Patents Assigned to Hoffman-La Roche Inc.
  • Arlethynyl derivatives
    Patent number: 9315498
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: April 19, 2016
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Pyridine-2-amides useful as CB2 agonists
    Patent number: 9303012
    Abstract: The invention relates to CB2 agonists of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: April 5, 2016
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Stefanie Bendels, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans, Ernst Schaffter, Tanja Schulz-Gasch
  • Substituted isoxazole amide compounds as inhibitors of stearoyl-CoA desaturase 1 (SCD1)
    Patent number: 9296711
    Abstract: The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compound of formula (I) as well as pharmaceutical compositions containing such compounds. The compound of formula (I) are SCD1 inhibitors and may be useful in treating cancer.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: March 29, 2016
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Shawn David Erickson, Paul Gillespie, Eric Mertz
  • Combination therapy for proliferative disorders
    Patent number: 9295669
    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 interferon for treating a patient suffering from a proliferative disorder, in particular a solid tumor, for example, colorectal cancer, melanoma, and thyroid cancer. In particular, the present invention relates to such a therapy wherein the interferon is peginterferon alfa-2a and the disorder is melanoma containing the V600E b-Raf mutation.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: March 29, 2016
    Assignee: Hoffman La-Roche Inc.
    Inventors: Kapil Dhingra, Brian Higgins, Kenneth Kolinsky, Richard J. Lee, Brian Lestini, Kathryn Packman, Fei Su
  • Amino acid sequence presenting fusion polypeptide and its use
    Patent number: 9266962
    Abstract: Herein is reported a fusion polypeptide according to formula (I): NH2—S2—X1—S1—COOH, wherein X1 comprises either a random amino acid sequence or an amino acid sequence derived from a first polypeptide, S2 and S1 are non-overlapping amino acid sequences derived from a second polypeptide, and denotes a peptide bond, wherein the second polypeptide is a polypeptide with peptidyl-prolyl cis/trans-isomerase activity (PPIase activity) or is derived from the FKBP-fold domain family, wherein X1 is inserted in place of the insert-in-flap-domain of the second polypeptide.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: February 23, 2016
    Assignee: Hoffman-La Roche Inc.
    Inventors: Herbert Andres, David Casagolda Vallribera, Hartmut Duefel, Michael Gerg, Christian Scholz, Michael Schraeml
  • Ethynyl derivatives
    Patent number: 9227959
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH R1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: January 5, 2016
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Arylethynyl derivatives
    Patent number: 9221802
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is phenyl, 3-fluorophenyl, 4-fluorophenyl or 2,5-di-fluorophenyl; or to a pharmaceutically acceptable acid addition salt, in enantiomerically pure form with the absolute configuration as shown in formula I. It has now surprisingly been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) which show advantageous biochemical-, physicochemical- and pharmacodynamic-properties compared to compounds of prior art.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: December 29, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • SUBSTITUTED HETERO-AZEPINONES
    Publication number: 20150361059
    Abstract: There are provided compounds of the formula wherein: V, W, X, Y, Z, R1, R2, R3, R4, R5 and R6 are described herein. The compounds are useful for the treatment of proliferative diseases, including cancer.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 17, 2015
    Applicant: Hoffman-La Roche Inc.
    Inventors: Andrew F. Donnell, Xiaochun Han, Robert Francis Kester, Norman Kong, Kang Le, Yan Lou, Christophe Michoud, John Anthony Moliterni, Stacy Remiszewski, Kenneth Carey Rupert, Weiya Yun
  • ANTIPROLIFERATIVE BENZO [B] AZEPIN-2-ONES
    Publication number: 20150353499
    Abstract: Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3 and R4 are described in this application, and methods of using said compounds in the treatment of cancer.
    Type: Application
    Filed: July 11, 2013
    Publication date: December 10, 2015
    Applicant: Hoffman-La Roche Inc.
