At 2-position And At 4- Or 6-position Patents (Class 544/309)
  • Patent number: 6380387
    Abstract: Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: April 30, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 6376667
    Abstract: Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.
    Type: Grant
    Filed: November 24, 1998
    Date of Patent: April 23, 2002
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Hui Shao
  • Publication number: 20020045753
    Abstract: A compound of the formula 1
    Type: Application
    Filed: September 4, 2001
    Publication date: April 18, 2002
    Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Patent number: 6372691
    Abstract: The present invention relates to a method for controlling weeds in corn field which comprises applying a herbicidal composition comprising 2-[2-chloro-4-fluoro-5-{3-methyl-2,6-dioxo-4-(trifluoromethyl)-1,2,3,6-tetrahydropyrimidin-1-yl}phenoxy]propionic acid ester as an active ingredient to corn fields after seeding corn. According to the present method, kinds of weeds in corn fields can be controlled widely and no problematic phytotoxicity to corn is caused.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: April 16, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 6362337
    Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: March 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Otto Schallner, Katharina Voigt, Markus Dollinger, Hans-Joachim Santel
  • Publication number: 20020035109
    Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-,states characterized by thrombotic activity.
    Type: Application
    Filed: August 7, 2001
    Publication date: March 21, 2002
    Applicant: Berlex Laboratories, Inc.
    Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
  • Publication number: 20020032210
    Abstract: 1 The present invention discloses compounds having formula (I) wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
    Type: Application
    Filed: April 19, 2001
    Publication date: March 14, 2002
    Inventors: Bjarne H. Dahl, Palle Christophersen
  • Patent number: 6355799
    Abstract: Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: March 12, 2002
    Assignee: ISK Americas Incorporated
    Inventors: Sandeep Gupta, Shao-Yong Wu, Masamitsu Tsukamoto, David A. Pulman, Bai-Ping Ying
  • Patent number: 6355796
    Abstract: An improved process and intermediate compounds for the preparation of 2-(N,N-disubstituted)amino-4-(perfluoroalkyl)-1,3-oxazin-6-one compounds having the structural formula I and an improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having the structural formula V
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: March 12, 2002
    Assignee: BASF Aktiengesellschaft
    Inventor: Venkataraman Kameswaran
  • Publication number: 20020022727
    Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) 1
    Type: Application
    Filed: February 14, 2001
    Publication date: February 21, 2002
    Inventors: Bernd Gallenkamp, Reinhard Lantzsch, Lothar Rohe, Lubbertus Mulder
  • Patent number: 6348471
    Abstract: The invention relates to novel pyrimidyloxyphenylacetic acid derivatives, to a plurality of processes for their preparation and to their use to fungicides, and also to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 12, 2000
    Date of Patent: February 19, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Ralf Tiemann, Astrid Mauler-Machnik, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 6344460
    Abstract: The present invention provides compounds comprising propynyl uracils having the formula wherein R1 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R2 is iodine or bromine; and R3 is propynyl, 3-iodopropynyl, 3-bromopropynyl, substituted or unsubstituted 2-furanyl, substituted or unsubstituted 3-furanyl, substituted or unsubstituted 2-pyrrolidinyl, substituted or unsubstituted 3-pyrrolidinyl, D-ribose, or deoxyribose. Another embodiment of the invention encompasses propynyl uracils having the formula wherein R4 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R5 is hydrogen or propynyl; and R6 is iodine or bromine. Also, methods of preparing these propynyl uracils are provided.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: February 5, 2002
    Assignee: Lonza Inc.
    Inventor: Peter C. Nirchio
  • Publication number: 20020009748
    Abstract: Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally through employment of a tether moiety. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.
