Boron Or Silicon Containing Patents (Class 544/229)
  • Patent number: 6943250
    Abstract: Anionic polymerization initiators useful in the preparation of polymers having a protected amine functional group. The amine functionality is part of a heterocyclic radical and includes a protecting group.
    Type: Grant
    Filed: March 6, 2001
    Date of Patent: September 13, 2005
    Assignee: FMC Corporation
    Inventor: Thorsten Werner Brockmann
  • Patent number: 6916555
    Abstract: In an organic luminescence device formed of one or plural layers of organic films between an anode and a cathode, at least one layer is any one of a luminescence layer, an electron injection layer and an electron-transporting layer and is formed of at least a spiro compound of formula (I-a) or (I-b) having a carbon atom or a silicon atom as a spiro atom and having four ring structures including at least one nitrogen atom-containing ring structure. By the use of the spiro compound of the formula (I-a) or (I-b), the resultant organic luminescence device produces a high-luminance fluorescent luminescence at a low voltage for a long period of time.
    Type: Grant
    Filed: March 12, 2003
    Date of Patent: July 12, 2005
    Assignee: Canon Kabushiki Kaisha
    Inventors: Koichi Suzuki, Akihiro Senoo, Kazunori Ueno
  • Patent number: 6916925
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 12, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Patent number: 6911551
    Abstract: The present invention relates to substituted boron or aluminum spiro compounds and their use in the electronic industry. The compounds of the invention are used as electron transport material, hole blocking material and/or as host material in organic electroluminescence and/or phosphorescence devices, as electron transport material in photocopiers, as electron acceptor or electron transport material in solar cells, as charge transport material in organic ICs (circuits) and in organic solid-state lasers or organic photodetectors.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: June 28, 2005
    Assignee: Covion Organic Semiconductors GmbH
    Inventors: Philipp Stössel, Hubert Spreitzer, Heinrich Becker, Jacqueline Drott
  • Patent number: 6844437
    Abstract: The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-flourophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R,6S)-2,2-dimethyl[1,3]-dioxan-4-yl)acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.
    Type: Grant
    Filed: February 15, 2000
    Date of Patent: January 18, 2005
    Assignees: Astrazeneca AB, Shionogi & Co. Ltd.
    Inventors: Nigel P Taylor, Loius J Diorazio, Haruo Koike, Mikio Kabaki
  • Patent number: 6818631
    Abstract: Fungicidal pyrimidine derivatives and the use as a fungicide of the compounds of formula (1): wherein R1 is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl C3-C6cycloalkyl, C1-C6alkoxy, C3-C6cycloalkoxy, C1-C6alylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, phenyl, pyridinyl or azolyl groups, (being optionally substituted by one or more substituents); or N(R4)C(O)R5, R2 is polyfluoroalkyl, R3 is fluorine, chlorine, bromine or iodine; ethenyl or ethynyl (being optionally substituted by one or more of halogen), R4 and R5 are, independently, H, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl groups, (being optionally substituted by one or more of halogen or cyano); or R4 and R5 can join together to form a 5 or 6-membered ring, Q is a heteroaromatic ring selected from the following ring system; imidazol-1-yl, pyrazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-1-yl, benzimidazol-1-yl or tetrazol-5-yl groups, (being optionally substituted by one or more of substituents).
    Type: Grant
    Filed: August 15, 2003
    Date of Patent: November 16, 2004
    Assignee: Nippon Soda Co. Ltd.
    Inventors: Yuki Nakagawa, Sergey Bobrov, Charles R. Semer, IV, Thomas A. Kucharek, Masahiro Haramoto
  • Publication number: 20040224923
    Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.
    Type: Application
    Filed: December 18, 2003
    Publication date: November 11, 2004
    Inventors: Ving Lee, Stephen J. Benkovic
  • Patent number: 6815514
    Abstract: The invention describes ligands of formula (I), wherein LIG represents an &eegr;5-ligand substituted by a group R1 and a group (R″)m; X represents a 1 to 3 atom bridge; Y represents a nitrogen or phosphorus atom; Z represents a carbon, nitrogen or phosphorus atom.
