Patent Pulse: A Spotlight on Recent Highlights from Small Molecule Patents
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Roles of the Chloro and Methoxy Groups in Drug Discovery
In this Flash Talk, Yoshihiro Ishihara discussed the beneficial effects of chloro and methoxy substituents on intermolecular interactions, as well as the unique advantages and disadvantages of employing these substituents in drug discovery.
As part of our Flash Talk webinar series, we present a PDF of Yoshihiro Ishihara's slide deck and full text questions and answers from his talk, entitled "Roles of the Chloro and Methoxy Groups in Drug Discovery." Check out the recording of the talk on our Drug Hunter YouTube channel.
Where Do Recent Small Molecule Clinical Candidates Come From?
Modern hit-finding technologies are incredible. Dean Brown and Jonas Bostrom at AstraZeneca have a very nice review out summarizing the hit-finding strategies for 66 clinical candidates published from 2016-2017. Some highlights include a clinical candidate from DNA-encoded libraries at GSK, the discovery of an RNA-binding drug candidate by [...]
Olutasidenib: Potentially Longer Complete Remissions in AML with a Second-Generation IDH1 Inhibitor
Olutasidenib, discovered by Forma Therapeutics and marketed by Rigel, is an oral, brain-penetrant, selective mIDH1 inhibitor. It was granted Orphan Drug Designation and approved in December 2022 by the FDA for adults with relapsed/refractory acute myeloid leukemia. Approval was granted based on a Ph. I/II trial showing a 35% CR+CRh rate and a favorable 25.9-month median duration. This article describes the discovery and development of olutasidenib, how it is distinct from other mIDH inhibitors, and its potential in treating gliomas.
Molecules on the Move: Reversible BTKi in MS, THR-beta Agonist in NASH, and More
This article compiles recent high-profile clinical readouts and related news with small molecules of general interest and structures where they are available. Targets and indications discussed in this article include BTK for MS, Axl, TYRO3, and Mer for oncology, HIF prolyl-hydroxylase in anemia, ET/AT in nephrology, a JAK2 inhibitor for myelofibrosis, and THR-beta in NASH. [...]
Computational Partnership in Small Molecule Drug Discovery
The real magic happens when chemists can integrate computational models into their assay cascades, thanks to trust in their predictions. To get there, grounding computational predictions in physics and experimental reality makes all the difference. In this article, Abba E. Leffler, Ph.D. from Schrödinger tells us about: How to make [...]
