Sunday |
2:00 pm - 9:00 pm | Arrival and Check-in |
6:00 pm | Dinner |
7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
7:40 pm - 9:30 pm | Small Molecule Anti-Fibrotics |
| Discussion Leader: Jehrod Brenneman (Boehringer-Ingelheim Pharmaceuticals Inc., USA) |
7:40 pm - 8:10 pm | Lara Kallander (GlaxoSmithKline, USA) "BMP1/TLL1/TLL2 Inhibitors for Treating Fibrotic Disease" |
8:10 pm - 8:15 pm | Discussion |
8:15 pm - 8:45 pm | Tom Heightman (Astex Pharmaceuticals, United Kingdom) "Highly Potent Cell-Penetrant Inhibitors of the KEAP1-NRF2 Protein-Protein Interaction via X-Ray Fragment Screening" |
8:45 pm - 8:55 pm | Discussion |
8:55 pm - 9:25 pm | Sabine Hadida (Vertex Pharmaceuticals, Inc., USA) "The Discovery of CFTR Modulators for the Treatment of Cystic Fibrosis" |
9:25 pm - 9:30 pm | Discussion |
Monday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Neglected Tropical Diseases |
| Discussion Leader: Cindy Parrish (GlaxoSmithKline, USA) |
9:00 am - 9:30 am | Christopher B. Cooper (TB Alliance, USA) "Antitubercular 3-(4-Aminophenyl)Oxazolidin-2-Ones: Progress Towards Better, Safer TB Agents" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Isabel Castellote Alvaro (GlaxoSmithKline, Spain) "Antimalarial Pyrazines: A Long and Winding Road from a Phenotypic Hit to a Pre-Clinical Candidate" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Stacie S. Canan (Celgene Global Health, USA) "Design
of Compounds for Animal African Trypanosomosis (AAT): From Parasite Screen to
Target Animal Model" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Valentina Molteni (Genomics Institute of the Novartis Research Foundation, USA) "Pan-Kinetoplastid Growth Inhibitors: Towards One Treatment for Multiple Diseases" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Enabling New Technologies in Medicinal Chemistry |
| Discussion Leader: Matthew Bourbeau (Amgen, USA) |
7:30 pm - 8:00 pm | Jeffrey Dodge (Eli Lilly and Company, USA) "HDX: Structure-Based Drug Design Without Crystallography" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Woody Sherman (Schrodinger, USA) "Next Generation Free Energy Calculations in Drug Discovery" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Ian Churcher (GlaxoSmithKline Medicines Research Centre, United Kingdom) "Medicinal Chemistry Beyond Small Molecule Inhibition: New Possibilities Through Induced Intracellular Protein Degradation" |
9:20 pm - 9:30 pm | Discussion |
Tuesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Exciting Advances Toward New Treatments for Autoimmune Disorders |
| Discussion Leader: Dustin Mergott (Eli Lilly and Company, USA) |
9:00 am - 9:30 am | Michelle Machacek (Merck & Co., USA) "Strategies for the Design of Inhaled Kinase Inhibitors: Discovery of MK-8351, an Inhaled Spleen Tyrosine Kinase (SYK) Inhibitor for the Treatment of Asthma" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Steve Staben (Genentech, Inc., USA) "Inhibition of NF-κB-Inducing Kinase (NIK)" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Group Photo / Coffee Break |
11:00 am - 11:30 am | Peter Toogood (Lycera, USA) "Modulation of the Mitochondrial ATPase for the Treatment of Inflammatory Bowel Disease" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Atli Thorarensen (Pfizer, USA) "Design of a JAK3-Specific Inhibitor Allowing for the Interrogation of JAK3 Signaling in Humans" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Advances in Lead Generation |
| Discussion Leader: Joerg Holenz (AstraZeneca, USA) |
7:30 pm - 8:00 pm | Franz Von Nussbaum (Bayer SAS, France) "Driving Tumors into a Mitotic Catastrophe - Lead Generation of Mps1 Inhibitors Leading to Two Clinical Candidates: BAY1161909 and BAY1217389" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Erin DiMauro (Amgen, USA) "Discovery of Efficient, Selective, CNS-Penetrant Leads for Glycine Receptor Potentiation" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Katherine Lee (Pfizer, USA) "Lead Generation Strategies: Discovery of a Potent, Selective and Lipophilic Efficient IRAK4 Inhibitor, a Clinical Candidate from Fragment-Based Drug Design" |
