Patents Represented by Attorney George W. Johnston
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Patent number: 8314250Abstract: The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.Type: GrantFiled: October 15, 2010Date of Patent: November 20, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Kevin W. Anderson, Paul Gillespie, Nicholas J. S. Huby, Norman Kong, John L. Roberts, Pamela L. Rossman, Sung-Sau So
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Patent number: 8314225Abstract: The current invention comprises a nucleic acid encoding the amino acid sequence of the C-terminal part of the CH3-domain of an immunoglobulin of the class IgA or IgG, or the C-terminal part of the CH4-domain of an immunoglobulin of the class IgE or IgM, wherein the glycine-lysine-dipeptide comprised in the amino acid sequence of the C-terminal part of the CH3- or CH4-domain is encoded by the nucleic acid ggaaaa, or the nucleic acid ggcaaa, or the nucleic acid gggaaa, or the nucleic acid gggaag, or the nucleic acid ggcaag, or the nucleic acid ggaaag.Type: GrantFiled: June 25, 2008Date of Patent: November 20, 2012Assignee: Hoffman-La Roche Inc.Inventors: Ulrich Goepfert, Silke Hansen, Hendrik Knoetgen, Erhard Kopetzki, Oliver Ploettner
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Patent number: 8309299Abstract: The present invention relates to a method for determining a subject's resistance to treatment with 2,2-dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N?-(2,2,3,3,3-pentafluoro-propyl)-malonamide by measuring the levels a biomarker or biomarkers present in a biological sample obtained from the subject, the biomarker being IL6 and/or IL8. The present invention also relates to a combination therapy for a patient suffering from a proliferative disorder comprising administering to the patient 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N?-(2,2,3,3,3-pentafluoro-propyl)-malonamide and an anti-IL6 and/or an anti-IL8 agent.Type: GrantFiled: May 2, 2011Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: John Frederick Boylan, Wei He
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Patent number: 8309340Abstract: The present invention provides apo crystals and co-crystals of insulin-degrading enzyme (IDE) and their uses in drug development.Type: GrantFiled: December 22, 2008Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Joerg Benz, Dominique Burger, Martine Stihle, Ralf Thoma
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Patent number: 8309310Abstract: The present invention relates to a generic method for detecting a kinase or phosphatase activity. The method comprises the following steps: incubating a kinase or phosphatase activity sample with a kinase or phosphatase substrate molecule comprising either a fluorophore having a detectable readout or molecule with an aromatic group which serves as a quencher of the fluorophore, incubating the mixture of step a) with a detection entity comprising either a fluorophore or a molecule with an aromatic group and a binding partner, wherein the substrate molecule and the detection entity are capable of binding to the binding partner and the binding of the substrate molecule and the detection entity to the binding partner lead to an altered readout of the fluorophore, and measuring the readout of the fluorophore in the mixture of step b), wherein an altered readout of the fluorophore compared to a blank is indicative for the presence of a kinase or phosphatase activity in the sample.Type: GrantFiled: September 1, 2008Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Thilo Enderle, Doris Roth
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Patent number: 8309581Abstract: The present invention relates to compounds of formula (I), as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A, B, R1, R2, R3, R4, R5, n, m and p have the significance defined herein.Type: GrantFiled: September 20, 2010Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Markus Rudolph, Sven Taylor
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Patent number: 8309734Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: October 19, 2009Date of Patent: November 13, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Rainer E. Martin, Ulrike Obst Sander, Hans Richter, Christoph Ullmer
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Patent number: 8299077Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.Type: GrantFiled: February 24, 2010Date of Patent: October 30, 2012Assignee: Roche Palo Alto LLCInventors: Steven Berthel, Fariborz Firooznia, Daniel Fishlock, Jun-Bae Hong, Yan Lou, Matthew Lucas, Timothy D. Owens, Keshab Sarma, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Patent number: 8299023Abstract: Provided herein are neuropeptide-2 receptor agonists of the formula (I): Y—R1—R2—X—R3—R4—R5—R6—R7—R8—R9—R10—R11—R12—R13—R14—NH2??(I) (SEQ ID NO: 1), as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.Type: GrantFiled: August 25, 2009Date of Patent: October 30, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Waleed Danho, David Charles Fry, Robert Alan Goodnow, Jr., Wajiha Khan, Joseph Swistok, Jefferson Wright Tilley
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Patent number: 8293770Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: October 2, 2009Date of Patent: October 23, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angelique Patiny-Adam, Hasane Ratni, Claus Riemer
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Patent number: 8293730Abstract: The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.Type: GrantFiled: November 16, 2009Date of Patent: October 23, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
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Patent number: 8293916Abstract: The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.Type: GrantFiled: November 5, 2009Date of Patent: October 23, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Paul Spurr, Eric Vieira
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Patent number: 8288431Abstract: There is provided a compound of the formula wherein X, Y, W, R1, R2 and R3 are as described herein. The compounds have activity as anticancer agents.Type: GrantFiled: January 19, 2011Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Jing Zhang, Zhuming Zhang
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Patent number: 8288541Abstract: The invention is concerned with novel piperazine amide derivatives of formula (I) wherein R1 to R11, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: August 6, 2008Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Ulrike Obst Sander, Stephan Roever, Tanja Schulz-Gasch, Matthew Wright, Rene Wyler
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Patent number: 8288403Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: GrantFiled: November 4, 2009Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Patent number: 8268784Abstract: Provided herein are neuropeptide-2 receptor agonists of the formula (I): as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. X is 4-oxo-6-(1-piperazinyl)-3(4H)-quinazoline-acetic acid (Pqa). These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.Type: GrantFiled: August 6, 2009Date of Patent: September 18, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karin Conde-Knape, Waleed Danho, George Ehrlich, Nader Fotouhi, David Charles Fry, Wajiha Khan, Anish Konkar, Cristina Martha Rondinone, Joseph Swistok, Rebecca Anne Taub, Jefferson Wright Tilley
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Patent number: 8268870Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: December 13, 2011Date of Patent: September 18, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun
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Patent number: 8268820Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: GrantFiled: March 19, 2010Date of Patent: September 18, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Daniel Hunziker, Chrisitan Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 8268314Abstract: The present invention relates to bispecific antibodies against human VEGF and against human ANG-2, methods for their production, pharmaceutical compositions containing said antibodies, and uses thereof.Type: GrantFiled: October 2, 2009Date of Patent: September 18, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Monika Baehner, Ulrich Brinkmann, Guy Georges, Remko Albert Griep, Sabine Imhof-Jung, Anita Kavlie, Hubert Kettenberger, Christian Klein, Joerg Thomas Regula, Wolfgang Schaefer, Juergen Michael Schanzer, Werner Scheuer, Stefan Seeber, Markus Thomas
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Patent number: 8268840Abstract: This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.Type: GrantFiled: April 29, 2009Date of Patent: September 18, 2012Assignee: Roche Palo Alto LLCInventors: Frederick Brookfield, Florence Eustache, Michael Patrick Dillon, David Michael Goldstein, Leyi Gong, Xiaochun Han, Joan Heather Hogg, Jaehyeon Park, Deborah Carol Reuter, Eric Brian Sjogren