Dario Doller earned a Ph.D. in Organic Chemistry from the Facultad de Ciencias Exactas y Naturales, UBA, Argentina. He conducted postdoctoral studies with Sir Derek Barton at Texas A&M University. His industrial career includes Rohm & Haas, Schering-Plough Research Institute, 3-Dimensional Pharmaceuticals, Gliatech, Neurogen, Lundbeck, CoNCERT, Sage, Sunovion Pharmaceuticals, Lucy Therapeutics, and iNeuro Therapeutics, where he is currently director of medicinal chemistry. He contributed to the discovery of the marketed PAR-1 antagonist vorapaxar and the clinical compounds NGD-4715, Lu AF09535, and CTP-692. He coauthored over 100 articles, patents or patent applications, and book chapters, and edited the book Allosterism in Drug Discovery. Current interests include molecular concepts at the chemistry/biology interface to enhance the translatability of preclinical research.

PART 1: CURRENT STATUS AND THERAPY OVERVIEW
Drug discovery in the Century of Biology
Academic vs. Industrial CNS drug discovery: An evolving relationship
The role of Venture Capital in drug discovery
Spin-off companies
The NIH role catalyzing the discovery of novel treatments
PART 2: KEY QUESTIONS FOR CONTEMPORARY CNS DRUG DISCOVERY
The end: defining CNS diseases (molecular vs phenotype)
Target selection in the treatment of CNS diseases
The use of animal models in brain drug research
Biomarkers in CNS drug discovery
PET imaging in CNS drug discovery
PART 3: PSYCHEDELIC-INSPRIRED DRUG DISCOVERY
Update on ketamine, esketamine, arketamine
Non-hallucinogenic antidepressants
Cannabinoids as therapeutics for brain disease
PART 4: UNION MAKES STRENGTH: COMBINING DRUGS TO PRODUCE NOVEL CNS THERAPEUTICS
Xanomeline-trospium for schizophrenia
Olanzapine-samidorphan
Dextromethorphan-bupropion
Levodopa prodrug
Apomorphine
PART 5: EMERGING CHEMICAL MODALITIES FOR BRAIN DISEASES
PROTACs in CNS drug discovery
Small molecule allosteric modulators
Progress using biologics drugs for CNS diseases (CGRP migraine, Anti-amyloid antibodies, MSA/PD and a-SYN antibodies)
Using mechanistic studies for CNS diseases
What is the best surrogate of brain penetration?
Brain cancer treatments (brain penetration of kinase inhibitor)
PART 6: EPILOGUE
Treating brain disease in the next decade