Patents by Inventor Ralph Diodone

Ralph Diodone 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).

  • Publication number: 20140046066
    Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
    Type: Application
    Filed: September 13, 2013
    Publication date: February 13, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Ulrike Bromberger, Ralph Diodone, Stefan Hildbrand, Roland Meier
  • Publication number: 20140039002
    Abstract: The present invention provides solid forms of the compound of formula 1 and pharmaceutical uses thereof.
    Type: Application
    Filed: February 21, 2012
    Publication date: February 6, 2014
    Applicants: F. Hoffmann-La Roche AG, Plexxikon Inc.
    Inventors: Ralph Diodone, Karsten Fähnrich, Urs Schwitter, Shan-Ming Kuang, Baoshu Zhao, Prabha N. Ibrahim, Gary Conard Visor
  • Publication number: 20120309969
    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: June 13, 2012
    Publication date: December 6, 2012
    Inventors: André Bubendorf, Annette Deynet-Vucenovic, Ralph Diodone, Olaf Grassmann, Kai Lindenstruth, Emmanuel Pinard, Franziska E. Rohrer, Urs Schwitter
  • Publication number: 20120232273
    Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11b S)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido [2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
    Type: Application
    Filed: May 25, 2012
    Publication date: September 13, 2012
    Inventors: Ulrike Bromberger, Ralph Diodone, Stefan Hildbrand, Roland Meier
  • Publication number: 20110313196
    Abstract: The present invention relates to a process for the preparation of benzamide derivatives which are useful as intermediates in the preparation of pharmaceutically active compounds.
    Type: Application
    Filed: June 6, 2011
    Publication date: December 22, 2011
    Inventors: Stephan Bachmann, Fritz Bliss, Ralph Diodone, Stefan Hildbrand, Michael Kammerer, Christophe Pfleger, Reinhard Reents, Michelangelo Scalone
  • 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
  • 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
  • Publication number: 20110112136
    Abstract: The present invention is related to an improved method for the manufacture of Micro-precipitated Bulk Powder (MBP) containing the active pharmaceutical ingredient Propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide and Hydroxypropylmethylcellulose Acetate Succinate (HPMCAS). The invention is further directed to pharmaceutical compositions containing said MBP, as well as its use in the manufacture of medicaments for the treatment of cancer.
    Type: Application
    Filed: November 8, 2010
    Publication date: May 12, 2011
    Inventors: Ralph Diodone, Stephan Lauper, Hans-Juergen Mair, Johannes Pudewell, Frank Wierschem
  • Publication number: 20100311971
    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, 2010
    Publication date: December 9, 2010
    Inventors: Andre Bubendorf, Annette Deynet-Vucenovic, Ralph Diodone, Olaf Grassmann, Kai Lindenstruth, Emmanuel Pinard, Franziska E. Rohrer, Urs Schwitter
  • Publication number: 20100310659
    Abstract: Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.
    Type: Application
    Filed: March 31, 2010
    Publication date: December 9, 2010
    Inventors: Dipen Desai, Ralph Diodone, Zenaida Go, Prabha N. Ibrahim, Raman Iyer, Hans-Juergen Mair, Harpreet K. Sandhu, Navnit H. Shah, Gary Visor, Nicole Wyttenbach, Stephan Lauper, Johannes Pudewell, Frank Wierschem
  • Publication number: 20090105480
    Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
    Type: Application
    Filed: August 19, 2008
    Publication date: April 23, 2009
    Inventors: Ulrike Bromberger, Ralph Diodone, Stefan Hildbrand, Roland Meier
  • Publication number: 20080214561
    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: December 19, 2007
    Publication date: September 4, 2008
    Inventors: Andre Bubendorf, Annette Deynet-Vucenovic, Ralph Diodone, Olaf Grassmann, Kai Lindenstruth, Emmanuel Pinard, Franziska E. Rohrer, Urs Schwitter