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 diseases such as, for example, obesity.
Type:
Grant
Filed:
December 5, 2008
Date of Patent:
January 26, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Paul Gillespie, Robert Alan Goodnow, Jr., Shawn David Erickson, Richard Jones
Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
Type:
Grant
Filed:
August 29, 2006
Date of Patent:
January 26, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V Mayweg, Werner Neidhart
Abstract: The present invention relates to compounds of formula I wherein X—Y, R1, and n are as defined herein and to their pharmaceutically active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
Type:
Grant
Filed:
June 25, 2008
Date of Patent:
January 26, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
Abstract: The present invention relates to the design of trimeric polypeptides using polypeptide structural elements derived from the tetranectin protein family, and their use in rational de novo design and production of multi-functional molecules including the application of the multi-functional molecules in protein library technology, such as phage display technology, diagnostic and therapeutic systems, such as human gene therapy and imaging. The trimeric polypeptides being constructed as a monomer polypeptide construct comprising at least one tetranectin trimerising structural element (TTSE) which is covalently linked to at least one heterologous moiety, said TTSE being capable of forming a stable complex with two other TTSEs; or as an oligomer which is comprised of two monomer polypeptide constructs as mentioned above, and which comprises three TTSEs or a multiplum of three TTSEs, or which is comprised of three monomer polypeptide constructs.
Type:
Grant
Filed:
June 14, 2006
Date of Patent:
January 5, 2010
Assignees:
Anaphore, Inc., Hoffman-La Roche, Inc.
Inventors:
Hans Christian Thogersen, Michael Etzerodt, Thor Las Holtet, Niels Jonas Heilskov Graversen, Jette Sandholm Kastrup, Bettina Bryde Nielsen, Ingrid Kjoller Larsen
Abstract: The present invention relates to compounds of formula (Ia), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, R1, R2, R3 and R4 are as defined in the description and claims.
Type:
Grant
Filed:
March 22, 2007
Date of Patent:
January 5, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
Abstract: The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.
Type:
Grant
Filed:
January 24, 2008
Date of Patent:
December 8, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
Type:
Grant
Filed:
November 8, 2006
Date of Patent:
December 1, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Lothar Kling, Ulrike Reiff, Manfred Schwaiger, Georg Tiefenthaler, Wolfgang von der Saal, Thomas von Hirschheydt
Abstract: The present invention relates to compounds of formula (I) wherein R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of 113 receptors.
Type:
Grant
Filed:
November 8, 2006
Date of Patent:
November 24, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.
Type:
Grant
Filed:
May 19, 2006
Date of Patent:
November 17, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Stefan Abrecht, Jean-Michel Adam, Alec Fettes, Joseph Foricher, Bruno Lohri, Patrizio Mattei, Gerard Moine, Rudolf Schmid, Ulrich Zutter
Abstract: The present invention relates to compounds of formula I wherein R1, R2, X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Type:
Grant
Filed:
October 7, 2008
Date of Patent:
November 3, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Matthias Heinrich Nettekoven, Olivier Roche, Rosa Maria Rodriguez-Sarmiento
Abstract: There are presented compounds of the formula or pharmaceutically acceptable salts thereof, wherein Y1, Y2, X1, X2, X3 and R are as described in this application. These compounds are believed to inhibit MDM2-p53 interaction and as such the compounds will have anti-hyperproliferative cellular activity.
Type:
Grant
Filed:
March 13, 2006
Date of Patent:
August 25, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
Abstract: The invention describes compounds of the general formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are herein described, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as antiproliferative agents and may be especially useful for the treatment of cancer.
Type:
Grant
Filed:
June 20, 2006
Date of Patent:
August 18, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Kin-Chun Luk, Sung-Sau So, Jing Zhang, Zhuming Zhang
Abstract: The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.
Type:
Grant
Filed:
February 22, 2005
Date of Patent:
August 18, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alexander Alanine, Konrad Bleicher, Wolfgang Guba, Wolfgang Haap, Dagmar Kube, Thomas Luebbers, Jean-Marc Plancher, Olivier Roche, Mark Rogers-Evans, Gisbert Schneider, Jochen Zuegge
Abstract: The present invention relates to compounds of formula I wherein R1 to R6 are as described herein, which compounds are active at the GABAB receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.
Type:
Grant
Filed:
October 27, 2005
Date of Patent:
August 18, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Parichehr Malherbe, Raffaello Masciadri, Roger David Norcross, Hasane Ratni, Andrew William Thomas
Abstract: Antibodies against insulin like growth factor I receptor (IGF-IR), methods for their production, pharmaceutical compositions containing said antibodies, and uses for such antibodies are disclosed. Antibodies against IGF-IR are implicated in antitumor therapy.
Type:
Grant
Filed:
October 9, 2007
Date of Patent:
August 11, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Yvo Graus, Erhard Kopetzki, Klaus-Peter Kuenkele, Olaf Mundigl, Paul Parren, Frank Rebers, Ralf Schumacher, Jan van de Winkel, Martine Vriesema-van Vugt
Abstract: This invention relates to anti-P-selectin antibodies and, in particular, to anti-P-selectin antibodies and variants thereof that contain an Fc part derived from human origin and do not bind complement factor C1q. These antibodies have new and inventive properties causing a benefit for a patient suffering from critical limb ischemia or peripheral arterial occlusive disease (CLI/PAOD).
Type:
Grant
Filed:
April 8, 2005
Date of Patent:
July 21, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Yvo Graus, Jacques Himber, Miranda Jansen-Molenaar, Dorothee Kling, Erhard Kopetzki, Paul Parren, Frank Rebers, Beat Steiner, Anne Stern, Pamela Strein, Kay-Gunnar Stubenrauch, Jan van de Winkel, Martine van Vugt
Abstract: Monoclonal antibodies, or fragments thereof, are used for isolating and/or identifying at least one cell population. The cell population can include any of the following types of cells: haematopoietic stem cells, neuronal stem cells, neuronal progenitor cells, mesenchymal stem cells and mesenchymal progenitor cells. The antibodies, or fragments thereof, bind to an antigen which is the same as that bound by an antibody which is produced by the hybridoma cell lines CUB1, CUB2, CUB3 and CUB4, which were deposited in the DSMZ under the numbers DSM ACC2569, DSM ACC2566 and DSM ACC2565, on Aug. 14, 2002, and DSM ACC2551, on Jul. 12, 2002.
Type:
Application
Filed:
March 10, 2009
Publication date:
July 16, 2009
Applicant:
HOFFMAN-LA ROCHE INC.
Inventors:
HANS-JOERG BUEHRING, REINER LAMMERS, SELIM KUCI, TIM CONZE
Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Type:
Grant
Filed:
November 20, 2007
Date of Patent:
July 7, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Li Chen, Wayne Wen Lai, Matthias Nettekoven, Olivier Roche, Deye Zheng
Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Compounds of the invention are GlyT-1 inhibitors and are useful for the treatment of CNS disorders such as psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders, or Alzheimer's disease.
Type:
Grant
Filed:
January 31, 2006
Date of Patent:
July 7, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
Abstract: This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.
Type:
Grant
Filed:
August 6, 2008
Date of Patent:
July 7, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, John Anthony Moliterni, Omar Jose Morales