Triethylene Diamines Patents (Class 544/351)
  • Patent number: 10011562
    Abstract: The present invention relates to long-chain dimethylaniline derivative compounds, their preparation methods, self-assembled texture, and uses thereof. Said compounds show ultralong acting anaesthetic effect, and belong to N-diethylaminoacetyl-2,6-dimethylaniline compounds, having a structure according to formula (I). Said compounds may self-assemble into micelle or gel in an aqueous solvent, and exert an in vivo elongated local anesthetic actions. Local anesthesia and/or analgesic activity can last more than 72 hours. The biomaterials can self-assemble into micelles or gels in water and have local anesthetic effect, as well as can further be used as the coating of medicinal bioactive molecules for treatment of pain, itching and the like and/or the drug carriers, together with as pharmaceutical adjuvants for delivery system. Thus, said materials have a favorable perspective.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: July 3, 2018
    Assignee: WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
    Inventors: Lei Tang, Jin Liu, Wensheng Zhang, Jun Yang, Bowen Ke, Qinqin Yin
  • Patent number: 8952156
    Abstract: A process is disclosed for separating the output from the reaction of EDDN or EDMN with hydrogen in the presence of THF, a catalyst, TETA or DETA, water, and optionally organic compounds having higher and lower boiling points than TETA or DETA. Hydrogen is removed, and the output is supplied to a distillation column DK1 in which an azeotrope, optionally comprising organic compounds with a boiling point lower than TETA or DETA, is removed from the top. A product comprising TETA or DETA is removed from the bottom and passed into a distillation column DK2, removing THF. A stream comprising TETA or DETA passes from the bottom of DK2. The DK1 azeotrope is condensed. Phase separation is induced by the addition of an organic solvent essentially immiscible with water, and the mixture is separated. The organic phase is recycled into DK1 and the water phase is discharged.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: February 10, 2015
    Assignee: BASF SE
    Inventors: Hermann Luyken, Sebastian Ahrens, Gordon Brasche, Jens Baldamus, Robert Baumann, Randolf Hugo, Stephanie Jaegli, Johann-Peter Melder, Jörg Pastre, Boris Buschhaus
  • Publication number: 20140350253
    Abstract: The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.
    Type: Application
    Filed: December 26, 2012
    Publication date: November 27, 2014
    Applicant: The Regents Of The University Of California
    Inventors: Vivek Rauniyar, Aaron D. Lackner, Gregory L. Hamilton, F. Dean Toste, Robert J. Phipps, Hunter Shunatona, Natalja Frueh, Yiming Wang, Jeffrey Wu, Jigar Patel, Takashi Honjo
  • Publication number: 20140323412
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 30, 2014
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140294718
    Abstract: Disclosed is an sorbent for removing sulfur dioxide (SO2) contained in combustion flue gases or in the atmosphere by using a diamine-based ionic liquid or a diamine compound supported by a polymer resin. To be specific, the present invention relates to a method of using a tertiary diamine compound immobilized on a polymer surface as a SO2 sorbent and also relates to a novel sorbent for absorbing or adsorbing a sulfur dioxide hydrate (SO2.H2O) formed by a bond between SO2 and water.
    Type: Application
    Filed: November 22, 2013
    Publication date: October 2, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyun Joo LEE, Seung Rok LIM, Kean Im LEE, Chang Soo KIM, Hoon Sik KIM, Ji Sik CHOI, Sang Deuk LEE
  • Publication number: 20140243281
    Abstract: Provided herein are pediatric dosage forms for use in the treatment of a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of the pediatric dosage form comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are said pediatric dosage form for use in the treatment of a pediatric liver disease, for use in decreasing the levels of serum bile acids or hepatic bile acids, for use in the treatment of pruritis, for use in reducing liver enzymes or bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 28, 2014
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20130309168
    Abstract: The invention provides a family of agents that target bacterial infection, which can be used as imaging agents or therapeutic agents. The agents can be used to image sites of bacterial infection as well as other physiological processes in a subject.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 21, 2013
    Applicant: VisEn Medical, Inc.
    Inventor: VisEn Medical, Inc.
  • Publication number: 20130303505
    Abstract: TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
    Type: Application
    Filed: August 11, 2010
    Publication date: November 14, 2013
    Inventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt
  • Publication number: 20130273800
    Abstract: The present disclosure provides novel oligo phenylene ethynylene (OPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various OPEs show antibacterial, antiviral and anti-fungal activity.
    Type: Application
    Filed: July 13, 2011
    Publication date: October 17, 2013
    Applicant: Office of Technology Licensing
    Inventors: David G. Whitten, Kirk S. Schanze, Eunkyung Ji, Thomas S. Corbitt, Zhijun Zhou, Dimitri Dascier, Ying Wang, Linnea K. Ista, Anand Parthsaray
  • Publication number: 20130261039
    Abstract: A method of removing a residue from a surface, including applying to the surface a composition including (a) a quaternary ammonium hydroxide having a general formula (I): as defined herein, and (b) a dipolar aprotic solvent substantially free of water; and removing at least a substantial portion of the residue from the surface.
    Type: Application
    Filed: March 27, 2012
    Publication date: October 3, 2013
    Applicant: SACHEM, INC.
    Inventor: Charles B. Little
  • Publication number: 20130210828
    Abstract: The present disclosure provides novel poly(phenylene ethynylene) (PPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various PPEs show antibacterial, antiviral and antifungal activity.
    Type: Application
    Filed: July 13, 2011
    Publication date: August 15, 2013
    Inventors: David G. Whitten, Kirk S. Sehanze, Anand Parthsaray, Eunkyung Ji, Motokatsu Ogawa, Thomas S. Corbitt, Dimitri Dascier, Ying Wang, Linnea K. Ista
  • Publication number: 20130019949
    Abstract: Provided are compounds with a donor moiety, a first acceptor moiety and a second acceptor moiety, as shown by Formula (I): With the unique molecular design, compounds of Formula (I) can provide a desirable power conversion efficiency. Moreover, this invention also provides organic thin-film solar cells comprising the above-mentioned compounds.
    Type: Application
    Filed: January 3, 2012
    Publication date: January 24, 2013
    Inventors: KEN-TSUNG WONG, HAO-WU LIN, LI-YEN LIN, FRANCIS LIN, YI-HONG CHEN, SHI-WEN CHIU
  • Publication number: 20130023661
    Abstract: The present invention relates to the use of compounds of the formula (I) as fluorinating reagents, to a process for the fluorination of organic compounds by reaction thereof with compounds of the formula (I), and to compounds of the formula (I).
    Type: Application
    Filed: March 7, 2011
    Publication date: January 24, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Nikolai (Mykola) Ignatyev, Aleksandra Atatrah, Peter Barthen, Walter Frank
  • Patent number: 8178470
    Abstract: Herein are disclosed adducts of amines and polycarboxylic acids, and methods of making such adducts. Such adducts can be used to remove cyanogen chloride. Also disclosed are methods of providing such adducts on supports to form filter media. Also disclosed are methods of combining such filter media with catalysts and/or with porous polymeric webs to form filter systems.
    Type: Grant
    Filed: February 1, 2011
    Date of Patent: May 15, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: Duane D. Fansler, Allen R. Siedle, Zhongshu Tan, Thomas E. Wood
  • Patent number: 8158629
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: April 17, 2012
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
  • Publication number: 20120028979
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Application
    Filed: October 6, 2011
    Publication date: February 2, 2012
    Inventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU
  • Publication number: 20120000790
    Abstract: A method and ionic liquid for the electrorecovery of metal from a metal salt including at least one metal ion. The method includes the steps of dissolving the metal salt in an ionic liquid, the ionic liquid including an ionic liquid cation and an ionic liquid anion; whereby the metal ion of the metal salt forms a metal complex in solution with at least the ionic liquid cation; and subjecting the metal complex to an electrical potential between a cathode and anode to recover metal at the cathode. The ionic liquid includes an ionic liquid cation and an ionic liquid anion, wherein the ionic liquid cation has an affinity for the metal ion which is at least about equal to that of the ionic liquid anion for the metal ion.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 5, 2012
    Applicant: COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION
    Inventors: Theo Rodopoulos, Michael David Horne, Thomas Ruether
  • Patent number: 8067419
    Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: November 29, 2011
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christoph Binkert, Christoph Boss, Olivier Corminboeuf, Corinna Grisostomi, Solange Meyer
  • Patent number: 7973030
    Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: July 5, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
  • Patent number: 7964600
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: June 21, 2011
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
  • Publication number: 20110070179
    Abstract: Compositions are disclosed comprising novel fluorinated cationic alcohols in a cosmetically acceptable vehicle. The fluorinated compounds alter a surface property of the hair to provide hair conditioning, for example. In embodiments, the compounds have improved water solubility and deposition properties.
    Type: Application
    Filed: September 16, 2010
    Publication date: March 24, 2011
    Applicant: Living Proof, Inc.
    Inventors: David T. Puerta, Lorna Nagamoottoo-Casse, Kevin T. Love
  • Publication number: 20100317624
    Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Application
    Filed: June 7, 2010
    Publication date: December 16, 2010
    Inventors: Allison Laura CHOY, Ann EAKIN, Olga QUIROGA, Brian SHERER
  • Patent number: 7790722
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: September 7, 2010
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
  • Publication number: 20100204438
    Abstract: The present invention relates to a process for preparing triethylenediamine (TEDA) derivatives, comprising the following steps: a) reacting a dihydropyrazine with an olefin, b) if appropriate hydrogenating after step a). The present invention further also relates to novel TEDA derivatives as such and to their use as incorporable polyurethane catalysts.
    Type: Application
    Filed: August 29, 2008
    Publication date: August 12, 2010
    Applicant: BASF SE
    Inventors: Gunther Van Cauwenberge, Johann-Peter Melder, Joachim-Thierry Anders, Christoph Benisch, Rainer Klopsch, Gregor Daun, Christian Dully, Boris Buschhaus, Henning Böckemeier, Evelyn Pox
  • Publication number: 20100179156
    Abstract: The present invention is directed to providing antimicrobial surfaces containing 1,4-diazoniabicyclo[2.2.2]octane and hydrocarbon groups and/or chains. More specifically, the present invention is directed to antimicrobial compositions wherein the hydroxyl groups on polyols are replaced by 1,4-diazoniabicyclo[2.2.2]octane. The invention is also directed to methods of making antimicrobial compositions containing polyols.
    Type: Application
    Filed: August 28, 2007
    Publication date: July 15, 2010
    Inventors: Robert Engel, JaimeLee Iolani Rizzo, Karin Melkonian Fincher
  • Patent number: 7608710
    Abstract: A surfactant comprising a polyether segment including at least one pendant alkoxyfluoroalkyl group, and a cationic substituent defined by one of the formulae: or the substituted derivatives thereof.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: October 27, 2009
    Assignee: OMNOVA Solutions Inc.
    Inventors: Charles M. Kausch, Yongsin Kim, Richard R. Thomas, David L. Hardman, Jr.
  • Publication number: 20090088437
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Application
    Filed: May 29, 2008
    Publication date: April 2, 2009
    Inventors: Wenge XIE, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
  • Patent number: 7176313
    Abstract: An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof, which shows excellent antibacterial activity against Mycobacterium tuberculosis and atypical acid-fast bacteria and exhibits good pharmacokinetics and safety
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: February 13, 2007
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Kenji Namba, Mayumi Tanaka, Rie Miyauchi
  • Patent number: 7053236
    Abstract: The present invention relates to methods for the synthesis of chiral non-racemic products, e.g., enantiomerically-enriched hemiesters, from prochiral and meso starting materials, e.g., prochiral and meso cyclic anhydrides. The present invention also relates to catalysts for the aforementioned methods, and methods for synthesizing these catalysts.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: May 30, 2006
    Assignee: Brandeis University
    Inventors: Li Deng, Yonggang Chen, Shikai Tian
  • Publication number: 20040186291
    Abstract: The present invention relates to a process for preparing TEDA solutions comprising a solvent selected from the group consisting of polyhydric alcohols and ethers of polyhydric alcohols. The process comprises passing gaseous TEDA into the solvent and subsequently treating the solutions with one or more suitable adsorbents. This gives solutions which have only low color numbers and are color-stable on storage. The solutions can be used as such in preferred applications of TEDA, preferably polyurethane production.
