Patents Represented by Attorney, Agent or Law Firm Patricia S. Rocha-Tramaloni
  • Process for the preparation of thiazolidinedione derivatives
    Patent number: 6531609
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-LA Roche Inc.
    Inventor: Michelangelo Scalone
  • Tetralone derivatives
    Patent number: 6531472
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: March 11, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
  • Nitrile derivatives that inhibit cathepsin K
    Patent number: 6531612
    Abstract: Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: March 11, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Tobias Gabriel, Michael Pech, Sabine Wallbaum
  • Naphthostyrils
    Patent number: 6531598
    Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk
  • Process for preparation of 2-phenyl acetic acid derivatives
    Patent number: 6531597
    Abstract: The present invention is a process for the preparation of a compound of formula The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fabienne Hoffmann-Emery, Michelangelo Scalone, Paul Spurr
  • Thienopyrrolidinones
    Patent number: 6528653
    Abstract: The invention is directed to substituted thieno[2,3-b]pyrrolidin-5-ones. The compounds are useful as inhibitors of cellular production of tumor necrosis factor (TNF-&agr;) and as antiproliferative agents. These compounds are useful in the treatment or control of neuro-degenerative diseases, cardiovascular diseases, cancer or inflammatory diseases.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: March 4, 2003
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Adrian Liam Gill, William Harris
  • Inhibitors for urokinase receptor
    Patent number: 6528619
    Abstract: The present invention provides peptides as inhibitors of the binding of urokinase to the urokinase receptor. The peptides have the general structural formula (I): X1-[X2]n-X3-X4-K-Y-F-X5-X6-I-X7-W-[X8]m  (I) in which X1, X2, X3, X4, X5, X6, X7 and X8 each denote an aminocarboxylic acid, n and m are each independently 0 or 1, K denotes an aminocarboxylic acid with a lysine side chain, Y denotes an aminocarboxylic acid with a tyrosine side chain, F denotes an aminocarboxylic acid with a phenyl-alanine side chain, I denotes an aminocarboxylic acid with an isoleucine side chain, W denotes an aminocarboxylic acid with a tryptophan side chain, and the monomeric building blocks are linked by —CONR1— or —NR1CO— bonds where R1 in each case independently denotes hydrogen, methyl or ethyl, and pharmaceutically compatible salts and derivatives thereof.
    Type: Grant
    Filed: January 10, 2000
    Date of Patent: March 4, 2003
    Assignee: Roche Diagnostics GmbH
    Inventors: Markus Bürgle, Heinrich Graeff, Horst Kessler, Viktor Magdolen, Bernhard König, Marcus Koppitz, Christoph Riemer, Manfred Schmitt, Ulrich Weidle
  • Benzothiazole derivatives with activity as adenosine receptor ligands
    Patent number: 6521754
    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: June 14, 2001
    Date of Patent: February 18, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Alanine, Alexander Flohr, Aubry Kern Miller, Roger David Norcross, Claus Riemer
  • Heterocyclic sulfonamides
    Patent number: 6521631
    Abstract: The compounds of formula (I) wherein R1 has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: February 18, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Philippe Coassolo, Werner Neidhart, Sébastien Roux, Peter Weiss
  • Stereo-specific synthesis of shimikic acid derivatives with improved efficiency
    Patent number: 6518048
    Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula starting from an isophthalic acid derivative of formula 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: February 11, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Iding, Beat Wirz, Ulrich Zutter
  • Aromatic and heteroaromatic substituted 1,2,4-triazolo pyridine derivatives
    Patent number: 6514989
    Abstract: The invention is a compound of formula or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined in the specification. A compound of formula I has a good affinity to the adenosine receptor and can therefore be used for the treatment or protection of diseases mediated by this receptor.
    Type: Grant
    Filed: May 29, 2002
    Date of Patent: February 4, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Heinrich Nettekoven, Bernd Puellmann
  • Tricyclic alkylhydroxamate derivatives
    Patent number: 6512123
    Abstract: Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.
    Type: Grant
    Filed: April 22, 2002
    Date of Patent: January 28, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Adelbert Grossmann, Wolfgang von der Saal, Tim Sattelkau, Ulrich Tibes
  • Glutamate receptor antagonists
    Patent number: 6509328
    Abstract: The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: January 21, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Benzazepinone-derivatives
    Patent number: 6506744
    Abstract: Compounds of formula I as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations for the treatment or prevention of neoplasms, tumor metastasis, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infection caused by viruses, bacteria or fungi.
    Type: Grant
    Filed: July 7, 2000
    Date of Patent: January 14, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Alexander Chucholowski, Thomas Weller
  • Substituted [1,2,4]triazolo[1,5a]pyridine derivatives with activity as adenosine receptor ligands
    Patent number: 6506772
    Abstract: Substituted [1,2,4]triazolo[1,5a]pyridine derivatives and pharmaceutically active salts thereof with activity as adenosine receptor ligands are disclosed. These compounds are useful for treatment of diseases responsive to modulation of the adenosine receptor.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: January 14, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Brodbeck, Matthias Heinrich Nettekoven
  • Process for the preparation of vinyl-pyrrolidinone cephalosporin derivatives
    Patent number: 6504025
    Abstract: Disclosed is a process for the preparation of vinyl-pyrrolidinone cephalosporine derivatives of formula Also disclosed are intermediate compounds of formulas wherein R1 and R2 are as defined herein.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: January 7, 2003
    Assignee: Basilea Pharmaceutica AG
    Inventors: Paul Hebeisen, Hans Hilpert, Roland Humm
  • Naphthostyrils
    Patent number: 6504034
    Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: January 7, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Yi Chen, Apostolos Dermatakis, Frederick Martin Konzelmann, Jin-Jun Liu, Kin-Chun Luk
  • Amorphous form of cell cycle inhibitor having improved solubility and bioavailability
    Patent number: 6492530
    Abstract: The present invention provides a method of preparing an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: December 10, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Antonio A. Albano, Wantanee Phuapradit, Harpreet K. Sandhu, Navnit Hargovindas Shah
  • Para-amine substituted phenylamide glucokinase activators
    Patent number: 6489485
    Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: December 3, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fred Thomas Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
  • Amorphous form of cell cycle inhibitor having improved solubility and bioavailability
    Patent number: 6486329
    Abstract: The present invention provides a method for preparing an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: November 26, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Antonio A. Albano, Wantanee Phuapradit, Harpreet K. Sandhu, Navnit Hargovindas Shah