Single Bond Between 3,4-positions Patents (Class 546/150)
  • Patent number: 11084777
    Abstract: The present invention relates to a method for preparing alkylamines using carbon monoxide and the use of this method in the manufacturing of vitamins, pharmaceutical products, adhesives, acrylic fibres and synthetic leathers, pesticides, surfactants, detergents and fertilisers. It also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, surfactants, detergents and fertilisers, comprising a step of preparing alkylamines by the method according to the invention. The present invention further relates to a method for preparing marked alkylamines and uses thereof.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: August 10, 2021
    Assignee: Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Solène Savourey, Thibault Cantat, Tawfiq Nasr-Allah
  • Patent number: 9637485
    Abstract: The invention provides novel compounds having the general formula: wherein R1 to R6, W and X are as described herein and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: October 29, 2015
    Date of Patent: May 2, 2017
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Xingchun Han, Min Jiang, Jianhua Wang, Chengang Zhou, Yongguang Wang, Song Yang
  • Publication number: 20150133427
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: October 15, 2014
    Publication date: May 14, 2015
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20150105559
    Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.
    Type: Application
    Filed: March 4, 2013
    Publication date: April 16, 2015
    Applicant: Kyushu University, National University Corporation
    Inventors: Takashi Ohshima, Hiroyuki Morimoto, Yuhei Shimizu
  • Publication number: 20150031893
    Abstract: This disclosure relates to methods of using 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of Alzheimer's disease, other tauopathies and related neurodegenerative diseases.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 29, 2015
    Inventors: Pascal BARNEOUD, Veronique BLANCHARD-BREGEON, Veronique MARY, Jean MENAGER, Philippe DELAY-GOYET, Mathilde LOPEZ GRANCHA, Thomas ROONEY, Nathalie SCHUSSLER
  • Publication number: 20140228343
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Patent number: 8779145
    Abstract: Industrially applicable process for preparing 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, and salts thereof.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: July 15, 2014
    Assignee: Sanofi
    Inventor: Steven Elenbaas
  • Patent number: 8748615
    Abstract: Industrially applicable process for preparing 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, and salts thereof.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: June 10, 2014
    Assignee: Sanofi
    Inventors: Steven Elenbaas, Robert Allan Farr, John Michael Kane
  • Patent number: 8741924
    Abstract: Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: June 3, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Betty A. Diamond
  • Publication number: 20140005177
    Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
    Type: Application
    Filed: March 8, 2012
    Publication date: January 2, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
  • Publication number: 20130310555
    Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
    Type: Application
    Filed: May 17, 2013
    Publication date: November 21, 2013
    Applicant: Illinois Institute of Technology
    Inventor: Hyun-Soon Chong
  • Publication number: 20130245270
    Abstract: The present invention describes tripodal catechol derivatives with a flexible basic framework for the functionalisation of surfaces, and methods for their production and use. The central atom of the flexible framework is hereby a tertiary aliphatic carbon atom. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, e.g. with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Application
    Filed: September 7, 2011
    Publication date: September 19, 2013
    Applicant: JUSTUS-LIEBIG-UNIVERSITAT GIESSEN
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • Patent number: 8507523
    Abstract: Disclosed are therapeutic tetrahydroisoquinoline compositions for the treatment of cancer, these compositions having selectivity for cancer cells while demonstrating few, if any, deleterious side effects on normal cells.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: August 13, 2013
    Inventors: Renukadevi Patil, Charles Ryan Yates, Duane D. Miller, Eldon E. Geisert
  • Publication number: 20130137718
    Abstract: Industrially applicable process for preparing 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, and salts thereof.
    Type: Application
    Filed: August 31, 2012
    Publication date: May 30, 2013
    Applicant: SANOFI
    Inventor: Steven ELENBAAS
  • Patent number: 8415474
    Abstract: The present invention provides an efficient process for the preparation of hexahydroisoquinolines from dihydroisoquinolines. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: April 9, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Frank W. Moser, Peter X. Wang, Gary L. Cantrell, David W. Berberich
  • Publication number: 20120323003
    Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.
    Type: Application
    Filed: August 24, 2012
    Publication date: December 20, 2012
    Applicant: SANOFI
    Inventors: Juan Antonio DIAZ MARTIN, Maria Dolores JIMENEZ BARGUENO
  • Patent number: 8278324
    Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: October 2, 2012
    Assignee: Glaxo Group Limited
    Inventors: Jag Paul Heer, Thomas Daniel Heightman
  • Patent number: 8173648
    Abstract: The invention provides a type of novel 1,2,3,4-tetrahydroisoquinoline derivatives with a structure of formula (I): wherein R1 represents propargyl or cyclopropylmethyl; wherein R2 represents N-ethyl-N-methylamino, 1-Pyrrolidyl, 1-Piperidinyl, or 1-Morpholinyl. The invention provides further a process for preparing said derivatives and a pharmaceutical composition containing the same. Said derivatives can be used to modulate the proteolytic process of amyloid precursor proteins (APP), and provides further novel compounds useful for treating Alzheimer's disease (AD).
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: May 8, 2012
    Assignee: National Defense Medical Center
    Inventors: Ming-Kuan Hu, Yung-Feng Liao
  • Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • Publication number: 20120034270
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 9, 2012
    Applicant: Akaal Pharma Pty Ltd
    Inventors: Damian W. Grobelny, Gurmit S. Gill
  • Patent number: 8097636
    Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: November 12, 2008
    Date of Patent: January 17, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Stamos, Esther Martinborough, Nicole Zimmermann, Timothy Neubert, Mehdi Michel Djamel Numa, Tara Whitney, Tara Leanne Hampton
  • Publication number: 20120003330
    Abstract: The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: May 31, 2011
    Publication date: January 5, 2012
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Chengzhi Zhang, Manoucherhr Shahbaz
  • Publication number: 20110280804
    Abstract: Compounds having the general formula III?, or IV? wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S—R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and heterocycli
    Type: Application
    Filed: June 1, 2011
    Publication date: November 17, 2011
    Applicants: The Board of Trustees of the Leland Stanford Junior University, University of Mississippi
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Frederick T. Chin, Michelle L. James, Bin Shen, Sanjiv Gambhir
  • Patent number: 8008500
    Abstract: A method of preparing a tetrabenazine compound (TBZ compound) having structure I comprising the steps of reacting a nucleophilic alkenyl species with aldehyde compound II and oxidizing the resultant allylic alcohol to provide enone III. The protecting group P1 on the tetrahydroisoquinoline nitrogen is removed and the resultant deprotected intermediate is induced to undergo an amino cyclization reaction to provide a product TBZ compound having structure I. The method may be used to prepare either enantiomeric form of tetrabenazine; (+)-tetrabenazine or (?)-tetrabenazine. Alternatively the method may be adapted to provide a mixture enriched in one tetrabenazine enantiomer, a racemic mixture, or a diastereomeric mixture of tetrabenazine compounds. In addition, the present invention provides novel synthetic intermediate compositions which may be used to prepare either or both enantiomers of tetrabenazine, derivatives of tetrabenazine, and analogs of tetrabenazine.
    Type: Grant
    Filed: June 8, 2007
    Date of Patent: August 30, 2011
    Assignee: General Electric Company
    Inventors: Michael James Rishel, Kande Kankananamalage Dayarathna Amarasinghe, Sean Richard Dinn, Bruce Fletcher Johnson
  • Patent number: 7994109
    Abstract: This invention relates to organic catalysts comprising iminium or oxaziridinium moieties, cleaning compositions comprising such catalysts; and processes for making and using such catalysts and cleaning products.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: August 9, 2011
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, George Douglas Hiler, II, Susumu Murata, Rebecca Massie Grey
  • Publication number: 20110185796
    Abstract: The present invention provides compounds which are useful, e.g., as reference markers for analyzing the purity of cisatracurium and salts thereof, a test method for determining the said purity and processes for preparing reference markers.
    Type: Application
    Filed: April 28, 2009
    Publication date: August 4, 2011
    Applicant: CHEMAGIS Ltd.
    Inventors: Oded Arad, Vladimir Naddaka, Eyal Klopfer, Shady Saeed, Lior Shahar, Vitaly Shteinman
  • Publication number: 20110166349
    Abstract: Methods are provided for the catalytic hydroamination of compounds having an alkyne or allene functional group, in which the compound is contacted with ammonia or an amine in the presence of a catalytic amount of a gold complex under conditions sufficient for hydroamination to occur.
    Type: Application
    Filed: May 8, 2009
    Publication date: July 7, 2011
    Applicant: The Regents of the University of California
    Inventors: Guy Bertrand, Vincent Lavallo, Guido D. Frey, Bruno Donnadieu, Michele Soleil-Havoup
  • Patent number: 7972822
    Abstract: An enzymatic process for preparing aliphatic polycarbonates via terpolymerization or transesterification using a dialkyl carbonate, an aliphatic diester, and an aliphatic diol or triol reactant. A catalyst having an enzyme capable of catalyzing an ester hydrolysis reaction in an aqueous environment is subsequently added to the reaction mixture. Next, polymerization of the reaction proceeds for an allotted time at a temperature?100° C. Finally, the copolymer is isolated from an the catalyst via filtration.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: July 5, 2011
    Assignee: Polytechnic Institute of New York University
    Inventors: Richard A. Gross, Zhaozong Jiang
  • Publication number: 20110077400
    Abstract: Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form.
    Type: Application
    Filed: June 4, 2009
    Publication date: March 31, 2011
    Inventors: Paul Lobben, Rulin Zhao, Bei Wang, Bang-Chi Chen, Shuang Liu, Min Hu, Yuh-Lin Allen Yang, Matthew Isherwood, Rasidul Amin, Wenge Cui
  • Publication number: 20110071300
    Abstract: The present invention provides an efficient process for the preparation of hexahydroisoquinolines from dihydroisoquinolines. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.
    Type: Application
    Filed: September 24, 2010
    Publication date: March 24, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Christopher W. Grote, Frank W. Moser, Peter X. Wang, Gary L. Cantrell, David W. Berberich
  • Publication number: 20110046378
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease
    Type: Application
    Filed: February 17, 2009
    Publication date: February 24, 2011
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
  • Publication number: 20100311760
    Abstract: Compounds having the formula I wherein wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: June 9, 2010
    Publication date: December 9, 2010
    Inventors: Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
  • Patent number: 7846930
    Abstract: Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
    Type: Grant
    Filed: May 13, 2008
    Date of Patent: December 7, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventor: John M. Keith
  • Publication number: 20100217003
    Abstract: Provided are 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivatives and synthesis methods thereof. The compounds significantly inhibit the production of nitrogen monoxide (NO) and superoxide in an activated microglial cell and expressions of TNF-?, IL-1? inducive NO synthase and cyclooxygenase-2 genes. They also prevent NF-kB shift to a nucleus, decrease reactive oxygen species (ROS), inhibit expression of GTP cyclohydrolase I gene and over-production of tetrahydrobiopterin (BH4), and protect dopaminergic neurons from injury due to activated microglial cells. Consequently, the compounds are effective in treating inflammatory and neurodegenerative diseases.
    Type: Application
    Filed: December 10, 2007
    Publication date: August 26, 2010
    Inventors: On-You Hwang, Dae-Yoon Chi, Hyo-Jin Son, Jai-Woong Seo
  • Publication number: 20100168093
    Abstract: The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.
    Type: Application
    Filed: April 30, 2007
    Publication date: July 1, 2010
    Inventors: Miguel Angel Pericas-Brondo, Antoni Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobés, Carmen Garcia Granda
  • Patent number: 7741316
    Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: June 22, 2010
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Patent number: 7691879
    Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: April 6, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Nathan R. Kett, Christopher J. Dinsmore, Gerald S. Ponticello, David A. Claremon
  • Publication number: 20100040545
    Abstract: The present invention relates to methods of synthesising radiolabelled compounds, to the precursors useful in such methods and to the radiolabelled compounds obtainable by such methods. More particularly, the present invention relate to methods, precursors and radiolabelled compounds useful in Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) especially for imaging neuroreceptors with radiolabelled agonists.
    Type: Application
    Filed: December 19, 2007
    Publication date: February 18, 2010
    Inventors: Erik Arstad, David Turton
  • Publication number: 20100016309
    Abstract: The invention provides a type of novel 1,2,3,4-tetrahydroisoquinoline derivatives with a structure of formula (I): wherein R1 represents propargyl or cyclopropylmethyl; wherein R2 represents N-ethyl-N-methylamino, 1-Pyrrolidyl, 1-Piperidinyl, or 1-Morpholinyl. The invention provides further a process for preparing said derivatives and a pharmaceutical composition containing the same. Said derivatives can be used to modulate the proteolytic process of amyloid precursor proteins (APP), and provides further novel compounds useful for treating Alzheimer's disease (AD).
    Type: Application
    Filed: July 16, 2008
    Publication date: January 21, 2010
    Applicant: NATIONAL DEFENSE MEDICAL CENTER
    Inventors: Ming-Kuan Hu, Yung-Feng Liao
  • Patent number: 7629358
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: March 16, 2005
    Date of Patent: December 8, 2009
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Paul Alan Glossop, David Anthony Price, Russell Andrew Lewthwaite, Mark Edward Bunnage, Kim James, Graham Lunn
  • Patent number: 7557076
    Abstract: This invention relates to cleaning compositions comprising organic catalysts having enhanced enzyme compatibility and processes for making and using such cleaning compositions.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: July 7, 2009
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, George Douglas Hiler, II, Rebecca Massie Grey, Mark Robert Sivik, Ludwig Voelkel, Frank Dietsche, Christian Bittner
  • Publication number: 20090163719
    Abstract: There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or diastereomer in the product composition being greater than the ratio of second to first enantiomer or diastereomer in the enantiomerically enriched composition.
