Patents Represented by Attorney George W. Johnston

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  • Cyclohexyl sulfonamide derivatives
    Patent number: 8017773
    Abstract: The present invention relates to compounds of formula I wherein R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: January 18, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Olivier Roche
  • N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions
    Patent number: 8017607
    Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Imidazopyridines
    Patent number: 8017604
    Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Rubén Alvarez Sánchez, Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Pharmaceutical compositions containing lipase inhibitors
    Patent number: 8012494
    Abstract: A pharmaceutical composition comprises at least one inhibitor of lipases, preferably an inhibitor of gastrointestinal and pancreatic lipases, such as orlistat, at least one surfactant, and at least one dispersant.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: September 6, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Passchier Christiaan de Smidt, Paul Hadvary, Hans Lengsfeld, Thomas Rades, Hans Steffen, Joseph Tardio
  • Pyridine and pyrimidine derivatives as MGLUR2 antagonists
    Patent number: 8012986
    Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and methods for treating CNS disorders with the same.
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: September 6, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Juergen Wichmann, Thomas Woltering
  • Pyrrolopyrazinyl urea kinase inhibitors
    Patent number: 8012974
    Abstract: The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I, wherein the variables R1, R2, R3, R4, and R5 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: September 6, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joe Timothy Bamberg, Johannes Cornelius Hermann, Remy Lemoine, Michael Soth
  • Pyrrolidine aryl-ether as NK-3 receptor antagonists
    Patent number: 8012998
    Abstract: The invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, R4, n, o, p, and q are as defined herein and to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The 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: August 4, 2008
    Date of Patent: September 6, 2011
    Assignee: Hoffmann—LA Roche Inc.
    Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
  • Methyl-benzimidazole derivatives
    Patent number: 8008503
    Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 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: August 25, 2010
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang
  • TAAR1 ligands
    Patent number: 8008305
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 8008298
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X 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: February 20, 2009
    Date of Patent: August 30, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
  • Indazole or 4,5,6,7-tetrahydro-indazole derivatives
    Patent number: 8008505
    Abstract: This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
  • N-(2-amino-phenyl)-acrylamides
    Patent number: 7999000
    Abstract: The present invention is directed to the compounds of formula wherein R1 to R4 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: August 16, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jason Christopher Wong, Xihan Wu
  • 2-aminoquinoline derivatives
    Patent number: 7994324
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives, in particular compounds of formula (I) wherein R1 and R2 are as described herein, pharmaceutical compositions containing such compounds, and methods for their manufacture. The compounds of the invention are 5-HT5A receptor antagonists 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: February 27, 2009
    Date of Patent: August 9, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Substituted thieno[3,2-C]pyridine-7-carboxylic acid derivatives
    Patent number: 7994321
    Abstract: There are provided compounds of the formula wherein R1, R2, R3, X, Y, Q, Ring A and Ring B are as described. The compounds exhibit activity as anticancer agents.
    Type: Grant
    Filed: July 20, 2007
    Date of Patent: August 9, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Yi Chen, Xin-Jie Chu, Kin-Chun Luk
  • 4,5-dihydro-oxazol-2-yl amine derivatives
    Patent number: 7989449
    Abstract: The present invention relates to a compounds of formula I wherein R1, R1?, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (?-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 2, 2011
    Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Guido Marconi, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl
  • 2-aminoquinolines
    Patent number: 7989628
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The compounds 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: February 27, 2009
    Date of Patent: August 2, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Anthranilic acid derivatives
    Patent number: 7989657
    Abstract: The invention is concerned with novel anthranilic acid derivatives of formula (I) wherein R1 to R14, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: August 2, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Uwe Grether, Nicole A Kratochwil, Robert Narquizian, Constantinos Panousis, Jens-Uwe Peters
  • Ortho aminoamides for the treatment of cancer
    Patent number: 7977372
    Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: July 12, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
  • Process for the preparation of acid halides
    Patent number: 7977509
    Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: July 12, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ursula Hoffmann
  • Pyrazol derivatives
    Patent number: 7977358
    Abstract: The invention is concerned with novel pyrazol derivatives of formula (I), wherein R1, R2, R3, R4, X and Y are as defined herein, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor and/or CCR-5 receptor and can be used as medicaments.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: July 12, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche