Patents Assigned to F. Hoffman-La Roche AG
  • Publication number: 20120258966
    Abstract: Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Application
    Filed: March 8, 2012
    Publication date: October 11, 2012
    Applicants: F. HOFFMAN-LA ROCHE AG, PIRAMED LIMITED
    Inventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
  • Patent number: 8263633
    Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: September 11, 2012
    Assignee: F. Hoffman-La Roche AG
    Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
  • Patent number: 8252792
    Abstract: Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: August 28, 2012
    Assignee: F. Hoffman-La Roche AG
    Inventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohal
  • Patent number: 8247397
    Abstract: Combinations of PI3K inhibitor compounds having Formulas I and II and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hyperproliferative disorders such as cancer. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: August 21, 2012
    Assignees: Genentech, Inc., F. Hoffman-La Roche AG
    Inventors: Marcia Belvin, Lori Friedman, Klaus Hoeflich, Deepak Sampath, Ulka Vijapurkar, Jeffrey Wallin, Leisa Johnson, Mallika Singh, Sonal Patel
  • Patent number: 8242104
    Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: August 14, 2012
    Assignee: F. Hoffman-La Roche AG
    Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
  • Patent number: 8153639
    Abstract: Fused pyrimidines of formula (I): wherein A, n, R1, R2, and R3 have any of the values defined herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Grant
    Filed: May 4, 2007
    Date of Patent: April 10, 2012
    Assignee: F. Hoffman-La Roche AG
    Inventors: Irina S. Chuckowree, Adrian J. Folkes, Paul Goldsmith, Timothy C. Hancox, Stephen J. Shuttleworth
  • Patent number: 8124010
    Abstract: A reusable container for the sterile transfer of pharmaceutical recipients, in particular of syringe bodies. The container comprises an outer case and a sterilizable interior, wherein the interior is microbially isolated from the environment of the container. The interior has at least one holder for accommodating at least one nest for storing a plurality of pharmaceutical recipients. The nest can be removably accommodated in the holder. The container further has at least one container door for removing or introducing the nest into the interior and at least one lock for coupling the container to a sterile space. The lock is configured in such a way that, after coupling to the sterile space, it is possible to open the container door without substantially suspending sterility.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: February 28, 2012
    Assignee: F. Hoffman-La Roche AG
    Inventors: Rolf-Dieter Gabel, Martin Knierim
  • Patent number: 8101607
    Abstract: Provided herein are methods of treating diseases or disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, which method includes administering to a patient in need thereof a compound that is a fused pyrimidine of formula (I):
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: January 24, 2012
    Assignee: F. Hoffman-La Roche AG
    Inventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
  • Patent number: 7919235
    Abstract: Oligonucleotides for genotyping the thymidylate synthase gene are provided. The number of tandem repeats in the promoter region of the thymidylate synthase gene can be identified based on the hybridization of an oligonucleotide of the invention to the genomic DNA of a subject. Therefore, the genotype of the thymidylate synthase gene can be identified based on the number of tandem repeats. The genotype relates to the responsiveness of a subject towards an antitumor agent.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: April 5, 2011
    Assignee: F. Hoffman-La Roche AG
    Inventors: Hideyuki Yasuno, Kazushige Mori
  • Publication number: 20100285011
    Abstract: The problem to be solved is to provide an antibody-containing formulation which is stable and suited for subcutaneous administration, wherein dimerization and deamidation is prevented during long-term storage. The present application is directed to a stable antibody-containing liquid formulation characterized by containing arginine and methionine.
    Type: Application
    Filed: December 26, 2008
    Publication date: November 11, 2010
    Applicants: Chugai Seiyaku Kabushiki Kaish, F.Hoffman - La Roche AG
    Inventors: Toshiyuki Morichika, Daisuke Kameoka, Yoshimi Imaeda, Terutoshi Maeda, Oliver Boris Stauch
  • Publication number: 20100222427
    Abstract: The present invention provides a pharmaceutical composition comprising: one or more excipients selected from sugars and sugar alcohols in which equilibrium water content is 1% by weight or less at 25° C. and at 70% relative humidity; and oseltamivir phosphate, wherein an amount of each of glucose and mannose contained in the sugars and sugar alcohols as impurities is 0.01% by weight or less.
    Type: Application
    Filed: February 20, 2007
    Publication date: September 2, 2010
    Applicants: CHUGAI SEIYAKU KABUSHIKI KAISHA, F. HOFFMAN-LA ROCHE AG
    Inventors: Ryuji Kubota, Tomoaki Ohta, Tomoaki Hirayama, Hiroyuki Maeda, Christian Volland, Hans-Guenter KAeStle
  • Patent number: 7776856
    Abstract: Fused pyrimidines of formula (I): where A is a thiophene or furan ring and R1-R3 and n are defined in the specification. These compounds have activity as inhibitors of PI3K and may thus be used to treat diseased and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: August 17, 2010
    Assignee: F. Hoffman-La Roche AG
    Inventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
  • Publication number: 20100196953
    Abstract: The present invention relates to the production of a variant of recombinant trypsin with increased substrate specificity for arginine versus lysine in non-animal host organisms. Moreover, the present invention relates to a variant of recombinant trypsin and their production. Also provided are use of recombinant porcine pancreatic trypsin variants for cleavage of precursors of insulins, and kits containing the variant of trypsin.
    Type: Application
    Filed: August 26, 2006
    Publication date: August 5, 2010
    Applicants: SANOFI-AVENTIS DEUTSCHLAND GMBH, F. HOFFMAN-LA ROCHE AG
    Inventors: Frank Geipel, Stephan Glaser, Christoph Hoh, Erhard Kopetzki, Rainer Mueller, Frank Zocher
  • Patent number: 7400982
    Abstract: The present invention relates to automated generation of multi-dimensional structure activity and structure property relationships.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: July 15, 2008
    Assignee: F. Hoffman-La Roche AG
    Inventors: Holger Fischer, Manfred Kansy
  • Patent number: 6855548
    Abstract: Acid-stable proteases homologous to those derived from strains of the genus Nocardiopsis, their use in animal feed, feed-additives and feed compositions containing such proteases, and methods for the treatment of vegetable proteins using such proteases.
    Type: Grant
    Filed: February 8, 2001
    Date of Patent: February 15, 2005
    Assignee: F. Hoffman-La Roche AG
    Inventors: Carsten Sjoeholm, Peter Rahbek Oestergaard
  • Publication number: 20040161448
    Abstract: The present invention relates to acid-stable proteases homologous to those derived from strains of the genus Nocardiopsis, their use in animal feed, feed-additives and feed compositions containing such proteases, and methods for the treatment of vegetable proteins using such proteases.
    Type: Application
    Filed: November 14, 2003
    Publication date: August 19, 2004
    Applicant: F. Hoffman-La Roche AG
    Inventors: Carsten Sjoeholm, Peter Rahbek Oestergaard
  • Patent number: 6613282
    Abstract: An optical-chemical sensor which is suitable for the continuous and discontinuous determination by luminescence optics of the concentration of chloride in an aqueous sample and which comprises a luminescence indicator (I) and a polymer (H) carrying the luminescence indicator (I) is characterized in that the luminescence indicator (I) is a non-lipophile acridine or bisacridine compound and the polymer (H) is a linear-chain hydrophile polymer soluble in an organic solvent, whereby it is possible to excite the sensor by commercially available LEDs, to manufacture very large numbers thereof at a moderate cost and in a reproducible way and, preferably, to use it for the determination of physiological chloride concentrations and the sensor furthermore has a wide dynamic measuring range for the determination of chloride; a high sensitivity, stability and reproducibility; a high selectivity for chloride; and a low pH cross-sensitivity.
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: September 2, 2003
    Assignee: F. Hoffman-La Roche AG
    Inventors: Christian Huber, Tobias Werner, Otto S. Wolfbeis, Douglas E. Bell, Susannah Young
  • Publication number: 20030101803
    Abstract: An optical-chemical sensor which is suitable for the continuous and discontinuous determination by luminescence optics of the concentration of chloride in an aqueous sample and which comprises a luminescence indicator (I) and a polymer (H) carrying the luminescence indicator (I) is characterized in that the luminescence indicator (I) is a non-lipophile acridine or bisacridine compound and the polymer (H) is a linear-chain hydrophile polymer soluble in an organic solvent, whereby it is possible to excite the sensor by commercially available LEDs, to manufacture very large numbers thereof at a moderate cost and in a reproducible way and, preferably, to use it for the determination of physiological chloride concentrations and the sensor furthermore has a wide dynamic measuring range for the determination of chloride; a high sensitivity, stability and reproducibility; a high selectivity for chloride; and a low pH cross-sensitivity.
    Type: Application
    Filed: January 2, 2003
    Publication date: June 5, 2003
    Applicant: F. Hoffman-La Roche AG
    Inventors: Christian Huber, Tobias Werner, Otto S. Wolfbeis, Douglas E. Bell, Susannah Young
  • Patent number: D620106
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: July 20, 2010
    Assignee: F. Hoffman-La Roche AG
    Inventor: Luc Van der Stappen
  • Patent number: D623738
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: September 14, 2010
    Assignee: F. Hoffman La-Roche AG
    Inventor: Luc Van der Stappen