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:
Application
Filed:
March 3, 2014
Publication date:
July 10, 2014
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Silke Hansen, Klaus-Peter Kuenkele, Dietmar Reusch, Ralf Schumacher
Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
Type:
Application
Filed:
February 24, 2014
Publication date:
July 10, 2014
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
Abstract: The invention provides methods for identifying patient who may benefit from treatment with an anti-cancer therapy comprising a VEGF antagonist. The invention also provides methods for monitoring a patients' response to the anti-cancer therapy. The invention also provides kits and articles of manufacture for use in the methods.
Type:
Application
Filed:
March 13, 2013
Publication date:
July 10, 2014
Applicants:
GENENTECH. INC., HOFFMANN-LA ROCHE INC.
Inventors:
Hoffmann-La Roche Inc., Genentech. Inc.
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 current invention reports a method for the recombinant production of a secreted heterologous immunoglobulin in a CHO cell comprising the following steps: i) providing a CHO cell, which is adapted to growth in suspension culture, adapted to growth in serum-free medium, mycoplasma free, and virus free, ii) providing a vector comprising a prokaryotic origin of replication, a first nucleic acid conferring resistance to a prokaryotic selection agent, a second nucleic acid encoding the heavy chain of said heterologous immunoglobulin, a third nucleic acid encoding the light chain of said heterologous immunoglobulin, a fourth nucleic acid conferring resistance to a eukaryotic selection agent, iii) transfecting said CHO cell, wherein said transfecting comprises a) transfecting said CHO cell with said vector comprising a fourth nucleic acid conferring resistance to a first eukaryotic selection agent, b) selecting a CHO cell by growth in cultivation medium containing said first eukaryotic selection agent, c) transfe
Type:
Grant
Filed:
October 9, 2008
Date of Patent:
July 8, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Ulrich Goepfert, Hendrik Knoetgen, Erhard Kopetzki, Anne Stern
Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; 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.
Type:
Grant
Filed:
April 11, 2012
Date of Patent:
July 8, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.
Type:
Grant
Filed:
August 30, 2012
Date of Patent:
July 8, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
Abstract: The invention relates to anti-HER3 antigen binding proteins, e.g. anti-HER3 antibodies, that bind to the beta-hairpin of HER3, methods for selecting these antigen binding proteins, their preparation and use as medicament.
Type:
Application
Filed:
November 6, 2013
Publication date:
July 3, 2014
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Birgit Bossenmaier, David Casagolda Vallribera, Guy Georges, Michael Gerg, Gerhard Niederfellner, Christian Scholz, Michael Schraeml
Abstract: The invention relates to anti-HER3/HER4 antigen binding proteins, e.g. anti-HER3/HER4 antibodies, that bind to the beta-hairpin of HER3 and the beta-hairpin of HER4, methods for selecting these antigen binding proteins, their preparation and use as medicament.
Type:
Application
Filed:
November 6, 2013
Publication date:
July 3, 2014
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Birgit Bossenmaier, Guy Georges, Michael Gerg, Gerhard Niederfellner, Christian Scholz, Michael Schraeml
Abstract: The invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R2, R3 and R4 are as defined in the specification, comprising the steps of a) catalytic asymmetric hydrogenation of an enamine of the formula wherein R1 is lower alkyl, in the presence of a transition metal catalyst containing a chiral diphosphane ligand, b) introduction of an amino protecting group Prot and c) amidation of the ester to form an amide of formula wherein R2, R3, R4 and Prot are as defined in the specification.
Type:
Application
Filed:
March 6, 2014
Publication date:
July 3, 2014
Applicant:
HOFFMANN-LA ROCHE INC.
Inventors:
Stefan Abrecht, Michelangelo Scalone, Rudolf Schmid
Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.
Type:
Grant
Filed:
July 12, 2011
Date of Patent:
July 1, 2014
Assignee:
Hoffmann-La Roche Inc
Inventors:
Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is a useful pharmaceutical active compound.
Type:
Grant
Filed:
August 22, 2013
Date of Patent:
July 1, 2014
Assignee:
Hoffmann - La Roche Inc.
Inventors:
Declan Costello, Gerard John Hamett, Pirmin Hidber, Ursula Hoffmann, Thomas McCarthy, Reinhard Reents, Dennis A. Smith, Timothy Smyth
Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl] 2-methylthiopropionate which is useful as a pharmaceutically active compound.
Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
January 13, 2014
Date of Patent:
June 17, 2014
Assignee:
F. Hoffmann-La Roche AG
Inventors:
James J. Crawford, Daniel F. Ortwine, BinQing Wei, Wendy B. Young
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.
Abstract: Herein is reported a method for the purification of a protein comprising erythropoietin and a single poly (ethylene glycol) residue from reaction by-products or not reacted starting material by a cation exchange chromatography method. It has been found that by employing a cation exchange SP Sephacrylâ„¢ S 500 HR chromatography material conditioned to a conductivity of 21 mS/cm and a linear gradient elution a fusion protein of erythropoietin and a single poly (ethylene glycol) residue can be obtained in a single step with high purity and yield.
Type:
Application
Filed:
November 26, 2013
Publication date:
June 12, 2014
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Roberto Falkenstein, Wolfgang Koehnlein, Wolfgang Kuhne, Hartmut Schurig (deceased)
Abstract: The present invention relates to 1,4-Oxazepines 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:
March 9, 2012
Date of Patent:
June 10, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans, Didier Rombach, Andrew Thomas, Thomas Woltering, Wolfgang Wostl
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.
Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Type:
Application
Filed:
February 4, 2014
Publication date:
June 5, 2014
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Robert Than Hendricks, Johannes Hermann, Saul Jaime-Figueroa, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee