Patents Represented by Attorney George W. Johnston

Find this attorney in the Justia Lawyer Directory

  • Azaindole glucokinase activators
    Patent number: 8222416
    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 metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: July 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Li Chen, Wendy Lea Corbett, Lichun Feng, Nancy-Ellen Haynes, Robert Francis Kester, Sung-Sau So, Jefferson Wright Tilley
  • Spiroindolinone derivatives
    Patent number: 8217051
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: July 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jing Zhang, Zhuming Zhang
  • Spiroindolinone pyrrolidines
    Patent number: 8217044
    Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: July 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
  • 5-aryl pyridines as 11-beta inhibitors for the treatment of diabetes
    Patent number: 8211913
    Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: July 3, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
  • Three part assay for kinase or phosphatase activity
    Patent number: 8206941
    Abstract: The present invention relates to a method of determining kinase or phosphatase activity based on a three parts system. The method comprises contacting a binding partner which can bind phosphorylated peptides, a detection molecule and a substrate peptide. Determination of activities is achieved by measuring energy transfer between an energy donor and an energy acceptor that are present on the detection molecule and the substrate molecule.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: June 26, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thilo Enderle, Doris Roth
  • Antibodies against human CCN1 and uses thereof
    Patent number: 8207307
    Abstract: Disclosed herein are methods for the recombinant expression of mammalian cell membrane-bound human CCN1 or a CCN1 domain thereof in mammalian cells, comprising transforming a mammalian host cell with a vector encoding CCN1 or a CCN1 domain thereof C-terminally fused to a mammalian cell transmembrane domain (CCN1 fusion protein), expressing said CCN1 or CCN1 domain fusion protein in said host cell, and recovering said membrane bound CCN1 or said CCN1 domain thereof. Disclosed herein is the use of such membrane bound CCN1 and domain for the generation of corresponding antibodies. Antibodies against human CCN1 are useful for the treatment of diseases.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: June 26, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hendrik Knoetgen, Hans-Willi Krell, Sandra Miller, Jens Niewoehner, Dirk Ponsel, Engin Toksoez
  • Substituted benzothiazoles as orexin antagonists
    Patent number: 8207220
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: June 26, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Ortho-aminoanilides for the treatment of cancer
    Patent number: 8202866
    Abstract: The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. 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: August 19, 2009
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu
  • Spiro-piperidine derivatives
    Patent number: 8202993
    Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Piperidine sulphonamide derivatives
    Patent number: 8202888
    Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Pyrazinecarboxamide derivatives as HDL-cholesterol raising agents
    Patent number: 8188093
    Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.
    Type: Grant
    Filed: June 29, 2010
    Date of Patent: May 29, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
  • GPR119 receptor agonists
    Patent number: 8188098
    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 metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shawn David Erickson, Paul Gillespie, Kevin Richard Guertin, Prabha Saba Karnachi, Kyungjin Kim, Chun Ma, Warren William McComas, Sherrie Lynn Pietranico-Cole, Lida Qi, Jefferson Wright Tilley, Qiang Zhang
  • 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
    Patent number: 8188079
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: May 29, 2012
    Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.
    Inventors: Matteo Andreini, David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
  • Diabetogenic rat model
    Patent number: 8187572
    Abstract: The present invention provides a method of producing diabetic rats, and a method for identifying compounds that reverse diabetes in said rats.
    Type: Grant
    Filed: July 5, 2006
    Date of Patent: May 29, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Agnes Benardeau, Emmanuelle Hainaut, Philippe Verry
  • Naphthylacetic acids
    Patent number: 8188090
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q and R1-R3 are defined in the detailed description and claims. The invention is also concerned with the compounds of formula Z: and pharmaceutically acceptable salts and esters thereof, wherein R1-R3 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 and Z as well as pharmaceutical compositions containing such compounds. The compounds of formula I and Z 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: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Sung-Sau So, Baoxia Wang, HongYing Yun
  • 2-aminoquinolines
    Patent number: 8188284
    Abstract: The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These 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: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Heterocyclic-substituted phenyl methanones
    Patent number: 8188139
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
  • Inhibitors of JNK
    Patent number: 8183254
    Abstract: The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: May 22, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Humberto Bartolome Arzeno, James Patrick Dunn, David Michael Goldstein, Leyi Gong, Xiaochun Han, Joan Heather Hogg, Alam Jahangir, Wylie Solang Palmer, Deborah Carol Reuter, Tania Silva, Parcharee Tivitmahaisoon, Teresa Alejandra Trejo-Martin, Shao-Yong Wu
  • 2-aminoquinolines
    Patent number: 8183380
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Pyridine derivatives as mGluR2 antagonists
    Patent number: 8183262
    Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering