Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
  • 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: 20140256747
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.
    Type: Application
    Filed: October 26, 2012
    Publication date: September 11, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
  • Publication number: 20140248378
    Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 4, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
  • Publication number: 20140235638
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 21, 2014
    Applicant: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140228368
    Abstract: The present invention is directed to pyrimidine compounds 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: August 20, 2012
    Publication date: August 14, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
  • Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Publication number: 20140206633
    Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.
    Type: Application
    Filed: February 3, 2011
    Publication date: July 24, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
  • Publication number: 20140187535
    Abstract: The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R1, R2, R3, Qa, W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Benzimidazole-Type Piperidine Compound.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.
    Inventors: Nobuyuki TANAKA, Kenji YAMAWAKI, Jiangchao YAO, Jianming YU, Xiaoming ZHOU
  • Publication number: 20140187543
    Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
    Type: Application
    Filed: September 25, 2013
    Publication date: July 3, 2014
    Inventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
  • Patent number: 8765757
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Publication number: 20140179670
    Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.
    Type: Application
    Filed: July 31, 2012
    Publication date: June 26, 2014
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
  • Publication number: 20140171431
    Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
    Type: Application
    Filed: May 15, 2012
    Publication date: June 19, 2014
    Inventors: Jianhua Shen, Yiping Wang, Kai Wang
  • Patent number: 8748603
    Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: June 10, 2014
    Assignee: AstraZeneca AB
    Inventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
  • Patent number: 8748443
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: June 10, 2014
    Assignee: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Patent number: 8741914
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: June 3, 2014
    Assignee: AbbVie Inc.
    Inventors: Todd W. Rockway, David A. Betebenner, David A. DeGoey, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Dachun Liu, Kenton L. Longenecker, John K. Pratt, Kent D. Stewart, Rolf Wagner, Clarence J. Maring
  • Publication number: 20140148400
    Abstract: Derivatized coumarin-based pharmaceutical compositions and methods to use them are provided. The compositions are characterized in that they inhibit the activity of tumor-related CAIX and CAXII to a greater degree than they inhibit the activity of CAI and CAII. The compositions can be used to suppress tumor growth and/or suppress tumor metastases in a mammal.
    Type: Application
    Filed: November 12, 2013
    Publication date: May 29, 2014
    Applicants: METASIGNAL THERAPEUTICS INC., CNRS-DIRE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES
    Inventors: Claudiu Supuran, Shoukat Dedhar, Fabrizio Carta, Jean-Yves Winum, Paul C. McDonald
  • Patent number: 8734777
    Abstract: Compounds having the formula (I) wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: May 27, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Jim Li, Francisco Xavier Talamas
  • Patent number: 8735413
    Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: May 27, 2014
    Assignee: AstraZeneca AB
    Inventors: Stephen Connolly, Mark Richard Ebden, Iain Alastair Stewart Walters, Thomas Langer, Alan Robert Steven, Craig Robert Stewart, Paula Margaret Tomlin, Andrew John Williams
  • Patent number: 8722883
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 13, 2014
    Assignee: AstraZeneca AB
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Cherylin Francis Preston, Jeffrey Paul Stonehouse, Neal Michael Smith
  • Publication number: 20140128374
    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: November 5, 2013
    Publication date: May 8, 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: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8686155
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Publication number: 20140038822
    Abstract: Use of substituted spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof for enhancement of stress tolerance in plants. The invention relates to the use of spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof of the formula (I) in which the respective substituents have the meanings given in the description, for increasing stress tolerance in plants with respect to abiotic stress, and also for increasing plant growth and/or for increasing plant yield.
    Type: Application
    Filed: December 27, 2011
    Publication date: February 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jens Frackenpohl, Lothar Willms, Thomas Müller, Stefan Lehr, Pascal Von Koskull-Döring, Ines Heinemann, Christopher Hugh Rosinger, Isolde Häuser-hahn, Martin Jeffrey Hills
  • Publication number: 20140038919
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: February 6, 2014
    Applicant: AbbVie Inc.
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
  • Patent number: 8637509
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: January 28, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
  • Publication number: 20140011799
    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: July 8, 2013
    Publication date: January 9, 2014
    Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
  • Publication number: 20140011798
    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: January 24, 2013
    Publication date: January 9, 2014
    Applicant: NOVARTIS AG
    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: 8609860
    Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: December 17, 2013
    Assignee: KTB Tumorforschungsgesellschaft mbH
    Inventors: André Warnecke, Ivonne Müller
  • Publication number: 20130324724
    Abstract: Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Nhut Diep, Yuriy B. Kalyan
  • Publication number: 20130324529
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Publication number: 20130316904
    Abstract: The invention relates to 3-(benzylsulfinyl)-5,5-dimethyl-4,5-dihydroisoxazole derivatives and 5,5-dimethyl-3-[(1H-pyrazol-4-ylmethyl)sulfinyl]-4,5-dihydroisoxazole derivatives of the formula (I) and their salts processes for their preparation and their use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventor: Bayer Cropscience AG
  • Publication number: 20130317024
    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: May 22, 2013
    Publication date: November 28, 2013
    Applicant: NOVARTIS AG
    Inventors: Simona Cotesta, Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8592582
    Abstract: The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a ?-diketone compound (3) to produce the pyrimidinylpyrazole compound: wherein R1 and R3 are each independently an alkyl group having 1 to 4 carbon atoms, and R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. The method is excellent in the environmental compatibility and economic efficiency.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: November 26, 2013
    Assignee: Shiseido Company, Ltd.
    Inventors: Hirotada Fukunishi, Naoto Hanyu, Masaru Suetsugu, Takuya Hiruma
  • Publication number: 20130310374
    Abstract: The present invention relates to substituted imidazo[4,5-c]quinoline derivatives of formula (I), wherein R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of the present invention and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammation and angiogenesis related disorders.
    Type: Application
    Filed: December 5, 2011
    Publication date: November 21, 2013
    Applicant: PIRAMAL ENTERPRISES LIMITED`
    Inventors: Sanjay Kumar, Rajiv Sharma, Vijaykumar Bhagwan Deore, Nilambari Nilkanth Yewalkar, Veena R. Agarwal, Nilesh Dagia, Nishigandha Naik
  • Publication number: 20130261301
    Abstract: The invention relates to fungicides and can be used for treating diseases caused by fungi, and also for preventing damage to various materials and agricultural products by fungi. The fungicide is a 2,4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidiene)amino-1,3-pyrimidine salt of general formula: (A) or a dimer thereof: (B), where X is selected from the series consisting of: Na+, K+, Li+ and NH4+. An effective preparation having anti-fungal activity with a broad spectrum of action is created.
    Type: Application
    Filed: March 3, 2011
    Publication date: October 3, 2013
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
  • Publication number: 20130252963
    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, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • 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: 20130252984
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 26, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
  • Publication number: 20130245010
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Patent number: 8530490
    Abstract: Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug. A uracil compound represented by the general formula (I) or a salt thereof: wherein n represents an integer of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, or the like; Y represents a linear or branched alkylene group having 1 to 8 carbon atoms, or the like; and Z represents —SO2NR1R2 or —NR3SO2—R4, wherein R1 and R2 each represent an alkyl group having 1 to 6 carbon atoms, an aralkyl group which is optionally substituted, or the like; R3 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R4 represents an aromatic hydrocarbon group, an unsaturated heterocyclic group, or the like.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: September 10, 2013
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Publication number: 20130225524
    Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, and R5 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: November 3, 2011
    Publication date: August 29, 2013
    Inventors: Deping Chai, Mariela Colon, Christopher Dodson, Kevin J. Duffy, Antony Nicholas Shaw
  • Patent number: 8519128
    Abstract: The present invention is a compound having the general formula (I), (II), or (III) or a pharmacologically acceptable salt, solvate, or hydrate thereof, and a pharmaceutical composition containing such a compound, or its pharmacologically acceptable ester, or other pharmacologically acceptable derivative thereof as an active ingredient. The compound has an excellent ACAT 2-inhibiting activity by a mechanism different from that of a statin drug and is useful as a therapeutic or prophylactic agent for obesity, adiposis, hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, and arteriosclerosis, as well as obesity-derived hyperlipidemia, hypercholesterolemia, disorder of lipid metabolism, arteriosclerosis, and hypertension.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: August 27, 2013
    Assignee: The Kitasato Institute
    Inventors: Hiroshi Tomoda, Tohru Nagamitsu, Satoshi Omura
  • Publication number: 20130209397
    Abstract: Compounds having the formula (I) wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: August 10, 2011
    Publication date: August 15, 2013
    Applicant: Roche Palo Alto LLC
    Inventors: Jim Li, Francisco Xavier Talamas
  • Patent number: 8501238
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: August 6, 2013
    Assignee: AbbVie Inc.
    Inventors: Charles A. Flentge, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G. Z. Zhang
  • Patent number: 8501750
    Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • Publication number: 20130190338
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130165460
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130158056
    Abstract: The present invention is directed to 2-alkoxy pyrimidine compounds 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: September 26, 2011
    Publication date: June 20, 2013
    Inventors: Christopher D. Cox, Izzat T. Raheem, William D. Shipe, Cory R. Theberge
  • Publication number: 20130150578
    Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 1, 2011
    Publication date: June 13, 2013
    Applicant: CADILA PHARMACEUTICALS LIMITED
    Inventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
  • Publication number: 20130143907
    Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.
    Type: Application
    Filed: October 4, 2012
    Publication date: June 6, 2013
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventor: Eisai R&D Management Co., Ltd.