Small Molecules

Home | Small Molecules | Discovery | Medicinal Chemistry | Medicinal Chemistry Publications

Medicinal Chemistry Publications

  • Liu, L.; Johnson, P. D.; Prime, M. E.; Khetarpal, V.; Brown, C. J.; Anzillotti, L.; Bertoglio, D.; Chen, X.; Coe, S.; Davis, R.; Dickie, A. P.; Esposito, S.; Gadouleau, E.; Giles, P. R.; Greenaway, C.; Haber, J.; Halldin, C.; Haller, S.; Hayes, S.; Herbst, T.; Herrmann, F.; Heßmann, M.; Hsai, M. M.; Khani, Y.; Kotey, A.; Lembo, A.; Mangette, J. E.; Marriner, G. A.; Marston, R. W.; Mills, M. R.; Monteagudo, E.; Forsberg-Moren, A.; Nag, S.; Orsatti, L.; Sandiego, C.; Schaertl, S.; Sproston, J.; Staelens, S.; Tookey, J.; Turner, P. A.; Vecchi, A.; Veneziano, M.; Muñoz-Sanjuan, I.; Bard, J.; Dominguez, C.“Design and Evaluation of [18F]CHDI-650 as a Positron Emission Tomography Ligand to Image Mutant Huntingtin Aggregates,” J. Med. Chem. 2023, 66, 641.
  • Liu, L.; Malagu, K.; Haughan, A. F.; Khetarpal, V.; Stott, A. J.; Esmieu, W.; Vater, H. D.; Webster, S. J.; Van de Poel, A. J.; Clissold, C.; Cosgrove, V.; Sutton, B.; Spencer, J. A.; Breccia, P.; Gancia, E.; Bonomo, S.; Ladduwahetty, T.; Lazari, O.; Patel, H.; Atton, H. C.; Clifton, S.; Mota, D. M.;  Magnani, D.; O’Neill, A.; Stebbeds, M.; Macabuag, N.; Todd, D.; Herva, M. E.; Mitchell, P.; Visser, M.; Compte Sancerni, S.; Grand Moursel, L.; da Silva, M.; Kritikou, E.; Heikkinen, T. T.; Bolkvadze, T.; Fodale, V.; Spadafora, D.; Daldin, M.; Bresciani, A.; Mangette, J. E.; Doherty, E. M.; Lee, M. R.; Herbst, T.; Monteagudo, E.; Macdonald, D.; Plotnikov, N. V.; Chambers, M.; McAllister, G.; Muňoz-Sanjuan, I.; Dominguez, C. “Identification and Optimization of RNA-Splicing Modulators as Huntingtin Protein-Lowering Agents for the Treatment of Huntington’s Disease,” J. Med. Chem. 2023, 66, 13205.
  • Macabuag, N.; Esmieu, W.; Breccia, P.; Jarvis, R.; Blackaby, W.; Lazari, O.; Urbonas, L.; Eznarriaga, M.; Williams, R.; Strijbosch, A.; Van de Bospoort, R.; Matthews, K.; Clissold, C.; Ladduwahetty, T.; Vater, H.; Heaphy, P.; Stafford, D. G.; Wang, H.-J.; Mangette, J. E.; McAllister, G.; Beaumont, V.; Vogt, T. F.; Wilkinson, H. A.; Doherty, E. M.; Dominguez, C. “Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington’s Disease Pathology,” J. Med. Chem. 2022, 65, 12445.
  • Liu, L.; Johnson, P. D.; Prime, M. E.; Khetarpal, V.; Lee, M. R.; Brown, C. J.; Chen, X.; Clark-Frew, D.; Coe, S.; Conlon, M.; Davis, R.; Ensor, S.; Esposito, S.; Moren, A. F.; Gai, X.; Green, S.; Greenaway, C.; Haber, J.; Halldin, C.; Hayes, S.; Herbst, T.; Herrmann, F.; Heßmann, M.; Hsai, M. M.; Kotey, A.; Mangette, J. E.; Mills, M. R.; Monteagudo, E.; Nag, S.; Nibbio, M.; Orsatti, L.; Schaertl, S.; Scheich, C.; Sproston, J.; Stepanov, V.; Varnäs, K.; Varrone, A.; Wityak, J.; Mrzljak, L.; Munoz-Sanjuan, I.; Bard, J. A.; Dominguez, C. “[11C]CHDI-626, a PET Tracer Candidate for Imaging Mutant Huntingtin Aggregates with Reduced Binding to AD Pathological Proteins,” J. Med. Chem. 2021, 64, 12003.
  • Liu, L.; Prime, M. E.; Lee, M. R.; Khetarpal, V.; Brown, C. J.; Johnson, P. D.; Miranda-Azpiazu, P.; Chen, X.; Clark-Frew, D.; Coe, S.; Davis, R.; Dickie, A.; Ebneth, A.; Esposito, S.; Gadouleau, E.; Gai, X.; Galan, S.; Green, S.; Greenaway, C.; Giles, P.; Halldin, C.; Hayes, S.; Herbst, T.; Herrmann, F.; Heßmann, M.; Jia, Z.; Kiselyov, A.; Kotey, A.; Krulle, T.; Mangette, J. E.; Marston, R. W.; Menta, S.; Mills, M. R.; Monteagudo, E.; Nag, S.; Nibbio, M.; Orsatti, L.; Schaertl, S.; Scheich, C.; Sproston, J.; Stepanov, V.; Svedberg, M.; Takano, A.; Taylor, M.; Thomas, W.; Toth, M.; Vaidya, D.; Vanräs, K.; Weddell, D.; Wigginton, I.; Wityak, J.; Mrzljak, L.; Munoz-Sanjuan, I.; Bard, J. A.; Dominguez, C. “Imaging mutant huntingtin aggregates: Development of a potential PET ligand,” J. Med. Chem. 2020, 63, 8608.
  • Huang, Z.; Williams, R. B.; Martin, S. M.; Lawrence, J. A.; Norman, V. L.; O’Neil-Johnson, M.; Harding, J.; Mangette, J. E.; Liu. S.; Guzzo, P. R.; Starks, C. M.; Eldridge, G. R. “Bifidenone: Structure−Activity Relationship and Advanced Preclinical Candidate,” J. Med. Chem. 2018, 61, 6736.
  • Cioffi, C. L.; Dobri, N.; Freeman, E. E.; Conlon, M. P.; Chen, P.; Stafford, D. G.; Schwartz, D. M. C.; Golden, K. C.; Zhu, L.; Kitchen, D. B.; Barnes, K. D.; Racz, B.; Qin, Q.; Michelotti, E.; Cywin, C. L.; Martin, W. H.; Pearson, P. G.; Johnson, G.; Petrukhin, K. “Design, Synthesis, and Evaluation of Nonretinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneratoin and Stargardt Disease,” J. Med. Chem. 2014, 57, 7731.
  • Cioffi, C. L.; Racz, B.; Freeman, E. E.; Conlon, M. P.; Chen, P.; Stafford, D. G.; Schwarz, D. M. C.; Zhu, L.; Kitchen, D. B.; Barnes, K. D.; Dobri, N.; Michelotti, E.; Cywin, C. L; Martin, W. H.; Pearson, P. G.; Johnson, G.; Petrukhin, K. “Bicyclic [3.3.0]-Octahydrocyclopental[c]pyrrolo Antagonists of Retinol Binding Protein4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease,” J. Med. Chem. 2015, 58, 5863.
  • Cioffi, C. L.; Liu, S.; Wolf, M. A. ; Guzzo, P. R.; Sadalapure, K.; Parthasarathy, W.; Loong, D. T. J.; Maeng, J-H.; Carulli, E.; Fang, Z.; Karunakaran, K.; Matta, L.; Choo, S. H.; Panduga, S.; Buckle, R. N.; Davis, R. N.; Sakwa, S. A.; Gupta, P.; Sargent, B. J.; Moore, N. A.; Luche, M. M.; Carr, G. J.; Khmelnitsky, Y. L.; Ismail, J.; Chung, M.; Bai, M.; Leong, W. Y.; Sachdev, N.; Swaminathan, S. Mhyre, A. J. “Synthesis and Biological Evaluation of N-((1-4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1,” J. Med. Chem. 2016, 59, 8473.
  • Rynearson, K. D.; Buckle, R. N.; Herr, R. J.; Mayhew, N. J.; Chen, X.; Paquette, W. D.; Sakwa, S. A.; Yang, J.; Barnes, K. D.; Nguyen, P.; Mobley, W. C.; Johnson, G.; Lin, J. H.; Tanzi, R. E.; Wagner, S. L. “Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators,” Bioorg. Med. Chem. 2020, 28, 114734.