Philip B. Cox
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View article: Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site
Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site Open
View article: Contemporary Computational Applications and Tools in Drug Discovery
Contemporary Computational Applications and Tools in Drug Discovery Open
In the past decade or so there has been a dramatic increase in the number of computational applications and tools that have been developed to enable medicinal chemists to prosecute modern drug discovery programs more efficiently. The upsur…
View article: Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design
Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design Open
Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and MAPK signaling pathways. The development of biologic drugs that inhibit TNFα has …
View article: Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character
Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character Open
The pressure to deliver new medicines to the patient continues to grow along with increases in compound failure rate, thus putting the current R&D model at risk. Analysis has shown that increasing the three-dimensionality of potential drug…
View article: Design and Synthesis of Pyrrolidine-based Fragments That Sample Three-dimensional Molecular Space
Design and Synthesis of Pyrrolidine-based Fragments That Sample Three-dimensional Molecular Space Open
Fragment-based drug discovery (FBDD) is a well-established technology for lead compound generation in drug discovery. As this technology has evolved, the design of fragments for screening has also evolved to engender not just an understand…
View article: Access to 3D Alicyclic Amine-Containing Fragments through Transannular C–H Arylation
Access to 3D Alicyclic Amine-Containing Fragments through Transannular C–H Arylation Open
In this Letter, we adapt a recently reported Pd-catalyzed transannular C(sp3)–H arylation of alicyclic amines for applications in fragment-based drug discovery (FBDD). We apply this method to the synthesis of a series of 6-arylated 3-azabi…
View article: Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection
Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection Open
Recently, there has been an increasing focus on the pursuit of targets considered to be less druggable that offer potential for development of promising new therapeutic agents for the treatment of diseases with large unmet medical need, pa…