Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
  • Publication number: 20140371230
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 18, 2014
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • 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
  • Publication number: 20140364446
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 1?,4?-thio nucleoside compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula 3001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof; wherein Base, RA, RB, W, X, Y, and Z are as described herein.
    Type: Application
    Filed: June 4, 2014
    Publication date: December 11, 2014
    Inventors: David DUKHAN, Gilles GOSSELIN, Cyril B. DOUSSON
  • Publication number: 20140364387
    Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.
    Type: Application
    Filed: June 30, 2014
    Publication date: December 11, 2014
    Inventors: William A. GODDARD, III, Mark MENNA, Stephan PANDOL, Ravinder ABROL
  • Patent number: 8906933
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: December 9, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20140357633
    Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 4, 2014
    Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
  • Publication number: 20140357612
    Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: May 29, 2014
    Publication date: December 4, 2014
    Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
  • Patent number: 8901301
    Abstract: Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-3-fluoro-benzenesulfonamide, pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: December 2, 2014
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Hongyao Zhu
  • 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
  • Patent number: 8900638
    Abstract: The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part: a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: December 2, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazumichi Yamamoto, Hiroyoshi Koyama
  • Publication number: 20140349971
    Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventor: Paul STOFFELS
  • Publication number: 20140350026
    Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.
    Type: Application
    Filed: November 9, 2012
    Publication date: November 27, 2014
    Inventors: Xianjin Luo, Weidong Ye
  • Publication number: 20140350036
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 27, 2014
    Inventors: Robert Vince, Abbas Raza, Christine Dreis
  • Publication number: 20140348958
    Abstract: A compound of formula (I), a positional or structural isomer thereof, or a pharmaceutically acceptable base addition salt or acid addition salt thereof, use thereof as a medicament, in particular an anticancer medicament.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 27, 2014
    Inventors: Pierre Chalard, Florence Caldefie-Chezet, Laetitia Delort, Kirti Patel
  • Publication number: 20140350015
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 27, 2014
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Publication number: 20140349990
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 20, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
  • 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
  • Publication number: 20140343062
    Abstract: The invention includes methods, compositions, and kits useful for treating a viral infection by coadministering 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with lopinavir or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 19, 2014
    Publication date: November 20, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Brian P. KEARNEY, Anita A. MATHIAS
  • Publication number: 20140343006
    Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20140343056
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 20, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
  • Publication number: 20140343033
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Applicant: Takeda Califomia, Inc.
    Inventors: Edcon Chang, Michael B. Wallace
  • Publication number: 20140343084
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: July 10, 2014
    Publication date: November 20, 2014
    Inventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
  • Patent number: 8889701
    Abstract: The instant invention relates to a novel compound representing a substituted phosphoramidic acid—a (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 1 or a (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 2, or a pharmaceutically acceptable salt, a hydrate, a crystalline form or a stereoisomer thereof, as defined in the specification. The novel compound is used for a pharmaceutical composition with at least one pharmaceutically acceptable excipient as well as with an inosine 5 monophosphate dehydrogenase inhibitor, HCV protease NS3 inhibitor, HCV protease NS3/4A inhibitor, and RNA polymerase NS5A inhibitor. The novel compound is useful as a viral polymerase HCV NS5B inhibitor and can be used for treating a disease caused by hepatitis C virus (HCV).
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: November 18, 2014
    Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Oleg Dmitrievich Mitkin
  • Patent number: 8889700
    Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: November 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
  • Patent number: 8889699
    Abstract: The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: November 18, 2014
    Assignee: Delta-Fly Pharma, Inc.
    Inventors: Masakazu Fukushima, Shozo Yamada, Ryo Oyama
  • Publication number: 20140336209
    Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.
    Type: Application
    Filed: July 22, 2014
    Publication date: November 13, 2014
    Inventors: Naohiro TAKEMOTO, Kenji MURATA, Norihito MURAYAMA, Chikaomi YAMADA
  • Publication number: 20140336143
    Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
    Type: Application
    Filed: December 4, 2013
    Publication date: November 13, 2014
    Applicants: GILEAD PHARMASSET LLC, BETH ISRAEL DEACONESS MEDICAL CENTER, EMORY UNIVERSITY
    Inventors: Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
  • Publication number: 20140336172
    Abstract: The present invention relates to novel 2H-indazoles of the general formula (I), methods for the preparation thereof and the use thereof for the production of pharmaceutical agents for the treatment of diseases and indications which are linked with the EP2-receptor.
    Type: Application
    Filed: November 26, 2012
    Publication date: November 13, 2014
    Inventors: Nico Bräuer, Anne Mengel, Ulrike Röhn, Andrea Rotgeri, Bernd Buchmann, Bernhard Lindenthal, Antonius Ter Laak
  • Publication number: 20140336167
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 13, 2014
    Applicant: ABBVIE INC.
    Inventors: Ramzi F. Sweis, Michael L. Curtin, Marina A. Pliushchev, Todd M. Hansen, Kenton Longenecker
  • Publication number: 20140336210
    Abstract: This invention relates to aryl urea compounds in combination with cytotoxic or cytostatic agents for use in treating raf kinase mediated diseases such as cancer.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Applicant: Bayer HealthCare LLC
    Inventors: CARTER A. Christopher, GIBSON Neil, HIBNER Barbara, HUMPHREY W. Rachel, TRAIL Pamela, VINCENT W. Patrick, ZHAI Yifan
  • Publication number: 20140336195
    Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 13, 2014
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Publication number: 20140336176
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: PFIZER INC.
    Inventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
  • Publication number: 20140336194
    Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Applicant: NOVARTIS AG
    Inventor: Shi Yin FOO
  • Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Patent number: 8883759
    Abstract: There is provided an agent for potentiating the effects of an anti-tumor agent. An anti-tumor effect potentiator containing, as an active ingredient, a uracil compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents a C1-5 alkylene group and one of methylene groups constituting the alkylene group is optionally substituted with an oxygen atom; R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a hydrogen atom or a halogen atom; and R3 represents a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl) C1-6 alkyl group, a halogeno-C1-6 alkyl group or a saturated heterocyclic group.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: November 11, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Publication number: 20140329799
    Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 6, 2014
    Inventors: W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. Mcelroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Criag R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
  • Publication number: 20140329816
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Application
    Filed: July 26, 2012
    Publication date: November 6, 2014
    Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
  • Publication number: 20140328891
    Abstract: Medical implants are provided which release a fluoropyrimidine or an analog thereof, thereby inhibiting or reducing the incidence of infection associated with the implant.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: William L. Hunter, David M. Gravett, Philip M. Toleikis, Richard T. Liggins, Troy A.E. Loss
  • Publication number: 20140328823
    Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, skin cancer.
    Type: Application
    Filed: July 15, 2014
    Publication date: November 6, 2014
    Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Patent number: 8877749
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: November 4, 2014
    Assignee: Bristol-Myers Squibbs Company
    Inventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
  • Publication number: 20140323508
    Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 30, 2014
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Publication number: 20140323507
    Abstract: In some embodiments, the present invention provides methods of treating a tumor in a subject. In some embodiments, the methods may include a step of administering to the subject a therapeutic composition that comprises: (a) mycophenolic acid, an analogue thereof, or a derivative thereof; and (b) at least one anti-neoplastic agent. In some embodiments, the antineoplastic agent may include at least one of 5-fluouracil (5-FU), paclitaxel, oxaliplatin, doxorubicin, etoposide, irinotecan, bleomycin, imiquimod, 13-cis-retinoic acid, and combinations thereof. In some embodiments, the relative concentrations of the mycophenolic acid, the analogue thereof, or the derivative thereof, and the at least one anti-neoplastic agent correspond to their respective IC50 values.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 30, 2014
    Applicant: Texas A & M University System
    Inventors: Robert Y. Tsai, Tao Lin
  • Patent number: 8871775
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: October 28, 2014
    Assignee: Glaxo Group Limited
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Publication number: 20140315935
    Abstract: The invention provides for molecular classification of disease and, particularly, molecular markers for lung cancer prognosis and therapy selection and methods and systems of use thereof.
    Type: Application
    Filed: February 21, 2014
    Publication date: October 23, 2014
    Inventors: Susanne Wagner, Steven Stone, Alexander Gutin, Julia Reid
  • Publication number: 20140315936
    Abstract: The present invention provides a method of treating HIV-1 infection in a subject. The method comprises administering to the subject a combination of anti-HIV-1 agents wherein the combination comprises an effective dose of Apricitabine and an effective dose of Atazanavir.
    Type: Application
    Filed: November 15, 2012
    Publication date: October 23, 2014
    Inventors: Jonathan Alan Victor Coates, Susan Wendy Cox
  • Publication number: 20140315927
    Abstract: The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: Andrew Simon Bell, lain Brian GARDNER, Karl Richard GIBSON, David Cameron PRYDE, Florian Michel WAKENHUT
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Publication number: 20140308336
    Abstract: Drug-eluting devices and methods for the treatment of tumors of the pancreas, biliary system, gallbladder, liver, small bowel, or colon, are provided. Methods include deploying a drug-eluting device having a film which includes a mixture of a degradable polymer and a chemotherapeutic drug, wherein the film has a thickness from about 2 ?m to about 1000 ?m, into a tissue site and releasing a therapeutically effective amount of the chemotherapeutic drug from the film to treat the tumor, wherein the release of the therapeutically effective amount of the drug from the film is controlled by in vivo degradation of the polymer at the tissue site.
    Type: Application
    Filed: April 10, 2014
    Publication date: October 16, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Laura Indolfi, Elazer R. Edelman, Robert S. Langer, Jeffrey W. Clark, David T. Ting, Cristina Rosa Annamaria Ferrone, Matteo Ligorio
  • Publication number: 20140309234
    Abstract: The present invention provides methods for treating fibrotic diseases by administering a compound having the general structural formula (I)
    Type: Application
    Filed: March 10, 2014
    Publication date: October 16, 2014
    Applicant: ANGION BIOMEDICA CORP
    Inventors: Lambertus J.W.M Oehlen, Bijoy Panicker, Latha Paka
  • Publication number: 20140309226
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X1, X2, R3, R4, R5, Rx, R7, R9, R10 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 16, 2014
    Inventors: Jay Bradford Fell, John P. Fischer, Ronald J. Hinklin