Tag Archives: Boehringer Ingelheim

GPCR structure and modeling

Posted on April 18, 2011 by mcb

A recently published letter from scientists at Boehringer Ingelheim nicely summarizes recent advances in our understanding of G protein-coupled receptor (GPCR) structure and function. X-ray structures of the inactive forms of bovine rhodopsin (2000), β2 adrenergic receptor (2007 – with antibody … Continue reading →

Posted in Computational Methods, GPCR ligands | Tagged , , , , , , , , , , | 1 Comment

Discovery of MK-1220 (Hepatitis C NS3/4A protease inhibitor)

Posted on March 10, 2011 by mcs1001

A recent letter in ACS Med.Chem.Lett. details the optimisation of a series of inhibitors of the Hepatitis C virus (HCV) NS3/4A protease, and is interesting in that it provides detailed pharmacokinetic data for a series of macrocyclic lactones, a class of therapeutic … Continue reading →

Posted in Clinical Candidates, Enzyme Inhibitors, Med Chem Strategy | Tagged , , , , , , , , , , , , , , , , , , , , , , , , | 1 Comment

Discovery of Rivaroxaban (Factor Xa Inhibitor)

Posted on January 14, 2011 by mcb

The discovery of novel anticoagulants, and the search for novel orally active agents in particular, has been a long and difficult journey.  However, the recent (2008) launches of Bayer’s Factor Xa inhibitor (Rivaroxaban, BAY 59-7939) and Boehringer Ingelheim’s Thrombin inhibitor … Continue reading →

Posted in Enzyme Inhibitors, Launched Drugs | Tagged , , , , , , , , , , , , | 1 Comment

Atropisomerism in Drug Discovery

Posted on January 10, 2011 by mcb

Following up on their earlier mini-review, the authors of this recent paper outline their work at Boehringer Ingelheim on developing methodology and strategies for dealing with the issue of atropisomerism in drug discovery.  The authors highlight the fact that, whilst the … Continue reading →

Posted in Computational Methods, Med Chem Strategy | Tagged , , , , | Leave a comment