Patents Represented by Attorney George W. Johnston

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  • 3-trifluoromethyl-pyrazine-2-carboxylic acid amide derivatives as HDL-cholesterol raising agents
    Patent number: 8088920
    Abstract: The present invention relates to pyrazine derivatives of the formula and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: January 3, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Matthew Wright
  • Leukotriene B4 inhibitors
    Patent number: 8088936
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: January 3, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Romyr Dominique, Robert Alan Goodnow, Jr., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Benzimidazole derivatives
    Patent number: 8088930
    Abstract: The invention is concerned with novel benzimidazole derivatives of formula (I) wherein A, n and R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: January 3, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor
  • Spiropiperidine derivatives
    Patent number: 8084609
    Abstract: The present invention is concerned with novel spiro-piperidine 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. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: December 27, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Biomarker for farnesyl pathway
    Patent number: 8084262
    Abstract: The invention generally provides methods to determine the extent to which a compound interferes with steroid metabolism, comprising a novel biomarker of a felinine derivative. The invention also provides such novel felinine derivative biomarker.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: December 27, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frank Dieterle, Goetz Schlotterbeck, Hans Senn, Laura Suter-Dick
  • Pyrimidyl derivatives as protein kinase inhibitors
    Patent number: 8080552
    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: December 19, 2007
    Date of Patent: December 20, 2011
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Guy Georges, Matthias Koerner, Irene Kolm, Ulrike Reiff, Wolfgang Schaefer, Edgar Voss, Stefan Weigand
  • 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
  • 3,3?-spiroindolinone derivatives
    Patent number: 8076482
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, W, W?, V, V?, V?, R1, R2 and R3 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: December 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Xingchun Han, Song Yang, Zhuming Zhang
  • Prodrugs of thyroid hormone analogs
    Patent number: 8076334
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: December 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nancy-Ellen Haynes, Nathan Scott, Jefferson Wright Tilley
  • Indoles
    Patent number: 8076360
    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: December 13, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Process
    Patent number: 8071803
    Abstract: The present invention relates to a process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutically active compounds.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: December 6, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Bruno Lohri
  • Indazole derivatives
    Patent number: 8071628
    Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, 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 in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: December 6, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Heterocyclyl compounds
    Patent number: 8071586
    Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, 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 8, 2009
    Date of Patent: December 6, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
  • Imidazo [4,5-B] pyridine and pyrrolo [2,3-B] pyridine protein kinase inhibitors
    Patent number: 8067599
    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-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: September 4, 2007
    Date of Patent: November 29, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Konrad Honold, Wolfgang Schaefer, Stefan Scheiblich
  • 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
  • Imidazolidine derivatives
    Patent number: 8063088
    Abstract: The invention is concerned with novel imidazolidine derivatives of formula (I) wherein R1 to R3, A, D and E 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: June 4, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
  • Solid forms of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine
    Patent number: 8063076
    Abstract: The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: November 22, 2011
    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
  • Acetylenyl-pyrazolo-pyrimidine derivatives
    Patent number: 8063048
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Wylie Solang Palmer, Juergen Wichmann, Thomas Johannes Woltering
  • Substituted hydantoins
    Patent number: 8063085
    Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, John Anthony Moliterni, Omar Jose Morales
  • Pyrrolidine ether derivatives as NK3 receptor antagonists
    Patent number: 8063075
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R?, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention 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: June 2, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer