Patents Represented by Attorney George W. Johnston
  • Patent number: 8263656
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R4 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: Grant
    Filed: August 13, 2009
    Date of Patent: September 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Paul Gillespie, Robert Alan Goodnow, Jr., Tai-An Lin, Achyutharao Sidduri, Sung-Sau So, Jenny Tan
  • Patent number: 8258158
    Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: September 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
  • Patent number: 8258134
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts 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 metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Grant
    Filed: March 9, 2009
    Date of Patent: September 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
  • Patent number: 8258149
    Abstract: The invention provides novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein, compositions including the compounds and methods of preparing and using the compounds.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: September 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Yongguo Li, Guolong Wu
  • Patent number: 8252826
    Abstract: This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: August 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
  • Patent number: 8242276
    Abstract: The present invention provides novel methods for preparing N—(S)-1 -azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic ?-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: August 14, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jodie Brice, Miall Cedilote, Zhiming Dong, Pingsheng Zhang
  • Patent number: 8242153
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: August 14, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Patent number: 8242247
    Abstract: The present invention relates to novel domain exchanged, bivalent, bispecific antibodies, their manufacture and use.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: August 14, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian Klein, Wolfgang Schaefer
  • Patent number: 8232412
    Abstract: The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic ?-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: July 31, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Thomas Cleary, Yaohui Ji, Thimma Rawalpally
  • Patent number: 8227458
    Abstract: The present invention is concerned with arylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. arylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein, their manufacture, and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: July 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Patrick Schnider
  • Patent number: 8227491
    Abstract: The present invention relates to a compound of formula I, in all its isomeric forms and pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Roever, Matthew Wright
  • Patent number: 8227505
    Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: July 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Stefan Hildbrand, Bruno Lohri, Wolfgang Wostl
  • Patent number: 8227195
    Abstract: The current invention comprises a method for determining of an antibody against a drug antibody in a sample using an immunoassay comprising a capture drug antibody and a tracer drug antibody, wherein the method comprises providing i) a capture drug antibody, which is the drug antibody conjugated to a solid phase, ii) a tracer drug antibody, which is the drug antibody conjugated to a detectable label, contacting the capture drug antibody separately with i) the sample, ii) the sample, to which the drug antibody in monomeric form has been added, iii) the sample, to which the drug antibody in oligomeric form has been added, and determining an antibody against the drug antibody in the sample by a positive immunoassay in i) and a negative immunoassay in ii) and iii).
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: July 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kay-Gunnar Stubenrauch, Markus Zadak
  • Patent number: 8227613
    Abstract: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: July 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
  • Patent number: 8227577
    Abstract: The present invention relates to novel domain exchanged, bivalent, bispecific antibodies, their manufacture and use.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: July 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Christian Klein, Wolfgang Schaefer
  • Patent number: 8227478
    Abstract: Compounds of formula I modulate JNK: wherein X1 and X2 are each simultaneously N or CH; X3 is CH—R2 or N—SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: July 24, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Leyi Gong, Alam Jahangir, Deborah Carol Reuter
  • Patent number: 8227461
    Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: July 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • Patent number: 8222246
    Abstract: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: July 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Stephen Deems Gabriel, Steven Paul Hanlon, Roland Jakob-Roetne, Matthew C. Lucas, Paul Spurr, Andrew Thomas, Pius Waldmeier
  • Patent number: 8222230
    Abstract: The present invention provides novel formulations of isobutyric acid (2R,3R,4R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-4-fluoro-2-isobutyryloxymethyl-4-methyl-tetrahydro-furan-3-yl ester) and hydroxypropylcellulose that provide high bulk density, low particle size better suited for improved compression and flow, good compression, and fast dissolution profiles.
    Type: Grant
    Filed: January 18, 2010
    Date of Patent: July 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ashish Chatterji, Dipen Desai, Harpreet Sandhu, Navnit Hargovindas Shah
  • Patent number: RE43568
    Abstract: This invention relates to anti-P-selectin antibodies and, in particular, to anti-P-selectin antibodies and variants thereof that contain an Fc part derived from human origin and do not bind complement factor C1q. These antibodies have new and inventive properties causing a benefit for a patient suffering from critical limb ischemia or peripheral arterial occlusive disease (CLI/PAOD).
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: August 7, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Yvo Graus, Jacques Himber, Miranda Jansen-Molenaar, Dorothee Kling, Erhard Kopetzki, Paul Parren, Frank Rebers, Beat Steiner, Anne Stern, Pamela Strein, Kay-Gunnar Stubenrauch, Jan Van de Winkel, Martine Van Vugt