Patents Represented by Attorney George W. Johnston
  • Patent number: 8349824
    Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: January 8, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Jens-Uwe Peters
  • Patent number: 8349844
    Abstract: The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: January 8, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 8350028
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for 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: March 5, 2009
    Date of Patent: January 8, 2013
    Assignee: Hofmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 8349893
    Abstract: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: January 8, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Patent number: 8344137
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: January 1, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
  • Patent number: 8343543
    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: August 19, 2011
    Date of Patent: January 1, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karsten Maeder, Rainer Eugen Martin, Susanne Raab, Lukas Christoph Scheibler, Thomas Schindler, Marco Schroeder
  • Patent number: 8344161
    Abstract: The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I or salts thereof, wherein X and Y are each independently hydrogen or a halogen atom, with the proviso that at least one of X or Y is a halogen atom. The compounds of formula I are useful as starting materials or intermediates for the preparation of pharmaceutically active compounds, especially for compounds, which are useful for the treatment of central nervous system disorders.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: January 1, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fabienne Hoffmann-Emery, Kurt Puentener, Hasane Ratni
  • Patent number: 8334287
    Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: December 18, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Eric Vieira, Juergen Wichmann
  • Patent number: 8329912
    Abstract: The present invention relates to mono-sulfate and hemi-sulfate salts of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine, to crystalline and amorphous forms thereof and to their use in pharmaceutical formulations.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas Cleary, Alexander Glomme, Olaf Grassmann, Shan-Ming Kuang, Roland Meier, Doreen Miller, Regina Moog, Franziska E. Rohrer, Jason Yang
  • Patent number: 8329724
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • Patent number: 8329699
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R1 and R2 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee
  • Patent number: 8329904
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, m, A, R1 and R2 have the significance given in the description. The compounds are useful as HSL inhibitors and may be used in the treatment or prophylaxis of diabetes, dyslipidemia, atherosclerosis or obesity.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
  • Patent number: 8329939
    Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Stefan Hildbrand, James Jappy, Dinesh Maganbhai Patel, Christophe Pfleger, Robert John Ernest Tidswell, Rene Trussardi
  • Patent number: 8324250
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: December 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 8324211
    Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: December 4, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth
  • Patent number: 8324248
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u 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: January 25, 2010
    Date of Patent: December 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 8318759
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: November 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
  • Patent number: 8318764
    Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Alam Jahangir, Stephen M Lynch, Michael Soth, Hanbiao Yang
  • Patent number: 8318719
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
  • Patent number: 8318749
    Abstract: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and 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: November 9, 2009
    Date of Patent: November 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian