Inventors:
Bernard Silverman - Needham MA, US
Mark Todtenkopf - Franklin MA, US
Daniel Deaver - Franklin MA, US
Lauren DiPetrillo - Somerville MA, US
International Classification:
A61K 31/485, C07D 221/28, C07D 489/08, A61P 1/00
US Classification:
514282, 514289, 546 74, 546 45
Abstract:
The present invention relates to a novel functional peripherally-acting μ opioid receptor antagonist of Formula I:The novel compounds of the present invention have reduced oral bioavailability without compromising opiate-induced analgesia in the CNS. The compounds of the present invention are further efficacious at low doses and are useful in treating gastrointestinal conditions associated with opioid analgesic therapy.