    Type: Application
    Filed: May 13, 1998
    Publication date: January 24, 2002
    Inventor: PHILLIP DAN COOK
  • Publication number: 20020010334
    Abstract: A process for the preparation of a compound of formula I 1
    Type: Application
    Filed: June 22, 2001
    Publication date: January 24, 2002
    Inventor: Xun Li
  • Publication number: 20020007070
    Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: 1
    Type: Application
    Filed: April 6, 2001
    Publication date: January 17, 2002
    Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
  • Patent number: 6339155
    Abstract: The uracil compounds represented by the formula [V]: wherein R1 represents C1-C5 perfluoroalkyl group and Q represents an aromatic group, can be produced by making the amide compounds represented by the formula [II]: wherein R1 and Q have the same meanings defined above, or its hydrate react with a cyanate salt in the presence of a protonic acid.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: January 15, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Hirofumi Mishima
  • Publication number: 20020004503
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: April 18, 2001
    Publication date: January 10, 2002
    Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
  • Patent number: 6329418
    Abstract: The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure according to the following Formula (I): wherein R1, R2, X, Z, m, and n are defined below. to This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of diseases and conditions which are characterized by unwanted metalloprotease activity. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for metalloprotease-related maladies using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: December 11, 2001
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Michael George Natchus, Biswanath De, Neil Gregory Almstead, Yetunde Olabisi Taiwo, Stanislaw Pikul
  • Patent number: 6313072
    Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.
    Type: Grant
    Filed: February 18, 1999
    Date of Patent: November 6, 2001
    Assignee: American Cyanamid Company
    Inventors: Stephen Scheiblich, Thomas Maier, Axel Kleemann, Helmut Siegfried Baltruschat
  • Patent number: 6313295
    Abstract: An improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having the structural formula I from carbamate compounds having the structural formula II
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: November 6, 2001
    Assignee: BASF Aktiengesellschaft
    Inventor: Venkataraman Kameswaran
  • Patent number: 6306866
    Abstract: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
    Type: Grant
    Filed: March 6, 1998
    Date of Patent: October 23, 2001
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
  • Patent number: 6303783
    Abstract: There are provided 1-(3-heterocyclyphenyl)isothio-urea, -isourea, -guanidine and -amidine compounds of formula I Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.
    Type: Grant
    Filed: August 4, 1999
    Date of Patent: October 16, 2001
    Assignee: American Cyanamid Co.
    Inventor: Gary Mitchell Karp
  • Patent number: 6297223
    Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-fluorouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, iodo, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 aklynyl.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: October 2, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
  • Patent number: 6297377
    Abstract: This invention relates generally to benzocycle-substituted pyrimidines and triazines and the use thereof to protect against degradation by environmental forces, inclusive of ultraviolet light, actinic radiation, oxidation, moisture, atmospheric pollutants and combinations thereof. The new class of benzocycle-substituted pyrimidines and triazines comprises a benzocycle attached to the triazine or pyrimidine ring, and preferably an additional aryl ring containing a hydroxyl group, either free or blocked to form a latent stabilizer, ortho- to the point of attachment to the triazine or pyrimidine ring. These materials may, under the appropriate circumstances, be bonded to formulations comprising coatings, polymers, resins, organic compounds and the like via reaction of the bondable functionality with the materials of the formulation. A method for stabilizing a material by incorporating such benzocycle-substituted pyrimidines and triazines is also disclosed.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: October 2, 2001
    Assignee: Cytec Technology Corporation
    Inventors: Ram B. Gupta, Dennis J. Jakiela, Robert G. Fischer
  • 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: 6277789
    Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: August 21, 2001
    Inventors: Roland Andree, Otto Schallner, Katharina Voigt, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6268374
    Abstract: The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularly useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil.
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: July 31, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
  • Patent number: 6251828
    Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: June 26, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6245714
    Abstract: New substituted phenyl uracils are described which have general formula (I), in which R1 is halogen, or optionally substituted alkyl, R2 is optionally substituted alkyl, R3 is an amino group or optionally substituted alkyl, alkenyl or alkynyl, R4 is a cyano group or halogen, R5 is a cyano group or thiocarbamoyl, R6 group (2) or group (3) in which Q1 and Q2 are oxygen or sulphur, R7 is hydrogen or optionally substituted alkyl, R8 is hydrogen or optionally substituted alkyl, alkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkylsulfonylamino, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkyloxy, cycloalkylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, aryl, aryloxy, arylamino, arylcarbonylamino, arylsulfonylamino, arylalkyl, arylalkoxy or arylalkylamino group, R9 and R10 are alkyl. A method for production of said compounds and their use as herbicides are described.
