In the last year, a small team of TriMen chemists (4 FTEs), working in close collaboration with chemists from the client’s laboratory, has played a key role in optimization of a lead inhibitor structure for a novel asthma related target. Within 6 months from the project inception, a 5uM screening hit has been optimized into lead molecule with low nanomolar in vitro potency and good PK profile.
Case study B:
Over three years a team of chemists (3FTEs) have synthesized over 300 complex, multifunctional amino acids as inhibitors of a metalloenzyme target of pharmaceutical interest. Single nanomolar in vitro activity was achieved and selected compounds were tested in the animal model studies.
Case study C:
Since 2005 through 2011 TriMen has synthesized over 2,500 peptide-like compounds with potential antimicrobial activity for SAR studies. Some of these compounds have been requested by the customer in multigram amounts and within aggressive time lines - which were successfully met.
Case study D:
Two HIV protease inhibitors have been synthesized in TriMen on the customer's order for the needs of the toxicological studies. TriMen was asked for the preparation of 25g of each compound. They required 22 – 25 synthetic steps to be accomplished and both were featured with 3 contiguous chiral centers. In both cases important optimizations to the published synthetic pathway were introduces (eg. asymmetric synthesis instead of the original resolution of the racemate methodology) and the ordered compounds were delivered on time.