1,3-diazines Patents (Class 544/242)
  • Patent number: 10202357
    Abstract: The invention is directed to new class of quinolone heterocyclic aromatic molecules (Renotinibs) and their use in the treatment of cancer, in particular, cancer that harbor abnormal human epidermal growth factor receptors (EGFRs).
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: February 12, 2019
    Assignee: RenoTarget Therapeutics, Inc.
    Inventors: Jujun Wang, Allen Tsao, Xiaomei Liu
  • Patent number: 10010551
    Abstract: The invention relates to spiro deriviatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: July 3, 2018
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Patent number: 9951039
    Abstract: Filamenting temperature-sensitive mutant Z (FtsZ) protein plays a crucial role in the bacterial cell division machinery and is a validated drug target for antibacterial agents. The present invention relates to FtsZ-interacting compounds that possess a 2,4,6-trisubstituted pyrimidine scaffold. Some of these compounds possess potent anti-staphylococcal properties and potent antibacterial activities against clinically isolated MRSA strains. Compounds have been identified to exhibit low spontaneous frequency of resistance, low toxicity as well as the ability to rescue G. mellonella larvae infected with lethal dose of the MRSA ATCC 43300 strain. Characterization by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purified S. aureus FtsZ protein verified the interaction of 2,4,6-trisubstituted pyrimidine with the FtsZ protein, further confirmed by observations of iconic filamentous cell phenotype and mislocalization of the Z-ring formation.
    Type: Grant
    Filed: September 29, 2016
    Date of Patent: April 24, 2018
    Assignees: THE HONG KONG POLYTECHNIC UNIVERSITY, THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY
    Inventors: Kwok-yin Wong, Tak-Hang Chan, Kin-Fai Chan
  • Patent number: 9923148
    Abstract: Disclosed are electroluminescent devices that comprise organic layers that contain certain organic compounds containing one or more pyrimidine moieties. The organic compounds containing one or more pyrimidine moieties are suitable components of blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in for example mobile phones, televisions and personal computer screens.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: March 20, 2018
    Assignee: UDC Ireland Limited
    Inventors: Thomas Schafer, Patrice Bujard, Jonathan Rogers, Kristina Bardon
  • Patent number: 9920048
    Abstract: The present invention provides methods of inhibiting Raf kinase activity in a patient, the method comprising administering to the patient a compound having formula I: or a pharmaceutically acceptable salt thereof, wherein Rx, Ry, R1, L1, L2, Cy1, and Cy2 are as defined as set forth in the specification.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: March 20, 2018
    Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Weirong Chen, Jennifer Cossrow, Lloyd Franklin, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Benjamin Lane, Adam Littke, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
  • Patent number: 9879038
    Abstract: Disclosed is a novel tenofovir disoproxil edisylate salt having the structure of Chemical Formula 1.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: January 30, 2018
    Assignee: JW PHARMACEUTICAL CORPORATION
    Inventors: Do-Kyu Pyun, Won-Kyoung Lee, Su-Ha Park
  • Patent number: 9844539
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: December 19, 2017
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Patent number: 9777024
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Grant
    Filed: November 11, 2015
    Date of Patent: October 3, 2017
    Assignee: Tetra Discovery Partners, LLC
    Inventors: Mark E. Gurney, Timothy J. Hagen, Xuesheng Mo, A. Samuel Vellekoop, Donna L. Romero, Robert F. Campbell, Joel R. Walker, Lei Zhu
  • Patent number: 9737536
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives intreating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: August 22, 2017
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Patent number: 9585965
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: March 7, 2017
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
  • Patent number: 9469640
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: October 18, 2016
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Patent number: 9440982
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: September 13, 2016
    Assignee: Eolas Therapeutics, Inc.
    Inventors: Theodore M. Kamenecka, Yuanjun He, Rong Jiang, William Nguyen, Xinyi Song, Robert Jason Herr, Qin Jiang
  • Patent number: 9376445
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives intreating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: June 28, 2016
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Patent number: 9309254
    Abstract: The invention relates to spiro derivatives, to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: April 12, 2016
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
  • Patent number: 9221827
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: December 29, 2015
    Assignee: Melinta Therapeutics, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Shili Chen, Zoltan F. Kanyo, Matthew H. Scheideman, Yuanqing Tang
  • Patent number: 9221843
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: December 29, 2015
    Assignee: Tetra Discovery Partners, LLC
    Inventors: Mark E. Gurney, Timothy J. Hagen, Xuesheng Mo, A. Samuel Vellekoop, Donna L. Romero, Robert F. Campbell, Joel R. Walker, Lei Zhu
  • Patent number: 9059414
    Abstract: As a novel substance having a novel skeleton, provided is a novel phosphorescent organometallic iridium complex that can emit phosphorescence in a blue green to red wavelength region and has high emission efficiency. The phosphorescent organometallic iridium complex has a ligand having a pyridyl pyrimidine skeleton, i.e., the phosphorescent organometallic iridium complex has a ligand having a structure represented by the following general formula (G0). Note that in the formula, R1 and R4 to R6 separately represent hydrogen or an alkyl group having 1 to 6 carbon atoms; and R2 and R3 separately represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, a phenyl group that may have a substituent, and a pyridyl group that may have a substituent.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: June 16, 2015
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Tomoka Nakagawa, Tomoya Yamaguchi, Hiromi Seo, Satoshi Seo
  • Publication number: 20150148322
    Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
    Type: Application
    Filed: March 15, 2012
    Publication date: May 28, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pascale A.J. Pouzet, Peter Nickolaus, Ulrike Werthmann, Rogelio P. Frutos, Bing-Shiou Yang, Soojin Kim, Jason Alan Mulder, Nitinchandra Patel, Chris H. Senanayake, Thomas G. Tampone, Xudong Wei
  • Patent number: 9040490
    Abstract: A cytosine analog, a method of preparation of a cytosine analog, a DNA methyltransferase 1 inhibitor, and a method for DNA methylation inhibition, is provided for the treatment of diseases associated with deviations from normal DNA methylation. The analog of cytosine may be comprised of 1, N4, 5 and 6-substituted derivatives of cytosine or 5,6-dihydrocytosine, wherein the analog can be described by the chemical formula where R1 is H, R3, R4, 2?-deoxyribosyl, R4 is alkyl or aryl, X is N or C, wherein if X in the analog of formula I is N, then R5 is no substituent and if X in the analog of formula I and/or II is C or if X in the analog of formula II is N, then R5 and R6 are independently alkyl, aryl, hydroxyalkyl, aminoalkyl, hydroxyl, carboxyl, amino group, alkoxyl, aryloxyl, aminoalkyl, aminoaryl, thio group, sulfonyl, sulfinyl or halogen.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: May 26, 2015
    Assignee: INSTYTUT CHEMII BIOORGANICZNEJ PAN
    Inventors: Jan Barciszewski, Wojciech T. Markiewicz, Ewelina Adamska, Beata Plitta, Malgorzata Giel-Pietraszuk, Eliza Wyszko, Maria Markiewicz, Agnieszka Fedoruk-Wyszomirska, Tadeusz Kulinski, Marcin Chmielewski
  • Patent number: 9029534
    Abstract: Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Denise A. Colby, Andrew Anthony Martins, Benjamin James Roberts, Robert William Scott, Nicole S. White
  • Publication number: 20150115232
    Abstract: A chrysene-based compound and an organic light-emitting device including the same, the chrysene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: April 17, 2014
    Publication date: April 30, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Kwang-Hyun KIM, Young-Kook KIM, Eun-Young LEE
  • Patent number: 9012632
    Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: April 21, 2015
    Assignee: Riken
    Inventors: Masaaki Suzuki, Hisashi Doi, Hiroko Koyama
  • Patent number: 8993754
    Abstract: Provided is an iridium complex having a substructure represented by the following formula (1), which is a luminescent element material capable of luminescence with high brightness/high efficiency and excellent in durability and can be used in a luminescent element, etc.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: March 31, 2015
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventor: Hideo Konno
  • Publication number: 20150087651
    Abstract: The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 26, 2015
    Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doubler, Jerome Michel Claude Fortin, Nacer Lounis
  • Publication number: 20150076479
    Abstract: The invention provides an organic compound incorporating a specific structure into a pyridine skeleton or a 1,3,5-triazine skeleton and adapting the molecular weight to a specific range, a composition comprising the organic compound and a solvent, organic electroluminescent element comprising a layer that is formed by using the composition, and the uses thereof.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 19, 2015
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Koichi Ishibashi, Hideki Gorohmaru, Wataru Shimizu, Tomomi Okamoto
  • Patent number: 8980886
    Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: March 17, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
  • Patent number: 8980935
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: March 17, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Publication number: 20150069347
    Abstract: A condensed cyclic compound and an organic light-emitting device including the same, the condensed cyclic compound being represented by Formula 1:
    Type: Application
    Filed: June 3, 2014
    Publication date: March 12, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Kwang-Hyun KIM, Seok-Hwan HWANG, Young-Kook KIM, Jun-Ha PARK, Hye-Jin JUNG, Eun-Young LEE, Jong-Woo KIM, Jin-O LIM, Sang-Hyun HAN, Eun-Jae JEONG, Soo-Yon KIM
  • Publication number: 20150069297
    Abstract: A liquid crystal compound having high stability to heat and light, etc., a high clearing point, a low minimum temperature of liquid crystal phase, a low viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant, and good compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound, and a LCD element using the composition are described. The compound is represented by formula (1): wherein, for example, R1 is C1-10 alkyl, ring A1, ring A2, ring A3, ring A4 and ring B1 are independently 1,4-cyclohexylene, 1,4-phenylene, 1,4-phenylene in which at least one hydrogen is substituted with halogen, 1,3-dioxane-2,5-diyl, or tetrahydropyran-2,5-diyl, Z1, Z2, Z3 and Z4 are single bonds, l, m, n and o are independently 0 or 1, and l+m+n+o?1.
    Type: Application
    Filed: February 7, 2013
    Publication date: March 12, 2015
    Inventor: Hiroyuki Tanaka
  • Publication number: 20150069332
    Abstract: [This] charge transport material which comprises a compound expressed by the following formula has a high efficiency and drive durability after high-temperature storage and resists the occurrence of dark spots (X101 represents a sulfur atom or an oxygen atom; R101 and R102 represent each independently an alkyl group, an aryl group, a heteroaryl group, a fluorine atom, or a silyl group, and may further be substituted with these groups; n101 represents an integer from 0 to 11; n102 represents an integer from 0 to 7; a plurality of R101 and R102 [groups] may be the same or different; and L101 represents a single bond or a divalent linking group; however, one of R101, L101, and R102 includes a fluorine atom, a fluoroalkyl group, a cycloalkyl group, a cycloalkylene group, a silyl group, an alkylsilyl group, an arylsilyl group, or a silicon atom linking group.
    Type: Application
    Filed: March 29, 2012
    Publication date: March 12, 2015
    Applicant: UDC IRELAND LIMITED
    Inventors: Tetsu Kitamura, Kousuke Watanabe
  • Patent number: 8969366
    Abstract: Pyrimidinylpyrrolopyridinone derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: March 3, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Chiara Marchionni, Fabio Zuccotto, Alessandra Badari, Mauro Angiolini, Davide Carenzi, Marina Caldarelli, Maurizio Pulici
  • Patent number: 8952014
    Abstract: The present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Patent number: 8940185
    Abstract: To provide a novel liquid crystal compound having general physical properties necessary for the compound, namely, stability to heat, light and so forth, a wide temperature range of a liquid crystal phase, a high clearing point, a good compatibility with other compounds, a large refractive index anisotropy, a large dielectric anisotropy and a small viscosity. The liquid crystal compound is provided as compound (1): wherein, for example, R1 is alkyl having 1 to 20 carbons; ring A1 and ring B1 are 1,4-cyclohexylene or 1,4-phenylene; Z1 and Z2 are a single bond, —CH2CH2—, —CH?CH— or —C?C—; L1 is fluorine; L2, Y1 and Y2 are hydrogen, fluorine or chlorine; and X1 is halogen, —C?N or alkyl having 1 to 10 carbons, and in the alkyl, arbitrary —CH2— may be replaced by —O— or —S—, and m is 1 and n is 0.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: January 27, 2015
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventor: Hiroyuki Tanaka
  • Patent number: 8933084
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: January 13, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
  • Patent number: 8921548
    Abstract: Provided is a novel substance that can emit phosphorescence. Alternatively, provided is a novel substance with high emission efficiency. An organometallic complex in which a 4-arylpyrimidine derivative is a ligand and iridium is a central metal is provided. Specifically, an organometallic complex having a structure represented by a general formula (G1) is provided. In the general formula (G1), R1 represents a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted aryl group having 6 to 10 carbon atoms, R2 represents any of hydrogen, a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms, and a substituted or unsubstituted phenyl group, R3 represents hydrogen or a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms, and Ar1 represents a substituted or unsubstituted arylene group having 6 to 10 carbon atoms.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: December 30, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Tomoya Yamaguchi, Satoko Shitagaki, Takahiro Ushikubo, Satoshi Seo, Yui Yamada, Hiromi Nowatari
  • Patent number: 8921377
    Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: December 30, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
  • Patent number: 8901132
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: December 2, 2014
    Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Patent number: 8901133
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Patent number: 8895734
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: November 25, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Patent number: 8884008
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: November 11, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • 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
  • Patent number: 8859591
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: October 14, 2014
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8859566
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: October 14, 2014
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Patent number: 8859766
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: October 14, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140239273
    Abstract: An anthracene derivative is represented by a formula (1) below, in which at least one of Ar1, Ar2, Ar3, L1, L2 and L3 is a group derived from a skeleton represented by a formula (10) below,
    Type: Application
    Filed: December 18, 2013
    Publication date: August 28, 2014
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Sayaka MIZUTANI, Takayasu Sado
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Patent number: 8791299
    Abstract: 3D protein modeling and virtual screening of commercially-available compounds were performed to identify new inhibitors of the herpesvirus DNA polymerase, a key enzyme in the viral replication cycle. Two compounds (Nos 2 and 9) were particularly active against HSV-1 and HSV-2 strains and one compound (No 3) inhibited specifically cytomegalovirus (CMV) strains (overall hit rate of 25%). Some of the tested compounds inhibited wild-type viruses and strains resistant to current antiviral agents. New chemical entity derivatives of compound 2 with binding potential to the DNA polymerase retained an excellent activity against HSV-1, HSV-2 and VZV like the parental compound, as well against strains resistant to current antiviral agents. These non-nucleosidic herpesvirus DNA polymerase inhibitors with in vitro activity against drug-resistant clinical isolates warrant further pre-clinical studies.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: July 29, 2014
    Assignee: Universite Laval
    Inventors: Guy Boivin, Sheng-Xiang Lin, Melanie Martin, Arezki Azzi