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Economist Paula Stephan Talks Chemistry Job Placement at #ACSDallas

Liveblogging First-Time Disclosures of Drug Structures from #ACSDallas

Watch this space, chem-keteers.

Starting at 2PM Central time TODAY, I’ll be continuing my spring tradition of live-blogging the public unveiling of drug structures from ACS Dallas.

This spring’s symposium, unfortunately, only contains one true ‘reveal’ – schizophrenia drug candidate AQW051, from Novartis. The other structures are already public. (Three were covered at prior ACS meetings and are part of a ‘where are they now’ talk). I’ve included vintage hand-drawn structures to refresh our collective memories.

BMS-663068

BMS-663068 – first presented at ACS Anaheim

asunaprevir

asunaprevir- first presented at ACS Fall 2009 (not liveblogged)

BMS-791325

BMS-791325- first presented at ACS San Diego

MK-1064


MK-1064 – structure published in December 2013

 

UPDATE 12:00PM Central time- screengrab of the afternoon’s program

ACS Medi first disclosures spring 2014

1:40PM – grabbed a seat in the second row, by a power outlet. Wifi seems to be behaving. May the liveblogging commence! If you’re on Twitter, watch #ACSMEDI and #ACSDallas hashtags.

2:45PM
AQW051 structure

AQW051
Company: Novartis Institutes for BioMedical Research
Meant to treat: cognitive impairment associated with schizophrenia (ie, impairment to memory and decision-making)
Mode of action: partial agonist at the alpha7 nicotinic acetylcholine receptor
Medicinal chemistry tidbit: Novartis started with a lead called JN403, but cardiotoxicity issues limited progress with this molecule. high throughput screening led to 11 chemical families, including quinuclidine ethers, which led to AQW051. Hurth’s team noticed that changes to the molecule’s phenyl moiety made big differences in selectivity for related receptors and other parameters.
Status in the pipeline: Phase II clinical trials
Related documents: WO2007068476, WO2007068475, WO2006005608, WO2005123732, WO2004022556; Bioorg. Med. Chem. Lett. 2009, 1287-1291

3:30PM

MK-1064 (see above for structure)
Company: Merck Research Laboratories
Meant to treat: insomnia
Mode of action: selective orexin 2 receptor antagonist
Medicinal chemistry tidbit: MK-1064 is a more selective version of Merck’s dual-orexin receptor antagonist suvorexant, which after setbacks is on the cusp of reaching the market.
Research suggests that orexin 2 plays the primary role in wakefulness, so a more selective antagonist could provide relief from insomnia. Merck’s early orexin 2 receptor antagonists were not sufficiently selective and had metabolic issues (eg, pump proteins). Lowering molecular weight and blocking metabolic hot-spots led to MK-1064
Status in the pipeline: Completed Phase I clinical trials
Related documents: ChemMedChem 2014, DOI: 10.1002/cmdc.201300447 ; BMCL 2013, 23, 6620

3:56PM

asunaprevir and BMS-791325 (now has generic name – beclabuvir) (structures above)
Company: Bristol-Myers Squibb
Meant to treat: hepatitis C virus
Mode of action: asunaprevir inhibits viral NS3 protease; beclabuvir inhibits viral RNA polymerase, however, it is not a nucleoside mimic and so binds outside the polymerase active site
Status in the pipeline: Phase III clinical trials
Among several clinical tests discussed in Dallas, asunaprevir and beclabuvir were tested as part of a triple-drug cocktail with daclatasvir, BMS’s experimental NS5A inhibitor. Phase 2b study-The triple regimen dosed for 12 weeks achieved cure rates of up to 94%.
Related documents: Gastroenterology 2014, DOI: 10.1053/j.gastro.2013.10.057; New Engl. J. Med. 2012, DOI: 10.1056/NEJMoa1104430 ; J. Med. Chem. 2014, DOI: 10.1021/jm500297k; J. med. Chem. 2014, DOI: 10.1021/jm4016894

4:30PM

BMS-663068
Company: Bristol-Myers Squibb
Meant to treat: HIV-1
Mode of action: BMS-663068 is a prodrug. Once activated it binds directly to the HIV virus to prevent viral attachment to and entry into immune cells.
Status in the pipeline: Phase III clinical trials
In a Phase 2b clinical trial, BMS-663068 showed similar response rates at tamping down HIV infection to a combination of Reyataz, BMS’s antiretroviral protease inhibitor, and AbbVie’s Norvir, which blocks human cytochrome P450 enzymes to extend Reyataz’s half-life.
Related documents: J. Med. Chem. 2013, 1656; J. Med. Chem. 2012, 2048 ; CROI Meeting, 2014, Abstract 86

That’s it, folks. THANKS to everyone for following along.

Guest Post: “Why I Am Blogging on amphoteros.com” by Andrei Yudin

Today’s guest post is by Andrei Yudin, Professor of Chemistry at the University of Toronto. His research group aims to build new bridges between basic chemistry research and drug discovery. During a sabbatical, Yudin launched a blog, and soon discovered that blogging brings several tangible benefits to his group as well as his research program. You can read his blog at www.amphoteros.com.

I have always been intrigued by science blogging, but the barrier to give it a shot of my own has been steep. When I started my sabbatical in July of 2013, I realized that I would have some extra time, making it the best moment for me to begin blogging. The idea of connecting with a target audience of fellow researchers using a new means was especially attractive to me. In addition, as I was running experiments during my sabbatical, my graduate students and faculty colleagues were curious about what it was I was cooking in the lab. I did not want them to think that I was “breaking bad”, so I decided to put it all out there – my successes, my failures, and a good dose of self-ridicule. This is how www.amphoteros.com saw its first post on July 20, 2013.

I quickly realized that there were relatively few research-oriented chemistry blogs, which stands in contrast to other disciplines such as biology. While the culture of chemistry is different and chemists do not often feel the need to collaborate with one another, our craft is becoming more interdisciplinary and new ways of communicating scientific findings and/or sharing opinions are only going to help.

At the moment, amphoteros is driven by my keen interest in science advances both basic and applied. People ask me how I find time for writing and coming up with original subject matter on a daily basis. I somehow do not feel challenged by this: there is always something “bloggable” I can come up with during my train ride back home. I cover a range of subjects and I always look forward to the feedback I get from the readers. The usual way I conceive my posts is by thinking about one of the dominant thoughts that has been consuming me on a given day. Typically, these musings are related to a particular publication, although I do not make a distinction between what’s current and what’s old. To me, something that is important, yet published 50 years ago, is current. In terms of content, I like to have a lot of graphics on my posts. This gives me a chance to practice ideas for my future lecture presentations. In academia, we always think about new ways of presenting our research in lectures, yet it is tough to sit down and implement them. I partially address this problem using my blog posts: many of them serve their purpose in lectures.

While I blog, I find it encouraging to communicate with like-minded individuals who provide interesting comments. People often contact me by email and say that they enjoy the content I offer. I also like receiving requests to cover certain topics. I am keen to see which subjects on the blog are particularly popular. Straightforward tracking mechanisms enable me to dig deeper into those areas.

My blogging activities have led to other tangible outcomes as well. For instance, I find it easier to recruit students as many of them find the material I write about both educational and interesting. I have gotten both graduate and postdoctoral applications as a direct result of my writings. I also find that, by following my blog posts, students who take my classes are better engaged with the material I teach. Blogging is also turning into a great mechanism to keep in touch with my former students.

One of the emerging trends I see is my lab engagement in writing blog posts. I already had several students guest-post interesting material and anticipate that these offerings will expand in the future. It is 2014 now, my sabbatical is over. Yet the blog is in good shape, I find time to write, and the readership is growing.

