Aminopyrrolidineamide inhibitors of site-1 protease

Creators: Hay, Bruce A.; Abrams, Barbara; Zumbrunn, Allice Y.; Valentine, James J.; Warren, Laurie C.; Petras, Stephen F.; Shelly, Lorraine D.; Xia, Angela; Varghese, Alison H.; Hawkins, Julie L.; Van Camp, Jennifer A.; Robbins, Michael D.; Landschulz, Katherine; Harwood, H. James, Jr.

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Abstract

The discovery and efficacy of a series of potent aminopyrrolidineamide-based inhibitors of sterol regulatory element binding protein site-1 protease is described.

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© 2007 Elsevier Ltd. Received 16 May 2007, Revised 4 June 2007, Accepted 5 June 2007, Available online 10 June 2007. The authors wish to thank Robert Corr, Neal Falcone, Anthony Provatas, Jack Oscarson, and the Pfizer Groton automated synthesis and registration laboratory for preparation of the initial S1P library and Kosea Frederick and Kazuko Sagawa for pharmacokinetic modeling of PF-429242 in rats.

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Aminopyrrolidineamide inhibitors of site-1 protease

Abstract

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