Patents Examined by Joseph K. McKane
  • Patent number: 8575197
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: November 5, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Kentaro Asahi, Hiroyuki Tobinaga
  • Patent number: 8551396
    Abstract: Provided herein are materials that can achieve up to 14% hydrogen absorption by weight in ambient conditions, which is a marked improvement over the hydrogen absorption values found in the prior art. Further provided are experimental conditions necessary to produce these materials. In order to produce the hydrogen storage material, a transition metal (or Lithium) is vaporized in a pi bond gas in conditions that permit only a few bonding collisions to occur between the vaporized transition metal atoms and pi bond gas molecules before the resulting bonded material is collected.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: October 8, 2013
    Assignee: University of Virginia Patent Foundation
    Inventors: Bellave S. Shivaram, Adam B. Phillips
  • Patent number: 8551992
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: October 8, 2013
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8546400
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: January 9, 2013
    Date of Patent: October 1, 2013
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8546374
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: Abbvie Inc.
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
  • Patent number: 8541625
    Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: September 24, 2013
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Vladimir V. Popik, Andrei A. Poloukhtine, Geert-Jan Boons, Margaretha Wolfert
  • Patent number: 8530689
    Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R1 and R2 are each, independently, C1-C12 alkyl, CO2R3, OR4, R5(OR6), or C6-C18 aryl; R3-R6 are each, independently, C1-C12 alkyl or C6-C12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R7-0H with BH3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R7 is a C2-C12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: September 10, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Virgil Percec, Brad Matthew Rosen, Daniela A. Wilson, Christopher J. Wilson
  • Patent number: 8524899
    Abstract: Methods and compositions are provided for forming complexes between dsDNA and novel oligomers comprising fused six-membered rings. By appropriate choice of target sequences and oligomers, complexes comprising oligomer-DNA are obtained with high association constants. The formation of complexes can be used for identification of specific dsDNA sequences, for inhibiting gene transcription, and as a therapeutic for inhibiting proliferation of undesired cells or modulation of expression of specific genes.
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: September 3, 2013
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Christoph A. Briehn, Dorte Renneberg, Philipp Weyermann, Raymond Doss, Michael Marques
  • Patent number: 8524897
    Abstract: The invention relates to 5-cyano-3-methyl-pyridine-2-carboxylic acid [3-((3R,6R)-5-amino-3,6-dimethyl-6-trifluoromethyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-amide in crystalline form, to its preparation, its medical use and to medicaments comprising said compound in crystalline form.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: September 3, 2013
    Assignee: Novartis AG
    Inventor: Rita Ramos
  • Patent number: 8524915
    Abstract: The invention relates to a process for the preparation of a compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III) reacting the halobenzyne of formula (III) so formed with (IV) wherein R1 and R2 are hydrogen or C1-C6alkyl; to (V), b) hydrogenating V in the presence of a metal catalyst to (VI), c) ozonising (VI) to (VII) d) converting (VII) in the presence of a phosphane and CCI4 or CHCI3 to (VIII) (VIII), and either e1) reacting VIII with NH3 in the presence of a catalyst to (IX) and f) reacting IX in the presence of a base with the compound of formula (X), to the compound of formula (I); or e2) reacting the compound of formula (VIII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with (Xa), to the compound of formula (I).
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: September 3, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Florian Schleth, Thomas Vettiger, Michael Rommel, Hans Tobler
  • Patent number: 8513291
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: August 20, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
  • Patent number: 8492556
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8487109
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Matthias Urmann, Nis Halland, Jorge Alonso
  • Patent number: 8487115
    Abstract: An ester compound represented by formula (1): wherein R3 represents hydrogen or methyl, R4 represents hydrogen or C1-C4 alkyl, and R5 represents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: July 16, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Noritada Matsuo
  • Patent number: 8476269
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
  • Patent number: 8471074
    Abstract: Process for manufacturing dichloropropanol according to which, a) in a liquid reaction medium containing water, which is in contact with a gaseous phase, glycerol is reacted with hydrogen chloride under a partial pressure of hydrogen chloride in the gaseous phase greater than 0.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: June 25, 2013
    Assignee: Solvay (Societe Anonyme)
    Inventors: Philippe Krafft, Patrick Gilbeau, Dominique Balthasart, Maurizio Paganin
  • Patent number: 8461348
    Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: June 11, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Matsunaga, Yoshihisa Nakada, Yusuke Ohba, Hideyuki Nakagawa
  • Patent number: 8461340
    Abstract: There are provided, according to the present invention, a method for producing a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative, the method characterized in that a trans-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative or a mixture of the trans- and cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivatives is isomerized in the presence of an aluminum compound represented by a formula Al(OR1)3 (wherein R1 represents a hydrocarbon group in which a carbon atom having an oxygen atom bonded thereto is a secondary carbon atom). In the process, a ketone compound may be further added, in addition to the aluminum compound.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: June 11, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Hiroshi Hakuta, Tsutomu Imagawa, Hirohito Oooka, Shinya Fukuhara
  • Patent number: 8455499
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: June 4, 2013
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
  • Patent number: 8445690
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: May 21, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao