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.

公开(公告)号：US20150338404A1

公开(公告)日：2015-11-26

申请号：US14758908

申请日：2013-12-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Neil Burford ,  Andrew Alt

IPC: G01N33/566

CPC classification number: G01N33/566 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/10

Abstract: Disclosed are positive allosteric modulators (PAMs) and silent allosteric modulators (SAMs) for mu (μ)-opioid receptors that may be useful for the treatment of pain, either alone or in combination with orthosteric opioid receptor agonists. Methods for treating pain and modulating mu (μ)-opioid receptors are also disclosed.

Abstract translation: 公开了用于mu（μ） - 阿片样受体的阳性变构调节剂（PAM）和沉默变构调节剂（SAM），其可用于治疗疼痛，单独或与正常阿片受体激动剂组合。 还公开了治疗疼痛和调节μ（μ） - 阿片受体的方法。

公开(公告)号：US09784740B2

公开(公告)日：2017-10-10

申请号：US14758908

申请日：2013-12-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Neil Burford ,  Andrew Alt

IPC: G01N33/566

CPC classification number: G01N33/566 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/10

Abstract: Disclosed are positive allosteric modulators (PAMs) and silent allosteric modulators (SAMs) for mu (μ)-opioid receptors that may be useful for the treatment of pain, either alone or in combination with orthosteric opioid receptor agonists. Methods for treating pain and modulating mu (μ)-opioid receptors are also disclosed.