Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/301)
  • Patent number: 9660196
    Abstract: Organic dye for a Dye Sensitized Solar Cell (DSSC) comprising at least one electron donor group and at least two electron acceptor groups, each of said electron acceptor groups being bound to said electron donor group through a ?-conjugated unit. Said organic dye is particularly useful in a dye sensitized photoelectric transformation element, which, in its turn, can be used in a Dye Sensitized Solar Cell (DSSC).
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: May 23, 2017
    Assignee: ENI S.p.A.
    Inventors: Alessandro Abbotto, Maurizio Filippo Acciarri, Paolo Biagini, Simona Olga Binetti
  • Patent number: 9359366
    Abstract: Disclosed are intermediates of Ticagrelor and a preparation method therefor, and a preparation method for Ticagrelor. Specifically, disclosed is an intermediate, namely, a compound of Formula (VI), for preparing Ticagrelor. Further disclosed is a method for preparing the intermediate and a method for preparing Ticagrelor by using the intermediate. Ticagrelor is prepared by using the intermediate, so that the synthesis process is simple, and a defect that long reaction times under high temperature that are required in the existing methods are avoided. The method is suitable for mass production in industry, energy consumption is reduced, pollution of the environment is reduced, and discharge of waste is reduced.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: June 7, 2016
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Suncadia Pharmaceuticals Co., Ltd.
    Inventors: Shaoguang Sun, Defu Song, Biao He, Xiaobo Lai
  • Publication number: 20150141357
    Abstract: The present invention relates to methods of inhibiting shikimate pathway, comprising administering to a subject a pharmaceutically acceptable composition comprising a compound having a formula: or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 21, 2015
    Applicant: NATIONAL TSING HUA UNIVERSITY
    Inventors: Wen-Ching Wang, Shih-Ching Chou, Ming-Hua Hsu
  • Patent number: 8999959
    Abstract: The invention relates to medicine and can be used for treating liver lesions caused by chemical or biological agents. The drug for treating liver lesions caused by chemical or biological agents is embodied as 1-(4-bromophenyl)-6-hydroxy-5-nitroso-1,2,3,4-tetrahydropyrimidine-2.4-dione: (I), or salts thereof having the general formula: (II), where X is selected from Na+, K+, Li+, NH4+, NH2CONH3+ or another pharmacologically acceptable cation. The effectiveness of the preparation in treating liver diseases of different etiologies is increased.
    Type: Grant
    Filed: October 10, 2011
    Date of Patent: April 7, 2015
    Inventors: Viktor Veniaminovich TETS, Georgy Viktorovich TETS, Konstantin Andreevich Krasnov
  • 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: 20140336383
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 13, 2014
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Publication number: 20140275134
    Abstract: The disclosed subject matter provides certain N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or development of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: October 16, 2012
    Publication date: September 18, 2014
    Inventors: John P. Toscano, Daryl A. Guthrie
  • Patent number: 8815884
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: August 26, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 8652364
    Abstract: A polymer film comprising at least one compound represented by formula (I) is disclosed. A1 and A2 each independently represent a group having a Hammett's ?p value of 0.2 or more, or bond each other to form a cyclic active methylene structure; and X1 and X2 each independently represent a hydrogen atom, aryl group, hetero-cyclic group, cyano, N-alkyl- or N-aryl-carbamoyl, or alkyl- or aryl-oxycarbonyl, or bond each other to form a saturated ring in which nitrogen and carbon atoms are embedded, and the group and ring may have at least one substituent.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: February 18, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Shunya Katoh, Hiroko Kamee
  • Publication number: 20130237704
    Abstract: The invention relates to medicine and can be used for treating liver lesions caused by chemical or biological agents. The drug for treating liver lesions caused by chemical or biological agents is embodied as 1-(4-bromophenyl)-6-hydroxy-5-nitroso-1,2,3,4-tetrahydropyrimidine-2.4-dione: (I), or salts thereof having the general formula: (II), where X is selected from Na+, K+, Li+, NH4+, NH2CONH3+ or another pharmacologically acceptable cation. The effectiveness of the preparation in treating liver diseases of different etiologies is increased.
    Type: Application
    Filed: October 10, 2011
    Publication date: September 12, 2013
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Konstantin Andreevich Krasnov
  • Publication number: 20130150390
    Abstract: A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.
    Type: Application
    Filed: December 12, 2012
    Publication date: June 13, 2013
    Inventors: Mie Kaino, Hiroyuki Meguro
  • Publication number: 20130072487
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Application
    Filed: November 2, 2012
    Publication date: March 21, 2013
    Applicant: GLAXOSMITHKLINE LLC
    Inventor: GLAXOSMITHKLINE LLC
  • Publication number: 20120322802
    Abstract: The present invention relates to novel 2,4-pyrimidine derivatives and a use thereof, and more particularly, to pyrimidine derivatives which are effective for systemic lupus erythematosus, a composition for preventing and treating systemic lupus erythematosus comprising the same as an active ingredient and a method for screening the same. The present inventors found novel materials inhibiting surface translocation of gp96 by mimicking a function of AIMP1 which is a molecular anchor for an intracellular residence of gp96, and identified in vitro and in vivo activity of the materials for preventing and treating SLE by alleviating SLE plasma in autoimmune diseases. Therefore, the present invention provides a novel method for screening a therapeutic agent for SLE, and preventing or treating SLE using the mechanism.
    Type: Application
    Filed: November 2, 2010
    Publication date: December 20, 2012
    Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, SNU R&DB FOUNDATION
    Inventors: Sunghoon Kim, Jung Min Han, Hyeong Rae Kim, Dong Ju Jeon, Jong Hwan Song, Kyung Eun Park
  • Patent number: 8288420
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: October 16, 2012
    Assignee: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishakumar Basawannappa Hadimani, Haeil Park, Jared Miller Wagner, Peter A. Crooks
  • Patent number: 8273879
    Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: September 25, 2012
    Assignee: AstraZeneca AB
    Inventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
  • Publication number: 20120220610
    Abstract: The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed.
    Type: Application
    Filed: March 25, 2010
    Publication date: August 30, 2012
    Applicant: CORNELL UNIVERSITY
    Inventors: Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
  • Publication number: 20120029000
    Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
    Type: Application
    Filed: March 25, 2010
    Publication date: February 2, 2012
    Applicant: MAPI PHARMA LIMITED
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Publication number: 20110263567
    Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.
    Type: Application
    Filed: September 11, 2009
    Publication date: October 27, 2011
    Applicant: Semmelweis Egyetem
    Inventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
  • Patent number: 8044211
    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z—X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.
    Type: Grant
    Filed: May 1, 2007
    Date of Patent: October 25, 2011
    Assignee: Chroma Therapeutics Ltd.
    Inventors: David Charles Festus Moffat, Stephane Pintat, Stephen Davies
  • Publication number: 20110092526
    Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.
    Type: Application
    Filed: October 19, 2010
    Publication date: April 21, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Stuart Norman Lile Bennett, Frederick Woolf Goldberg, Andrew Leach, Paul Robert Owen Whittamore, Pernilla Sörme
  • Publication number: 20100240682
    Abstract: To provide an excellent agent for prevention or treatment of an inflammatory disease. The agent for prevention or treatment of an inflammatory disease contains a thymidine phosphorylase inhibitor as an active ingredient, wherein when the thymidine phosphorylase inhibitor is 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a salt thereof, the inflammatory disease is an inflammatory disease other than inflammatory bowel disease.
    Type: Application
    Filed: October 10, 2008
    Publication date: September 23, 2010
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuki Sakamoto, Yoshikazu Sugimoto
  • Publication number: 20100210467
    Abstract: It is intended to provide an agent for improving sugarcane Brix which increases the sugar productivity from pressed juice after harvesting and promotes ripening when applied to sugarcane and, therefore, by which a sugar yield comparable to sugarcane harvested at the best harvest season can be established even from sugarcane before reaching the harvest season, which comprises at least one member of the compounds represented by the following general formula (I) wherein A represents an oxygen atom, a sulfur atom, or a hydroxymethylene group; Y represents a carboxyl group, an alkyloxycarbonyl group, a halogenated methylsulfonylamino group or a diphenylmethylideneiminoxycarbonyl group, either in a free form or forming a salt; and R represents a halogen atom, an alkyl group, a hydroxy-, alkoxy- or alkoxyiminoalkyl group or a 4,6-dimethoxypyrimidin-2-yloxy group, or Y and R may be bonded together to form a group —C(?O)—O—CH(CH3)—.
    Type: Application
    Filed: October 24, 2008
    Publication date: August 19, 2010
    Inventors: Masanori Kobayashi, Shuji Ohno, Yoshihiro Yamaji, Ryo Hanai, Jose Antonio De Souza Junior, Helio Massatoshi Tukamoto
  • Publication number: 20100113444
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Application
    Filed: June 22, 2007
    Publication date: May 6, 2010
    Inventors: Kevin J. Duffy, Duke M. Fitch, Jian Jin, Ronggang Liu, Antony N. Shaw, Kenneth Wiggall
  • Publication number: 20100104985
    Abstract: The present invention relates to a compound for photoresist, selected from the group consisting of a compound comprising an oxonol dye skeleton, a cyanine dye, a styryl dye, a compound comprising a merocyanine dye skeleton, a compound comprising a phthalocyanine dye skeleton, an azo compound, and a complex compound of an azo compound and a metal ion. The present invention further provides a photoresist liquid comprising at least one of the compound for photoresist and a method of etching a surface being processed using the photoresist liquid.
    Type: Application
    Filed: March 5, 2008
    Publication date: April 29, 2010
    Inventor: Tetsuya Watanabe
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Publication number: 20090186913
    Abstract: Methods for inhibiting a neoplasm in a subject and methods of inhibiting undesired angiogenesis that include administering to a subject a therapeutically effective amount of at least one novel tetrahalogenated compound, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 10, 2008
    Publication date: July 23, 2009
    Inventors: William D. Figg, Erin Gardner, Michael Gutschow, Agnieszka Ambrozak
  • Publication number: 20090104713
    Abstract: Phenobarbital derivatives synthesized out of the alkyl chain at the 5-position, particularly with hydrophilic properties, and carrying an active ester at the end, allow formation of aminodextran conjugates that give curves in the desired range of the assay in the ONLINE TDM microparticle assay format when matched against the Roche FPIA antibody specific for phenobarbital (“an antibody specific for phenobarbital”).
    Type: Application
    Filed: September 23, 2008
    Publication date: April 23, 2009
    Inventor: Raymond Hui
  • Publication number: 20090088490
    Abstract: A simultaneous two-photon absorption three-dimensional recording material includes at least one kind of dye having at least one polymerizable group.
    Type: Application
    Filed: September 26, 2008
    Publication date: April 2, 2009
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaharu AKIBA, Hiroo TAKIZAWA
  • Publication number: 20090080074
    Abstract: A polymer film includes: a wavelength dispersion regulator represented by formula (I): wherein R1 and R2 each independently represents a hydrogen atom, an alkyl group or an aryl group, provided that both R1 and R2 are not hydrogen atoms at the same time; and R3 and R4 each independently represents an electron-withdrawing substituent, and R1 and R2, or R3 and R4 may be bonded together to form a ring, and wherein the polymer film has a retardation value that satisfies the following formulae (1) and (2): 70 nm?Rth(548)?300 nm??Formula (1) Rth(628)<Rth(548)<Rth(446)??Formula (2) wherein Rth(?) represents a retardation value expressed in nm in a film thickness direction measured at a wavelength of ? nm.
    Type: Application
    Filed: September 4, 2008
    Publication date: March 26, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Nobutaka Fukagawa, Masaki Noro, Teruki Niori
  • Patent number: 7482355
    Abstract: Compounds of formula (1), pharmaceutically acceptable salts, solvates and in vivo hydrolysable esters thereof, have activity as pharmaceuticals, in particular as modulators of chemokine receptor (especially CXCR2) activity, and may be in the treatment (therapeutic or prophylactic) of conditions/diseases in human and non-human animals which are exacerbated or caused by excessive or unregulated production of chemokines.
    Type: Grant
    Filed: August 20, 2003
    Date of Patent: January 27, 2009
    Assignee: AstraZeneca AB
    Inventors: Mark Richard Ebden, Premji Meghani, Anthony Ronald Cook, John Steele, Lal Lashkar Singh Cheema
  • Publication number: 20090023085
    Abstract: A photosensitive composition includes a compound represented by Formula (I) and a curable composition contains the compound of Formula (I) and a polymerizable compound. A compound is represented by a Formula (1) and a photocurable composition contains the compound of Formula (1) and a polymerizable compound. In Formula (I), R, R1 and R2 each independently represent a hydrogen atom or a monovalent substituent. In Formula (1), R and B each independently represent a monovalent substituent, A represents a divalent organic group, and Ar represents an aryl group.
    Type: Application
    Filed: July 17, 2008
    Publication date: January 22, 2009
    Applicant: FUJIFILM CORPORATION
    Inventor: Tomotaka Tsuchimura
  • Patent number: 7456191
    Abstract: This invention relates to pyrimidine derivatives of general formula (I) in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.
    Type: Grant
    Filed: March 22, 2006
    Date of Patent: November 25, 2008
    Assignee: Schering AG
    Inventors: Ulrich Luecking, Gerhard Siemeister, Rolf Jautelat
  • Publication number: 20080234254
    Abstract: The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.
    Type: Application
    Filed: June 7, 2005
    Publication date: September 25, 2008
    Applicant: UNIVERSITY OF LEEDS
    Inventors: Ronald Grigg, Andrew Cook
  • Publication number: 20080146594
    Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.
    Type: Application
    Filed: November 8, 2007
    Publication date: June 19, 2008
    Applicant: Ligand Pharmaceutical, Inc.
    Inventors: Jyun-Hung Chen, E. Adam Kallel, Thomas Lau, Matthew H. McNeill, Todd A. Miller, Bao N. Nguyen, Richard J. Penuliar, Dean P. Phillips, Daniel A. Ruppar, Lin Zhi, Jackline E. Dalgard
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7205307
    Abstract: The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: April 17, 2007
    Assignee: Icagen, Inc.
    Inventors: Grant A. McNaughton-Smith, George S. Amato, Paul C. Fritch
  • Patent number: 7119201
    Abstract: The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione; metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, W, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: April 28, 2003
    Date of Patent: October 10, 2006
    Assignee: Pfizer Inc
    Inventors: Lawrence Alan Reiter, Kevin Daniel Freeman-Cook
  • Patent number: 7074925
    Abstract: N-substituted derivatives of 5-oximinobarbituric add of the general formula where X is sulfur; R1 is selected from the group consisting of saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl; and R2 is selected from the group consisting of hydrogen, saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl possessing a biological activity.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: July 11, 2006
    Inventor: Rimma Lliinichna Ashkinazi
  • Patent number: 7067663
    Abstract: Pyrimidine compound (I) useful as a pharmaceutical intermediate, a process for preparing the pyrimidine compound (I), to intermediates used in the process, and use of the pyrimidine compound (I) in the preparation of pharmaceuticals. The process comprises hydrogenating a compound of formula (IV): wherein Ar is a phenyl optionally substituted by halogen, C1-4 alkyl or C1-4 alkoxy; to give a compound of formula (II): and reacting the compound of formula (II) with a salt of a compound of formula (III): to provide the compound of formula (I).
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: June 27, 2006
    Assignee: AstraZeneca AB
    Inventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
  • Patent number: 7060826
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Grant
    Filed: July 14, 2005
    Date of Patent: June 13, 2006
    Assignee: Targaeept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
  • Patent number: 6960688
    Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: November 1, 2005
    Assignee: AstraZeneca AB
    Inventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
  • Patent number: 6919332
    Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: April 28, 2003
    Date of Patent: July 19, 2005
    Assignee: Pfizer Inc.
    Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia
  • Patent number: 6900222
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: May 31, 2005
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 6841671
    Abstract: The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: January 11, 2005
    Assignee: Pfizer Inc.
    Inventors: Mark C. Noe, Martin J. Wythes, Brian S. Bronk
  • Patent number: 6833372
    Abstract: Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: December 21, 2004
    Assignee: Pfizer, Inc.
    Inventors: Lance C. Christie, Mark B. Anderson, Jun Feng, Yufeng Hong, Ved P. Pathak, Ranjan J. Rajapakse, Eileen V. Tompkins, Haresh Vazir, Haitao Li
  • Patent number: 6800590
    Abstract: This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture. The compound has the following structure: wherein, D or E is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl or C1-C4 haloalkoxy; R1 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy; R2 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 carbamyl, C1-C4 alkoxycarbonyl, C1-C4 haloalkyl, cyano, nitro, carboxy or its alkali metal, alkali earth metal and organoammonium salts, C1-C4 alkylamido, C1-C4 haloalkylamido, heterocyclic amido, benzamido or substituted benzamido, benzo or substituted benzo compounds; R3 is hydrogen, C1-C4 alkanoyl, C1-C4 haloalkanoyl, benzoyl or C1-C4 alkoxyacetyl; X is CH or N; n=1-3.
    Type: Grant
    Filed: April 9, 2003
    Date of Patent: October 5, 2004
    Assignees: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Zheijiang Chemical Industry Research Institute
    Inventors: Long Lü, Jie Chen, Jun Wu, Wen Ling, Lisheng Mao, Mingzhi Li, Xian Cai, Weili Peng, Yong Wu, Shenggan Wu, Hongjun Wang, Guochao Wang, Hu Cui, Shidong Han, Weilian Qiu, Yonghua Wang
  • Patent number: RE39056
    Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: April 4, 2006
    Assignee: Merck & Co, Inc.
    Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman
  • Patent number: RE39266
    Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: September 5, 2006
    Assignee: Dr. Reddy's Laboratories, Limited
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K. S. Pakala
  • Patent number: RE42462
    Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: October 7, 1995
    Date of Patent: June 14, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
  • Patent number: RE42477
    Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: June 21, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack