Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists |
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| Affiliation: | 1. AstraZeneca, Department of Medicinal Chemistry, Montréal H4S 1Z9, Canada;2. AstraZeneca/OmegaChem, Department of Medicinal Chemistry, Montréal H4S 1Z9, Canada;3. AstraZeneca, Department of Bioscience, Montréal H4S 1Z9, Canada;4. Astrazeneca, DMPK, Montréal H4S 1Z9, Canada;1. Department of Chemistry, Northwestern University, Evanston, IL 60208-3113, USA;2. Cambria Pharmaceuticals, Cambridge, MA 02142, USA;3. Department of Molecular Biosciences, Rice Institute for Biomedical Research, Northwestern University, Evanston, IL 60208-3500, USA;4. Department of Molecular Biosciences, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, Northwestern University, Evanston, IL 60208-3113, USA;1. Oncology Innovative Medicines, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, United States;2. Respiratory and Inflammation Innovative Medicines, AstraZeneca R&D Molndal, SE-43813 Molndal, Sweden;1. Global Discovery Chemistry, Novartis Institutes for BioMedical Research, WKL-136.3.26, CH-4002 Basel, Switzerland;2. Neuroscience, Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland;3. Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland;4. Medicinal Chemistry, Aurigene Discovery Technologies Limited, 39-40, KIADB Industrial Area, Phase II, Electronic City, Hosur Road, Bangalore 560100, India;5. School of Biomedical Sciences, Faculty of Medicine, Dentistry and Health Sciences, The University of Melbourne, Parkville, Victoria 3010, Australia;6. The Florey Institute of Neuroscience and Mental Health, Parkville Campus, Kenneth Myer Building at Genetics Lane, on Royal Parade, University of Melbourne, Parkville, 3010, Australia;1. Astbury Centre for Structural Molecular Biology, University of Leeds, Leeds, LS2 9JT, UK;2. School of Chemistry, University of Leeds, Leeds, LS2 9JT, UK;3. Redbrick Molecular, The Bioincubator, 40 Leavygreave Road, Sheffield, S3 7RD, UK;1. Takeda California, 10410 Science Center Drive, San Diego 92121, USA;2. Takeda Pharmaceutical Company, Ltd, 2-26-1, Muraokahigashi, Fujisawa, Kanagawa 251-855, Japan |
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| Abstract: | A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization. |
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| Keywords: | TRPA1 Antagonist Ligand gated ion channel |
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