This Week on CENtral Science: #FlameChallenge 3, Informex, and more

Tweet (with Instagram!!) of the Week:


To the Network:

Fine Line: State of the Vibe

Just Another Electron Pusher: I’ll get around to procrastinating later

Newscripts: Flame Challenge 2014 and Amusing News Aliquots

Terra Sigillata: Promoting Chemistry’s Positive Public Image

The Watch Glass: All-Chemical All-American Football Team and Equipment Mart and Thermoelectric Materials and Comets

This Week on CENtral Science: Informex #inf14 , Industrial Accidents, and More

Apparently, Gmail was down today. (Sarcasm there. I certainly noticed.) Plenty of Gmail tweets out there, but this wins:

Tweet of the Week:




To the Network:

Fine Line: C&EN Talks at Informex and Buh-buh-buh-buh-buh-Bad! and Ohhhhhhhhh~ Miami!

Newscripts: Amusing News Aliquots

The Safety Zone: Prosecuting companies rather than executives for wrongdoing

The Watch Glass: High Temperature Superconductors and Supercritical Water

This Week on CENtral Science: Another Chemical Spill, McKinsey Training, and more

Tweet of the Week:

To the Network:
Newscripts: Amusing News Aliquots

The Safety Zone: Friday chemical safety round up and How freight company Saia trains and monitors its drivers and How McKinsey makes training mandatory

The Watch Glass: Guiding Black Academics and Selman A. Waksman and Chemical Spill 911

This Week on CENtral Science: Rainbow Flame Test Safety, #Topchem, and more

Tweet of the Week:
Tip o’ the hat to friend of CENtral Science Biochembelle for pointing this one out:

To the Network:

Grand CENtral
: “Top Chemistry Moments of 2013″ Google Hangout #topchem 1/9 3PM Eastern

The Safety Zone
: Performing the ‘rainbow’ flame test demo safely

Newscripts: Amusing News Aliquots

The Watch Glass: Chemical Lab Safety and the Impact of OSHA and Surviving Stress and Insulators

“Top Chemistry Moments of 2013″ Google Hangout #topchem 1/9 3PM Eastern

UPDATE 1/10/14: View the archived webcast here:

Everyone loves a good year-end roundup. Chemists are no exception.

But condensing a year’s worth of discoveries into a neat little “top 10″ package is bound to stir up some discussion. What goes on the list? Who got left out?

We hope you readers will help hash out these questions at C&EN’s second Google Hangout, “Top Chemistry Moments of 2013“. It’s on Thursday, January 9, at 3PM Eastern US time. For those new to Google Hangouts, they are video chats broadcast live on the web. You can watch from Google Plus or YouTube. After the chat is finished it is archived on YouTube for anyone to view.

Join the Hangout here.

Carmen Drahl and Lauren Wolf will speak with Laura Howes and Ashutosh Jogalekar about the people and the research that made chemistry news in 2013, and talk about what to watch in 2014.

Follow the conversation, and ask questions to the speakers on Twitter using the hashtag #topchem.

Laura HowesLaura Howes is Editor of Science in School, the European journal for science teachers that highlights cutting-edge research and teaching. She is a former science correspondent for Chemistry World magazine. Follow her on Twitter at @L_Howes.
Ashutosh JogalekarAsh Jogalekar does molecular modeling at Ensemble Therapeutics, a biotech startup in Cambridge, MA focused on using the specific base-pairing properties of DNA to synthesize novel macrocycle drugs. Ash has been blogging at “The Curious Wavefunction” for about eight years and at Scientific American Blogs since 2012. His main interests are in the history of chemistry, in understanding the relationship between chemical models and reality, and in studying chemistry as a tool-driven rather than an idea-driven revolution. Follow him on Twitter @curiouswavefn.
Lauren K. WolfLauren Wolf is an associate editor at Chemical & Engineering News. Follow her on Twitter @laurenkwolf.
Carmen DrahlCarmen Drahl is a senior editor at Chemical & Engineering News. Follow her on Twitter @carmendrahl.