    Inventors: Xiaochun Han, Yan Lou, Christophe Michoud, Steven Gregory Mischke, Stacy Remiszewski, Kenneth Carey Rupert
  • Arylethynyl pyrimidines
    Patent number: 9199971
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is hydrogen or halogen; R2 is C1-3-alkyl or —(CH2)n—O—CH3; n is 2 or 3; m is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) with improved properties for the treatment of schizophrenia, cognitive diseases, fragile X syndrome or autism.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: December 1, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Combination therapy of anti-HER3 antibodies
    Patent number: 9180185
    Abstract: The present invention relates to the combination therapy of anti-HER3 antibodies with certain anti-HER antibodies.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: November 10, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Frieder Bauss, Birgit Bossenmaier, Thomas Friess, Christian Gerdes, Max Hasmann, Marlene Thomas, Martin Weisser
  • Bicyclic dihydroisoquinoline-1-one derivatives
    Patent number: 9133158
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: September 15, 2015
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Johannes Aebi, Kurt Amrein, Wenming Chen, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Zhanguo Wang, Mingwei Zhou
  • 1,3-oxazines as BACE1 and/or BACE2 inhibitors
    Patent number: 9115098
    Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines 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: May 2, 2014
    Date of Patent: August 25, 2015
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Hans Hilpert, Wolfgang Wostl
  • Antibodies against human angiopoietin 2
    Patent number: 9109027
    Abstract: The present invention relates to a method of treating a disease or disorder in a patient comprising administering, to a patient in need of such treatment, an antibody which binds specifically to human angiopoietin-2 (ANG-2). The present invention also relates to a method for preventing metastasis in a patient suffering from primary cancer comprising administering, to a patient in need of such preventative treatment, an antibody which binds specifically to human angiopoietin-2 (ANG-2).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: August 18, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Ulrich Brinkmann, Remko Albert Griep, Klaus Kaluza, Anita Kavlie, Christian Klein, Joerg Thomas Regula, Werner Scheuer
  • Antibodies against human angiopoietin 2
    Patent number: 9073986
    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: February 6, 2013
    Date of Patent: July 7, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Ulrich Brinkmann, Remko Albert Griep, Klaus Kaluza, Anita Kavlie, Christian Klein, Joerg Thomas Regula, Werner Scheuer
  • Antibodies against human CSF-1R and uses thereof
    Patent number: 8999327
    Abstract: The present invention relates to antibodies against human CSF-1R (anti-CSF-1R antibody), methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: April 7, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Nikolaos Dimoudis, Georg Fertig, Alexander Fidler, Klaus Kaluza, Marlene Pickl, Carola Ries, Stefan Seeber, Kerstin Krueger
  • Ethynyl compounds
    Patent number: 8957213
    Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or 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 can be used for the treatment of schizophrenia or cognitive disorders.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: February 17, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
    Patent number: 8927535
    Abstract: The present invention provides cyclopropyl-fused-1,3-thiazepines 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: June 29, 2012
    Date of Patent: January 6, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventor: Thomas Woltering
  • 2'-4'-DIFLUORO-2'-METHYL SUBSTITUTED NUCLEOSIDE DERIVATIVES AS INHIBITORS OF HCV RNA REPLICATION
    Publication number: 20150004135
    Abstract: The present disclosure relates to compounds of Formula (I): Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of using the compounds of Formula (I) and/or compositions comprising the compounds of Formula (I) for the treatment of HCV.
    Type: Application
    Filed: December 17, 2012
    Publication date: January 1, 2015
    Applicants: HOFFMAN-LA ROCHE INC., RIBOSCIENCE LLC
    Inventors: Jing Zhang, Zhuming Zhang
  • Antibodies against human CSF-1R and uses thereof
    Patent number: 8900581
    Abstract: The present invention relates to antibodies against human CSF-1R (anti-CSF-1R antibody), methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: December 2, 2014
    Assignee: Hoffman-La Roche Inc.
    Inventors: Nikolaos Dimoudis, Georg Fertig, Alexander Fidler, Klaus Kaluza, Marlene Pickl, Carola Ries, Stefan Seeber, Kerstin Krueger