate is reacted using a catalyst, wherein the diisocyanate used is obtained by quenching a gaseous reaction mixture in the phosgenation of diamines in the gas phase, wherein the gaseous reaction mixture comprises at least a diisocyanate, phosgene and hydrogen chloride, wherein a quenching liquid is sprayed into the gas mixture which flows continuously from a reaction zone into a downstream quenching zone, and wherein the quenching liquid is sprayed in by at least two spray nozzles which are arranged at the inlet of the quenching zone at equal intervals along the circumference of the quenching zone.
    Type: Application
    Filed: November 26, 2009
    Publication date: November 10, 2011
    Applicant: BAYER MATERIALSCIENCE AG
    Inventors: Frank Richter, Reinhard Halpaap
  • Publication number: 20110218194
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: May 16, 2011
    Publication date: September 8, 2011
    Applicant: Schering Corporation & Pharmacopeia Drug Discovery Inc.
    Inventors: Zhaoning Zhu, Brian A. Mckittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachel C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
  • Publication number: 20110212949
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: July 4, 2009
    Publication date: September 1, 2011
    Inventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Füßlein, Achim Hense, Joachim Kluth, Hans-Georg Schwarz, Adeline Köhler, Olga Malsam, Arnd Voerste, Angela Becker
  • Publication number: 20110178293
    Abstract: Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.
    Type: Application
    Filed: September 22, 2009
    Publication date: July 21, 2011
    Applicant: LEGOCHEM BIOSCIENCE LTD.
    Inventors: Young Lag Cho, Sang Eun Chae, Sung Yoon Baek, Yeon Ok Kim, Seong Jin Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Publication number: 20110112083
    Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.
    Type: Application
    Filed: June 5, 2009
    Publication date: May 12, 2011
    Applicant: LEGOCHEM BIOSCIENCE LTD.
    Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Patent number: 7939685
    Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: May 10, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Albert Loren Casalnuovo
  • Publication number: 20110092459
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Application
    Filed: June 5, 2009
    Publication date: April 21, 2011
    Applicant: PRISM Biolab Corporation
    Inventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
  • Publication number: 20110071126
    Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
    Type: Application
    Filed: March 12, 2010
    Publication date: March 24, 2011
    Inventors: Salvacion CACATIAN, David A. CLAREMON, Lawrence W. DILLARD, Klaus FUCHS, Niklas HEINE, Lanqi JIA, Katerina LEFTHERIS, Brian McKEEVER, Angel MORALES-RAMOS, Suresh B. SINGH, Shankar VENKATRAMAN, Guosheng WU, Zhongren WU, Zhenrong XU, Jing YUAN, Yajun ZHENG
  • Patent number: 7910058
    Abstract: Applicants have produced a chromophore and a polymer that are highly sensitive to the presence of various agents, including organophosphates, pesticides, neurotoxins, metal ions, some explosives, and biological toxins. The detection is accomplished by detecting a change in the fluorescence characteristics of the chromophore or polymer when in the presence of the agent to be detected. The chromophore and polymer may be incorporated into sensors of various types, and they are adaptable for potential field use in areas where detection of these types of agents is desired.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: March 22, 2011
    Assignee: NDSU—Research Foundation
    Inventors: Johnson Thomas, Philip Boudjouk
  • Publication number: 20110059946
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Application
    Filed: September 10, 2010
    Publication date: March 10, 2011
    Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin
  • Publication number: 20100267711
    Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.
    Type: Application
    Filed: June 25, 2010
    Publication date: October 21, 2010
    Applicant: CytRx Corporation
    Inventors: László Vígh, Péter Literáti Nagy, Jenó Szilbereky, László Ürögdi, Andrea Jednákovits, László Jaszlits, Katalin Bíró, Ede Màrvànyos, Mihály Barabás, Erzsébet Hegedüs, László Korányi, Mária Kürthy, Gábor Balogh, Ibolya Horváth, Zsolt Török, Éva Udvardy, György Dormán, Dénes Medzihradszky, Bea Mézes, Eszter Kovács, Ernó Duda, Beatrix Farkas, Attila Glatz
  • Publication number: 20100256128
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: May 28, 2008
    Publication date: October 7, 2010
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Brian A. McKittrick, John W. Clader, Mark D. McBriar, Anandan Palani
  • Patent number: 7767667
    Abstract: It has now been found that certain novel heterocyclic derivitives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, -, where R,R,R6, R7, R8, RI1, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound with at least one insecticidally compatable carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: August 3, 2010
    Assignee: FMC Corporation
    Inventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
  • Patent number: 7763609
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: July 27, 2010
    Assignees: Schering Corporation, Pharmacopeia, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Publication number: 20100168091
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated 3-amyloid deposits or 3-amyloid levels in a patient.
    Type: Application
    Filed: March 5, 2010
    Publication date: July 1, 2010
    Applicant: Wyeth LLC
    Inventors: Michael Sotirios Malamas, Keith Douglas Barnes, Matthew Robert Johnson
  • Patent number: 7718818
    Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: May 18, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Albert Loren Casalnuovo