At 2-, 4-, And 6-positions (e.g., Barbituric Acid, Etc.) Patents (Class 544/299)
  • 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: 6613773
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: September 2, 2003
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Patent number: 6608071
    Abstract: The invention relates to compounds of formula I wherein r is from 0 to 2; n is from 0 to 2; m is from 0 to 4; A, B, D and E are each independently of the others N or CH, with the proviso that not more than two of those radicals are N; G is lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa (—O—), thia (—S—) or imino (—NH—), or is lower alkylene substituted by acyloxy or by hydroxy; Q is lower alkyl, especially methyl; R is H or lower alkyl; X is imino, oxa or thia; Y is lower alkyl or, especially, aryl, heteroaryl or unsubstituted or substituted cycloalkyl; and Z is amino, mono- or di-substituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-di-substituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lowe
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: August 19, 2003
    Assignee: Novartis AG
    Inventors: Karl-Heinz Altmann, Guido Bold, Paul William Manley
  • Publication number: 20030135047
    Abstract: Process for preparing 4,6-dimethoxy-2-(methylsulfonyl)-1,3-pyrimidine by reacting 4,6dichloro-2-(methyltio)-1,3-pyrimidine in an inert organic solvent with an alkali metal methoxide, transfer of the resulting 4,6-dimethoxy-2-(methylthio)-1,3-pyrimidine into an aqueous-acidic medium and subsequent oxidation of this compound, of appropriate in the presence of a catalyst, wherein the oxidation is followed by a purification step in which the aqueous-acidic reaction mixture is adjusted with aqueous base to a pH in the range of 5-8 and stirred either in the presence or in the absence of an organic solvent, and the use of this compound for preparing herbicides, for example 7-[(4,6 dimethoxy-pyrimidin-2-yl)thio]-3-methylphthalide.
    Type: Application
    Filed: January 6, 2003
    Publication date: July 17, 2003
    Inventors: Beat Jau, Bernhard Urwyler
  • Patent number: 6579982
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: June 17, 2003
    Assignee: Pfizer Inc.
    Inventor: Julian Blagg
  • Patent number: 6562542
    Abstract: An image-forming material is described, comprising on an support an acid-generating agent selected from a sulfonic acid ester of a specific structure generating an acid by the action of heat and the polymer thereof, and a compound causing a light absorption change in the absorption region of from 350 to 700 nm by an intramolecular or intermolecular reaction by the action of an acid. The image-forming material has a high sensitivity and excellent storage stability and gives low haze and good images in the case of performing image formation using a high-output laser light.
    Type: Grant
    Filed: March 28, 2001
    Date of Patent: May 13, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Atsuhiro Ohkawa, Seiya Sakurai
  • Patent number: 6552030
    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: May 4, 2001
    Date of Patent: April 22, 2003
    Assignee: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Patent number: 6518425
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: February 11, 2003
    Assignees: Emory University, Triangle Pharmaceuticals, Inc.
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
  • Patent number: 6452011
    Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: September 17, 2002
    Assignee: Albany Molecular Research, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6444682
    Abstract: Nucleotide or base analogues having structure (3) or (4) wherein X═O or NH or S and each R6 is independently H or alkyl or alkenyl or alkoxy or aryl or a reporter moiety.
    Type: Grant
    Filed: April 18, 2000
    Date of Patent: September 3, 2002
    Assignee: Nycomed Amersham PLC
    Inventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
  • Patent number: 6444824
    Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is and where m is 1 or 3-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hyrogen, an alkyl moiety, and an aryl moiety.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: September 3, 2002
    Assignee: Albany Molecular Research, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Publication number: 20020095037
    Abstract: Method of producing thiobarbituric acid derivatives of formula I 1
    Type: Application
    Filed: August 20, 2001
    Publication date: July 18, 2002
    Inventors: Bernhard Urwyler, Thomas Rapold, Marco Pasafaro
  • Patent number: 6417359
    Abstract: A compound having the formula: wherein X′ is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0, but not equal to 0; A, A′ and A″ are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z′ is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z″ is hydrogen or a substituent other than hydrogen; Y is C═O, C(OH)R′ or C—A, where R′ is hydrogen or lower alkyl.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: July 9, 2002
    Assignee: Targacept, Inc.
    Inventors: Peter Anthony Crooks, Haeil Park, Balwinder Singh Bhatti, William Scott Caldwell, Gary Maurice Dull
  • Patent number: 6380258
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle, L.L.C.
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Publication number: 20020013330
    Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.
    Type: Application
    Filed: April 24, 2001
    Publication date: January 31, 2002
    Inventors: Pascal Druzgala, Peter G. Milner
  • Publication number: 20020006575
    Abstract: The invention relates to a positive-working, radiation-sensitive mixture which contains an organic polymeric binder which is insoluble in water but soluble or at least swellable in aqueous alkaline solution and at least one IR-absorbing cyanine dye having a betaine structure or having a betaine structure and containing an anion and having the formula (I) 1
    Type: Application
    Filed: July 29, 1999
    Publication date: January 17, 2002
    Applicant: Otfried Gaschler
    Inventors: OTFRIED GASCHLER, ANDREAS ELSAESSER, JOERG JUNG, HANS-JOACHIM SCHLOSSER
  • Patent number: 6335332
    Abstract: The invention is directed to barbituric acid derivatives having inhibitory activity for matrix maetalloproteases comprised of formula (I): pharmaceutical compositions thereof, processes for preparing the derivatives, and methods for treating diseases associated with elevated or uncontrolled levels of matrix metalloprotease activity, e.g., cancer, specifically tumor progression and tumor metastasis, inflammation, or as a method of contraception.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: January 1, 2002
    Assignee: Roche Diagnostics GmbH
    Inventors: Ambrogio Oliva, Gianpiero De Cillis, Frank Grams, Valeria Livi, Gerd Zimmermann, Ernesto Menta, Hans-Willi Krell
  • Patent number: 6310069
    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: March 24, 2000
    Date of Patent: October 30, 2001
    Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor Inc.
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K. S. Pakala
  • Patent number: 6288071
    Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Henry Szczepanski, Martin Zeller, Ottmar Franz HĂĽter
  • Patent number: 6281219
    Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.
    Type: Grant
    Filed: July 12, 1999
    Date of Patent: August 28, 2001
    Assignee: American Cyanamid Co.
    Inventors: Salvatore John Cuccia, William Wakefield Wood, Brian Lee Buckwalter, John Francis Chiarello, Linda Barbara Fleming
  • Patent number: 6254669
    Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: July 3, 2001
    Assignee: Zeneca Limited
    Inventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
  • Patent number: 6235903
    Abstract: A process for preparing endothelin receptor antagonists of the sulfanyl type of the general formula I by nucleophilic reaction of a carboxylic acid derivative of the formula II with a sulfide of the formula III to give endothelin receptor antagonists of the formula I.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: May 22, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilhelm Amberg, Rolf Jansen, Dagmar Klinge
  • Patent number: 6177437
    Abstract: The invention is directed to novel 6-aromatic substituted uracil compounds of formula I therapeutic compositions comprising the compounds, and methods of treating Herpes simplex virus Type I and Type II recurrent infections and Herpes simplex virus Type I and Type II encephalitis in humans using the compounds and/or therapeutic compositions.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: January 23, 2001
    Assignee: University of Massachusetts Medical Center
    Inventor: George E. Wright
  • Patent number: 6174901
    Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: January 16, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
  • Patent number: 6153560
    Abstract: Pyrimidyl phenyl and pyrimidyl benzyl ethers of the general formula I ##STR1## and their salts and N-oxides, where the substituents and indices have the following meanings:Q is (CO.sub.2 CH.sub.3).dbd.CHCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3, C(CONHCH.sub.3).dbd.CHOCH.sub.3, C(CONH.sub.2).dbd.NOCH.sub.3, C(CONHCH.sub.3).dbd.NOCH.sub.3 or N(OCH.sub.3)--CO.sub.2 CH.sub.3 ;n is 0 or 1;R.sup.1 is hydrogen or an organic radical bonded via a carbon atom;R.sup.2 is hydrogen, cyano, halogen or an organic radical bonded via a carbon, oxygen, sulfur or nitrogen atom;R.sup.3 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.2 -haloalkyl;R.sup.4 is hydrogen, cyano, nitro, halogen or an organic radical bonded via a carbon, oxygen, sulfur or nitrogen atom;y is 0, 1, 2 or 3, it being possible for the radicals R.sup.5 to be different if y is 2 or 3;R.sup.5 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: September 9, 1998
    Date of Patent: November 28, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Oberdorf, Wassilios Grammenos, Hubert Sauter, Thomas Grote, Bernd Muller, Reinhard Kirstgen, Herbert Bayer, Arne Ptock, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6121303
    Abstract: A compound of formula I ##STR1## wherein R.sub.1 is nitro, halogeno or cyano group and R.sub.2 is a group selected from ##STR2## wherein Y and Z are independently oxygen, sulfur or NR, wherein R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group and X.sub.1 and X.sub.2 are NR, where R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group, or a pharmaceutically acceptable salt or ester thereof. Pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: February 23, 1999
    Date of Patent: September 19, 2000
    Assignee: Orion-yhtyma Oy
    Inventors: Reijo Backstrom, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
  • Patent number: 6087498
    Abstract: There is provided a process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds. The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: July 11, 2000
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Salvatore John Cuccia, Robert Brigance
  • Patent number: 5932730
    Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, 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: August 3, 1999
    Assignee: BASF Aktiengesellschaft
    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: 5922727
    Abstract: The present invention relates to novel compound of general formula (I) and pharmaceutically acceptable salts thereof, and process for the preparation of such derivatives and to pharmaceutical compositions containing the same as active ingredients. ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 represents independently hydrogen atom, halogen atom, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 thioalkyl, C.sub.3 -C.sub.8 optionally substituted cyclicalkyl, unsaturated alkyl, substituted alkyl hydroxyl or aryl hydroxyl, C.sub.1 -C.sub.10 alkylamine, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.4 lower thioalkoxy; Z represents oxygen atom, sulfur atom, carbon atom and carbonyl group; X represents oxygen atom, sulfur atom; n represents an integer of 1-3; and (sub)cycloalk(en)yl represents ##STR2## in which R.sub.4 and R.sub.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: July 13, 1999
    Assignee: Samjin Pharmaceutical Co., Ltd
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Joong-Young Kim, Sun-Hwan Lee, Ho-Seok Kwon, Jae-Eung Lee, Jeong-Ho Joo, Byung-Chul Kim, Dong-Wook Kang
  • Patent number: 5859009
    Abstract: Substituted spiroalkylamino and -alkoxy heterocycles, processes for their preparation, and their use as pesticides and fungicidesThe invention relates to compounds of the formula ##STR1## in which Het is optionally substituted 4-pyridyl or 4-pyrimidinyl; X is NH, O or S(O).sub.0-2 ; E is a bond or alkanediyl; Y and Z are CH.sub.2, O and/or S(O).sub.0-2 ; W is (CH.sub.2).sub.0-4 ; R.sup.4 and R.sup.5 are halogen, (halo)alkyl, (halo)alkoxy or alkylthio; r and s are 0-2; U is a bond, O, S(O).sub.0-2 or optionally substituted imino; and V is a bond CO, SO.sub.2, --CQ--T-- or --CT'.dbd.N--; or U+V together are a double bond; and R.sup.6 is as defined in the description. The invention furthermore relates to processes for their preparation and to their use as pesticides and fungicides.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: January 12, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Wolfgang Schaper, Rainer Preuss, Peter Braun, Manfred Kern, Werner Knauf, Burkhard Sachse, Ulrich Sanft, Anna Waltersdorfer, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
  • Patent number: 5849910
    Abstract: This invention provides an improved process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds having the structural formula I ##STR1## The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: December 15, 1998
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 5840732
    Abstract: This invention provides a new condensed imidazole compound possessing inhibitory activity of adhesion molecule expression.This invention also provides a therapeutic and prophylactic agent for diabetic nephritis and/or autoimmune disease and an immunosuppressor for organ transplantation.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: November 24, 1998
    Assignee: Takeda Chemical Industries Ltd.
    Inventors: Muneo Takatani, Hitoshi Ikeda, Kyoko Iida, Hidenori Abe
  • Patent number: 5820781
    Abstract: R.sub.1 --A--(X).sub.m --(B).sub.n --R.sub.2 (I)R.sub.3 --J--(Y).sub.p --(Z).sub.q --R.sub.4 (II)Liquid crystal compounds of formula (I) are described, where formula (I) is given as R.sub.1 --A--(X).sub.m --(B).sub.n --R.sub.2 where A is selected from nathyl, fluorinated naphthyl, brominated naphthyl, B is selected from phenyl, methylated phenyl, brominated phenyl, fluorinated phenyl, thiophene, pyrimidine and pyridine, R.sub.1 and R.sub.2 are independently selected from alkyl, alkoxy, alkynyl, thioalkyl, Br, CN, SCN, NCS, perfluoroalkyl, perfluoroalkoxy and hydrogen, X is selected from C.tbd.C, COO and C.tbd.C, m is 0 or 1, n is 0 or 1 where m is 1 and n is 0 where m is 0; provided that where A is naphthyl, n is 1 and m is 0 then B is selected from methylated phenyl, brominated phenyl, thiophene, pyrimidine and pyridine; and further provided that where A is naphthyl, X is C.tbd.C, m is 1 and n is 1, then B is selected from thiophene, pyrimidine and pyridine.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 13, 1998
    Assignee: The Secretary of State for Defence in her Britannic Majesty's Government of the United Kingdom of Great Britain & Northern Ireland
    Inventors: Kenneth Johnson Toyne, John William Goodby, Alexander Seed, George William Gray, Damien Gerad McDonnel, Edward Peter Raynes, Sally Elizabeth Day, Kenneth John Harrison, Michael Hird
  • Patent number: 5777118
    Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: July 7, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5726128
    Abstract: 1. A benzyloxypyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.3 -C.sub.5 alkenyloxy, C.sub.1 -C.sub.4 alkylthio, or cyano;each X, which may be identical or different if n is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, or C.sub.1 -C.sub.4 haloalkyl;each Y, which may be identical or different if m is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, or C.sub.1 -C.sub.4 haloalkoxy;G represents O or S; andn and m each independently represent an integer of 0 to 5.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: March 10, 1998
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Masato Arahira
  • Patent number: 5723412
    Abstract: A 2-benzyloxy-4-phenoxypyrimidine derivative represented by the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.3 -C.sub.5 alkenyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkylthio, cyano, or phenyl;each X, which may be identical or different if n is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, or C.sub.1 -C.sub.4 alkoxy;each Y, which may be identical or different if m is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio, or C.sub.1 -C.sub.4 haloalkylthio; andn and m each independently represent an integer of 0 to 5, which is useful as a herbicide.
    Type: Grant
    Filed: July 13, 1995
    Date of Patent: March 3, 1998
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Masato Arahira
  • Patent number: 5719285
    Abstract: Polychloropyrimidines, in particular 4,6-dichloropyrimidine and 2,4,6-trichloropyrimidine, are obtained in a particularly advantageous manner from polyhydroxypyrimidines or tautomeric keto compounds thereof and excess phosphorus oxychloride in the presence of a tertiary amine if, in this reaction,a) 0.75 to 1.5 mol of phosphorus trichloride and 0.7 to 1.
    Type: Grant
    Filed: August 11, 1995
    Date of Patent: February 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventor: Guido Steffan
  • Patent number: 5714606
    Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: February 3, 1998
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Oscar L. Acevedo, Normand Hebert
  • Patent number: 5707995
    Abstract: Compounds of formula (I) in which X.sup.1 and X.sup.2 each represents oxygen; S(O).sub.n, n being 0, 1 or 2; or CO, CH.sub.2 or NR, R being hydrogen or alkyl; R.sup.1 and R.sup.10 are each hydrogen or halogen; R.sup.2 and R.sup.9 are each hydrogen, halogen, cyano, nitro, alkyl, halo-alkyl, alkoxy, alkylthio, amino, mono- or di-alkylamino, alkoxyalkyl, haloalkoxyalkyl or alkoxycarbonyl; R.sup.3 and R.sup.8 are each hydrogen, chlorine, alkyl, haloalkyl, haloalkenyl, halo-alkynyl, haloalkoxy, haloalkoxycarbenyl, haloalkylthio, haloalkoxyalkyl, haloalkylsulphinyl, or haloalkylsulphonyl, nitro or cyano; R.sup.4 and R.sup.7 are each hydrogen, halogen, alkyl or alkoxy; R.sup.5 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulphonyl or phenyl; and R.sup.6 is hydrogen or, when R.sup.5 is hydrogen, alkyl; provided that either each phenyl is unsubstituted or at least one of R.sup.3 and R.sup.8 is not hydrogen, have useful pesticidal activity.
    Type: Grant
    Filed: July 24, 1995
    Date of Patent: January 13, 1998
    Assignee: American Cyanamid Company
    Inventors: David Munro, Royston Davis, Janet Anne Day, Jacqueline Anne Wilkin, William W. Wood
  • Patent number: 5700295
    Abstract: The invention relates to compounds of formula ##STR1## wherein the variables have the meanings given in the claims. The compounds are suitable for use as UV absorbers for the photochemical stabilisation of undyed, dyed or printed textile fiber materials and for enhancing the sun protection factor thereof.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: December 23, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Francesco Fuso, Gerhard Reinert
  • Patent number: 5674870
    Abstract: Previously unknown anti-tumor, anti-infectious, immune system modulatory and anti-depressive properties of a family of barbituric acid derivatives are provided herein. Preferred derivatives are 4,6(1H, 5H)-pyrimidinedione, 1,3-dibutyldihydro-2thioxo; and 4,5,6(1H)-pyrimidinetrione, 1,3-dibutyldihydro-2thioxo. These compounds are effective for killing tumor cells, especially carcinoma (breast and prostate cancer), lymphoma and leukemia cells; for killing pathogenic organisms, especially viruses; for stimulating T cell formation and for alleviating symptoms of depression and are readily tolerated by the animal being treated.
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: October 7, 1997
    Inventor: Kirpal S. Gulliya
  • Patent number: 5667722
    Abstract: An antiferroelectric liquid crystal compound represented by the following general formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having 6 to 16 carbon atoms; R.sup.2 represents a straight chain alkyl group having 3 to 8 carbon atoms or a branched alkyl group having 4 to 10 carbon atoms; and * means an asymmetric carbon atom, and an antiferroelectric liquid crystal composition comprising at least one liquid crystal compound as defined above. The optically active compound of the present invention is highly miscible with a number of known antiferroelectric liquid crystal compounds and thus capable of providing liquid crystal materials having improved temperature properties. A liquid crystal composition containing the optically active compound of the present invention is applicable to electro-optical devices with the use of antiferroelectric liquid crystals.
    Type: Grant
    Filed: May 23, 1996
    Date of Patent: September 16, 1997
    Assignee: Takasago International Corporation
    Inventors: Yukiharu Iwaya, Mamoru Yamada, Hitoshi Kondo, Toshimitsu Hagiwara
  • Patent number: 5614541
    Abstract: New catechol derivatives and pharmaceutically acceptable salts and esters thereof useful as pharmaceutical antioxidants are disclosed. Cellular damage by oxygen derived radicals is a significant factor in heart disease, rheumatoid arthritis, cancer, inflammatory disease, transplant rejection reactions and ischemia.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: March 25, 1997
    Assignee: Orion-yhtym a Oy
    Inventors: Reijo B ackstr om, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
  • Patent number: 5552546
    Abstract: A salt of 2-ethoxy-4,6-dihydroxypyrimidine (DHEP) is prepared by contacting a salt of O-ethylisourea with dimethyl malonate in the presence of a methoxide base to form the salt of DHEP. The salt of DHEP can optionally be protonated with an acid to form neutral DHEP. The reaction is typically conducted in a methanol solvent at a temperature less than about 30.degree. C. Typically, the monosodium salt of DHEP is prepared by contacting O-ethylisourea hydrochloride with dimethyl malonate in the presence of sodium methoxide and methanol solvent.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: September 3, 1996
    Assignee: DowElanco
    Inventors: Douglas L. Pearson, Jon A. Orvik, Gary A. Roth, Carmen A. Scott, Ron B. Leng, Dawn L. Shiang
  • Patent number: 5494888
    Abstract: The present invention relates to 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid iminoester derivative of the general formula I; process of their preparation and a method for their application as herbicides: ##STR1## wherein R and Q are as defined in the specification.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: February 27, 1996
    Assignee: Lucky Ltd.
    Inventors: Chang U. Hur, Jin H. Cho, Ho S. Lee, Sang K. Yoo, Su M. Hong, Hong W. Kim, Jae S. Rim, Yeong T. Bae, Sang H. Chae, Jeong S. Kim, Byoung B. Lee, Hun S. Oh, Woo B. Choi
  • Patent number: 5463055
    Abstract: A process is described for the production of 2-ethoxy-4,6-dihydroxypyrimidine or its alkali salt which is an important intermediate in the field of pharmaceuticals and agrochemicals. This compound can be produced using the process according to the invention in good yields and high purity by reacting an O-ethylisourea salt that is preferably formed as an intermediate from cyanamide or chloroformamidinium salts or free O-ethylisourea with an alcoholate and a malonic acid dialkyl ester or a salt of the malonic acid dialkyl ester in alcohol and, if desired, subsequent acidification.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: October 31, 1995
    Assignee: SKW Trostberg Aktiengesellschaft
    Inventors: Helmut Hintermaier, Ursula Maier, Stefan Weiss
  • Patent number: 5459265
    Abstract: There is disclosed a silver halide photographic light-sensitive material having a hydrophilic colloid layer containing a dye which is photochemically inactive and can readily be decolored and/or eluted in a photographic processing course. The silver halide photographic light-sensitive material comprises a hydrophilic colloid layer containing at least one dye dispersed in the form of a solid fine particle represented by Formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, L.sub.1, L.sub.2, L.sub.3 are defined in the disclosure.In a preferred embodiment, the maximum absorption wavelength .lambda.max of the dye in the hydrophilic colloid layer satisfies the following equation:.lambda.max>[.lambda.max(DMF)+20.times.(n+1)] nmwherein .lambda.max(DMF) and n are defined in the disclosure. There is also disclosed an oxonol compound which is useful as a dye.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: October 17, 1995
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Koji Wariishi, Keiichi Suzuki
  • Patent number: 5439908
    Abstract: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, O or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: August 8, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna
  • Patent number: 5420133
    Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: May 30, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
  • Patent number: 5395926
    Abstract: Compounds of formula ##STR1## wherein R is hydrogen or a group ##STR2## M.sub.1 and M.sub.2 are each independently of the other an alkali metal or alkaline earth metal or aluminum or a group of formula ##STR3## wherein n is 1, 2 or 3, and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or C.sub.1 -C.sub.8 alkyl,X.sub.1 and X.sub.2 are each independently of the other --N.dbd. or --CH.dbd.,Q.sub.1 and Q.sub.2 are each independently of the other radicals of formula ##STR4## These compounds have excellent suitability for pigmenting organic material of high molecular weight, preferably polyolefins, and have superior lightfastness.
    Type: Grant
    Filed: September 22, 1993
    Date of Patent: March 7, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Stefan Hari, Olof Wallquist