    Type: Grant
    Filed: May 28, 2003
    Date of Patent: November 9, 2004
    Assignee: Borealis Technology Oy
    Inventors: Ove Andell, Janne Maaranen, Jouni Hoikka, Tiina Vanne, Soile Rautio
  • Patent number: 6787544
    Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: September 7, 2004
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura
  • Patent number: 6774130
    Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: August 10, 2004
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Stephen J. Klaus, Anil M. Kumar, Baoqing Gong
  • Publication number: 20040147744
    Abstract: Pyrimidines of formula I 1
    Type: Application
    Filed: July 9, 2003
    Publication date: July 29, 2004
    Inventors: Klaus-Juergen Pees, Waldemar Pfrengle, Gavin Heffernan
  • Patent number: 6747150
    Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
    Type: Grant
    Filed: March 19, 2003
    Date of Patent: June 8, 2004
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Patent number: 6747033
    Abstract: Compounds of formula I in which R1 is alkyl, alkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, trihydrocarbylsilyl, formyl, alkanoyl or alkoxycarbonyl group being attached either to the nitrogen in the 3- or 4-position; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic groups containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R3 is phenyl, cycloalkyl or 5- or 6-membered heteroaryl containing besides carbon atoms one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R4 is halogen, amino, alkoxy, haloalkoxy, alkylamino or dialkylamino; wherein the bent line indicates that the double Bond may be located between the 3- and 9-position or the 4- and 9-Position; and the zigzag line indicates that the groups connected may have the (E)- or (Z)-configuration; R
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: June 8, 2004
    Assignee: BASF Aktiengesellschaft
    Inventor: Waldemar Pfrengle
  • Patent number: 6737124
    Abstract: Chiral nonracemic, chiral racemic and achiral compounds useful as component of LC compositions which have a silane tail group which is partially fluorinated. The silane tail group comprises a perfluoroalkyl group. The silane tail group of this invention has the formula: where k is 0 or an integer ranging from 1-10; m and n are integers ranging from 1 to about 20; j is 0 or an integer ranging from 1 to 20; Z is —O— or a single bond; R1, R1′, R2 and R2′ are alkyl groups or perfluorinated alkyl groups; and RF is a perfluorinated alkyl group. The invention also provides LC compositions comprising one or more compounds of the invention with partially fluorinated silane tails. The invention also provides optical devices, particularly display devices which contain an aligned layer of an LC composition comprising one or more silane compounds of this invention.
    Type: Grant
    Filed: January 3, 2001
    Date of Patent: May 18, 2004
    Assignee: Displaytech, Inc.
    Inventors: Neil Gough, Xin-Hua Chen, William N. Thurmes, Michael Wand
  • Publication number: 20040091785
    Abstract: The invention relates to a method of preparing lithium complex salts and their intermediaries and to the use of these in electrolytes.
    Type: Application
    Filed: October 31, 2003
    Publication date: May 13, 2004
    Inventors: Andrei Leonov, Armin de Meijere, Michael Schmidt
  • Patent number: 6727241
    Abstract: The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1&agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.
    Type: Grant
    Filed: June 12, 2002
    Date of Patent: April 27, 2004
    Assignee: Chemocentryx
    Inventor: Brian McMaster
  • Patent number: 6699835
    Abstract: The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: March 2, 2004
    Assignees: The United States of America as represented by the Department of Health and Human Services, Millennium Pharmaceuticals, Inc.
    Inventors: Louis Plamondon, Louis Grenier, Julian Adams, Shanker Lal Gupta
  • Patent number: 6699855
    Abstract: The present invention relates to compounds of Formula (I): wherein A1 is methylene, ethylene or propylene group and A2 is N or CR5, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HCV NS3 protease, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: March 2, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiaojun Zhang, Wei Han
  • Publication number: 20040038940
    Abstract: The invention relates to processes for preparing a compound of the formula (V) 1
    Type: Application
    Filed: June 3, 2003
    Publication date: February 26, 2004
    Applicant: Pfizer Inc.
    Inventors: Stephane Caron, Jolanta Nowakowski
  • Patent number: 6696447
    Abstract: The present application describes compounds of general formula I where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on the ring system. The invention also includes enantiomers, salts and pharmaceutical compositions containing the compounds. The compounds may be used in treating patients for pain.
    Type: Grant
    Filed: September 27, 2002
    Date of Patent: February 24, 2004
    Assignee: AstraZeneca AB
    Inventors: William Brown, Niklas Plobeck, Christopher Walpole
  • Publication number: 20040024214
    Abstract: Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of the formula: 1
    Type: Application
    Filed: December 9, 2002
    Publication date: February 5, 2004
    Applicant: Medivir AB
    Inventors: M. Robert Leanna, Michael Rasmussen, Howard Morton, Zhenping Tian, Daniel Plata, Bradley D. Gates, Bikshandarkoil A. Narayanan
  • Patent number: 6680401
    Abstract: The invention relates to processes for the synthesis of aryl or alkene borates which comprises reacting: (i) an olefinic compound having a halogen or halogen-like substituent in a vinylic substitution position, or (ii) an aromatic ring having a halogen or halogen-like substituent in a ring substitution position, with a disubstituted monohydroborane in the presence of a Group 8-11 metal catalyst. The invention also relates to the use of these borates in coupling reactions. The invention further relates to certain disubstituted monohydroboranes and aryl or alkene borates.
    Type: Grant
    Filed: August 13, 2001
    Date of Patent: January 20, 2004
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Sebastian Mario Marcuccio, Mary Rodopoulos, Helmut Weigold
  • Publication number: 20040006047
    Abstract: What is described are amides of the formula (I) and salts thereof, 1
    Type: Application
    Filed: September 26, 2002
    Publication date: January 8, 2004
    Inventors: Wolfgang Schaper, Marion Beckmann, Uwe Doller, Gerhard Krautstrunk, Daniela Jans, Waltraud Hempel, Jutta Maria Waibel
  • Patent number: 6660738
    Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: December 9, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow
  • Publication number: 20030225275
    Abstract: The invention describes ligands of formula (I), wherein LIG represents an &eegr;5-ligand substituted by a group R1 and a group (R″)m; X represents a 1 to 3 atom bridge; Y represents a nitrogen or phosphorus atom; Z represents a carbon, nitrogen or phosphorus atom.
    Type: Application
    Filed: May 28, 2003
    Publication date: December 4, 2003
    Inventors: Ove Andell, Janne Maaranen, Jouni Hoikka, Tiina Vanne, Soile Rautio
  • Patent number: 6653295
    Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: November 25, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
  • Publication number: 20030199691
    Abstract: 1
    Type: Application
    Filed: April 7, 2003
    Publication date: October 23, 2003
    Inventors: Michael Brandt, Georg Fertig, Hans-Willi Krell, Thomas von Hirschheydt, Edgar Voss
  • Patent number: 6630588
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds are useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: October 7, 2003
    Assignee: 3M Innovative Properties Company
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Publication number: 20030162281
    Abstract: Intermediate compounds, including 2-(t-butyldimethylsilyloxymethyl)-3,4-[(dimethylmethylene)dioxy]-5-hydroxy-tricyclo[5.2.1.02,6]dec-8-ene, which are useful for the synthesis of neplanocin A having strong antitumor activity. Improved processes for the preparation of neplanocin A, starting from optically active 2-hydroxymethyl-5-hydroxy-tricyclo[5.2.1.02,6]deca-3,8-diene and via a key step comprising a retro-Diels-Alder reaction of the above intermediate.
    Type: Application
    Filed: February 21, 2003
    Publication date: August 28, 2003
    Applicant: CHISSO CORPORATION
    Inventors: Naoyuki Yoshida, Kunio Ogasawara
  • Publication number: 20030144246
    Abstract: This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1 represents alkyl or cycloalkylalkyl, R2 and R3 each independently represent alkyl or cycloalkyl or taken together with the adjacent carbon atom represent a saturated 3- to 6-membered carbocyclic or heterocyclic ring, the alkyl, cycloalkyl, carbocyclic or heterocyclic ring being unsubstituted or substituted, and R4 represents hydrogen, halogen cyano, alkyl, alkylthio, alkenyl, alkynyl, hydroxyalkyl, hydroxyalkynyl, alkoxyalkyl, alkoxyalkynyl, trialkylsilyl, aryl or heteroaryl, and pharmaceutically acceptable acid addition salts of these compounds, their use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addi
    Type: Application
    Filed: October 28, 2002
    Publication date: July 31, 2003
    Inventors: Peter Mohr, Philippe Pflieger
  • Patent number: 6599354
    Abstract: The present invention relates to new alkoxysilane-functional piperazinone derivatives, a process for their production, as well as their use as additives in sealants, adhesives, lacquers or coating agents.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: July 29, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Schmalstieg, Ralf Lemmerz, Ulrich Walter, Oswald Wilmes
  • Patent number: 6596727
    Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides The invention relates to compounds of the formula in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: July 22, 2003
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin
  • Publication number: 20030130512
    Abstract: A process for preparing purine derivatives, such as famciclovir and penciclovir, by reacting two intermediates and using a palladium(0) catalyst and a ligand. Intermediates useful in the process are also claimed.
    Type: Application
    Filed: February 19, 2003
    Publication date: July 10, 2003
    Inventors: Richard Freer, Graham Richard Geen, Thomas Weir Ramsay, Andrew Colin Share, Neil Michael Smith
  • Publication number: 20030100768
    Abstract: The present invention relates generally to a novel class of imidazolidinones of Formula (I): 1
    Type: Application
    Filed: December 12, 2001
    Publication date: May 29, 2003
    Inventors: Amy Qi Han, Peter W. Glunz
  • Patent number: 6569859
    Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: May 27, 2003
    Assignee: President and Fellows of Harvard College
    Inventor: Elias J. Corey
  • Publication number: 20030092676
    Abstract: 1
    Type: Application
    Filed: May 21, 2002
    Publication date: May 15, 2003
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
  • Publication number: 20030078235
    Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.
    Type: Application
    Filed: June 21, 2002
    Publication date: April 24, 2003
    Inventors: Yong-Moon Choi, Ki-Ho Lee
  • Patent number: 6551761
    Abstract: This invention relates to &agr;-ammonium ketones, iminium ketones or amidinium ketones in the form of their tetraaryl- or triarylalkylborate salts which can be photochemically converted into amines, imines or amidines as well as to a process for their preparation. This invention also relates to base-polymerisable or crosslinkable compositions comprising these &agr;-ammonium ketones, iminium ketones or amidinium ketones in the form of their tetra- or triarylalkylborate salts, to a process for carrying out photochemically induced, base-catalysed reactions as well as to their use as photoinitiators for base-catalysed reactions.
    Type: Grant
    Filed: September 7, 2000
    Date of Patent: April 22, 2003
    Assignee: Ciba Specialty Chemical Corporation
    Inventors: Véronique Hall-Goulle, Sean Colm Turner, Allan Francis Cunningham
  • Patent number: 6548668
    Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
    Type: Grant
    Filed: March 18, 2002
    Date of Patent: April 15, 2003
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Publication number: 20030064962
    Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): 1
    Type: Application
    Filed: December 12, 2001
    Publication date: April 3, 2003
    Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
  • Patent number: 6534506
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 6, 2001
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Diem N. Nguyen, Craig A. Stump, Theresa M. Williams
  • Publication number: 20030022864
    Abstract: A compound of Formula I 1
    Type: Application
    Filed: April 24, 2001
    Publication date: January 30, 2003
    Inventors: Khalid S. Ishaq, George J. Cianciolo
  • Publication number: 20030018032
    Abstract: Substituted bicyclic imidazo-3-yl-amines and medicaments comprising these compounds, useful, inter alia, as analgesics.
    Type: Application
    Filed: April 8, 2002
    Publication date: January 23, 2003
    Applicant: GRUENENTHAL GMBH
    Inventors: Matthias Gerlach, Corinna Maul
  • Publication number: 20030018198
    Abstract: Provided are a borosuccinimide compound obtained through reaction of (a) a succinic acid/anhydride substituted with an alkyl or alkenyl group having a number-average molecular weight of from 200 to 5,000, (b) a polyalkylene-polyamine of which at least 5 mol % has a terminal cyclic structure, and (c) a boron compound; and a succinimide compound obtained through reaction of (A) a succinic acid/anhydride substituted with an alkyl or alkenyl group having a molecular weight of from 200 to 5,000, with (D) a hydrocarbon-substituted polyalkylene-polyamine. These compounds are stable even at high temperatures and have good high-temperature detergency, and they are useful for ashless detergent dispersants having the ability to disperse fine particles. Also provided are a mixture of any of these compounds and a specific ester derivative; a lubricant additive and a fuel oil additive comprising the mixture as the essential ingredient; and a lubricant and a fuel oil composition containing the additive.