    Type: Grant
    Filed: November 24, 1998
    Date of Patent: June 12, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark Wilhelm Drewes, Roland Andree, Markus Dollinger
  • Patent number: 6242454
    Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: September 9, 1999
    Date of Patent: June 5, 2001
    Assignee: Berlex Laboratories Inc.
    Inventors: Monica Kochanny, Raju Mohan, Michael M. Morrissey, Howard P. Ng, Weiya Yun
  • Patent number: 6232318
    Abstract: Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: May 15, 2001
    Assignee: Merck & Co., Ltd.
    Inventors: Jennie B. Nerenberg, Mark G. Bock
  • Patent number: 6225470
    Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanediyl, Ar represents optionally substituted aryl, R1 represents optionally substituted alkyl and R2 represents hydrogen, halogen or alkyl, and to novel intermediates for this purpose and to processes for their preparation.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: May 1, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Gallenkamp, Reinhard Lantzsch, Lothar Rohe, Lubbertus Mulder
  • Patent number: 6207830
    Abstract: Aryl- or heteroaryluracils of formula I wherein R1 signifies methyl or ethyl; R2 signifies —CF3, —CClF2, —CCl2F, or —C2F5; and Q is an aryl or heteroaryl group; are produced whereby a compound of formula II O═C═N—Q  (II) is reacted at a temperature of −5° C. to +40° C. with an enamine of formula III wherein R19 signifies C1-C6-alkyl, in the presence of a solvent and of 0.1 to 0.4 equivalents of a base with respect to the employed enamine of formula III. The compounds of formula I are useful as herbicides. An example of the compounds of formula I is 2-chloro-5-(3,6-dihydro-2,6-dioxo-3-methyl-4-trifluoromethyl-1-(2H)pyrimidinyl)-benzoic acid 1-aalyloxycarbonyl-1-methyl-ethyl-ester.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: March 27, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Andrea Rolf Sting
  • Patent number: 6194575
    Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with urea.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: February 27, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Detlef Wollweber, Wolfgang Krämer, Eric Rivadeneira
  • Patent number: 6191275
    Abstract: An improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having the structural formula I from urea compounds having the structural formula II
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: February 20, 2001
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • 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: 6172225
    Abstract: The invention relates to a novel process for producing thereof hydroxyarenes of the general formula (I) in which n represents the numbers 1, 2, 3 or 4, R represents cyano, carboxyl, formyl, nitro, halogen or represents alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylcarbonyl or alkoxycarbonyl, each of which is optionally substituted, and Z represents hydrogen, cyano, nitro, halogen, alkyl, halogenoalkyl, or represents monocyclic or bicyclic, saturated or unsaturated heterocyclyl, heterocyclylamino or heterocyclylimino, each of which is optionally substituted, characterized in that halogenoarenes of the general formula (II) in which n, R and Z are each as defined above and X represents halogen are reacted with 3-hydroxy-propionitrile of the formula (III), HO—CH2CH2—CN  (III), if appropriate in the presence of a reaction auxiliary and if appropriate in the presence of a diluent, at temperatures between 0° C. and 100° C.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: January 9, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Linker, Wilhelm Haas, Otto Schallner, Kurt Findeisen, Roland Andree, Mark Wilhelm Drewes
  • Patent number: 6169182
    Abstract: The invention relates to a novel process for preparing substituted cyanophenyluracils of the general formula (I) in which R1, R2, R3 and R4 are each as defined in the description, said compounds being known as herbicidally active compounds, to novel substituted N-(cyanophenyl)aminoalkenamides as intermediates therefor and to an inventive process for their preparation.
    Type: Grant
    Filed: July 30, 1998
    Date of Patent: January 2, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Reinhard Lantzsch, Heinz-J{umlaut over (u)}rgen Wroblowsky
  • Patent number: 6166014
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: May 19, 1999
    Date of Patent: December 26, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6153619
    Abstract: There are provided compositions and methods comprising compounds of formula I: ##STR1## wherein R.sup.1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: November 28, 2000
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
  • Patent number: 6150382
    Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: May 21, 1999
    Date of Patent: November 21, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6136971
    Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: October 24, 2000
    Assignee: Roche Colorado Corporation
    Inventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
  • Patent number: 6130225
    Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined in the description, to a process for their preparation and to their use as herbicides.
    Type: Grant
    Filed: February 2, 1999
    Date of Patent: October 10, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark-Wilhelm Drewes, Roland Andree, Markus Dollinger
  • Patent number: 6121431
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: September 19, 2000
    Assignee: Medivir AB
    Inventors: Bjorn Olof Classon, Bengt Bertil Samuelsson, Ingemar Sven-Anders Kvarnstrom, Lars Goran Svansson, Stefan Carl Tore Svensson
  • Patent number: 6110870
    Abstract: The invention relates to new N-cyanoaryl-nitrogen hetero-cycles of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description,to a plurality of processes for their preparation, to their use as herbicides and to novel intermediates.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: August 29, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark-Wilhelm Drewes, Albrecht Marhold, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 6103898
    Abstract: Cyclic urea derivatives of the formula I ##STR1## in which X, X', Y, Y' and Z can have various meanings, are prepared by a) reacting a urea derivative of the formula II ##STR2## with a diketone of the formula III ##STR3## and b) hydrogenating the product from step a) in the presence of a metal-containing catalyst.
    Type: Grant
    Filed: September 28, 1998
    Date of Patent: August 15, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Kramer, Wolfgang Siegel
  • Patent number: 6080702
    Abstract: Disclosed are herbicidal heterocyclic benzisoxazoles and benzisoxazolidinones of formula (I): ##STR1## wherein A is (a), (b) or (c); U is N or NR; X is CO or CR.sup.2 ; and R, R.sup.1, R.sup.2, R.sup.3, Y and Z are as disclosed in the disclosure.
    Type: Grant
    Filed: September 14, 1998
    Date of Patent: June 27, 2000
    Assignee: FMC Corporation
    Inventors: George Theodoridis, Lester L. Maravetz, Scott D. Crawford
  • Patent number: 6077812
    Abstract: Novel herbicidal compounds, compositions containing them, and methods for their use in controlling weeds are disclosed. The novel herbicidal compounds are represented by formula I: ##STR1## where J is a 1-substituted-6-trifluoromethyl-2,4-pyrimidinedione-3-yl, a 1-substituted-6-trifluoromethyl-1,3,5-triazine-2,4-dion-1-yl, a 3,4,5,6-tetrahydrophthalimid-1-yl, a 4-difluoromethyl-4,5-dihydro-3-methyl-1,2,4-triazol-5(1H)-on-1-yl, a 5,6,7,8-tetrahydro-1H,3H-[1,3,4]thiadiazolo[3,5-a]pyridazineimin-1-yl, or a 1,6,8-triazabicyclo[4.3.0]-nonane-7,9-dion-8-yl ring attached at the 7 position of a benzofuran, benzoxazole, indole, 2,3-dihydrobenzimidazole or benzimidazole, and X is selected from hydrogen, halogen, cyano, nitro, and amino. Preferred R groups are optionally substituted alkyl groups.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: June 20, 2000
    Assignee: FMC Corporation
    Inventors: Scott D. Crawford, Lester L. Maravetz, George Theodoridis, Benjamin Dugan
  • Patent number: 6069250
    Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are as defined herein.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: May 30, 2000
    Assignee: Biochem Pharma Inc.
    Inventors: Tarek Mansour, Alex Cimpoia, Krzysztof Bednarski
  • Patent number: 6034087
    Abstract: Nucleoside derivatives represented by formula (I); ##STR1## wherein, R.sub.1 represents hydrogen, phosphate or phosphonate group, R.sub.2 represents substituted or unsubstituted pyrimidine or purine base, and Z represents S, SO, SO.sub.2, O or C; or pharmaceutically acceptable salts thereof. Compound (I) can be obtained by reacting a compound of the formula (II); ##STR2## wherein, R.sub.7 represents hydrogen or hydroxy-protecting group, L represents aromatic or nonaromatic acyl, halide or alkoxy, and Z represents S, SO, SO.sub.2, O or C, with a base.
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: March 7, 2000
    Assignee: Chong Kun Dang Corp.
    Inventors: Jung Woo Kim, Chong Ryul Lee, Koo Hun Chung, Soon Kil Ahn, Kyung Hoi Cha, Hoe Joo Son, Sung Jo Choi, Byeong Seon Jeong, Kyeong Bok Min