Patents by Inventor Emmanuel Pinard

Emmanuel Pinard has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS
    Publication number: 20120232084
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 13, 2012
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Substituted benzothiazoles as orexin antagonists
    Patent number: 8207220
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: June 26, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Piperidine sulphonamide derivatives
    Patent number: 8202888
    Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Heterocyclic-substituted phenyl methanones
    Patent number: 8188139
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
  • Amido-tropane derivatives
    Patent number: 8153653
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: April 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Radiolabelled inhibitors of the glycine 1 transporter
    Patent number: 8153679
    Abstract: The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. wherein R1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; and R2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: April 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Edilio Maurizio Borroni, Thomas Hartung, Roger David Norcross, Emmanuel Pinard
  • Quinolizidine and indolizidine derivatives
    Patent number: 8143273
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: March 27, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Heteroaromatic monoamides as orexinin receptor antagonists
    Patent number: 8133909
    Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: March 13, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS
    Publication number: 20120035195
    Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: August 3, 2011
    Publication date: February 9, 2012
    Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS
    Publication number: 20120022042
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Application
    Filed: September 30, 2011
    Publication date: January 26, 2012
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • AMIDO-TROPANE DERIVATIVES
    Publication number: 20110312993
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: June 15, 2011
    Publication date: December 22, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • QUINOLIZIDINE AND INDOLIZIDINE DERIVATIVES
    Publication number: 20110313165
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Carbocyclic GlyT-1 receptor antagonists
    Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • SOLID FORMS OF [4-(3-FLUORO-5-TRIFLUOROMETHYL-PYRIDIN-2-YL)-PIPERAZIN-1-YL-[5-METHANESULFONYL-2-((S)-2,2,2-TRIFLUORO-1-METHYL-ETHOXY)-PHENYL]-METHANONE
    Publication number: 20110295007
    Abstract: The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    Type: Application
    Filed: July 22, 2011
    Publication date: December 1, 2011
    Inventors: Andre Bubendorf, Annette Deynet-Vucenovic, Ralph Diodone, Olaf Grassmann, Kai Lindenstruth, Emmanuel Pinard, Franziska E. Rohrer, Urs Schwitter
  • Heterofused piperidines as orexin antagonists
    Patent number: 8067598
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring system, connected to the carbon atoms of the piperidine group selected from the group consisting of or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders in which orexin pathways are involved, like sleep disorders.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: November 29, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • GlyT1 receptor antagonists
    Patent number: 8063098
    Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
  • Solid forms of [4-(3-fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone
    Patent number: 8039473
    Abstract: The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: October 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Bubendorf, Annette Deynet-Vucenovic, Ralph Diodone, Olaf Grassmann, Kai Lindenstruth, Emmanuel Pinard, Franziska E. Rohrer, Urs Schwitter
  • TETRAHYDRO-PYRAN DERIVATIVES
    Publication number: 20110190349
    Abstract: The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.
    Type: Application
    Filed: January 21, 2011
    Publication date: August 4, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Di-aromatic substituted amides as inhibitors for GlyT-1
    Patent number: 7964645
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, R5, X, and n are as defined herein and the dotted line denotes an optional bond and pharmaceutically acceptable acid addition salts thereof. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: August 17, 2007
    Date of Patent: June 21, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Robert Narquizian, Emmanuel Pinard
  • 2-AMINO-5,5-DIFLUORO-5,6-DIHYDRO-4H-[1,3]OXAZIN-4-YL)-PHENYL]-AMIDES
    Publication number: 20110144097
    Abstract: The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 16, 2011
    Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Eoin Power, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl