公开(公告)号：US20170370929A1

公开(公告)日：2017-12-28

申请号：US15535652

申请日：2015-12-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Neil T. Burford ,  Ying Han ,  Martyn N. Banks ,  Litao Zhang ,  Samuel Gerritz ,  Andrew Alt

IPC: G01N33/566 ,  A61K45/06 ,  A61K31/00

CPC classification number: G01N33/566 ,  A61K31/00 ,  A61K45/00 ,  A61K45/06 ,  G01N2333/726 ,  G01N2500/10

Abstract: Described are the discovery, synthesis and pharmacological characterization of δ-opioid receptor-selective positive allosteric modulators (δ PAMs). These δ PAMs may increase the affinity and/or efficacy of the orthosteric agonists leu-enkephalin and SNC80, as measured by β-arrestin recruitment and adenylyl cyclase inhibition. The compounds may be useful pharmacological tools to probe the molecular pharmacology of the δ receptor and to explore the therapeutic potential of δ PAMs in diseases such as chronic pain and depression.