948990-75-8

Upstream product

• 474010-72-5 ((R)-4-benzoyl-2-methylpiperazin-1-yl)acetonitrile 
• 179232-29-2 methyl 4-bromo-2-fluorobenzoate 

Downstream Products

• 948990-80-5 1-((R)-4-benzoyl-2-methyl-piperazin-1-yl)-2-(4-bromo-2-dimethylamino-phenyl)-ethane-1,2-dione 
• 948990-81-6 1-((R)-4-benzoyl-2-methylpiperazin-1-yl)-2-(4-bromo-2-aminophenyl)ethane-1,2-dione 
• 1173176-97-0 1-((R)-4-benzoyl-2-methylpiperazin-1-yl)-2-[2-methylamino-4-bromophenyl]ethane-1,2-dione 
• 1173176-94-7 1-((R)-4-benzoyl-2-methylpiperazin-1-yl)-2-[2-benzyloxy-4-bromophenyl]ethane-1,2-dione 

Relevant academic research and scientific papers

Heterobiaryl human immunodeficiency virus entry inhibitors

Previously disclosed HIV (human immunodeficiency virus) attachment inhibitors, exemplified by BMS 806 (formally BMS378806, 1), are characterized by a substituted indole or azaindole ring linked to a benzoylpiperazine via a ketoamide or sulfonamide group. In the present report, we describe the discovery of a novel series of potent HIV entry inhibitors in which the indole or azaindole ring of previous inhibitors is replaced by a heterobiaryl group. Several of these analogues exhibited IC50 values of less than 5 nM in a pseudotyped antiviral assay, and compound 13k was demonstrated to exhibit potency and selectivity similar to those of 1 against a panel of clinical viral isolates. Moreover, current structure-activity relationship studies of these novel biaryl gp120 inhibitors revealed that around the biaryl, a fine crevice might exist in the gp120 binding site. Taken in sum, these data reveal a hitherto unsuspected flexibility in the structure-activity relationships for these inhibitors and suggest new avenues for exploration and gp120 inhibitor design. 2009 American Chemical Society.

PIPERAZINE AND PIPERIDINE BIARYL DERIVATIVES

This invention relates to piperazine and piperidine biaryl compounds of Formula (I) or a pharmaceutically acceptable prodrug, salt, polymorph, solvate, enantiomer, diastereomer, racemate, mixture of stereoisomers thereof, or derivative thereof; and to processes for preparing the compounds or pharmaceutical compositions containing the same. The compounds and pharmaceutical compositions of the present invention are provided for use in the treatment of HIV infection and/or AIDS.