Benzene Ring Containing Patents (Class 564/139)
  • Patent number: 11471868
    Abstract: This disclosure relates to synthetic coupling methods using catalytic molecules. In certain embodiments, the catalytic molecules comprise heterocyclic thiolamide, S-acylthiosalicylamide, disulfide, selenium containing heterocycle, diselenide compound, ditelluride compound or tellurium containing heterocycle.
    Type: Grant
    Filed: October 9, 2020
    Date of Patent: October 18, 2022
    Assignee: Emory University
    Inventors: Lanny Steven Liebeskind, Pavan Kumar Reddy Gangireddy
  • Patent number: 10889540
    Abstract: The present application provides a preparation method of a formamide compound, the preparation process includes: uniformly mixing raw material of methanoic acid and an amine compound selected from a primary amine or a secondary amine to prepare a homogeneous reaction system; the above homogeneous reaction system is heated to 160-230° C., allowing carbon monoxide to be decomposed from the homogeneous reaction system and participates in the reaction, and collecting the reaction product to obtain a formamide compound. The present application provides a new technology using a homogeneous method to synthesize a formamide compound, the reaction process needs no use of a catalyst, the operation process is simple and controllable, and the raw material of the amine compound has a high selectivity.
    Type: Grant
    Filed: January 15, 2018
    Date of Patent: January 12, 2021
    Assignee: BEIJING J-TEC TECHNOLOGY CO., LTD
    Inventors: Chenghan Tang, Yunjian Zhao, Anxing Wei, Wei Guo
  • Patent number: 9604911
    Abstract: Process for the industrial synthesis of the compound of formula (I):
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: March 28, 2017
    Assignee: LES LABORATOIRES SERVIER
    Inventors: Jean-François Briere, Raphaël Lebeuf, Vincent Levacher, Christophe Hardouin, Jean-Pierre Lecouve
  • Patent number: 9394241
    Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.
    Type: Grant
    Filed: October 28, 2013
    Date of Patent: July 19, 2016
    Assignee: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventor: Jung-Mo Ahn
  • Publication number: 20150148543
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: Feng Li, Yihan Wang
  • Patent number: 9024028
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: May 5, 2015
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Feng Li, Yihan Wang
  • Publication number: 20150065681
    Abstract: Disclosed herein is a method of preparing prepolymer particles. The method includes injecting a prepolymer in a solution state by bottom-up type injection to form prepolymer particles by removing a solvent from the prepolymer in a solution state. The method can prepare prepolymer particles, which can be used in solid-state polymerization, using a bottom-up type flash process.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Inventors: Jin Kyu KIM, So Young KWON, Sang Kyun IM, Ki Yon LEE, Suk Min JUN, Gook Geon BAE
  • Patent number: 8969620
    Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R1, R2 and R3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: March 3, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
  • Publication number: 20150025274
    Abstract: This invention relates to processes for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide (I) and intermediates thereof. Formula (I).
    Type: Application
    Filed: August 29, 2012
    Publication date: January 22, 2015
    Applicant: SIGNA S.A. DE C.V.
    Inventors: Pablo Miguel Bernal-Vazquez, José Miguel Lazcano-Seres, Yaneth Mariá-Antonieta Contreras-Martinez, Jorge Alberto Juárez-Lagunas, Donato Sánchez-Mereles, Juan Rolando Vázquez-Miranda, Armando Zambrano-Huerta
  • Patent number: 8907132
    Abstract: Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy-propionamide of formula-1 and intermediates thereof are provided.
    Type: Grant
    Filed: February 9, 2011
    Date of Patent: December 9, 2014
    Assignee: MSN Laboratories Private Limited
    Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Aluru Srinivas, Revu Satyanarayana
  • Publication number: 20140171649
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
    Type: Application
    Filed: January 26, 2012
    Publication date: June 19, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: Feng Li, Yihan Wang
  • Patent number: 8710098
    Abstract: A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: April 29, 2014
    Assignee: Institute of Medicinal Biotechnology Chinese Academy of Medical Science
    Inventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhuorong Li, Yanping Li, Jian Xu
  • Patent number: 8637707
    Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.
    Type: Grant
    Filed: July 3, 2009
    Date of Patent: January 28, 2014
    Assignees: BASF SE, Technische Universitaet Muenchen
    Inventors: Michael Keil, Michael Rack, Thomas Zierke, Markus Heinrich, Alexander Wetzel
  • Publication number: 20130267729
    Abstract: Disclosed are methods for preparing compounds of Formula 1 and 1A. The first method utilizes a benzyl carbamate amine protecting group and an intermediate of Formula 4. The second method utilizes a tert-butyl carbamate amine protecting group and an intermediate of Formula 7. The third method utilizes a dibenzyl amine protecting group. Also disclosed is a compound, phenylmethyl N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamate (a compound of Formula 4). Further disclosed is a method for preparing a compound of Formula 14 from a compound of Formula 15 and a compound of Formula 1 or 1A.
