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
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
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
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
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.
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
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
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.
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
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
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
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.
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.
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.
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