    Type: Application
    Filed: October 27, 2005
    Publication date: June 25, 2009
    Inventors: Andrew John Blacker, Matthew John Stirling
  • Publication number: 20090163542
    Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.
    Type: Application
    Filed: August 18, 2005
    Publication date: June 25, 2009
    Inventors: Antoni Torrens Jover, Josep Mas Prio, Susana Yenes Minguez, Monica Garcia Lopez, Alberto Dordal Zueras, Luz Romero Alonso, Helmut Henrich Buschmann
  • Publication number: 20090143272
    Abstract: This invention relates to organic catalysts comprising iminium or oxaziridinium moieties, cleaning compositions comprising such catalysts; and processes for making and using such catalysts and cleaning products.
    Type: Application
    Filed: February 5, 2009
    Publication date: June 4, 2009
    Inventors: Gregory Scot Miracle, George Douglas Hiler, II, Susumu Murata, Rebecca Massie Grey
  • Publication number: 20090126125
    Abstract: The present disclosure relates to the dyeing of keratin materials using thiol/disulfide styryl tetrahydroquinolinium fluorescent dyes. Disclosed herein is a dye composition comprising a thiol/disulfide styryl tetrahydroquinolinium fluorescent dye and a dyeing process with, for instance, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are thiol fluorescent dyes and the uses thereof in lightening keratin materials. This composition can be used to obtain a lightening effect which can be resistant and visible on dark keratin fibers.
    Type: Application
    Filed: September 19, 2008
    Publication date: May 21, 2009
    Inventors: Andrew GREAVES, Nicolas DAUBRESSE, Franco MANFRE
  • Publication number: 20090124655
    Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: November 12, 2008
    Publication date: May 14, 2009
    Inventors: Dean Stamos, Esther Martinborough, Nicole Zimmermann, Timothy Neubert, Mehdi Michel Djamel Numa, Tara Whitney, Tara Leanne Hampton
  • Patent number: 7504371
    Abstract: This invention relates to cleaning compositions comprising organic catalysts having enhanced enzyme compatibility and processes for making and using such cleaning compositions.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: March 17, 2009
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, George Douglas Hiler, II, Rebecca Massie Grey, Mark Robert Sivik, Ludwig Voelkel, Frank Dietsche, Christian Bittner
  • Patent number: 7468347
    Abstract: A polyol polymeric structure comprising a bleach activating moiety to give benefits in detergent compositions such as bleaching action, soil suspension, increased surfactant availability in the presence of free hardness.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: December 23, 2008
    Assignee: The Procter & Gamble Company
    Inventors: Jeffrey John Scheibel, Julie Ann Menkhaus, George Douglas Hiler, II, Marc Eric Gustwiller
  • Patent number: 7468348
    Abstract: A polyol polymeric structure comprising a bleach activating moiety to give benefits in detergent compositions such as bleaching action, soil suspension, increased surfactant availability in the presence of free hardness.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: December 23, 2008
    Assignee: The Procter & Gamble Company
    Inventors: Jeffrey John Scheibel, Julie Ann Menkhaus, George Douglas Hiler, II, Marc Eric Gustwiller
  • Publication number: 20080306269
    Abstract: A method of preparing a tetrabenazine compound (TBZ compound) having structure I comprising the steps of reacting a nucleophilic alkenyl species with aldehyde compound II and oxidizing the resultant allylic alcohol to provide enone III. The protecting group P1 on the tetrahydroisoquinoline nitrogen is removed and the resultant deprotected intermediate is induced to undergo an amino cyclization reaction to provide a product TBZ compound having structure I. The method may be used to prepare either enantiomeric form of tetrabenazine; (+)-tetrabenazine or (?)-tetrabenazine. Alternatively the method may be adapted to provide a mixture enriched in one tetrabenazine enantiomer, a racemic mixture, or a diastereomeric mixture of tetrabenazine compounds. In addition, the present invention provides novel synthetic intermediate compositions which may be used to prepare either or both enantiomers of tetrabenazine, derivatives of tetrabenazine, and analogs of tetrabenazine.
    Type: Application
    Filed: June 8, 2007
    Publication date: December 11, 2008
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Michael James Rishel, Kande Kankananamalage Dayarathna Amarasinghe, Sean Richard Dinn, Bruce Fletcher Johnson