Benzene Ring Bonded Directly At The 2- Position Of The Diazole Ring Patents (Class 548/310.7)
  • Patent number: 6593476
    Abstract: The present invention relates to a preparation process for 2-arylbenzimidazolesulfonic acids of the formula I: Ar is a substituted or unsubstituted phenyl or naphthyl radical and R is a C1-8-alkyl or C1-8-alkoxy radical. n is 1-4, m is 1-3 and o is 0-2. o-phenylenediamine is reacted in the presence of oleum with an arylcarboxylic acid or an arylcarboxylic acid derivative. Compounds prepared in this way can be used as UV filters, and as components in cosmetic compositions.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: July 15, 2003
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Ulrich Heywang, Michael Schwarz, Frank Pflücker
  • Patent number: 6541499
    Abstract: The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: April 1, 2003
    Assignee: Eli Lilly and Company
    Inventors: Jolie A Bastian, Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Valentine J Klimkowski, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Jeffrey T Mullaney, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Jennifer M Tinsley, Michael R Wiley, Minsheng Zhang
  • Publication number: 20020151720
    Abstract: Novel naphthol derivatives, and various azo compounds and metal complexes prepared by using the derivatives are provided.
    Type: Application
    Filed: January 16, 2002
    Publication date: October 17, 2002
    Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
  • Patent number: 6465484
    Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: October 15, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
  • Patent number: 6440401
    Abstract: Disclosed is a 2-phenyl-benzimidazolesulfonic acid according to the formula in which n is 0, 1 or 2 and m is 2 or 3, R1, R2, R3, R4 and R5, are each a radical such as H, C1-8-alkyl, C1-8-alkoxy, hydroxyl, sulfate, nitro, F, Cl, Br or I radicals, and R6 is a C1-8-alkyl or C1-8-alkoxy radical. This compound can be effectively used as a UV filter, and as part of a cosmetic formulation which comprise these compounds. A process for preparation of the compound is disclosed as well.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: August 27, 2002
    Assignee: Merck Patent Gesellschaft Mit Beschraenkter Haftung
    Inventors: Ulrich Heywang, Michael Schwarz, Frank Pflücker
  • Publication number: 20020099222
    Abstract: Heterocyclically substituted benzoylguanidines of the formula I 1
    Type: Application
    Filed: February 15, 2002
    Publication date: July 25, 2002
    Inventors: Andreas Weichert, Udo Albus, Hans-Willi Jansen, Heinz-Werner Kleemann, Hans-Jochen Lang
  • Patent number: 6387938
    Abstract: This invention provides novel benzimidazole derivatives represented by the formula (I); a process for producing the same; a drug containing at least one of such compounds as its active ingredient, in particular, a drug for preventing and/or treating diseases exhibiting eosinophilia, bronchial asthma and allergic diseases; and an enhancer for IFN-&ggr; production, and in particular, an antitumor agent or an antiviral agent based on the action of enhancing the IFN-&ggr; production which exhibits excellent oral bioavailability.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: May 14, 2002
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Mizuguchi, Nobuo Ohzawa, Yasuhiro Nakai, Kazuyuki Matsuura, Shuhei Ohnishi, Yutaka Kato, Tsutomu Satoh
  • Patent number: 6369235
    Abstract: The present invention provides compositions and methods for the treatment of HIV infection. In particular, the present invention provides non-nucleoside inhibitors of reverse transcriptase (RT), as well as methods to treat HIV infection using these non-nucleoside inhibitors of RT. In preferred embodiments, the present invention provides a novel class of substituted benzimidazoles, effective in the inhibition of human immunodeficiency virus (HIV) RT.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: April 9, 2002
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Marshall Morningstar, Thomas Roth
  • Publication number: 20020007071
    Abstract: This invention provides a series of substituted benzimidazoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides methods employing these substituted benzimidazoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these compounds.
    Type: Application
    Filed: November 30, 2000
    Publication date: January 17, 2002
    Inventors: Thomas Charles Britton, Robert Frederick Bruns, Buddy Eugene Cantrell, Philip Arthur Hipskind, Karen Lynn Lobb, James Arthur Nixon, Paul Leslie Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis Michael Zimmerman, Anne Marie Nunes, James Jeffry Howbert
  • Patent number: 6316620
    Abstract: A new class of chiral bidentate ligands to transition metals is disclosed which compounds have the following structure: wherein the substituents are as defined herein.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: November 13, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Carl A. Busacca
  • Patent number: 6310082
    Abstract: Benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R′ may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: October 30, 2001
    Assignee: Newcastle University Ventures Limited
    Inventors: Roger J Griffin, Alan H Calvert, Nicola J Curtin, David R Newell, Bernard T Golding
  • Publication number: 20010018525
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: January 26, 2001
    Publication date: August 30, 2001
    Inventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa M. Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
  • Patent number: 6271390
    Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.
    Type: Grant
    Filed: May 21, 1999
    Date of Patent: August 7, 2001
    Assignee: Avanir Pharmaceuticals
    Inventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
  • Patent number: 6251689
    Abstract: The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
    Type: Grant
    Filed: May 14, 1999
    Date of Patent: June 26, 2001
    Assignee: TELIK, Inc.
    Inventors: Edgardo Laborde, Yukiharu Matsumoto
  • Patent number: 6222044
    Abstract: 2-(aryl)-benz(ox, thi, imid)azoles are prepared by reacting an aromatic aldehyde with hydroxylamine to form an aromatic aldehyde oxime, halogenating the oxime to form an aromatic hydroxamoyl halide, and then reacting this halide with certain aromatic amine compounds. The products may be nitrated and then reduced to form the corresponding diamines, which are useful in making PIBX polymers.
    Type: Grant
    Filed: June 10, 1996
    Date of Patent: April 24, 2001
    Assignee: The Dow Chemical Company
    Inventor: Zenon Lysenko
  • Patent number: 6194396
    Abstract: This invention relates to a heterocyclic compound of the formula wherein a group of the formula: is a group of the formula X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: February 27, 2001
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
  • Patent number: 6184235
    Abstract: The present invention relates to novel compounds and medical methods of treatment of inflammation, atherosclerosis, restenosis, and immune disorders especially those associated with lymphocyte or monocyte accumulation such as arthritis and transplant rejection. More particularly, the present invention concerns the use of 2-phenyl benzimidazole derivatives.
    Type: Grant
    Filed: January 19, 1999
    Date of Patent: February 6, 2001
    Assignee: Warner-Lambert Company
    Inventors: David Thomas Connor, Shelly Ann Glase, Terri Stoeber Purchase, Bruce David Roth, Bharat Kalidas Trivedi