    Type: Application
    Filed: May 22, 2002
    Publication date: January 23, 2003
    Inventors: Hiroaki Koshima, Ikumi Terada
  • Publication number: 20030018012
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula I: 1
    Type: Application
    Filed: December 13, 2001
    Publication date: January 23, 2003
    Inventors: Michael J. Ricks, William H. Dent, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpattick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Matthew J. Henry, Jenifer L. Adamski Butz, Robert P. Gajewski
  • Publication number: 20030009029
    Abstract: The present invention relates to a process preparing compounds of the general formula (I) 1
    Type: Application
    Filed: June 5, 2002
    Publication date: January 9, 2003
    Applicant: Merck Patent GmbH
    Inventors: Herwig Buchholz, Urs Welz-Biermann
  • Publication number: 20030004137
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: January 2, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6489081
    Abstract: Compounds of formula I wherein R1, R2, and R3 independently of one another are hydrogen; C1-C20alkyl which is unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-8alkyl)O—(CO)—, (C1-C4alkyl)—(CO)O— or/and di(C1-C4alkyl)amino; or R1, R2, and R3 independently of one another are C3-C6alkenyl; phenyl which is unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-C8alkyl)O(CO)—, (C1-C4alkyl)—(CO)O— or/— and di(C1-C4alkyl)amino; or R1 and R2 together are C2-C9alkylene, o-xylylene, 2-butenylene, C3-C9oxaalkylene or C3-C9azaalkylene; R4, R5, R6, and R7 independently of one another are sec-C3-C20alkyl, tert-C4-C20alkyl or phenyl wherein these radicals are unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-C8alkyl)O(CO)—, (C1-C4alkyl)—(CO)O— or/and di(C1-C4alkyl)amino; or R4 and R5, and/or R6 and R7
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: December 3, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Akira Matsumoto, Yoshihiko Ito
  • Patent number: 6441169
    Abstract: Novel pyrimidin-4-one and pyrimidin-4-thione derivatives of formula (I) wherein A is phenyl, thienyl (including all 3 isomers), thiazolyl or pyridyl; X is oxygen or sulfur; R1 is hydrogen, halogen or trimethylsilyl; R2 is hydrogen, halogen or trimethysilyl; and at least one of R1 and R2 is not hydrogen; R3 is C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6haloalkenyl, C2-C6alkynyl, C2-C6haloalkynyl, —(CH2)n—C3-C8cycloalkyl which are unsubstitituted or substituted by halogen, C1-C6alkyl or C1-C6haloalkyl, C1-C4alkoxy-C1-C6alkyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkythio-C1-C6alkyl; C1-C4alkylthio-C2-C6alkenyl; C1-C4alkythio-C2-C6alkynyl; mono-C1-C4alkylamin-C1-C6alkyl; mono-C1-C4alkylamin-C1-C6alkenyl; mono-C1-C4alkylamin-C2-C6alkynyl; —(CH2)n—C1-C4alkoxy-C3-C6cycloalkyl; —(CH2)n—C1-C4alkylthio-C3-C6cycloalkyl; —(CH2)2-mono-C1-C4alkylamin-C3-C6cycloalkyl; or N═CR9R10; n is 1, 2, 3, or 4; R4, R5, R6, R7, and R8 are each independently of the
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: August 27, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Harald Walter
  • Patent number: 6437125
    Abstract: The invention provides a method of rearranging a compound of formula (I), wherein R and R′ are selected independently from hydrogen and C1-12alkyl; and R1 and R2 are selected independently from hydrogen, hydroxy, halo, C1-12alkyl- or aryl carbonate, amino, mono- or di-C1-12alkylamino, C1-12alkyl or arylamido, C1-12alkyl- or arylcarbonyl, C1-12alkyl- or arylcarboxy, C1-12alkyl- or arylcarbamoyl, C1-12alkyl, C2-12alkenyl, C2-12alkynyl, aryl, heteroaryl, C1-12alkoxy, aryloxy, azido, C1-12alkyl- or arylthio, C1-12alkyl- or arylsulfonyl, C1-12alkyl- or arylsilyl, C1-12alkyl- or arylphosphoryl, and phosphato; to form a compound of formula (II), wherein R, R′, R1 and R2 are as defined for formula (I); said method comprising treating the compound of formula (I) with a palladium (0) catalyst and a (diphenylphosphino)nC1-6 alkane, wherein n is an integer of 1-6. The invention also provides methods of R making penciclovir and famciclovir using this rearrangement reaction.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: August 20, 2002
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventors: Graham Richard Geen, Andrew Colin Share