Patents Represented by Attorney George W. Johnston

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  • Heterocyclic compounds
    Patent number: 8063042
    Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as herein defined, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
  • 7H-pyrido[3,4-D]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors
    Patent number: 8058283
    Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: November 15, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Honold, Jane Paul, Carl Roeschlaub, Wolfgang Schaefer, Stefan Scheiblich, Thomas Von Hirschheydt, Alan Whittle
  • Oxindole derivatives
    Patent number: 8058269
    Abstract: There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.
    Type: Grant
    Filed: September 17, 2007
    Date of Patent: November 15, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Li Chen, Song Yang, Jing Zhang, Zhuming Zhang
  • Azaspiro derivatives
    Patent number: 8044202
    Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: October 25, 2011
    Assignee: Hoffmann-la Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • 5-substituted benzoxazines
    Patent number: 8044047
    Abstract: The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) wherein X, R1 and R2 are as described herein, as well as their manufacture, pharmaceutical compositions containing them. Compounds of the present invention are 5-HT5A receptor antagonists, and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: October 25, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Thiazolyl-benzimidazoles
    Patent number: 8044213
    Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: October 25, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jianping Cai, Shaoqing Chen, Yi Chen, Xin-Jie Chu, Robert Alan Goodnow, Jr., Kang Le, Kin-Chun Luk, Steven Gregory Mischke, Peter Michael Wovkulich
  • Azaspiro derivatives
    Patent number: 8039624
    Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: October 18, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Piperidine-amide derivatives
    Patent number: 8039487
    Abstract: The invention is concerned with novel piperidine-amide derivatives of formula (I) wherein R1, R2, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and may be used to treat diseases associated with L-CPT1.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: October 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Biaryl sulfonamide derivatives
    Patent number: 8039493
    Abstract: The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: October 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
  • Lipase inhibiting composition
    Patent number: 8039508
    Abstract: Pharmaceutical compositions that contain a lipase inhibitor having a melting point ?37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: October 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karsten Maeder, Rainer Eugen Martin, Susanne Raab, Lukas Christoph Scheibler, Thomas Schindler, Marco Schroeder
  • 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
  • Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors
    Patent number: 8039490
    Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: October 18, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Azaspiro derivatives
    Patent number: 8034937
    Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: October 11, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Bicyclic sulfonamide derivatives which are L-CPT 1 inhibitors
    Patent number: 8030308
    Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Grant
    Filed: November 8, 2010
    Date of Patent: October 4, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
  • Substituted piperidines as somatostatin receptor subtype 5 (SSTR5) antagonists
    Patent number: 8026255
    Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: September 27, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
  • 4,4-disubstituted piperidine derivatives
    Patent number: 8026365
    Abstract: This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: September 27, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andreas Christ, Rainer Martin, Peter Mohr
  • Indoles
    Patent number: 8026259
    Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12,, R13,, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: September 27, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Characterization and identification of unique human adiponectin isoforms and antibodies
    Patent number: 8026345
    Abstract: The invention pertains to methods for measuring different forms of human adiponectin that are present in human plasma/serum, and more specifically methods are based on an ELISA assay that utilizes different monoclonal antibodies directed against adiponectin, in combination with different polyclonal antibodies directed against different domains of human adiponectin. The invention also provides unique isoforms of adiponectin and antibodies thereto, including polyclonal and monoclonal antibodies.
    Type: Grant
    Filed: January 2, 2008
    Date of Patent: September 27, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Charles Roger Burghardt, Jarema Peter Kochan, Erik Roy Rasmussen
  • N-benzyl pyrrolidine derivatives
    Patent number: 8022099
    Abstract: The present invention relates to a compound of formula I wherein Ar, R1, R2, R3, n, and o are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: October 23, 2009
    Date of Patent: September 20, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer
  • Spiro-piperidine derivatives
    Patent number: 8022213
    Abstract: Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them. The active compounds of the present invention are useful in the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general formula (I) wherein R1 to R11 and X are as defined in the description.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: September 20, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider