Patents Represented by Attorney George W. Johnston

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  • Glucocorticoid receptor antagonists
    Patent number: 8143280
    Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: September 15, 2008
    Date of Patent: March 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
  • Indoles
    Patent number: 8143281
    Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole 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 formula (I) wherein X, Y and R1 to R10 are as described in the specification.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: March 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Heterocyclyl compounds
    Patent number: 8138175
    Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I): wherein A, X, 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 may be used as medicaments.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: March 20, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
  • Substituted benzene compounds as modulators of the glucocorticoid receptor
    Patent number: 8138189
    Abstract: The present invention relates to compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: March 20, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Daniel Hunziker, Chrisitan Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Aminotetrahydroindazoloacetic acids
    Patent number: 8138208
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: July 6, 2009
    Date of Patent: March 20, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Heteroaromatic monoamides as orexinin receptor antagonists
    Patent number: 8133909
    Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: March 13, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Spiroindolinone derivatives
    Patent number: 8134001
    Abstract: There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof wherein W, V, X, Y, A, R and R? are as described herein. The compounds are useful as anticancer agents.
    Type: Grant
    Filed: November 18, 2008
    Date of Patent: March 13, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Qingjie Ding, Nan Jiang, Song Yang, Jing Zhang, Zhuming Zhang
  • Antibodies against human angiopoietin 2
    Patent number: 8133979
    Abstract: The present invention relates to antibodies against human Angiopoietin 2 (anti-ANG-2 antibodies), methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: March 13, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulrich Brinkmann, Remko Albert Griep, Klaus Kaluza, Anita Kavlie, Christian Klein, Joerg Thomas Regula, Werner Scheuer
  • Imidazolone and imidazoloidinone derivatives as 11b-HSD1 inhibitors
    Patent number: 8129423
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: March 6, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean Ackermann, Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart, Tadakatsu Takahashi
  • Aminotetrahydroindazoloacetic acids
    Patent number: 8124641
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: July 6, 2009
    Date of Patent: February 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun
  • Naphthylacetic acids
    Patent number: 8124629
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: February 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Paul Gillespie, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jenny Tan, Kshitij Chhabilbhai Thakkar
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8124604
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, 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-IV and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: February 28, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Imidazolidinone derivatives as 11B-HSD1 inhibitors
    Patent number: 8124636
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: February 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 8119636
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R 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: February 21, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, David Bernard Smith
  • Azacyclic derivatives
    Patent number: 8097634
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compounds inhibit hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, and obesity.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: January 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
  • Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors
    Patent number: 8097637
    Abstract: The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: January 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Leukotriene Binhibitors
    Patent number: 8093253
    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: February 23, 2009
    Date of Patent: January 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Romyr Dominique, Robert Alan Goodnow, Jr., Agnieszka Kowalczyk, Jianping Lou, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Leukotriene Binhibitors
    Patent number: 8093385
    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: July 28, 2008
    Date of Patent: January 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Romyr Dominique, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri
  • Antibodies against human tweak and uses thereof
    Patent number: 8093006
    Abstract: An antibody binding to TWEAK comprising as heavy chain variable domain a CDR3H selected from the group consisting of SEQ ID NO: 8, 16 or 24.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: January 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Monika Baehner, Hendrik Knoetgen, Jens Niewoehner
  • Substituted pyrazolo [1,5-a] pyrimidines as metabotropic glutamate antagonists
    Patent number: 8093263
    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: January 6, 2009
    Date of Patent: January 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering