Plural Chalcogens Bonded Directly To Ring Carbons Of The Six-membered Hetero Ring Patents (Class 546/296)
  • Patent number: 10252997
    Abstract: The present invention relates to a compound which may be useful as an agent for the prophylaxis or treatment of cancer, hepatitis, hepatic fibrosis, fatty liver and the like.
    Type: Grant
    Filed: March 30, 2016
    Date of Patent: April 9, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Ryo Mizojiri, Moriteru Asano, Daisuke Tomita, Hiroshi Banno, Michiko Tawada, Noriyuki Nii, Krista E. Gipson, Hironobu Maezaki, Shuntarou Tsuchiya, Mayumi Imai, Yuichiro Amano
  • Patent number: 10172358
    Abstract: The present disclosure relates to thiopicolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: January 8, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Kyle A. DeKorver, Kevin G. Meyer, Chenglin Yao, Karla Bravo-Altamirano, Ronald J. Heemstra, Brannon Sam, David M. Jones
  • Patent number: 10071965
    Abstract: The present invention provides novel 2-pyridone compounds and 4-pyridone compounds and methods of treating a subject infected with a pathogen of Staphylococcus aureus, Mycobacterium tuberculosis, Francisella tularensis, Burkholderia pseudomallei, Yersinia pestis, Escherichia coli and Proteus mirabilisone.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: September 11, 2018
    Assignee: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK
    Inventors: Peter Tonge, Pan Pan
  • Patent number: 10059720
    Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.
    Type: Grant
    Filed: May 28, 2015
    Date of Patent: August 28, 2018
    Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICALS CO., LTD.
    Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Yusuke Inagaki, Kazuyuki Tsuchiya, Tadaatsu Hanadate, Akira Kanai, Hiroyuki Kaizawa, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
  • Patent number: 10059672
    Abstract: The invention provides (1) processes for making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; (2) compositions useful in making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: August 28, 2018
    Assignee: YALE UNIVERSITY
    Inventors: Seth Herzon, Maung Kyaw Moe Tun
  • Patent number: 9260453
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: February 16, 2016
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Publication number: 20150148545
    Abstract: Disclosed in the present invention is a protein tyrosine phosphatase inhibitor. The preparation method therefor is: extracting the crude product from the Isaria Fumosorosea Wize solid or liquid fermentation broth using ethyl acetate, ethanol, methanol, or a mixed solvent of chloroform and methanol; separating the obtained extract using column chromatography on silica gel; and obtaining the target product. The inhibitor can be used to prepare pharmaceutical compositions for treating and preventing diabetes, obesity and cancers.
    Type: Application
    Filed: May 7, 2013
    Publication date: May 28, 2015
    Inventors: Duqiang Luo, Jun Zhang, Zhiqin Liu
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Patent number: 9012471
    Abstract: The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: April 21, 2015
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Paul Harris, Antonella Maffei, Yuli Xie, Donald Landry
  • Publication number: 20150080362
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 19, 2015
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Tamil Arasu, John David Baird, Wu Du, Olya Ginzburg, Yi Jin Kim Gorske, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Anthony Allan Turpoff, Richard Gerald Wilde, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150031876
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Application
    Filed: September 5, 2014
    Publication date: January 29, 2015
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Patent number: 8933079
    Abstract: Pyridone and pyridazinone derivatives that are active against the melanin-concentrating hormone (MCH) and useful as anti-obesity pharmaceuticals.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: January 13, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Oost, Ralf Lotz, Dirk Stenkamp
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Patent number: 8900797
    Abstract: The present invention provides a cross-linking agent capable of preventing formation of scum from a bottom anti-reflective coating, and also provides a composition for forming a bottom anti-reflection coating containing the agent. The cross-linking agent is a nitrogen-containing aromatic compound having at least one vinyloxy group or N-methoxymethylamide group, and the composition contains the cross-linking agent. The cross-linking agent of the formula (1) can be produced by reaction of a nitrogen-containing aromatic compound, a halogen compound having a vinyloxy group or N-methoxymethylamide group and a basic compound.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: December 2, 2014
    Assignee: AZ Electronic Materials (Luxembourg) S.A.R.L.
    Inventors: Shigemasa Nakasugi, Shinji Miyazaki, Munirathna Padmanaban, Alberto D. Dioses
  • Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Patent number: 8865908
    Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Patent number: 8865907
    Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: October 21, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yukihito Sumino, Kazuya Okamoto, Moriyasu Masui, Toshiyuki Akiyama
  • Patent number: 8859573
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: October 14, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Publication number: 20140303232
    Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Jeremy Lee BARYZA, Rohan Eric John BECKWITH, Keith BOWMAN, Crystal BYERS, Tanzina FAZAL, Gabriel Grant GAMBER, Cameron Chuck-munn LEE, Ritesh Bhanudasji TICHKULE, Chandra VARGEESE, Shuangxi WANG, Laura Ellen West, Thomas ZABAWA, Junping ZHAO
  • Publication number: 20140288017
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 8835461
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 16, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Publication number: 20140243353
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or fluorine, one of A and B is R2, the other is a group —X—Y—R3. R3 represents a carbocyclic or heterocyclic ring. Further variables are as defined in the specification. Also claimed are—processes for their preparation, pharmaceutical compositions containing them and their use in therapy of diseases such as schizophrenia, cognitive disorders and pain by modulating the D-amino acid oxidase enzyme (DAAO).
    Type: Application
    Filed: July 5, 2012
    Publication date: August 28, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: William Farnaby, Charlotte Fieldhouse, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller, Katherine Hazel
  • Publication number: 20140235673
    Abstract: The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Inventors: Zulan Pi, John Llyod, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
  • Patent number: 8809373
    Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: August 19, 2014
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
  • Publication number: 20140228310
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 14, 2014
    Applicant: InterMune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Publication number: 20140206880
    Abstract: A process for the preparation of 4-methyl-oxazole-5-carboxamide, an intermediate in the synthesis of pyridoxine, by reacting lower alkyl 4-methyl-oxazole-5-carboxy-late with a molar excess of anhydrous, liquid ammonia.
    Type: Application
    Filed: May 31, 2012
    Publication date: July 24, 2014
    Applicant: DSM IP ASSETS B.V.
    Inventors: Werner Bonrath, Jocelyn Fischesser, Hongyan Shen
  • Publication number: 20140200205
    Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
    Type: Application
    Filed: September 17, 2012
    Publication date: July 17, 2014
    Inventors: Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
  • Publication number: 20140186873
    Abstract: Disclosed herein are isotopically labeled antifungal antibiotics and related compounds. Also disclosed are methods for synthesizing these isotopically labeled molecules and using the same to study the distribution of these compounds in the biosphere as well as the products formed by the breakdown of these isotopically labeled compounds.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Inventors: Ronald Ross, Jr., Peter Lee Johnson, Kevin G. Meyer
  • Patent number: 8748582
    Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilize the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: June 10, 2014
    Assignee: Monash University
    Inventors: Milton T W Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
  • Patent number: 8741806
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: June 3, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, James Nicholas Scutt
  • Patent number: 8716318
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: May 6, 2014
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Publication number: 20140088308
    Abstract: Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials, dental bonding agents or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such dental restorative materials may help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.
    Type: Application
    Filed: November 12, 2013
    Publication date: March 27, 2014
    Applicant: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Xiaoming Xu, Shailaja Jayaramachandran
  • Publication number: 20140087311
    Abstract: The present invention provides a cross-linking agent capable of preventing formation of scum from a bottom anti-reflective coating, and also provides a composition for forming a bottom anti-reflection coating containing the agent. The cross-linking agent is a nitrogen-containing aromatic compound having at least one vinyloxy group or N-methoxymethylamide group, and the composition contains the cross-linking agent. The cross-linking agent of the formula (1) can be produced by reaction of a nitrogen-containing aromatic compound, a halogen compound having a vinyloxy group or N-methoxymethylamide group and a basic compound.
    Type: Application
    Filed: September 26, 2012
    Publication date: March 27, 2014
    Applicant: AZ ELECTRONIC MATERIALS (LUXEMBOURG) S.A.R.L.
    Inventors: Shigemasa NAKASUGI, Shinji MIYAZAKI, Munirathna PADMANABAN, Alberto D. DIOSES
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Patent number: 8673943
    Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: March 18, 2014
    Assignee: Apotex Technologies Inc.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao
  • Patent number: 8673919
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: March 18, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Michel Vernier, Hong Woo Kim, Marion Hitchcock, Shunqi Yan
  • Patent number: 8669362
    Abstract: Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1 P3, R3 and Rx are as described herein.
    Type: Grant
    Filed: September 5, 2013
    Date of Patent: March 11, 2014
    Assignees: Shiongi & Co., Ltd., VIIV Healthcare Company
    Inventors: Brian Johns, Maosheng Duan, Toshikazu Hakogi
  • Publication number: 20140031395
    Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.
    Type: Application
    Filed: February 2, 2012
    Publication date: January 30, 2014
    Applicant: Bionomics Limited
    Inventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
  • Publication number: 20140031370
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20140031555
    Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
    Type: Application
    Filed: October 2, 2013
    Publication date: January 30, 2014
    Applicants: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian Alvin JOHNS, Jason Gordon WEATHERHEAD, Toshikazu HAKOGI, Yasunori AOYAMA
  • Patent number: 8637672
    Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: January 28, 2014
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • Publication number: 20140005405
    Abstract: Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1 P3, R3 and Rx are as described herein.
    Type: Application
    Filed: September 5, 2013
    Publication date: January 2, 2014
    Applicants: VIIV Healthcare Company, Sionogi & Co., Ltd.
    Inventors: Brian JOHNS, Maosheng DUAN, Toshikazu HAKOGI
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Publication number: 20130310346
    Abstract: The present invention provides methods and compositions for treating or preventing bacterial infections, where a pharmaceutically acceptable iron chelator that reduces biological availability of iron for one or more strains of bacteria, such as VK28 or an analog or derivative thereof is administered to a patient in need of treatment. The method also provides methods and compositions where an iron chelator and an antibiotic are administered to a patient in need of treatment for a bacterial infection.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: Government of the United States, as represented by the Secretary of the Army
    Inventor: Daniel Zurawski
  • Publication number: 20130267546
    Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 10, 2013
    Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of Ari
    Inventors: Sidney HECHT, Omar KHDOUR, Jun LU, Pablo ARCE
  • Patent number: 8552187
    Abstract: Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1 P3, R3 and Rx are as described herein.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: October 8, 2013
    Assignees: Shionogi & Co., Ltd., VIIV Healthcare Company
    Inventors: Brian Alvin Johns, Maosheng Duan, Toshikazu Hakogi
  • Publication number: 20130252986
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Publication number: 20130237515
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.
    Type: Application
    Filed: February 28, 2013
    Publication date: September 12, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
  • Patent number: 8524747
    Abstract: The object of the present invention is to provide a pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B. The pharmaceutical composition that inhibits expression of iNOS and COX-2 without inhibiting NF-?B contains DTCM glutarimide of the Formula (I) as an effective ingredient, thereby being able to inhibit nitric oxide (NO) production and prostaglandin production.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: September 3, 2013
    Assignee: Keio University
    Inventors: Kazuo Umezawa, Yuichi Ishikawa, Shigeru Nishiyama, Miyuki Tachibana, Ayumi Kaneda
  • Patent number: 8524729
    Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: September 3, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshitaka Tomigahara, Kiyoshi Higashi, Junya Takahashi