At 2-, 4-, And 6-positions (e.g., Barbituric Acid, Etc.) Patents (Class 544/299)
  • Patent number: 10336711
    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: June 29, 2018
    Date of Patent: July 2, 2019
    Assignee: GlaxoSmithKline LLC
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 10307424
    Abstract: The invention relates to pharmacology and can be used for treating liver diseases of various etiologies, inter alia, in combination with other preparations. Claimed is a drug with hepatoprotective activity comprised of 3-(4-bromophenyl)-6,6-dihydroxy-5-hydroxyiminohexahydro-2,4-pyrimidinedione and salts thereof of general formula (I), where X is selected from the group: H, Na, K, or from the group of hydroxyalkylammonia derivatives of general formula (II), where R1, R2 are selected from the group: H, CH3, CH2CH3, CH2CH2OH; R3 is selected from the group: H, CH2OH; and n=1, 2; the drug can be prepared in the form of tablets or capsules for enteral administration; or in the form of a liquid or lyophilized substance for parenteral administration; or in the form of rectal suppositories; or in the form of capsules or tablets, or sweets for sucking; and may additionally contain the hepatoprotector Heptral; or the hepatoprotector Essentiale; or the hepatoprotector ursodeoxycholic acid.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: June 4, 2019
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets
  • Patent number: 9643935
    Abstract: Process for preparing 4,6-bis(aryloxy)pyrimidine derivatives. A process is provided for preparing 4,6-bis(aryloxy)pyrimidine derivatives. The process is conducted in water as reaction medium and catalyzed by one or more tertiary-amine catalyst(s). It has been found that a water based reaction substantially free of organic solvents can be carried out providing excellent yields by the addition of one or more tertiary-amine catalysts to the reaction medium. This provides a clean reaction and produces the desired product in high yields.
    Type: Grant
    Filed: May 27, 2014
    Date of Patent: May 9, 2017
    Assignee: CHEMINOVA A/S
    Inventor: Karl Bernhard Lindsay
  • 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: 8859573
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: October 14, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Patent number: 8859769
    Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.
    Type: Grant
    Filed: February 15, 2011
    Date of Patent: October 14, 2014
    Assignee: Actavis Group PTC EHF
    Inventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
  • Patent number: 8859060
    Abstract: A protective film of polarizer comprising an organic acid that has a solubility in water at 25° C. of at most 0.1% by mass and has an acid dissociation constant in a mixed solvent of tetrahydrofuran/water=6/4 by volume at 25° C. of from 2 to 7 can improve polarizer durability.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: October 14, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Nobutaka Fukagawa, Masato Nagura, Yoshio Ishii, Takayasu Yasuda, Naoyuki Nishikawa
  • Patent number: 8557834
    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: November 2, 2012
    Date of Patent: October 15, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 8552002
    Abstract: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
    Type: Grant
    Filed: June 23, 2005
    Date of Patent: October 8, 2013
    Assignees: Novartis AG, IRM LLC
    Inventors: Qiang Ding, Nathanael Schiander Gray, Bing Li, Yi Liu, Taebo Sim, Tetsuo Uno, Guobao Zhang, Carole Pissot Soldermann, Werner Breitenstein, Guido Bold, Giorgio Caravatti, Pascal Furet, Vito Guagnano, Marc Lang, Paul William Manley, Joseph Schoepfer, Carsten Spanka
  • Publication number: 20130030176
    Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.
    Type: Application
    Filed: February 15, 2011
    Publication date: January 31, 2013
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
  • Patent number: 8324208
    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: June 22, 2007
    Date of Patent: December 4, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Kevin J. Duffy, Duke M. Fitch, Jian Jin, Ronggang Liu, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 8242122
    Abstract: The invention is directed to methods and compositions for inhibiting caspase-independent apoptosis. In particular, methods and compositions for inhibiting Omi/HtrA2 activity, as well as method for identifying other inhibitors of Omi/HtrA2. Also disclosed are Omi/HtrA2 specific substrates and methods for identifying other substrates of Omi/HtrA2.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: August 14, 2012
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventor: Antonis S. Zervos
  • Patent number: 8124417
    Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: February 28, 2012
    Assignee: Japan Science and Technology Agency
    Inventors: Yoshio Umezawa, Takahito Ohshiro
  • Publication number: 20120046309
    Abstract: The present invention relates to the identification of inventive pyrimidine-2,4,6-triones (PYT compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the inventive PYT compounds.
    Type: Application
    Filed: May 5, 2010
    Publication date: February 23, 2012
    Applicants: NORTHWESTERN UNIVERSITY, CAMBRIA PHARMACEUTICALS, INC.
    Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanites, Richard I. Morimoto, Richard B. Silverman, Guoyao Xia
  • Patent number: 8101669
    Abstract: An exchange membrane containing modified maleimide oligomers comprising sulfonated poly(aryl ether ketone) (S-PAEK) and modified maleimide oligomers. The exchange membrane uses the modified maleimide oligomers having a hyper-branched architecture as matrix, and introduces them into S-PAEK to constitute semi-interpenetration network (semi-IPN), so as to intensify water holding capacity, chemical resistance, the electrochemical stability and thermal resistance of the ionic/proton exchange membrane. The exchange membrane can be used to fabricate the membrane electrode assemblies, fuel cells, and be applied them to the fields of seawater desalination, heavy water and sewage treatment, and biomass-energy resources.
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: January 24, 2012
    Assignees: Industrial Technology Research Institute, National Central University
    Inventors: Jing-Pin Pan, Tsung-Hsiung Wang, Jung-Mu Hsu, Peter P. Chu, Chien-Shun Wu, Bo-Jun Liu
  • Publication number: 20120004592
    Abstract: Tissue solubilizing compositions are provided. The compositions comprise 3-(decyl dimethyl ammonio) propane sulfonate and polyethylene glycol dodecyl ether, such as tetraethylene glycol dodecyl ether. The compositions may be useful to solubilize tissue, including skin, mucosal membrane, and other tissue. The compositions may be further useful to preserve and recover analytes contained within the solubilized skin, mucosal membrane, and other tissue.
    Type: Application
    Filed: April 27, 2011
    Publication date: January 5, 2012
    Applicant: The Regents of the University of California
    Inventors: Samir Mitragotri, Sumit Pallwal, Makoto Ogura, Russell M. Lebovitz
  • Patent number: 7776869
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: August 17, 2010
    Assignee: Amgen Inc.
    Inventors: Stuart C. Chaffee, Brian K. Albrecht, Brian L. Hodous, Matthew W. Martin, David C. McGowan, Erin F. DiMauro, Gade Reddy, Victor J. Cee, Philip R. Olivieri, Anthony Reed, Karina Romero
  • Patent number: 7713981
    Abstract: The invention is directed to methods and compositions for inhibiting caspase-independent apoptosis. In particular, methods and compositions for inhibiting Omi/HtrA2 activity, as well as method for identifying other inhibitors of Omi/HtrA2. Also disclosed are Omi/HtrA2 specific substrates and methods for identifying other substrates of Omi/HtrA2.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: May 11, 2010
    Assignee: University of Central Florida
    Inventor: Antonis Zervos
  • Patent number: 7678778
    Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: March 16, 2010
    Assignee: DEKK-TEC, Inc.
    Inventor: Lee Roy Morgan
  • Publication number: 20100055116
    Abstract: The present invention relates to compositions and methods for targeting c-Rel. In particular, the present invention provides compositions and methods for treating cancers, inflammatory diseases, autoimmune diseases, and transplant rejection by inhibiting c-Rel activity and for regulating c-Rel for research and drug screening applications.
    Type: Application
    Filed: April 13, 2007
    Publication date: March 4, 2010
    Inventors: Hsiou-chi Liou, Wenzhi Tian, Shuhua Cheng, Constance Y. Hsia, Alex Owyang, Jason J. Hsu
  • 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
  • Patent number: 7595317
    Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: September 29, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Bin Jiang, Lihua Chen, Zhonghui Lu, Joseph Barbosa, William J. Pitts
  • Publication number: 20090155917
    Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.
    Type: Application
    Filed: December 28, 2005
    Publication date: June 18, 2009
    Inventors: Yoshio Umezawa, Takahito Ohshiro
  • Patent number: 7465736
    Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: December 16, 2008
    Assignee: Laboratoires Serono S.A.
    Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
  • Patent number: 7439240
    Abstract: The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.
    Type: Grant
    Filed: June 23, 2003
    Date of Patent: October 21, 2008
    Assignee: AstraZeneca AB
    Inventors: Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
  • Publication number: 20080221325
    Abstract: An exchange membrane containing modified maleimide oligomers comprising sulfonated poly(aryl ether ketone) (S-PAEK) and modified maleimide oligomers. The exchange membrane uses the modified maleimide oligomers having a hyper-branched architecture as matrix, and introduces them into S-PAEK to constitute semi-interpenetration network (semi-IPN), so as to intensify water holding capacity, chemical resistance, the electrochemical stability and thermal resistance of the ionic/proton exchange membrane. The exchange membrane can be used to fabricate the membrane electrode assemblies, fuel cells, and be applied them to the fields of seawater desalination, heavy water and sewage treatment, and biomass-energy resources.
    Type: Application
    Filed: December 27, 2007
    Publication date: September 11, 2008
    Inventors: Jing-Ping Pan, Tsung-Hsiung Wang, Jung-Mu Hsu, Peter P. Chu, Chien-Shun Wu, Bo-Jun Liu
  • Patent number: 7294624
    Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: November 13, 2007
    Assignee: Bristol Myers Squibb Company
    Inventors: Jingwu Duan, Bin Jiang, Lihua Chen, Zhonghui Lu, Joseph Barbosa, William J. Pitts
  • Patent number: 7227021
    Abstract: The present invention provides a novel process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid. In particular, the present invention provides a process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid by reacting 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid with a Lewis acid to selectively remove one methoxymethyl group from 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid.
    Type: Grant
    Filed: April 25, 2006
    Date of Patent: June 5, 2007
    Assignee: Tara Pharmaceutical Industries Ltd
    Inventors: Daniella Gutman, Rosa Cyjon
  • Patent number: 7160893
    Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the specification. The invention also provides related pharmaceutical compositions, methods of use, and combinations.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: January 9, 2007
    Assignee: Warner-Lambert Company
    Inventors: James Lester Hicks, William Howard Roark
  • 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: 7064205
    Abstract: The present invention provides a novel process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid. In particular, the present invention provides a process for preparing 1-methoxymethyl-5,5-diphenylbarbituric acid by reacting 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid with a Lewis acid to selectively remove one methoxymethyl group from 1,3-bis(methoxymethyl)-5,5-diphenylbarbituric acid.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: June 20, 2006
    Assignee: Taro Pharmaceutical Industries Ltd.
    Inventors: Daniella Gutman, Rosa Cyjon
  • Patent number: 6974872
    Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 13, 2005
    Assignee: AMR Technology, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6953850
    Abstract: The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the specific deprotection of any substituent ono the saccharide ring, and greatly facilitates targeted or library-focused carbohydrate-related syntheses. In particular, the invention provides a universal monosaccharide building block of General Formula (I) or General Formula (II) in which A is a leaving group; X is hydrogen, O, N or N3; X1 is hydrogen, —CH2O—, —CH2NH—, —CH3, —CH2N3 or —COO—; and B, C, D and E are protecting groups that can be cleaved orthogonally, and in which B, C, D and E are absent when X is hydrogen or N3, and E is absent when X1 is hydrogen, CH3 or N3.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: October 11, 2005
    Assignee: Alchemia Pty. Ltd.
    Inventors: Gyula Dekany, John Papagerogiou, Laurent Francois Bornaghi
  • Patent number: 6936620
    Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, W, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: August 30, 2005
    Assignee: Bristol Myers Squibb Company
    Inventors: Jingwu Duan, Zhonghui Lu
  • Patent number: 6919458
    Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydr
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 19, 2005
    Assignee: AMR Technology, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6914160
    Abstract: This invention relates to compounds of formula (I)
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: July 5, 2005
    Assignee: Pfizer Inc
    Inventors: Duncan Robert Armour, Andrew Simon Bell, Paul John Edwards, David Ellis, David Hepworth, Mark Llewellyn Lewis, Christopher Ronald Smith
  • Patent number: 6835726
    Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: December 28, 2004
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
  • 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: 6765089
    Abstract: This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups that are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: July 20, 2004
    Assignee: Alchemia Pty Ltd
    Inventors: Istvan Toth, Gyula Dekany, Barry Kellam
  • Patent number: 6723843
    Abstract: The invention provides a system for solid-phase synthesis of oligosaccharides, based on the discovery that a 2-substituted-1,3-dioxocycloalkyl linker group of general formula (I) can be used to couple saccharide groups of both the O-glycoside and N-glycoside type to a polymer support. The invention provides reagents, reagent kits and methods for solid-phase oligosaccharide synthesis.
    Type: Grant
    Filed: August 30, 2002
    Date of Patent: April 20, 2004
    Assignee: Alchemia PTY LTD
    Inventors: Istvan Toth, Gyula Dekany, Barry Kellam
  • Patent number: 6720421
    Abstract: Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds, which have specific substituents and are useful in diazo thermal recording materials; and diazo thermal recording materials containing the barbituric acid derivative.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: April 13, 2004
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Akinori Fujita, Naoto Yanagihara, Yohsuke Takeuchi, Daisuke Arioka, Kimi Ikeda, Sachiko Arai
  • Patent number: 6706723
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: March 16, 2004
    Assignee: Pfizer, Inc.
    Inventors: Mark C. Noe, Lawrence A. Reiter, Martin J. Wythes
  • Patent number: 6686367
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: February 3, 2004
    Assignee: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Publication number: 20040010056
    Abstract: A colored dispersion comprising a polymer and a dye represented by General Formula (1):
    Type: Application
    Filed: June 20, 2003
    Publication date: January 15, 2004
    Applicant: KONICA CORPORATION
    Inventors: Mari Takahashi, Satoru Ikesu, Takatugu Suzuki, Kyoko Iwamoto
  • Patent number: 6673925
    Abstract: Method of producing thiobarbituric acid derivatives of formula I wherein R1 is SH, S−M+ or CH3S—, and M+ is an alkali metal ion, by hydrogenolysis of a compound of formula II wherein R2 is chlorine or CH3O—, with a) a hydrogenolysis agent in the presence of an inert solvent and by a direct reaction of the hydrogenolysis product with an alkali metal methylate in methanol, or b) with a hydrogenolysis agent in the presence of an inert solvent and in the presence of a methylation reagent, and subsequently with an alkali metal methylate in methanol, as well as the use of these compound of formula I in the production of 7-[(4,6-dimethoxy-pyrimidin-2-yl)thio]-3-methylphthalide.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: January 6, 2004
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Bernhard Urwyler, Thomas Rapold, Marco Passafaro
  • Patent number: 6670367
    Abstract: The invention relates to carboxylic acid derivatives of the formula I where the radicals have the meanings stated in the description, and to their use as drugs.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: December 30, 2003
    Assignee: Abbott GmbH & Co., KG
    Inventors: Wilhelm Amberg, Rolf Jansen, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Stefan Hergenröder, Manfred Raschack, Liliane Unger
  • 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