Patents Assigned to Hoffmann-La Roche
  • Patent number: 6953806
    Abstract: The present invention provides compounds of formula (I) wherein A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, U, V, W, m, n and p are as indicated in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia and hyperlipemia.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: October 11, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Georges Hirth, Hans-Peter Maerki, Olivier Morand
  • Patent number: 6951879
    Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: October 4, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
  • Patent number: 6951884
    Abstract: The invention relates to fluorobenzamide derivatives of the formula wherein R1, R2, R3 R4, R5, R6 and R7 are as defined herein. =, The compounds of the invention are selective monoamine oxidase B inhibitors and therefore they are suitable for the treatment of diseases mediated by monoamine oxidase B, such as Alzheimer's disease or senile dementia.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: October 4, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
  • Patent number: 6951875
    Abstract: The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.
    Type: Grant
    Filed: October 21, 2002
    Date of Patent: October 4, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
  • Patent number: 6946462
    Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.
    Type: Grant
    Filed: April 13, 2004
    Date of Patent: September 20, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
  • Patent number: 6946471
    Abstract: This invention is directed to compounds of formula (I), which are valuable therapeutics for the treatment of cancer and cancer related diseases.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: September 20, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Brandt, Georg Fertig, Hans-Willi Krell, Thomas von Hirschheydt, Edgar Voss
  • Patent number: 6943158
    Abstract: Compounds of formula I are p38 inhibitors: or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclyl, heterocyclylalkyl, or —Y1—C(O)—Y2—R11 (where Y1 and Y2 are independently either absent or an alkylene group and R11 is hydrogen, alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino); R3 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterosubstituted cycloalkyl, heterocyclyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(?O)—R4 (where R4 is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino), or acyl; Ar1 is aryl; X1 is O, NR5 or S, where R5 is hydrogen or alkyl; and X2 is a bond, O, NR6, S or CH2, where R6 is hydrogen or alkyl.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: September 13, 2005
    Assignees: Roche Palo Alto LLC, Hoffmann-La Roche Inc.
    Inventors: Jian Jeffrey Chen, Kin-Chun Thomas Luk
  • Patent number: 6939986
    Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: September 6, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Karpf, René Trussardi
  • Patent number: 6933387
    Abstract: The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I): as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: August 23, 2005
    Assignees: Hoffmann-La Roche Inc., Vernalis Research Limited
    Inventors: Jonathan Mark Bentley, Paul Hebeisen, Marc Muller, Hans Richter, Stephan Roever
  • Patent number: 6930086
    Abstract: This invention is directed to an erythropoietin mutein having in vivo biological activity for causing bone marrow cells to increase production of reticulocytes and red blood cells, in that the mutein is N-glycosylated at Asn38 and Asn83 but not N-glycosylated at Asn24. Such muteins have improved pharmaceutical properties.
    Type: Grant
    Filed: September 11, 2002
    Date of Patent: August 16, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Wilhelm Tischer
  • Patent number: 6916923
    Abstract: Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula I using intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.
    Type: Grant
    Filed: April 19, 2004
    Date of Patent: July 12, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Qingjie Ding, Jin-Jun Liu, Giacomo Pizzolato, Peter Michael Wovkulich
  • Patent number: 6916833
    Abstract: The present invention provides compounds having formula (I): and formula (II): wherein X, n, and R1-R12 are defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (I) or (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (I) or (II).
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: July 12, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kyungjin Kim, Emily Aijun Liu, Steven Gregory Mischke
  • Patent number: 6913883
    Abstract: The invention comprises a nucleic acid molecule with the sequence SEQ ID NO:5 and the complementary sequence, and its use in diagnosis and therapy. This nucleic acid molecule (IIP-10) is a gene which encodes an IGF-1 receptor binding polypeptide.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: July 5, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Tanja Ligensa, Ralf Schumacher, Michael Weidner
  • Patent number: 6914140
    Abstract: A novel process for the manufacture of compounds of the formula wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: July 5, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter Karl Matzinger, Michelangelo Scalone, Ulrich Zutter
  • Patent number: 6903095
    Abstract: This invention relates to phthalimido derivatives of the formula wherein X is —N? or —CH?, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.
    Type: Grant
    Filed: September 9, 2003
    Date of Patent: June 7, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
  • Patent number: 6900227
    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: July 24, 2003
    Date of Patent: May 31, 2005
    Assignee: Hoffmann-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
  • Patent number: 6897226
    Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
    Type: Grant
    Filed: July 9, 2003
    Date of Patent: May 24, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
  • Patent number: 6897222
    Abstract: The present invention provides compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
    Type: Grant
    Filed: March 15, 2004
    Date of Patent: May 24, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Claudio Gobbi, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Pierre Charles Wyss
  • Patent number: 6890947
    Abstract: Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R8, A, A1 and n have the significance indicated in the specification.
    Type: Grant
    Filed: September 10, 2003
    Date of Patent: May 10, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Binggeli, Beat Wirz, Uwe Grether, Hans Hilpert, Roland Humm, Hans Iding, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr
  • Patent number: 6887864
    Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.
    Type: Grant
    Filed: March 6, 2003
    Date of Patent: May 3, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher