Blog Profile / In the Pipeline

Filed Under:Medical / Pharmaceutical
Posts on Regator:2106
Posts / Week:9.3
Archived Since:November 3, 2010

Blog Post Archive

Doing the Right Thing

This is well outside my field of chemistry (a paper on iridium-catalyzed silane couplings), but I wanted to highlight it anyway. A grad student working on the project realized that one of the key products had been mischaracterized (not hard to do, with these compounds), and that this invalidated a good part of the published paper. Show More Summary

Put Away The Lecture Bottle

For fluorination fans, here's a new way to get trifluoromethyl groups in. Trifluoromethyl iodide is a useful reagent, or it would be if it weren't a gas. That makes it annoying to measure out and work with, especially on a small scale. Show More Summary

Dinitrophenol: A Possible Comeback

I've mentioned metabolic uncoupling as a possible diabetes therapy. The idea is that your mitochondria will plow though large amounts of lipids under these conditions, and there's plenty of evidence that knocking down free fatty acids and tissue lipid stores would be of great benefit for Type II patients. Show More Summary

Chlorine Azide For Everyone

One of my "Things I Won't Work With" compounds may have moved into a zone where I'd actually use it. This new paper in JOC describes in situ preparation of small amounts of chlorine azide, which can then react with alkene to give useful beta-chloro azide products. Show More Summary

Of Proteasome Inhibitors and PAINs

Amgen is out with some new data that might well justify their purchase of Onyx a year and a half ago. A big driver for that deal was the proteasome inhibitor Kyprolis (carfilzomib), and the company just reported results in a head-to-head...Show More Summary

Gene Editing Therapies Thunder Along

Here's a one-stop way to get caught up with all the therapeutic gene editing technologies out there, courtesy of Nature Medicine. Huge amounts of money are flowing into this area, because CRISPR/Cas9 looks so solid, compared to the various other things that have been tried in the past. Show More Summary

PAINs And Good Old Med Chem

The mainstreaming of the PAINs concept continues, with editorials from Jonathan Baell in ACS Med. Chem. Letters and Dan Erlanson in J. Med. Chem.. Both are definitely worth a read. Baell emphasizes that real hits tend to have real SAR around them. Show More Summary

AZ Spins Off Anti-Infectives

Word came yesterday that AstraZeneca is spinning off its anti-infectives division into a separate subsidiary company. This does not appear to have been their first choice - they've been shopping these assets around for actual cash, but had no takers (at least, on their terms). Show More Summary

Ibrutinib's Rise

Pharmacyclics and their reactive kinase inhibitor Imbruvica (ibrutinib) have come up a few times around here in the past. (And someone who was involved in its earlier development at Celera shows up here in the comments from time to time). Show More Summary

Double-Blinded Peer Review

Nature has decided to add an option for double-blind peer review - papers would be sent to the referees without author names or institutional affiliation on them. I think this is a worthwhile idea, but I agree with many of the points...Show More Summary

The Latest Fragment List

Practical Fragments has an updated list of all the drug that have made it into the clinic from fragment-based drug design. There are more than thirty of them, and there are probably more that aren't on the list yet. So while fragment-based...Show More Summary

All That Cash

From the LifeSciVC blog, here's a revealing comparison of the amount of money going into startups in this business. This is why I tend to get worked up about the number of stock buyback plans among the big pharma players. It would seem...Show More Summary

An Antibiotic Discovery Prize

Ezekiel Emanuel of the University of Pennsylvania has a proposal in the New York Times for a prize in antibiotic discovery: Let’s use prize money. What if the United States government — maybe in cooperation with the European Union and...Show More Summary

Cutbacks at Merck Serono

Merck/Serono (Merck KGaA of Darmstadt) is apparently cutting back in Billerica, their US research site. According to FierceBiotech, though, they're not saying by how much: "a limited number of discovery positions have been impacted in our research organization. Show More Summary

Is FEP Ready For the World?

Here's a paper that basically throws down the computational gauntlet. A large group of authors from Schrödinger, Nimbus, Columbia, Yale, and UC-Irvine say that their implementation of free energy perturbation (FEP) calculations really does lead to a significant number of more active compounds being predicted. Show More Summary

Para-Chloro Was Good Enough For Them, So It's Good Enough For Me

How many of the molecular pieces that we use in medicinal chemistry are historical accidents? I've wondered this from time to time. There's no doubt that drug structures are partly driven by ease of synthesis/commercial availability (these two go hand in hand), and these in turn are influenced by which reactions and feedstocks were exploited earlier. Show More Summary

More Price Hikes on Obscure Medication

Get ready for some twists and turns here. I wrote back in September about the business model of Retrophin, a company whose plans (at least for the foreseeable future) were to find small-market drugs, buy them from their obscure producers, and then raise their prices into geosynchronous orbit. Show More Summary

Bonne Chance, Brandicourt

Sanofi's CEO hunt has ended, and the roue de la fortune has pointed to Bayer's Olivier Brandicourt. (I'm tempted to keep dropping French phrases every couple of lines, but I figure that no one will stand for it, so you can work them in mentally as appropriate). Show More Summary

Unclick Undone, Unsurprisingly

The now-notorious "unclick" paper has been retracted. Last summer saw an editorial "Expression of Concern", and later it was reported by C&E News that a common author (Kelly Wiggins) of all three papers in this area had confessed to fabricating data. In light of this, the retraction notice is interesting. Show More Summary

Experience Phase III Failure, Twice

I'm going to use a short phrase that should make everyone who's ever been involved with clinical research shiver a little bit: post-hoc subgroup analysis. This comes up again and again in drug research (and has been the subject of several...Show More Summary

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