Benzene Ring Containing Patents (Class 564/139)
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Patent number: 11471868Abstract: 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: GrantFiled: October 9, 2020Date of Patent: October 18, 2022Assignee: Emory UniversityInventors: Lanny Steven Liebeskind, Pavan Kumar Reddy Gangireddy
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Patent number: 10889540Abstract: 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: GrantFiled: January 15, 2018Date of Patent: January 12, 2021Assignee: BEIJING J-TEC TECHNOLOGY CO., LTDInventors: Chenghan Tang, Yunjian Zhao, Anxing Wei, Wei Guo
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Patent number: 9604911Abstract: Process for the industrial synthesis of the compound of formula (I):Type: GrantFiled: December 4, 2014Date of Patent: March 28, 2017Assignee: LES LABORATOIRES SERVIERInventors: Jean-François Briere, Raphaël Lebeuf, Vincent Levacher, Christophe Hardouin, Jean-Pierre Lecouve
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Patent number: 9394241Abstract: 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: GrantFiled: October 28, 2013Date of Patent: July 19, 2016Assignee: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Jung-Mo Ahn
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Publication number: 20150148543Abstract: The invention features methods and compositions for the synthesis of multimerizing agents.Type: ApplicationFiled: January 28, 2015Publication date: May 28, 2015Inventors: Feng Li, Yihan Wang
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Patent number: 9024028Abstract: 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: GrantFiled: January 26, 2012Date of Patent: May 5, 2015Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Feng Li, Yihan Wang
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Publication number: 20150065681Abstract: 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: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Inventors: Jin Kyu KIM, So Young KWON, Sang Kyun IM, Ki Yon LEE, Suk Min JUN, Gook Geon BAE
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Patent number: 8969620Abstract: 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: GrantFiled: September 29, 2011Date of Patent: March 3, 2015Assignee: UCB Pharma GmbHInventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
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Publication number: 20150025274Abstract: This invention relates to processes for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide (I) and intermediates thereof. Formula (I).Type: ApplicationFiled: August 29, 2012Publication date: January 22, 2015Applicant: 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
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Patent number: 8907132Abstract: Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy-propionamide of formula-1 and intermediates thereof are provided.Type: GrantFiled: February 9, 2011Date of Patent: December 9, 2014Assignee: MSN Laboratories Private LimitedInventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Aluru Srinivas, Revu Satyanarayana
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Publication number: 20140171649Abstract: 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: ApplicationFiled: January 26, 2012Publication date: June 19, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: Feng Li, Yihan Wang
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Patent number: 8710098Abstract: 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: GrantFiled: September 28, 2009Date of Patent: April 29, 2014Assignee: Institute of Medicinal Biotechnology Chinese Academy of Medical ScienceInventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhuorong Li, Yanping Li, Jian Xu
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Patent number: 8637707Abstract: 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: GrantFiled: July 3, 2009Date of Patent: January 28, 2014Assignees: BASF SE, Technische Universitaet MuenchenInventors: Michael Keil, Michael Rack, Thomas Zierke, Markus Heinrich, Alexander Wetzel
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Publication number: 20130267729Abstract: 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: ApplicationFiled: September 23, 2011Publication date: October 10, 2013Applicant: E.I. du Pont de Nemours and CompanyInventor: Joerg Bruening
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Patent number: 8546612Abstract: 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: GrantFiled: November 12, 2012Date of Patent: October 1, 2013Assignee: Obschestvo S Ogranichennoi Otvetstvennostiyu PharmenterprisesInventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
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Publication number: 20130245269Abstract: 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: ApplicationFiled: September 7, 2011Publication date: September 19, 2013Applicant: JUSTUS-LIEBIG-UNIVERSITA GIESSENInventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
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Publication number: 20130210918Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.Type: ApplicationFiled: April 15, 2013Publication date: August 15, 2013Applicant: The Scripps Research InstituteInventors: Joel M. Gottesfeld, Kai Jenssen, David M. Herman, Ryan Burnett, C. James Chou
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Patent number: 8501993Abstract: 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: GrantFiled: May 11, 2009Date of Patent: August 6, 2013Assignee: Syngenta LimitedInventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, David Drouard
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Publication number: 20130190533Abstract: 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: ApplicationFiled: September 29, 2011Publication date: July 25, 2013Applicant: UCB PHARMA GMBHInventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
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Patent number: 8487134Abstract: 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: GrantFiled: October 9, 2008Date of Patent: July 16, 2013Assignee: Archimica, Inc.Inventors: Andreas Meudt, Richard Wisdom, Jason Helmke, Quofang Qiu, Paul Meek
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Patent number: 8461384Abstract: 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: GrantFiled: June 10, 2009Date of Patent: June 11, 2013Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Frank W. Moser, Christopher W. Grote, Gary L. Cantrell
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Patent number: 8445708Abstract: 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: GrantFiled: October 27, 2006Date of Patent: May 21, 2013Assignee: Reuter Chemischer Apparatebau KGInventors: Milan Soukup, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
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Patent number: 8431514Abstract: 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: GrantFiled: April 14, 2010Date of Patent: April 30, 2013Assignee: Syngenta Crop Protection LLCInventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Maienfisch
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Publication number: 20130041180Abstract: Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy-propionamide of formula-1 and intermediates thereof are provided.Type: ApplicationFiled: February 9, 2011Publication date: February 14, 2013Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Aluru Srinivas, Revu Satyanarayana
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Patent number: 8334411Abstract: 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: GrantFiled: March 11, 2009Date of Patent: December 18, 2012Assignee: Toray Industries, Inc.Inventors: Masateru Ito, Izumi Nakagawa, Koya Kato, Takashi Mimitsuka, Kenji Sawai, Shin-ichi Minegishi, Hideki Sawai, Katsushige Yamada
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Patent number: 8299241Abstract: 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: GrantFiled: December 4, 2007Date of Patent: October 30, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
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Publication number: 20120234204Abstract: 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: ApplicationFiled: March 17, 2011Publication date: September 20, 2012Applicants: Bayer MaterialScience AG, Bayer MaterialScience LLCInventors: Serkan Unal, Robert N. Hunt, Heiko Hocke
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Publication number: 20120209011Abstract: 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: ApplicationFiled: December 21, 2009Publication date: August 16, 2012Inventors: Chandrashekar Aswathanarayanappa, Pullela Venkata Srinivas, Divya Kangath, Thilak Gregory Soundararajan, Anegondi Sreenivasa Prasad, Suriyan Masinaickenpatty Raghavendran
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Publication number: 20120178783Abstract: 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: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Inventors: John S. Kovach, Francis Johnson
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Patent number: 8183413Abstract: 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: GrantFiled: January 16, 2007Date of Patent: May 22, 2012Assignee: Kaneka CorporationInventors: Narumi Kishimoto, Hiroaki Yasukouchi, Toshihiro Takeda
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Patent number: 8143442Abstract: 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: GrantFiled: March 31, 2009Date of Patent: March 27, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Gerard John Harnett, Ursula Hoffmann, Michael Jansen, Reinhard Reents, Tim Sattelkau, Dennis A. Smith, Helmut Stahr
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Patent number: 8143449Abstract: Process for the industrial synthesis of the compound of formula (I)Type: GrantFiled: August 3, 2009Date of Patent: March 27, 2012Assignee: Les Laboratoires ServierInventors: Christophe Hardouin, Jean-Pierre Lecouve
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Publication number: 20110309001Abstract: The invention relates to a class of novel surfactants that have utility in the recovery and/or extraction of oil.Type: ApplicationFiled: December 2, 2010Publication date: December 22, 2011Inventors: David Soane, Rosa Casado Portilla, John H. Dise, Robert P. Mahoney
