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.

Author: Carmen Drahl

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7 Comments

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

    Looking forward to it, Carmen!

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

  3. 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 ?

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

  5. GREAT TO KNOW THE STUCTURES OF FUTURE BLOCKBUSTERS, THANKS