    Type: Application
    Filed: January 29, 2004
    Publication date: September 23, 2004
    Inventors: Jurgen Ciprian, Matthias Frauenkron, Stephan Maurer, Johann-Peter Melder
  • Publication number: 20040127491
    Abstract: This invention relates to novel diazabicyclic biaryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: November 10, 2003
    Publication date: July 1, 2004
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Oestergaard Nielsen, Tino Dyhring Joergensen, Philip K. Ahring
  • Publication number: 20040029884
    Abstract: Compound corresponding to the general formula (I) 1
    Type: Application
    Filed: November 18, 2002
    Publication date: February 12, 2004
    Inventors: Thierry Gallet, Frederic Galli, Odile Leclerc, Alistair Lochead
  • Publication number: 20030236406
    Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
    Type: Application
    Filed: December 23, 2002
    Publication date: December 25, 2003
    Inventors: Kevin A. Babiak, Andrew Carpenter, Shine Chou, Pierre-Jean Colson, Payman Farid, Robert Hett, Christian H. Huber, Kevin J. Koeller, Jon P. Lawson, James Li, Eduardo K. Mar, Lawrence M. Miller, Vladislav Orlovski, James C. Peterson, Mark J. Pozzo, Claire A. Przybyla, Samuel J. Tremont, Jay S. Trivedi, Grace M. Wagner, Gerald A. Weisenburger, Benxin Zhi
  • Publication number: 20030207859
    Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.
    Type: Application
    Filed: January 9, 2003
    Publication date: November 6, 2003
    Inventors: James M. Balkovec, Mark L. Greenlee, Steven H. Olson, Gregory P. Rouen
  • Publication number: 20030199515
    Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of single crystals of ASBT inhibitors having high purity and low levels of solvent impurities.
    Type: Application
    Filed: August 23, 2002
    Publication date: October 23, 2003
    Applicant: G.D. SEARLE, LLC
    Inventors: Partha S. Mudipalli, Mark J. Pozzo, Jung Min Park
  • Publication number: 20030195218
    Abstract: Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.
    Type: Application
    Filed: January 15, 2003
    Publication date: October 16, 2003
    Applicant: Pharmacia Corporation
    Inventors: Kevin J. Koeller, Samuel J. Tremont
  • Publication number: 20030153760
    Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Application
    Filed: December 20, 2002
    Publication date: August 14, 2003
    Applicant: Merck & Co., Inc.
    Inventors: Paul Devine, Hansen Karl
  • Patent number: 6586434
    Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: July 1, 2003
    Assignee: G.D. Searle, LLC
    Inventors: Kevin A. Babiak, Andrew Carpenter, Shine Chou, Pierre-Jean Colson, Payman Farid, Robert Hett, Christian H. Huber, Kevin J. Koeller, Jon P. Lawson, James Li, Eduardo K. Mar, Lawrence M. Miller, Vladislav Orlovski, James C. Peterson, Mark J. Pozzo, Claire A. Przybyla, Samuel J. Tremont, Jay S. Trivedi, Grace M. Wagner, Gerald A. Weisenburger, Benxin Zhi
  • Publication number: 20030119840
    Abstract: Compounds of the general formula (I) 1
    Type: Application
    Filed: September 24, 2002
    Publication date: June 26, 2003
    Inventors: Frederic Galli, Samir Jegham, Odile Leclerc, Alistair Lochead, Alain Nedelec
  • Patent number: 6504066
    Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: January 7, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Paul Devine, Hansen Karl
  • Publication number: 20030004349
    Abstract: In a process for the purification of triethylenediamine (TEDA) in which TEDA is vaporized and the gaseous TEDA is passed into a liquid solvent and is subsequently crystallized from this, the mother liquor obtained after the TEDA has been crystallized is extracted with an extractant which is immiscible or only slightly miscible with the solvent of the mother liquor and in which TEDA is readily soluble, and the TEDA-depleted mother liquor obtained after extraction and/or the TEDA-enriched extractant which has been used for the extraction are/is returned to the process.
    Type: Application
    Filed: May 6, 2002
    Publication date: January 2, 2003
    Inventors: Ortmund Lang, Bernd Rumpf, Matthias Frauenkron, Dirk Funhoff, Thomas Manderbach, Bernd Stein
  • Publication number: 20020072467
    Abstract: A molded catalyst for production of triethylenediamine, wherein (1) the main components are silica and crystalline aluminosilicate, (2) the silica is amorphous, and the content of the silica is from 5 to 70 wt %, (3) the molar ratio of silica to alumina in the crystalline aluminosilicate is at least 12, and the content of the crystalline aluminosilicate is from 30 to 95 wt %, and (4) the hardness is at least 1 kg.
    Type: Application
    Filed: September 25, 2001
    Publication date: June 13, 2002
    Applicant: TOSOH CORPORATION
    Inventor: Tsukasa Ogawa
  • Publication number: 20020032329
    Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
    Type: Application
    Filed: March 8, 2001
    Publication date: March 14, 2002
    Inventors: Kevin A. Babiak, Andrew Carpenter, Shine Chou, Pierre-Jean Colson, Payman Farid, Robert Hett, Christian H. Huber, Kevin J. Koeller, Jon P. Lawson, James Li, Eduardo K. Mar, Lawrence M. Miller, Vladislav Orlovski, James C. Peterson, Mark J. Pozzo, Claire A. Przybyla, Samuel J. Tremont, Jay S. Trivedi, Grace M. Wagner, Gerald A. Weisenburger, Benxin Zhi
  • Patent number: 6153608
    Abstract: The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R.sup.1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R.sup.2 represents hydrogen, hydroxy, or halogen; R.sup.3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.
    Type: Grant
    Filed: July 29, 1998
    Date of Patent: November 28, 2000
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Hiroyoshi Hidaka, Akira Matsuura, Takushi Matsuzaki
  • Patent number: 6057321
    Abstract: The invention concerns compounds of general formula (I) ##STR1## in which R.sub.1 represents a methyl group, X.sub.1 represents a hydrogen atom, or OR.sub.1 and X.sub.1 together form a group of formula --O(CH.sub.2).sub.2 --,--O(CH.sub.2).sub.3 --, --O(CH.sub.2).sub.2 O-- or --O(CH.sub.2).sub.3 O--, X.sub.2 represents a hydrogen atom or an amino group, and X.sub.3 representing a halogen atom. The compounds are ligands of serotoninergic receptors of the 5-HT.sub.3 and/or 5-HT.sub.4 types, and act as 5-HT.sub.4 agonists and/or 5-HT.sub.3 antogonists.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: May 2, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Alistair Lochead, Samir Jegham, Alain Nedelec, Axelle Solignac
  • Patent number: 6046190
    Abstract: The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: April 4, 2000
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
  • Patent number: 5892035
    Abstract: A process for preparing a N,N'-difluorodiazoniabicycloalkane salt of the formula: ##STR1## by reacting a corresponding diazabicycloalkane or diazabicycloalkane Br.o slashed.nsted acid salt and fluorine in the presence of a Br.o slashed.nsted acid or in the presene or absence of a base, by reacting a corresponding N,N'-difluorodiazoniabicycloalkane salt and an acid or salt, by reacting a corresponding diazabicycloalkane and fluorine in the presence of a Br.o slashed.nsted acid and then reacting an intermediate product and an acid or salt, or by reacting a corresponding diazabicycloalkane Br.o slashed.nsted acid salt and fluorine in the presence or absence of a base and then reacting an intermediate product and an acid or salt.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: April 6, 1999
    Assignee: Daikin Industries Ltd.
    Inventors: Teruo Umemoto, Masayuki Nagayoshi, Ginjiro Tomizawa, Kenji Adachi
  • Patent number: 5756741
    Abstract: A process for preparing triethylenediamine by passing an amine compound over a catalyst at elevated temperature to afford a reaction product containing triethylenediamine and piperazine, the amine compound having, in the molecule, a moiety represented by the following general formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently a hydrogen atom or an alkyl group having 1 to 4 carbon atoms and X is oxygen or nitrogen characterized by adding an ethylating compound containing at least one nitrogen and/or oxygen atom to the reaction product and contacting the reaction product, under conditions sufficient to produce triethylenediamine from the ethylating compound and piperazine, with a condensation/cyclization shape-selective zeolite catalyst demonstrating a triethylenediamine/piperazine weight ratio uptake value of at least 6:1.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: May 26, 1998
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Nelson Armor, Jose Guadalupe Santiesteban, Hong-Xin Li
  • Patent number: 5741906
    Abstract: A process for preparing triethylenediamine by passing an ethanolamine, ethyleneamine, piperazine or morpholine over a pentasil-type zeolite at elevated temperature characterized by employing a ZSM-5 zeolite in the hydrogen or ammonium form which has been pretreated with an aqueous solution of a chelating agent capable of forming a chelate-aluminum complex.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: April 21, 1998
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Jose Guadalupe Santiesteban, Hong-Xin Li, John Nelson Armor
  • Patent number: 5716993
    Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.
    Type: Grant
    Filed: September 14, 1995
    Date of Patent: February 10, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda