Patents Assigned to Hoffmann-La Roche Inc.
  • Benzodioxole piperazine compounds
    Patent number: 8722683
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: May 13, 2014
    Assignee: Hoffmann LA-Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Pyrrolopyrimidone and pyrrolopyridone inhibitors of tankyrase
    Patent number: 8722661
    Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: May 13, 2014
    Assignees: Hoffmann-La Roche Inc., Genentech, Inc.
    Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
  • SEC-hydroxycyclohexyl derivatives
    Patent number: 8722721
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: May 13, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Werner Neidhart
  • NEW IMIDAZOLYLKETONE DERIVATIVES
    Publication number: 20140128429
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: February 13, 2013
    Publication date: May 8, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
  • Positive allosteric modulators (PAM)
    Patent number: 8716316
    Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: May 6, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • N-hydroxy-benzamids for the treatment of cancer
    Patent number: 8716285
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: May 6, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
  • Combination therapy
    Patent number: 8709419
    Abstract: The present invention relates to a combination therapy of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: April 29, 2014
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Kapil Dhingra, Brian Higgins, Kenneth Kolinsky, Richard J. Lee, Brian Lestini, Kathryn Packman, Fei Su
  • Bispecific, tetravalent antigen binding proteins
    Patent number: 8703132
    Abstract: The present invention relates to bispecific, tetravalent antigen binding proteins, methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Sabine Imhof-Jung, Christian Klein, Joerg Thomas Regula, Wolfgang Schaefer, Juergen Michael Schanzer
  • Azaspirodecanone compounds
    Patent number: 8703807
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Werner Neidhart
  • Nitrogen containing heteroaryl compounds
    Patent number: 8703768
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 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 as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Bridged piperidine derivatives
    Patent number: 8703763
    Abstract: The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karlheinz Baumann, Luke Green, Anja Limberg, Thomas Luebbers, Andrew Thomas
  • Glycosylated antibodies
    Patent number: 8703919
    Abstract: The invention provides an antibody comprising human IgG1 or IgG3 heavy chain constant domains that are glycosylated with a sugar chain at Asn297, said antibody being characterized in that the amount of fucose within said sugar chain is at least 99%, and in addition the amount of NGNA is 1% or less and/or the amount of N-terminal alpha 1,3 galactose is 1% or less, and uses thereof.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silke Hansen, Klaus-Peter Kuenkele, Dietmar Reusch, Ralf Schumacher
  • Bispecific anti-VEGF/anti-ANG-2 antibodies
    Patent number: 8703130
    Abstract: The present invention relates to bispecific antibodies against human VEGF and against human ANG-2, methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Monika Baehner, Ulrich Brinkmann, Guy Georges, Remko Albert Griep, Sabine Imhof-Jung, Anita Kavlie, Hubert Kettenberger, Christian Klein, Joerg Thomas Regula, Wolfgang Schaefer, Juergen Michael Schanzer, Werner Scheuer, Stefan Seeber, Markus Thomas
  • Isoindolinone derivatives
    Patent number: 8697705
    Abstract: The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: April 15, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Robert Francis Kester, Lucja Orzechowski
  • METHODS TO IDENTIFY RESPONSIVE PATIENTS
    Publication number: 20140099302
    Abstract: The present invention provides methods and kits for improving the progression-free survival of a patient suffering from gastrointestinal cancer and for assessing the sensitivity or responsiveness of the patient to treatment comprising bevacizumab.
    Type: Application
    Filed: October 4, 2013
    Publication date: April 10, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Paul Delmar, Dorothee Foernzler, Stefan Scherer
  • Piperidine sulphonamide derivatives
    Patent number: 8691846
    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: April 2, 2013
    Date of Patent: April 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Piperidinyl naphthylacetic acids
    Patent number: 8691993
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X 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: December 6, 2012
    Date of Patent: April 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jefferson Wright Tilley
  • IN VIVO SELECTION OF THERAPEUTICALLY ACTIVE ANTIBODIES
    Publication number: 20140093458
    Abstract: The present invention relates to non-invasive methods of in vivo selecting an antibody against a desired target on the surface of a mammalian cell of a subject by applying near-infrared fluorescence imaging (NIRF) as well as uses of NIRF in such methods. In addition, kits for the use in these methods comprising a panel of potentially therapeutic effective fluorescence labeled antibodies and means for NIRF imaging are provided.
    Type: Application
    Filed: September 5, 2013
    Publication date: April 3, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Michael Dobosz, Werner Scheuer
  • PHARMACEUTICAL FORMULATION COMPRISING AN ANTIBODY AGAINST P-SELECTIN AND A SUGAR SELECTED FROM SUCROSE AND TREHALOSE
    Publication number: 20140093512
    Abstract: This invention relates to a pharmaceutical formulation of an antibody against P-Selectin, a process for the preparation of the formulation and uses of the formulation.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Ulla Grauschopf, Hanns-Christian Mahler, Oliver Boris Stauch
  • Ion Exchange Chromatography with Improved Selectivity for the Separation of Polypeptide Monomers, Aggregates and Fragments by Modulation of the Mobile Phase
    Publication number: 20140081000
    Abstract: Herein is reported a method for producing a polypeptide in monomeric form comprising the following step: recovering the polypeptide in monomeric form from an ion exchange chromatography material by applying a solution comprising a non-ionic polymer and an additive.
    Type: Application
    Filed: September 12, 2013
    Publication date: March 20, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Sebastian Neumann