Patents Assigned to F. Hoffman-La Roche AG
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Publication number: 20120258966Abstract: 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: ApplicationFiled: March 8, 2012Publication date: October 11, 2012Applicants: F. HOFFMAN-LA ROCHE AG, PIRAMED LIMITEDInventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
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Patent number: 8263633Abstract: 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: GrantFiled: September 27, 2010Date of Patent: September 11, 2012Assignee: F. Hoffman-La Roche AGInventors: 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
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Patent number: 8252792Abstract: 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: GrantFiled: April 25, 2007Date of Patent: August 28, 2012Assignee: F. Hoffman-La Roche AGInventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohal
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Patent number: 8247397Abstract: 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: GrantFiled: September 10, 2008Date of Patent: August 21, 2012Assignees: Genentech, Inc., F. Hoffman-La Roche AGInventors: Marcia Belvin, Lori Friedman, Klaus Hoeflich, Deepak Sampath, Ulka Vijapurkar, Jeffrey Wallin, Leisa Johnson, Mallika Singh, Sonal Patel
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Patent number: 8242104Abstract: 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: GrantFiled: September 27, 2010Date of Patent: August 14, 2012Assignee: F. Hoffman-La Roche AGInventors: 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
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Patent number: 8153639Abstract: 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: GrantFiled: May 4, 2007Date of Patent: April 10, 2012Assignee: F. Hoffman-La Roche AGInventors: Irina S. Chuckowree, Adrian J. Folkes, Paul Goldsmith, Timothy C. Hancox, Stephen J. Shuttleworth
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Patent number: 8124010Abstract: 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: GrantFiled: August 12, 2010Date of Patent: February 28, 2012Assignee: F. Hoffman-La Roche AGInventors: Rolf-Dieter Gabel, Martin Knierim
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Patent number: 8101607Abstract: 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: GrantFiled: July 13, 2010Date of Patent: January 24, 2012Assignee: F. Hoffman-La Roche AGInventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
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Patent number: 7919235Abstract: 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: GrantFiled: September 30, 2002Date of Patent: April 5, 2011Assignee: F. Hoffman-La Roche AGInventors: Hideyuki Yasuno, Kazushige Mori
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Publication number: 20100285011Abstract: 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: ApplicationFiled: December 26, 2008Publication date: November 11, 2010Applicants: Chugai Seiyaku Kabushiki Kaish, F.Hoffman - La Roche AGInventors: Toshiyuki Morichika, Daisuke Kameoka, Yoshimi Imaeda, Terutoshi Maeda, Oliver Boris Stauch
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Publication number: 20100222427Abstract: 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: ApplicationFiled: February 20, 2007Publication date: September 2, 2010Applicants: CHUGAI SEIYAKU KABUSHIKI KAISHA, F. HOFFMAN-LA ROCHE AGInventors: Ryuji Kubota, Tomoaki Ohta, Tomoaki Hirayama, Hiroyuki Maeda, Christian Volland, Hans-Guenter KAeStle
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Patent number: 7776856Abstract: 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: GrantFiled: October 25, 2005Date of Patent: August 17, 2010Assignee: F. Hoffman-La Roche AGInventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
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Publication number: 20100196953Abstract: 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: ApplicationFiled: August 26, 2006Publication date: August 5, 2010Applicants: SANOFI-AVENTIS DEUTSCHLAND GMBH, F. HOFFMAN-LA ROCHE AGInventors: Frank Geipel, Stephan Glaser, Christoph Hoh, Erhard Kopetzki, Rainer Mueller, Frank Zocher
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Patent number: 7400982Abstract: The present invention relates to automated generation of multi-dimensional structure activity and structure property relationships.Type: GrantFiled: July 28, 2006Date of Patent: July 15, 2008Assignee: F. Hoffman-La Roche AGInventors: Holger Fischer, Manfred Kansy
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Patent number: 6855548Abstract: 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: GrantFiled: February 8, 2001Date of Patent: February 15, 2005Assignee: F. Hoffman-La Roche AGInventors: Carsten Sjoeholm, Peter Rahbek Oestergaard
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Publication number: 20040161448Abstract: 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: ApplicationFiled: November 14, 2003Publication date: August 19, 2004Applicant: F. Hoffman-La Roche AGInventors: Carsten Sjoeholm, Peter Rahbek Oestergaard
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Patent number: 6613282Abstract: 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: GrantFiled: July 6, 2001Date of Patent: September 2, 2003Assignee: F. Hoffman-La Roche AGInventors: Christian Huber, Tobias Werner, Otto S. Wolfbeis, Douglas E. Bell, Susannah Young
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Publication number: 20030101803Abstract: 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: ApplicationFiled: January 2, 2003Publication date: June 5, 2003Applicant: F. Hoffman-La Roche AGInventors: Christian Huber, Tobias Werner, Otto S. Wolfbeis, Douglas E. Bell, Susannah Young
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Patent number: D620106Type: GrantFiled: May 28, 2009Date of Patent: July 20, 2010Assignee: F. Hoffman-La Roche AGInventor: Luc Van der Stappen
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Patent number: D623738Type: GrantFiled: May 28, 2009Date of Patent: September 14, 2010Assignee: F. Hoffman La-Roche AGInventor: Luc Van der Stappen