Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A and n are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
April 17, 2013
Date of Patent:
November 17, 2015
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
Abstract: Herein is reported an antibody that specifically binds to human EPO receptor, wherein the antibody binds to EPO receptor fragment LPGPGGSVDIV (SEQ ID NO: 01) but that does not specifically bind to a protein obtainable from human endothelial cells that has a molecular weight of about 66 kD.
Abstract: The invention provides antibodies binding to TWEAK, including anti-TWEAK antibodies comprising a heavy chain variable domain CDR3 (CDR3H) selected from the group consisting of SEQ ID NO: 8, 16 or 24. The invention provides anti-TWEAK antibodies which are useful for the treatment of cancer, autoimmune diseases, rheumatoid arthritis, psoratic arthritis, muscle diseases, e.g. muscular dystrophy, multiple sclerosis, chronic kidney diseases, bone diseases, e.g. bone degeneration in multiple myeloma, systemic lupus erythematosus, lupus nephritis, and vascular injury.
Type:
Grant
Filed:
September 30, 2011
Date of Patent:
November 17, 2015
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
Monika Baehner, Hendrik Knoetgen, Jens Niewoehner
Abstract: The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 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 pharmaceuticals.
Type:
Grant
Filed:
February 16, 2010
Date of Patent:
November 17, 2015
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Daniela Alberati, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez Sarmiento, Mark Rogers-Evans, Markus Rudolph
Abstract: The present invention relates to blood brain barrier shuttles that bind receptors on the blood brain barrier (R/BBB) and methods of using the same.
Type:
Application
Filed:
February 2, 2015
Publication date:
November 12, 2015
Applicant:
HOFFMANN-LA ROCHE INC.
Inventors:
Bernd Bohrmann, Per-Ola Freskgard, Peter Maier, Jens Niewoehner, Alain Tissot-Daguette, Eduard Urich
Abstract: The invention relates to the use of a compound of formula I wherein A1 is phenyl or a five or six membered hereroaryl group, containing 1, 2 or 3 heteroatoms, selected from N or S; R1 is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen or cycloalkyl; A2 is phenyl; R2 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, S-lower alkyl substituted by halogen, S(O)2-lower alkyl substituted by halogen; n is 1 or 2; or a pharmaceutically acceptable acid addition salt, or a racemic mixture or its corresponding enantiomer and/or optical isomers thereof, for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.
Abstract: The present invention discloses compounds of Formulae I and II, wherein the variables in Formulae I and II are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formulae I and II in the treatment of HCV infection.
Type:
Grant
Filed:
October 8, 2012
Date of Patent:
November 10, 2015
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
John A. Brinkmann, Hongju Li, Ramakanth Sarabu, Sung-Sau So
Abstract: Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatment of, for example, Alzheimer's Disease.
Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.
Type:
Grant
Filed:
January 8, 2013
Date of Patent:
November 10, 2015
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
Abstract: The invention relates to the compounds of formula I and pharmaceutically acceptable salts and esters thereof, wherein R1-R11 are as defined in the 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 useful in differentiating stem cells into more mature or adult-like hepatocytes for use as drug screening platforms and in disease modeling applications.
Type:
Grant
Filed:
February 3, 2015
Date of Patent:
November 10, 2015
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Eric Chiao, Matthew Michael Hamilton, Sei Kameoka, Brian Leonard, Miriam Triyatni
Abstract: A novel process for the preparation of a fluorolactone derivative of the formula and of its acylated derivative of formula wherein R1 stands for a hydroxy protecting group is described. The acylated fluorolactones of formula V, particularly the benzoyl derivative with R1=benzyl are important precursors for the synthesis of prodrug compounds which have the potential to be potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.
Abstract: The invention relates to a compound of formula (I) wherein A1, A2 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Type:
Application
Filed:
February 20, 2015
Publication date:
October 29, 2015
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Lilli Anselm, David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Beat Spinnler
Abstract: The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Type:
Application
Filed:
December 2, 2013
Publication date:
October 29, 2015
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Beat FREI, Luca GOBBI, Uwe GRETHER, Atsushi KIMBARA, Matthias NETTEKOVEN, Stephan ROEVER, Mark ROGERS-EVANS, Tanja SCHULZ-GASCH
Abstract: The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X1, X4, R1, R2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (?4?1) and alpha-V-beta-3 (?V?3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins.
Type:
Application
Filed:
January 24, 2013
Publication date:
October 29, 2015
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Jayne CHIN, Robert Alan Goodnow, JR., Matthew Michael Hamilton, Achyutharao Sidduri
Abstract: The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
Type:
Application
Filed:
July 7, 2015
Publication date:
October 29, 2015
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Joseph A. Bilotta, Zhi Chen, Elbert Chin, Qingjie Ding, Shawn D. Erickson, Stephen D. Gabriel, Klaus G. Klumpp, Han Ma, Eric Mertz, Jean-Marc Plancher, Robert J. Weikert
Abstract: The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
Type:
Grant
Filed:
October 31, 2012
Date of Patent:
October 27, 2015
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
Johannes Cornelius Hermann, Andreas Kuglstatter, Matthew C. Lucas, Fernando Padilla, Jutta Wanner, Xiaohu Zhang
Abstract: The present invention relates to antibodies against human CSF-1R (CSF-1R antibody), methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
Type:
Grant
Filed:
March 3, 2011
Date of Patent:
October 27, 2015
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
Georg Fertig, Alexander Fidler, Klaus Kaluza, Marlene Thomas, Carola Ries, Stefan Seeber
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 inflammatory diseases and disorders such pulmonary fibrosis.
Type:
Grant
Filed:
September 2, 2013
Date of Patent:
October 27, 2015
Assignee:
HOFFMANN-LA ROCHE INC.
Inventors:
David Budd, Yimin Qian, Ryan Craig Schoenfeld, Achyutharao Sidduri