Abstract: The present invention relates to bispecific antibodies, methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.
Type:
Grant
Filed:
February 21, 2013
Date of Patent:
January 30, 2018
Assignee:
HOFFMAN-LA ROCHE INC.
Inventors:
Ulrich Brinkmann, Alexander Haas, Silke Metz, Juergen Michael Schanzer
Abstract: A method for cultivating a bacterial cell comprising the addition of an amino acid in an alkaline solution used for pH regulation. Also an aspect is a method for producing a polypeptide comprising the steps of a) providing a bacterial cell comprising a nucleic acid encoding the polypeptide, b) cultivating the provided cell, c) adjusting the pH value during the cultivating with a basic solution comprising an amino acid, d) recovering the polypeptide from the cell or the cultivation medium and thereby producing the polypeptide.
Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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 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:
January 10, 2013
Date of Patent:
July 11, 2017
Assignee:
Hoffman-La Roche Inc.
Inventors:
Shaoqing Chen, Johannes Cornelius Hermann, Nam T. Le, Matthew C. Lucas, Fernando Padilla
Abstract: Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.
Type:
Grant
Filed:
August 19, 2016
Date of Patent:
May 30, 2017
Assignees:
Plexxikon Inc., Hoffman-La Roche Inc.
Inventors:
Dipen Desai, Ralph Diodone, Zenaida Go, Prabha N. Ibrahim, Raman Iyer, Hans-Juergen Mair, Harpreet K. Sandhu, Navnit H. Shah, Gary Visor, Nicole Wyttenbach, Stephan Lauper, Johannes Pudewell, Frank Wierschem
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
April 14, 2016
Date of Patent:
May 2, 2017
Assignee:
Hoffman-La Roche Inc.
Inventors:
Johannes Aebi, Kurt Amrein, Robert Britton, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan
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 9, 2015
Date of Patent:
April 11, 2017
Assignee:
HOFFMAN-LA ROCHE INC.
Inventors:
Georg Fertig, Alexander Fidler, Klaus Kaluza, Marlene Thomas, Carola Ries, Stefan Seeber
Abstract: Compounds having the formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and methods of using the compounds as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors for the treatment or prophylaxis of type 2 diabetes, atherosclerosis, chronic kidney diseases, non-alcoholic steatohepatitis and cancer.
Type:
Grant
Filed:
December 18, 2014
Date of Patent:
March 28, 2017
Assignee:
Hoffman-La Roche Inc.
Inventors:
Bernd Buettelmann, Simona M. Ceccarelli, Holger Kuehne, Bernd Kuhn, Werner Neidhart, Ulrike Obst Sander, Hans Richter
Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
Type:
Grant
Filed:
August 27, 2015
Date of Patent:
January 31, 2017
Assignee:
Hoffman La-Roche Inc.
Inventors:
Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
Abstract: The invention relates to a safety device for an injection syringe, the injection syringe including a body having an injection needle fitted thereon, the device including a plunger rod including a distal plunger part slidably movable in the body of the syringe, and a proximal triggering part, configured to trigger the displacement of a protection sheath, from an injection position, wherein the needle is uncovered, towards a safety position, wherein the needle is covered by the sheath. The proximal triggering part is able to move relative to the distal plunger part once the distal plunger part is at the distal end of its stroke, to trigger the displacement of the protection sheath.
Type:
Grant
Filed:
January 6, 2014
Date of Patent:
September 20, 2016
Assignee:
HOFFMAN-LA ROCHE INC.
Inventors:
Mark Digby Teucher, Pascal Dugand, Loïc Sebileau, Daniel Peter, Maxime Gaillot, Jürg Liniger
Abstract: Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.
Type:
Grant
Filed:
March 31, 2010
Date of Patent:
September 20, 2016
Assignees:
Plexxikon Inc., Hoffman-La Roche Inc.
Inventors:
Dipen Desai, Ralph Diodone, Zenaida Go, Prabha N. Ibrahim, Raman Iyer, Hans-Juergen Mair, Harpreet K. Sandhu, Navnit H. Shah, Gary Visor, Nicole Wyttenbach, Stephan Lauper, Johannes Pudewell, Frank Wierschem
Abstract: The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. 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) can be used as medicament.
Abstract: The invention provides a Pseudomonas exotoxin A (PE) comprising an amino acid sequence having a substitution of one or more B-cell and/or T-cell epitopes. The invention further provides related chimeric molecules, as well as related nucleic acids, recombinant expression vectors, host cells, populations of cells, and pharmaceutical compositions. Methods of treating or preventing cancer in a mammal, methods of inhibiting the growth of a target cell, methods of producing the PE, and methods of producing the chimeric molecule are further provided by the invention.
Type:
Grant
Filed:
October 3, 2014
Date of Patent:
July 12, 2016
Assignees:
The United States of America, as represented by the Secretary, Department of Health and Human Services, Hoffman-La Roche Inc.
Inventors:
Ira H. Pastan, Ronit Mazor, Masanori Onda, Byungkook Lee, Gerhard Niederfellner, Sabine Imhof-Jung, Ulrich Brinkmann, Guy Georges
Abstract: The present invention relates to a novel process for the preparation of a pyrazole carboxylic acid derivative of the formula wherein R1 is C1-7-alkyl and R3 is C1-7-alkyl which is optionally substituted with halogen or C1-4-alkoxy. The pyrazole carboxylic acid derivative of the formula I can be used as building block in the preparation of pharmaceutically active principles e.g. for compounds acting as phosphodiesterase (PDE) inhibitors, particularly PDE10 inhibitors. PDE10 inhibitors have the potential to treat psychotic disorders like schizophrenia.
Type:
Grant
Filed:
February 16, 2015
Date of Patent:
May 24, 2016
Assignee:
Hoffman-La Roche Inc.
Inventors:
Bjoern Bartels, Fritz Bliss, Katrin Groebke Zbinden, Matthias Koerner
Abstract: The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
Abstract: This invention relates to novel 4-amino-imidazoquinoline compounds of the formula wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer or infectious diseases.
Type:
Grant
Filed:
April 22, 2015
Date of Patent:
May 10, 2016
Assignee:
HOFFMAN-LA ROCHE INC.
Inventors:
Sabine Hoves, Bernd Kuhn, Fabienne Ricklin, Stephan Roever
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 as, for example, pulmonary fibrosis.
Type:
Grant
Filed:
June 17, 2013
Date of Patent:
April 26, 2016
Assignee:
HOFFMAN-LA ROCHE INC.
Inventors:
Stephen Deems Gabriel, Matthew Michael Hamilton, Matthew C. Lucas, Yimin Qian, Achyutharao Sidduri