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Publication number: 20110313196Abstract: 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: ApplicationFiled: June 6, 2011Publication date: December 22, 2011Inventors: Stephan Bachmann, Fritz Bliss, Ralph Diodone, Stefan Hildbrand, Michael Kammerer, Christophe Pfleger, Reinhard Reents, Michelangelo Scalone
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Patent number: 8067635Abstract: 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: GrantFiled: October 5, 2007Date of Patent: November 29, 2011Assignee: Clariant Finance (BVI) LimitedInventors: Matthias Krull, Roman Morschhaeuser, Alexander Lerch, Helmut Ritter, Sarah Schmitz
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Publication number: 20110281954Abstract: 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: ApplicationFiled: May 17, 2011Publication date: November 17, 2011Inventors: Oliver Thiel, Charles Bernard, Robert Larsen, Michael John Martinelli, Masooma Tamim Raza
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Publication number: 20110269985Abstract: Compounds having stable isotopes 13C and/or 2H were synthesized from precursor compositions having solid phase supports or affinity tags.Type: ApplicationFiled: June 2, 2011Publication date: November 3, 2011Applicant: Los Alamos National Security, LLCInventors: Jurgen G. Schmidt, David B. Kimball, Marc A. Alvarez, Robert F. Williams, Rudolfo A. Martinez
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Publication number: 20110237678Abstract: 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: ApplicationFiled: April 26, 2011Publication date: September 29, 2011Applicant: BAYER CROPSCIENCE AGInventors: Darren MANSFIELD, Pierre-Yves COQUERON, Heiko RIECK, Philippe DESBORDES, Alain VILLIER, Marie-Claire GROSJEAN-COURNOYER, Pierre GENIX
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Publication number: 20110178108Abstract: 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: ApplicationFiled: September 28, 2009Publication date: July 21, 2011Applicant: Institute of Medicinal Biotechnology Academy of Medical ScienceInventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhourong Li, Yanping Li, Jlan Xu
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Patent number: 7968602Abstract: 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: GrantFiled: July 31, 2009Date of Patent: June 28, 2011Assignees: Wisconsin Alumni Research Foundation, University of California-Los Angeles, Ohio State Research FoundationInventors: Robert W. Curley, Jr., Margaret Clagett-Dame, Michael D. Collins, Victoria V. Abzianidze
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Patent number: 7964645Abstract: 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: GrantFiled: August 17, 2007Date of Patent: June 21, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Emmanuel Pinard
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Publication number: 20110137081Abstract: 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: ApplicationFiled: March 18, 2009Publication date: June 9, 2011Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Matthias Krull, Roman Morschhaeuser, Michael Seebach, Hans Juergen Scholz
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Patent number: 7923578Abstract: 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: GrantFiled: October 18, 2006Date of Patent: April 12, 2011Assignee: Instytut Chemii Bioorganicznej PanInventors: Jan Barciszewski, Leszek Rychlewski, Lech Celewicz, Krzysztof Ciszewski, Eliza Wyszko, Katarzyna Rolle
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Publication number: 20110021528Abstract: 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: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20100331575Abstract: 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: ApplicationFiled: August 11, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Masaru Mitsuda, Tadashi Moroshima, Kentaro Tsukuya, Kazuhiko Watabe, Masahiko Yamada
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Patent number: 7858823Abstract: 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: GrantFiled: March 31, 2009Date of Patent: December 28, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Ursula Hoffmann, Michael Jansen, Reinhard Reents, Helmut Stahr
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Publication number: 20100305316Abstract: 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: ApplicationFiled: December 4, 2007Publication date: December 2, 2010Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
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Patent number: 7745661Abstract: 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: GrantFiled: April 5, 2006Date of Patent: June 29, 2010Assignee: New Japan Chemical Co., Ltd.Inventors: Sachio Kitagawa, Masahide Ishikawa, Yoshihiro Ishibashi, Taiichiro Iwamura, Yoshihiro Kihara
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Publication number: 20100130782Abstract: 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: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: MERCK FROSST CANADA LTD.Inventors: Paul O'Shea, Francis Gosselin
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Publication number: 20100081843Abstract: 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: ApplicationFiled: October 5, 2007Publication date: April 1, 2010Inventors: Mathias Krull, Roman Morschhaeuser, Alexander Lerch, Helmut Ritter, Sarah Schmitz