Patents Examined by James O. Wilson
  • Pharmacokinetically improved compounds
    Patent number: 8916576
    Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: December 23, 2014
    Assignee: Surface Logix, Inc.
    Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam, Hemalatha Seshadri
  • Pesticidal pyrimidine compounds
    Patent number: 8916578
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Process of making gyrase and topoisomerase inhibitors
    Patent number: 8912326
    Abstract: The present application is directed to compounds, intermediates and methods for preparing compounds of formula (I) or a pharmaceutically acceptable salts thereof, wherein R is H or F, and each of R3, R4, and R5 are as defined herein. The compounds of formula (I) and pharmaceutical compositions comprising said compounds and salts inhibit bacterial gyrase and/or Topo IV and are useful in treating bacterial infections.
    Type: Grant
    Filed: May 28, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Shannon, Tiansheng Wang, Simon Giroux
  • Allosteric protein kinase modulators
    Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • 2-aldoximino-5-fluoropyrimidine derivatives
    Patent number: 8912207
    Abstract: This present disclosure is related to the field of 2-aldoximino-5-fluoropyrimidines and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: December 16, 2014
    Assignee: Dow AgroSciences, LLP.
    Inventors: Timothy A. Boebel, Beth Lorsbach, Timothy P. Martin, W. John Owen, Michael T. Sullenberger, Chenglin Yao
  • Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
    Patent number: 8912200
    Abstract: The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: December 16, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Jay Aaron Bertrand, Paola Gnocchi, Ilaria Motto, Marcella Nesi, Achille Panzeri, Paola Vianello
  • Substituted pyridazine derivatives
    Patent number: 8912183
    Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: December 16, 2014
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
  • 6-(sulfonylaryl)pyrido[2,3-D]pyrimidin-7(8H)-ones for the treatment of CNS disorders
    Patent number: 8912203
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: December 16, 2014
    Assignee: Afraxis Holdings, Inc.
    Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
  • (heterocycle/tetrahydropyridine)-(piperazinyl)-1-alcanone and (heterocycle/dihydropyrrolidine)-(piperazinyl)-1-alcanone derivatives, and use thereof as p75 inhibitors
    Patent number: 8906924
    Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: December 9, 2014
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Aminopyrimidine kinase inhibitors
    Patent number: 8901145
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: December 2, 2014
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Stephane A. Dumas, Chee-Seng Lee, Yvonne L. Flanders
  • Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
    Patent number: 8901144
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: December 2, 2014
    Assignee: SciFluor Life Sciences, LLC
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Low hygroscopic aripiprazole drug substance and processes for the preparation
    Patent number: 8901130
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: December 2, 2014
    Assignee: Ostuka Pharmaceutical Co., Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • Bi-heteroaryl compounds as Vps34 inhibitors
    Patent number: 8901147
    Abstract: The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I: or a pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: December 2, 2014
    Assignee: Novartis AG
    Inventors: Ivan Cornella Taracido, Edmund Harrington, Ayako Honda, Erin Keaney
  • Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
    Patent number: 8901303
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: December 2, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • Process for the preparation of substantially pure methylthionium chloride pentahydrate form A
    Patent number: 8901296
    Abstract: Substantially pure methylthioninium chloride pentahydrate form A is prepared from methylthioninium chloride by phase equilibration of suspensions, crystallization or solvent evaporation, whereby the water content of the solvent corresponds to a water activity of at least 0.4 at 25° C., and controlled drying of said methylthioninium chloride pentahydrate form A within its stability ranges of humidity, pressure and temperature.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: December 2, 2014
    Assignee: WisTa Laboratories Ltd.
    Inventors: Rolf Hilfiker, Timo Rager
  • Aminoalkylpyrimidine derivatives as histamine H4 receptor antagonists
    Patent number: 8901146
    Abstract: Aminoalkylpyrimidine derivatives of formula I, wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: December 2, 2014
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Elena Carceller Gonzalez, Marina Virgili Bernado, Robert Soliva Soliva, Carles Ferrer Costa
  • Benzyloxypyrimidine derivative, agricultural/ horticultural insecticide comprising derivative and method for using same
    Patent number: 8895574
    Abstract: A benzyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; A is a oxygen atom and the like, and m is an integer of 0-5, or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: November 25, 2014
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Ryota Kasahara, Hiroto Harayama, Eikou Satoh, Motofumi Nakano, Kosuke Fukatsu, Kayo Inukai
  • 1 H-pyrrolo[2,3-b]pyridine derivatives
    Patent number: 8895575
    Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
  • Phenoxy-substituted pyrimidines as opioid receptor modulators
    Patent number: 8895573
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A Miskowski, Scott L. Dax, Henry J Breslin, Bart L. De Corte, Wei He
  • Compounds and method for treatment of cancer
    Patent number: 8895556
    Abstract: The invention relates to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 25, 2014
    Assignee: Critical Outcome Technologies Inc.
    Inventors: Wayne R. Danter, Cheuk Kun Lau