Patents Examined by Kahsay T. Habte
  • Patent number: 8486934
    Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: July 16, 2013
    Assignee: Bayer CropScience AG
    Inventors: Bernd-Wieland Krüger, Achim Hense, Bernd Alig, Rüdiger Fischer, Christian Funke, Ernst Rudolf Gesing, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold, Peter Lümmen, Erich Sanwald
  • Patent number: 8481724
    Abstract: Disclosed herein are methods for synthesizing 2,4-pyrimidinediamines as well as intermediates used therein.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: July 9, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ulfried Felfer, Karl-Heinz Giselbrecht, Michael Wolberg
  • Patent number: 8481564
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: July 9, 2013
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Patent number: 8481723
    Abstract: The present invention relates to uracils of formula I wherein the variables are defined according to the description, processes and intermediates for preparing the uracils of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one uracil of the formula I to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: July 9, 2013
    Assignee: BASF SE
    Inventors: Anja Simon, Liliana Parra Rapado, Richard Roger Evans, Matthias Witschel, Trevor William Newton, Thomas Seitz, Helmut Walter
  • Patent number: 8476263
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: July 2, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Patent number: 8476264
    Abstract: The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: July 2, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Emmanuel Pinard, Thomas Woltering
  • Patent number: 8476265
    Abstract: Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH— represents a ?-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: July 2, 2013
    Assignees: AstraZeneca AB, Pulmagen Therapeutics (Synergy) Limited
    Inventors: Lilian Alcaraz, Andrew Bailey, Nicholas Kindon
  • Patent number: 8476428
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: July 2, 2013
    Assignee: International Business Machines Corporation
    Inventors: James Lupton Hedrick, Alshakim Nelson, Daniel Paul Sanders
  • Patent number: 8476266
    Abstract: A compound represented by formula (I), wherein R1 represents a hydrogen atom, etc., R2 and R3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R2 and R3 taken together represent optionally oxidized C2-5 alkylene group, R4 represents an optionally oxidized C1-6 alkyl group, etc., R5 represents an optionally oxidized C1-6 alkyl group, etc., R6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: July 2, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Atsushi Naganawa, Toshihiko Nagase
  • Patent number: 8476427
    Abstract: Provided herein are processes for the production of methionine or selenomethionine from homoserine. In particular, the processes proceed via the production of carbamate intermediates.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: July 2, 2013
    Assignee: Novus International, Inc.
    Inventors: Stephen J. Lorbert, Kevin A. Trankler, Richard Vonder Embse, Dayna L. Turner, Tracy Rode, James C. Peterson
  • Patent number: 8476461
    Abstract: Dipyrromethene-boron hydrophilic fluorescent compounds The invention concerns fluorescent and hydrophilic compounds meeting following formula (I): wherein: S1 is a group of formula —C?C-L?-A where L? is a linkage group and A is a polar functional group; S2 is a —C?C-L?-A group the same or different from S1; —F; —H; or a hydrocarbon chain optionally interrupted by one or more oxygen atoms, and use thereof, in particular in aqueous or hydrophilic media.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: July 2, 2013
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Gilles Ulrich, Raymond Ziessel, Song-Lin Niu, Alexandre Haefele, Thomas Bura
  • Patent number: 8471004
    Abstract: The invention is concerned with novel bicyclic compounds of formula (I), wherein A, L, E, F, G, R1, R2, R3, R4, R5, R6, R7, V, W and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: June 25, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei
  • Patent number: 8470825
    Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: June 25, 2013
    Assignee: Eisai Inc.
    Inventors: Weizheng Xu, Greg Delahanty, Jie Zhang
  • Patent number: 8466279
    Abstract: The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: June 18, 2013
    Assignee: Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
  • Patent number: 8461154
    Abstract: The present invention provides arylpiperazine derivatives having Formula I which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: June 11, 2013
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Patent number: 8455483
    Abstract: Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH— represents a ?-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: June 4, 2013
    Assignees: AstraZeneca AB, Pulmagen Therapeutics (Synergy) Limited
    Inventors: Lilian Alcaraz, Andrew Bailey, Nicholas Kindon
  • Patent number: 8450313
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, 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: Grant
    Filed: May 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Patent number: 8445484
    Abstract: The present invention refers to 3-aza-bicyclo [3.2.1] octane derivatives of general formula (I) their preparation, use and pharmaceutical compositions useful in the treatment of pathologies associated with microbial pathogens expressing aspartylprotease activity.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: May 21, 2013
    Assignees: Istituto Superiore di Sanita', Universita' Degli Studi di Firenze
    Inventors: Antonio Cassone, Flavia De Bernardis, Enrico Garaci, Andrea Trabocchi, Antonio Guarna
  • Patent number: 8445407
    Abstract: The present invention relates to tetrahydrophthalimides of formula I wherein the variables are defined according to the description, processes and intermediates for preparing the benzoxazinones of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one tetrahydrophthalimide of the formula I to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: May 21, 2013
    Assignee: BASF SE
    Inventors: Matthias Witschel, Trevor William Newton, Thomas Seitz, Helmut Walter, Bernd Sievernich, Anja Simon, Ricarda Niggeweg, Klaus Grossmann
  • Patent number: 8445483
    Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: May 21, 2013
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, John S. Gunn, Larry S. Schlesinger