Patents Examined by John Mabry
  • Patent number: 8592595
    Abstract: The present invention relates to a process for the preparation of optionally substituted (N-heterocyclyl) aryl ethers.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: November 26, 2013
    Assignee: Saltigo GmbH
    Inventor: Michael Kreis
  • Patent number: 8586749
    Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: November 19, 2013
    Assignees: University of Central Florida Research Foundation, Inc., Governing Council of the University of Toronto
    Inventors: James Turkson, Patrick Gunning
  • Patent number: 8575347
    Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: November 5, 2013
    Assignee: Glaxo Group Limited
    Inventors: Dramane Ibrahim Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Patent number: 8575345
    Abstract: A composition of matter suitable for the generation of hydrogen from water is described, the positively charged cation of the composition including the moiety of the general formula. [(PY5Me2)CoL]2+, where L can be H2O, OH?, a halide, alcohol, ether, amine, and the like. In embodiments of the invention, water, such as tap water or sea water can be subject to low electric potentials, with the result being, among other things, the generation of hydrogen.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 5, 2013
    Assignee: The Regents of the University of California
    Inventors: Jeffrey R. Long, Christopher J. Chang, Yujie Sun
  • Patent number: 8575353
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating a human for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: November 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 8569509
    Abstract: The use of thiazole-4-carboxylic esters and thioesters of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, Y1, Y2, Y3, W, X and G have the meanings given in the description, and also of agrochemically active salts thereof, as fungicides.
    Type: Grant
    Filed: April 18, 2009
    Date of Patent: October 29, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Pierre Cristau, Stefan Herrmann, Nicola Rahn, Arnd Voerste, Ulrike Wachendorff-Neumann, Tomoki Tsuchiya
  • Patent number: 8569507
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: October 29, 2013
    Assignee: Institut Univ. De Ciencia I Technologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8569521
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Anne Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao
  • Patent number: 8563732
    Abstract: The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ?O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: October 22, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Hidenori Mikamiyama, Naoki Tsuno
  • Patent number: 8563607
    Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: October 22, 2013
    Assignees: University of South Florida, McGill University, The Hong Kong Polytechnic University
    Inventors: Q. Ping Dou, Tak-Hang Chan, David M. Smith
  • Patent number: 8558001
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: October 15, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 8552030
    Abstract: The invention disclosed in this application relates to an improved process for the manufacture of d-threo-ritalinic acid hydrochloride and l-threo-ritalinic acid hydrochloride in an optically pure form by the resolution of dl-threo-ritalinic acid using a chiral carboxylic acid The d-threo-ritalinic acid hydrochloride prepared by the process of the present invention on esterification gives d-threo-methylphenidate, a very well known CNS stimulant.
    Type: Grant
    Filed: July 3, 2009
    Date of Patent: October 8, 2013
    Assignee: Malladi Drugs & Pharmaceuticals Ltd.
    Inventors: Tangirala Prakasam, Borkatte Narasimha Hitesh Kumar, Sangu Perumal, Kothandapani Loganathan
  • Patent number: 8546415
    Abstract: N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: October 1, 2013
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter A. Crooks, Linda P. Dwoskin, Joshua Ayers, Vladimir Grinevich, Sangeetha Sumithran
  • Patent number: 8546575
    Abstract: The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: October 1, 2013
    Assignee: Merck Patent GmbH
    Inventors: Caroline Leriche, Denis Carniato, Didier Roche, Christine Charon, Liliane Doare
  • Patent number: 8541585
    Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: September 24, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
  • Patent number: 8536342
    Abstract: Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: September 17, 2013
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kunihiko Higashiura, Taizo Ito, Takashi Ogino, Taisuke Hasegawa
  • Patent number: 8519134
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: August 27, 2013
    Assignee: Novartis AG
    Inventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
  • Patent number: 8519135
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Grant
    Filed: January 13, 2009
    Date of Patent: August 27, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Wei Chen, Antoni Krasinski
  • Patent number: 8513423
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: August 20, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Peter J. Connolly, Haiyan Bian, Xun Li, Li Liu, Mark J. Macielag, Mark E. McDonnell
  • Patent number: 8501783
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: August 6, 2013
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Paul D. Jones, Christophe Morisseau, Huazhang Huang, Hsing-Ju Tsai, Richard Gless, Jr.