    Type: Application
    Filed: September 23, 2011
    Publication date: October 10, 2013
    Applicant: E.I. du Pont de Nemours and Company
    Inventor: Joerg Bruening
  • Patent number: 8546612
    Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: October 1, 2013
    Assignee: Obschestvo S Ogranichennoi Otvetstvennostiyu Pharmenterprises
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
  • Publication number: 20130245269
    Abstract: The present invention describes tripodal catechol derivatives with an adamantyl basic framework for the functionalisation of surfaces, methods for their production and use. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, by way of example with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Application
    Filed: September 7, 2011
    Publication date: September 19, 2013
    Applicant: JUSTUS-LIEBIG-UNIVERSITA GIESSEN
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • Publication number: 20130210918
    Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.
    Type: Application
    Filed: April 15, 2013
    Publication date: August 15, 2013
    Applicant: The Scripps Research Institute
    Inventors: Joel M. Gottesfeld, Kai Jenssen, David M. Herman, Ryan Burnett, C. James Chou
  • Patent number: 8501993
    Abstract: The invention relates to a process for the preparation of intermediates useful in the preparation of fungicidally active phenylpropargylether derivatives. The process involves coupling of carboxylic acid with an amine in (a) the absence of a catalyst; (b) the presence of a boronic acid catalyst.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: August 6, 2013
    Assignee: Syngenta Limited
    Inventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, David Drouard
  • Publication number: 20130190533
    Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R1, R2 and R3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.
    Type: Application
    Filed: September 29, 2011
    Publication date: July 25, 2013
    Applicant: UCB PHARMA GMBH
    Inventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
  • Patent number: 8487134
    Abstract: The invention relates to processes for preparing acylated amphetamine, methamphetamine and dexamphetamine derivatives by reacting the parent amine with the to be-coupled acid or a salt of the to-be coupled acid which acid is optionally protected, in the presence of an alkylphosphonic acid anhydride as coupling agent and, if the acid was protected then cleaving the protecting group(s), in a one-pot reaction or in two or more separate steps.
    Type: Grant
    Filed: October 9, 2008
    Date of Patent: July 16, 2013
    Assignee: Archimica, Inc.
    Inventors: Andreas Meudt, Richard Wisdom, Jason Helmke, Quofang Qiu, Paul Meek
  • Patent number: 8461384
    Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: June 11, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Frank W. Moser, Christopher W. Grote, Gary L. Cantrell
  • Patent number: 8445708
    Abstract: The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.
    Type: Grant
    Filed: October 27, 2006
    Date of Patent: May 21, 2013
    Assignee: Reuter Chemischer Apparatebau KG
    Inventors: Milan Soukup, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
  • Patent number: 8431514
    Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: April 30, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Maienfisch
  • Publication number: 20130041180
    Abstract: Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy-propionamide of formula-1 and intermediates thereof are provided.
    Type: Application
    Filed: February 9, 2011
    Publication date: February 14, 2013
    Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Aluru Srinivas, Revu Satyanarayana
  • Patent number: 8334411
    Abstract: A method for producing a diamine includes purifying a diamine from an aqueous solution containing a diamine salt by adding an alkaline substance to the aqueous solution and then filtering the resulting solution by allowing the solution to pass through a nanofiltration membrane to remove the salt, thereby obtaining an aqueous diamine solution.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: December 18, 2012
    Assignee: Toray Industries, Inc.
    Inventors: Masateru Ito, Izumi Nakagawa, Koya Kato, Takashi Mimitsuka, Kenji Sawai, Shin-ichi Minegishi, Hideki Sawai, Katsushige Yamada
  • Patent number: 8299241
    Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: October 30, 2012
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
  • Publication number: 20120234204
    Abstract: The present invention provides a process for the production of functionalized carbon nanotubes. The inventive process for the production of functionalized carbon nanotubes involves reacting carboxylic acid moieties of oxidized carbon nanotubes with vapors of a compound containing carboxylic acid reactive groups to produce functionalized carbon nanotubes. The present invention also provides a composition made from a plastic resin and functionalized carbon nanotubes produced by reacting carboxylic acid moieties of oxidized carbon nanotubes with a vapor containing carboxylic acid reactive groups to produce functionalized carbon nanotubes. The inventive process is useful with single-walled carbon nanotubes, double-walled carbon nanotubes and multi-walled carbon nanotubes.
    Type: Application
    Filed: March 17, 2011
    Publication date: September 20, 2012
    Applicants: Bayer MaterialScience AG, Bayer MaterialScience LLC
    Inventors: Serkan Unal, Robert N. Hunt, Heiko Hocke
  • Publication number: 20120209011
    Abstract: This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C1-C7 alkyl; C7-C17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and (CH2)nOR2 wherein n is from 1 to 3 and R2 represents a C6-C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and R1 is selected from OR3 and NHR3 wherein R3 is C1-C6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.
    Type: Application
    Filed: December 21, 2009
    Publication date: August 16, 2012
    Inventors: Chandrashekar Aswathanarayanappa, Pullela Venkata Srinivas, Divya Kangath, Thilak Gregory Soundararajan, Anegondi Sreenivasa Prasad, Suriyan Masinaickenpatty Raghavendran
  • Publication number: 20120178783
    Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N; wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Inventors: John S. Kovach, Francis Johnson
  • Patent number: 8183413
    Abstract: Provided is a process for production of a ?-amino-?-hydroxy carboxamide derivative that is important in production of drugs or the like. In the presence of a predetermined solvent, a ?-(N-protected)amino-?-hydroxycarboxylic acid is reacted with an amine to conversion to a ?-(N-protected)amino-?-hydroxy carboxamide derivative; then the derivative is deprotected for conversion to a ?-amino-?-hydroxy carboxamide derivative; and the derivative is crystallized using a protic solvent to obtain a crystal. The high-purity ?-amino-?-hydroxy carboxamide derivative can be stably produced on an industrial scale by the process.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: May 22, 2012
    Assignee: Kaneka Corporation
    Inventors: Narumi Kishimoto, Hiroaki Yasukouchi, Toshihiro Takeda
  • Patent number: 8143442
    Abstract: A process for the preparation of a compound of formula (Ia): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: March 27, 2012
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Gerard John Harnett, Ursula Hoffmann, Michael Jansen, Reinhard Reents, Tim Sattelkau, Dennis A. Smith, Helmut Stahr
  • Patent number: 8143449
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: March 27, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Christophe Hardouin, Jean-Pierre Lecouve
  • Publication number: 20110309001
    Abstract: The invention relates to a class of novel surfactants that have utility in the recovery and/or extraction of oil.
    Type: Application
    Filed: December 2, 2010
    Publication date: December 22, 2011
    Inventors: David Soane, Rosa Casado Portilla, John H. Dise, Robert P. Mahoney
  • Publication number: 20110313196
    Abstract: The present invention relates to a process for the preparation of benzamide derivatives which are useful as intermediates in the preparation of pharmaceutically active compounds.
    Type: Application
    Filed: June 6, 2011
    Publication date: December 22, 2011
    Inventors: Stephan Bachmann, Fritz Bliss, Ralph Diodone, Stefan Hildbrand, Michael Kammerer, Christophe Pfleger, Reinhard Reents, Michelangelo Scalone
  • Patent number: 8067635
    Abstract: The invention relates to a method for producing tertiary amides of alkylphenyl carboxylic acids by reacting at least one secondary amine with at least one alkylphenyl carboxylic acid to form an ammonium salt, said ammonium salt being subsequently converted into the tertiary amide by means of microwave radiation.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: November 29, 2011
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Matthias Krull, Roman Morschhaeuser, Alexander Lerch, Helmut Ritter, Sarah Schmitz
  • Publication number: 20110281954
    Abstract: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.
    Type: Application
    Filed: May 17, 2011
    Publication date: November 17, 2011
    Inventors: Oliver Thiel, Charles Bernard, Robert Larsen, Michael John Martinelli, Masooma Tamim Raza
  • Publication number: 20110269985
    Abstract: Compounds having stable isotopes 13C and/or 2H were synthesized from precursor compositions having solid phase supports or affinity tags.
    Type: Application
    Filed: June 2, 2011
    Publication date: November 3, 2011
    Applicant: Los Alamos National Security, LLC
    Inventors: Jurgen G. Schmidt, David B. Kimball, Marc A. Alvarez, Robert F. Williams, Rudolfo A. Martinez
  • Publication number: 20110237678
    Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Application
    Filed: April 26, 2011
    Publication date: September 29, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Darren MANSFIELD, Pierre-Yves COQUERON, Heiko RIECK, Philippe DESBORDES, Alain VILLIER, Marie-Claire GROSJEAN-COURNOYER, Pierre GENIX
  • Publication number: 20110178108
    Abstract: A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.
    Type: Application
    Filed: September 28, 2009
    Publication date: July 21, 2011
    Applicant: Institute of Medicinal Biotechnology Academy of Medical Science
    Inventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhourong Li, Yanping Li, Jlan Xu
  • Patent number: 7968602
    Abstract: Analogs of 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-napthalenyl)-1-propenyl]benzoic acid and methods of manufacture and use thereof, such as for use in cancer prevention and treatment.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: June 28, 2011
    Assignees: Wisconsin Alumni Research Foundation, University of California-Los Angeles, Ohio State Research Foundation
    Inventors: Robert W. Curley, Jr., Margaret Clagett-Dame, Michael D. Collins, Victoria V. Abzianidze
  • Patent number: 7964645
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, R5, X, and n are as defined herein and the dotted line denotes an optional bond and pharmaceutically acceptable acid addition salts thereof. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: August 17, 2007
    Date of Patent: June 21, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Robert Narquizian, Emmanuel Pinard
  • Publication number: 20110137081
    Abstract: The invention relates to a continuous method for producing amides, according to which at least one carboxylic acid of formula (I) R3—COON ??(I) wherein R3 is hydrogen or an optionally substituted alkyl group comprising between 1 and 4 carbon atoms, is reacted with at least one amine of formula (II) HNR1R2 ??(II) wherein R1 and R2 are independently hydrogen or a hydrocarbon group comprising between 1 and 100 C atoms, to form an ammonium salt, and said ammonium salt is then reacted to form a carboxylic acid amide, under microwave irradiation in a reaction pipe, the longitudinal axis of the pipe being oriented in the direction of propagation of the microwaves of a monomode microwave applicator.
    Type: Application
    Filed: March 18, 2009
    Publication date: June 9, 2011
    Applicant: CLARIANT FINANCE (BVI) LIMITED
    Inventors: Matthias Krull, Roman Morschhaeuser, Michael Seebach, Hans Juergen Scholz
  • Patent number: 7923578
    Abstract: The subjects of the present invention are a method of manufacturing 3-(4-hydroxyphenyl)propanoic acid amide, its application in the manufacture of anti-aging compositions and an anti-aging composition. As phloretamide possesses a series of biological properties it might be use as a composition for skin having excellent anti-aging effect to prevent the sagging of skin and loss of luster.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: April 12, 2011
    Assignee: Instytut Chemii Bioorganicznej Pan
    Inventors: Jan Barciszewski, Leszek Rychlewski, Lech Celewicz, Krzysztof Ciszewski, Eliza Wyszko, Katarzyna Rolle
  • Publication number: 20110021528
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: October 1, 2010
    Publication date: January 27, 2011
    Applicant: PHARMACYCLICS, INC.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Publication number: 20100331575
    Abstract: This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1?,2?,3?(1S*,2R*),5?)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
    Type: Application
    Filed: August 11, 2010
    Publication date: December 30, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Masaru Mitsuda, Tadashi Moroshima, Kentaro Tsukuya, Kazuhiko Watabe, Masahiko Yamada
  • Patent number: 7858823
    Abstract: A process for the preparation of a compound of formula (I): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: December 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ursula Hoffmann, Michael Jansen, Reinhard Reents, Helmut Stahr
  • Publication number: 20100305316
    Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.
    Type: Application
    Filed: December 4, 2007
    Publication date: December 2, 2010
    Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
  • Patent number: 7745661
    Abstract: Disclosed are, for example, a process for producing a tricarboxylic acid tris(alkyl-substituted cyclohexylamide), the process comprising subjecting a tricarboxylic acid and an alkyl-substituted cyclohexylamine to an amidation reaction, either (a) in the presence of a boric acid compound and a phenol compound or (b) in the presence of a boric acid ester obtained by the dehydration condensation of a boric acid compound and a phenol compound, and optionally purifying the resulting crude reaction product.
    Type: Grant
    Filed: April 5, 2006
    Date of Patent: June 29, 2010
    Assignee: New Japan Chemical Co., Ltd.
    Inventors: Sachio Kitagawa, Masahide Ishikawa, Yoshihiro Ishibashi, Taiichiro Iwamura, Yoshihiro Kihara
  • Publication number: 20100130782
    Abstract: This invention describes an amidation process whereby amino acids of the Formulae IIA or IIB can be activated and treated with an amine in the presence of a base to yield amides of the Formula (I), without loss of optical purity.
    Type: Application
    Filed: March 31, 2008
    Publication date: May 27, 2010
    Applicant: MERCK FROSST CANADA LTD.
    Inventors: Paul O'Shea, Francis Gosselin
  • Publication number: 20100081843
    Abstract: The invention relates to a method for producing tertiary amides of alkylphenyl carboxylic acids by reacting at least one secondary amine with at least one alkylphenyl carboxylic acid to form an ammonium salt, said ammonium salt being subsequently converted into the tertiary amide by means of microwave radiation.
    Type: Application
    Filed: October 5, 2007
    Publication date: April 1, 2010
    Inventors: Mathias Krull, Roman Morschhaeuser, Alexander Lerch, Helmut Ritter, Sarah Schmitz