Abstract: Disclosed are substituted benzimidazole compounds of formula(I):
wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention are useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
November 5, 2002
Date of Patent:
November 30, 2004
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles Cywin, Jinbo Lee, Steven S. Pullen, Gregory Paul Roth, Christopher Ronald Sarko, Roger John Snow, Noel Stewart Wilson
Abstract: The present invention generally relates to an assay for identifying inhibitors of Human Papillomavirus (HPV), comprising:
a) contacting a HPV E2 transactivation domain with a probe to form a E2:probe complex and measuring a signal from said probe to establish a base line level;
b) incubating the E2:probe complex with a test compound and measuring the signal from said probe;
c) comparing the signal from step b) with the signal from step a);
wherein said probe is a compound of formula (I) or its enantiomers or diastereoisomers thereof:
wherein R1, A, X, W, Y, R3 and R4 are as defined herein; or a derivative thereof, wherein said derivative is a probe of formula (I) labeled with a detectable label or an affinity tag, wherein wavy lines represent bonds of unspecified stereochemistry; and wherein said signal is selected from: fluorescence, resonance energy transfer, time resolved fluorescence, radioactivity, fluorescence polarization, change in the intrinsic spectral properties, luminescence
Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo [1,2-&agr;]imidazol-2-one (1):
This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.
Type:
Grant
Filed:
February 15, 2002
Date of Patent:
August 27, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rogelio P. Frutos, Michael Dale Johnson