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Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA

Bookmark this page now, folks. On Wednesday, April 10, I will be here, liveblogging the public debut of five drug candidates’ structures. The “First Time Disclosures” Session at the ACS National Meeting in New Orleans runs from 2PM-4:55PM Central time. I am not able to conjure up a permalink to the session program, so here’s a screengrab instead.
NOLAblog-program
1:20PM I’m in hall R02, where the session’s set to begin in about 40 minutes. Found a seat with a power outlet nearby, so I’m good to go!
2:29PM
IMG_3813
BMS-906024
Company: Bristol-Myers Squibb
Meant to treat: cancers including breast, lung, colon, and leukemia
Mode of action: pan-Notch inhibitor
Medicinal chemistry tidbit: The BMS team used an oxidative enolate heterocoupling en route to the candidate– a procedure from Phil Baran’s lab at Scripps Research Institute. JACS 130, 11546
Status in the pipeline: Phase I
Relevant documents: WO 2012/129353
3:02PM
IMG_3810
LGX818
Company: Novartis Institutes for Biomedical Research and Genomics Institute of the Novartis Research Foundation
Meant to treat: melanoma with a specific mutation in B-RAF kinase: V600E
Mode of action: selective mutant B-RAF kinase inhibitor
Status in the pipeline: Phase Ib/II
Relevant documents: WO 2011/023773 ; WO 2011/025927
3:47PM
IMG_3812
AZD5423
Company: AstraZeneca
Meant to treat: respiratory diseases, in particular chronic obstructive pulmonary disease
Mode of action: non-steroidal glucocorticoid receptor modulators
Medicinal chemistry tidbit: This compound originated in part from a collaboration with Bayer Pharma.
Status in the pipeline: Phase II
Relevant documents: WO 2011/061527 ; WO 2010/008341 ; WO 2009/142568
4:17PM
IMG_3811
Birinapant (formerly known as TL32711)
Company: TetraLogic Pharmaceuticals
Meant to treat: cancer
Mode of action: blocks the inhibitor of apoptosis proteins to reinstate cancer cell death
Status in the pipeline: Phase II
Relevant documents: US 8,283,372
5:00PM
IMG_3814
MGL-3196 (previously VIA-3196)
Company: Madrigal Pharmaceuticals, acquired from VIA Pharmaceuticals, licensed from Roche
Meant to treat: high cholesterol/high triglycerides
Mode of action: mimics thyroid hormone, targeted to thyroid hormone receptor beta in the liver
Medicinal chemistry tidbit: this molecule was discovered at Roche’s now-shuttered Nutley site.
Status in the pipeline: completed Phase I trials
Relevant documents: WO 2007/009913 ; WO 2009/037172

And that’s it, folks! Watch the April 22nd issue of C&EN for more on this session.

7 Comments

  • Apr 4th 201314:04
    by Rachel

    It’s the most won-derful tiiiiime…of the ACS meeting!!!

    Looking forward to it, Carmen!

  • Apr 10th 201320:04
    by Glen Ernst

    Wish I’d been in attendance, but a current colleague was. Hope to attend in Indianapolis in September. Great job, Carmen!

  • Apr 13th 201323:04
    by Antony Williams

    I think that using the ChemSpider wikibox to create the Wiki articles will be a good way to migrate your drawings into Wikipedia…via ChemSpider depositions. http://www.slideshare.net/AntonyWilliams/generating-wikipedia-drugboxes-using-chemspider-functionality

  • Apr 14th 201313:04
    by Christopher Southan

    Good post but how did you get the patent nos.? See my pick up of the PubChem links at http://cdsouthan.blogspot.se/2013/04/joining-in-with-post-acs-new-drug.html

  • Apr 14th 201320:04
    by Antony Williams

    I have now added Wikipedia DrugBoxes for all of the drugs that you liveblogged…not sure whether you have the bandwidth to expand on the articles yourself ?

  • Apr 14th 201323:04
    by Carmen Drahl

    Thanks folks. Christopher- I picked up the patent no.’s with a search of author names from each abstract.

  • Apr 23rd 201300:04
    by DR ANTHONY CRASTO

    GREAT TO KNOW THE STUCTURES OF FUTURE BLOCKBUSTERS, THANKS

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