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Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor. 2013
Nicolas Dreyfus, and
Jason K Myers, and
Valentina O Badescu, and
Oscar de Frutos, and
Maria Luz de la Puente, and
Chunjin Ding, and
Sandra A Filla, and
Karsten Fynboe, and
Douglas L Gernert, and
Beverly A Heinz, and
Susan K Hemrick-Luecke, and
Kirk W Johnson, and
Michael P Johnson, and
Pilar López, and
Patrick L Love, and
Laura J Martin, and
Thierry Masquelin, and
Michael J McCoy, and
Javier Mendiola, and
Denise Morrow, and
Mark Muhlhauser, and
Gustavo Pascual, and
Thomas J Perun, and
Lance A Pfeifer, and
Lee A Phebus, and
Simon J Richards, and
Juan Antonio Rincón, and
Eric P Seest, and
Jikesh Shah, and
Jia Shaojuan, and
Rosa Maria A Simmons, and
Gregory A Stephenson, and
Eric G Tromiczak, and
Linda K Thompson, and
Magnus W Walter, and
Wayne W Weber, and
Hamideh Zarrinmayeh, and
Craig E Thomas, and
Elizabeth Joshi, and
Smriti Iyengar, and
Anette M Johansson
Research and Development, Eli Lilly and Company Ltd. , Sunninghill Road, Windlesham, Surrey GU20 6PH, United Kingdom.
The objective of the described research effort was to identify a novel serotonin and norepinephrine reuptake inhibitor (SNRI) with improved norepinephrine transporter activity and acceptable metabolic stability and exhibiting minimal drug-drug interaction. We describe herein the discovery of a series of 3-substituted pyrrolidines, exemplified by compound 1. Compound 1 is a selective SNRI in vitro and in vivo, has favorable ADME properties, and retains inhibitory activity in the formalin model of pain behavior. Compound 1 thus represents a potential new probe to explore utility of SNRIs in central nervous system disorders, including chronic pain conditions.
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