9:20 pm - 9:30 pm | Discussion |
Wednesday |
7:30 am - 8:30 am | Breakfast |
9:00 am - 12:30 pm | Approaches to the Treatment of Parkinson's Disease |
| Discussion Leader: Michael Ellis (Merck Research Laboratories, USA) |
9:00 am - 9:30 am | Marco Baptista (The Michael J. Fox Foundation for Parkinson's Research, USA) "LRRK2 Kinase Inhibitors: The Path to the Clinic" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Yeon-Hee Lim (Merck Research Laboratories, USA) "Discovery, SAR Evolution, and Clinical Evaluation of Adenosine A2A Antagonists for the Treatment of Parkinson's Disease" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | Holger Monenschein (Takeda California, USA) "The Discovery of GPR6 as a Novel Target for the Treatment of Parkinson's Disease" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Joerg Holenz (AstraZeneca, USA) "Discovery of the Selective and Brain-Penetrant Irreversible Myeloperoxidase (MPO) Inhibitor AZD3241" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Kinase Inhibitors in Oncology - Success Stories |
| Discussion Leader: Eugene Chekler (EMD Serono, USA) |
7:30 pm - 8:00 pm | Kurt Pike (AstraZeneca, United Kingdom) "Identifying High Quality, Potent and Selective Inhibitors of ATM Kinase: Discovery of AZD0156" |
8:00 pm - 8:10 pm | Discussion |
8:10 pm - 8:40 pm | Justin Ernst (eFFECTOR Therapeutics, USA) "Identification
of eFT508, an Oral, Potent and Highly Selective Inhibitor of
Mitogen-Activated
Protein Kinase Interacting Kinase (MNK) 1 and 2
via a
Disciplined, Iterative Structure-Based Drug Design Strategy" |
8:40 pm - 8:50 pm | Discussion |
8:50 pm - 9:20 pm | Bayard Huck (EMD Serono, Germany) "Identification of the Potent, Brain-Penetrant p70S6K/Akt Inhibitor M2698, a Novel Dual Inhibitor of the PI3K/Akt/mTOR Pathway" |
9:20 pm - 9:30 pm | Discussion |
Thursday |
7:30 am - 8:30 am | Breakfast |
8:30 am - 9:00 am | Business Meeting |
| Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair |
9:00 am - 12:30 pm | Late Breaking Topics: Disclosures of Clinical Candidates |
| Discussion Leader: Brock Shireman (Janssen R&D, USA) |
9:00 am - 9:30 am | Gregory Notte (Gilead Sciences, USA) "Discovery of GS-4997, a Highly Selective Inhibitor of Apoptosis Signal-Regulating Kinase 1 (ASK1)" |
9:30 am - 9:45 am | Discussion |
9:45 am - 10:15 am | Brad Savall (Janssen Research & Development, USA) "JNJ-54175446: A P2X7 Receptor Antagonist that Reduces IL-1β Levels for Major Depressive Disorders" |
10:15 am - 10:30 am | Discussion |
10:30 am - 11:00 am | Coffee Break |
11:00 am - 11:30 am | David Weinstein (Bristol-Myers Squibb, USA) "Discovery and Pre-Clinical Evaluation of a Novel Allosteric Inhibitor of TYK2" |
11:30 am - 11:45 am | Discussion |
11:45 am - 12:15 pm | Philip Harris (GlaxoSmithKline, USA) "Identification of a First-in-Class RIP1 Kinase Inhibitor in Clinical Trials for Immuno-Inflammatory Diseases" |
12:15 pm - 12:30 pm | Discussion |
12:30 pm | Lunch |
1:30 pm - 4:00 pm | Free Time |
4:00 pm - 6:00 pm | Poster Session |
6:00 pm | Dinner |
7:30 pm - 9:30 pm | Keynote Session: Embracing and Anticipating Change in a Dynamic Industry - View from One Medicinal Chemist |
| Discussion Leader: Bradley Tait (Brad Tait Enterprise LLC, USA) |
7:30 pm - 8:30 pm | Kazumi Shiosaki (MPM Capital, USA) "Embracing and Anticipating Change in a Dynamic Industry - View from One Medicinal Chemist" |
8:30 pm - 8:55 pm | Discussion |
8:55 pm - 9:15 pm | General Discussion |
9:15 pm - 9:30 pm | Closing Remarks |
Friday |
7:30 am - 8:30 am | Breakfast |
9:00 am | Departure |