Patents Represented by Attorney, Agent or Law Firm Patricia S. Rocha-Tramaloni
  • Patent number: 6835732
    Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
    Type: Grant
    Filed: December 5, 2002
    Date of Patent: December 28, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Alanine, Alexander Flohr, Aubry Kern Miller, Roger David Norcross, Claus Riemer
  • Patent number: 6831087
    Abstract: The invention relates to compounds of formulae: Compounds of the invention have a good affinity to the NMDA receptor and are useful for the treatment of diseases related to this receptor.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: December 14, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
  • Patent number: 6827907
    Abstract: A compound handling system handles a multiplicity of chemical or biological compounds or samples, and is especially adapted for high throughput screening of compounds that are stored and handled in aliquotted form. Aliquots are contained in individual containers and the containers are arranged in racks having holding spaces open at opposite ends. Insertion and removal of the containers is effected in either direction of movement, and each container may be sealed with foil to protect its integrity.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: December 7, 2004
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Christof Fattinger, Hansjörg Tschirky
  • Patent number: 6818774
    Abstract: Disclosed are isoquinolino derivatives of the formula wherein Y is >C═O or —CH2—, Z is >C═O or —CH2—, and R1, R2 and m are as defined herein as well as the pharmaceutically acceptable salts thereof. These compounds are MAO-B selective inhibitors useful, inter alia, in the treatment of Alzheimer's disease and/or senile dementia.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: November 16, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Michelangelo Scalone, Andrew William Thomas, Rene Wyler
  • Patent number: 6806370
    Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: October 19, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Torsten D. Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
  • Patent number: 6803381
    Abstract: The present invention relates to compounds of formula wherein R1 is hydrogen or lower alkyl; R2, R2′ are each independently hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X is O, S or two hydrogen atoms not forming a bridge; A1/A2 is phenyl; B is a group of formula  wherein R3 is lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl; Y is —O—, —S— or a bond; and Z is —O—; or a pharmaceutically acceptable salt thereof. These compounds are useful for the control or prevention of acute and/or chronic neurological disorders.
    Type: Grant
    Filed: May 14, 2003
    Date of Patent: October 12, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6800638
    Abstract: A compound of the formula (I) wherein A, R1, R2 and X have the meanings defined in the specification, process of manufacturing such as compound and a pharmaceutical composition with HDAC inhibitor activity and anti-cell proliferation activity containing such a compound.
    Type: Grant
    Filed: June 23, 2003
    Date of Patent: October 5, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Guy Georges, Adelbert Grossman, Olaf Mundigl, Wolfgang von der Saal, Tim Sattelkau
  • Patent number: 6794139
    Abstract: A pharmaceutical composition is disclosed, as well as its use in tumour diagnosis, therapy and prevention, methods for diagnosing, treating and preventing tumours, and antibodies and their use.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: September 21, 2004
    Assignee: Roche Diagnostics GmbH
    Inventors: Sabine Schiemann, Ulrich Weidle
  • Patent number: 6790852
    Abstract: The invention is directed to compounds of formula (I), which are valuable therapeutics for the treatment of cancer and related diseases.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: September 14, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Brandt, Georg Fertig, Hans-Willi Krell, Thomas von Hirschheydt, Edgar Voss
  • Patent number: 6787539
    Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceutic
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: September 7, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Heinz Stadler
  • Patent number: 6784173
    Abstract: Compounds of formula I wherein A, R1 and R2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: August 31, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulrike Leser-Reiff, Tim Sattelkau, Gerd Zimmermann
  • Patent number: 6770637
    Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: August 3, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thierry Godel, Torsten Hoffmann, Patrick Schnider, Heinz Stadler
  • Patent number: 6762320
    Abstract: This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5 R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: July 13, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
  • Patent number: 6756380
    Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rin
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: June 29, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Patent number: 6756374
    Abstract: Disclosed are novel diaminothiazoles of formula wherein R1, R2, R3, R4 and R5 are as herein disclosed. These compounds and their pharmaceutically acceptable salts and esters are selective inhibitors of Cdk4. As such, these compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and their pharmaceutically acceptable salts and esters, as well as intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: June 29, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Qingjie Ding, Paul Gillespie, Kyungjin Kim, Allen John Lovey, Warren William McComas, John Guilfoyle Mullin, Jr., Agostino Perrotta
  • Patent number: 6747026
    Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: June 8, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
  • Patent number: 6743789
    Abstract: The present invention is a compound of formula The compound and derivatives or pharmaceutically acceptable salts thereof of the invention have a good affinity and selectivity to the GABA A &agr;5 receptor and are useful for the treatment of diseases related to this receptor.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: June 1, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
  • Patent number: 6740760
    Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: May 25, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
  • Patent number: 6737409
    Abstract: Novel anti-tumor compounds of formula, are disclosed. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), the use of compounds of formula (I) for the treatment of cancer, and processes for the preparation of compounds (I).
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: May 18, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Toshihiko Fujii, Takehiro Okada, Mikio Taniguchi, Fumio Watanabe
  • Patent number: 6734179
    Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as described within. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they may be used in the treatment of diseases, related to this receptor.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: May 11, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer