Memorial Sloan Kettering Cancer Center

Sloan-kettering Institute for Cancer Research

Leland Stanford Junior University

University of Florida Research Foundation, Incorporated

University of Southern California

The University of North Carolina at Chapel Hill

University of Health Sciences & Pharmacy in St. Louis

Susruta Majumdar

Gavril W Pasternak

Bryan Leo Roth

Jay McLaughlin

Evan N Feinberg

Vijay S Pande

Andras Varadi

Rajendra Uprety

Rashad Karimov

Vsevolod Katritch

Saheem Zaidi

Gavril Pasternak

In some aspects, the present disclosure provides compounds of the formula: wherein the variables are as defined herein. In some embodiments, these compounds may be used to reduce the pain of a patient. These compounds may be used in pain relief and show an improved pharmaceutical profile relative to other commonly used opiates and opioid derivatives.

G-protein biased opioid receptor agonist/analgesics with reduced arrestin recruitment

Ligands of the mu, kappa, and delta opioid receptors and methods of using them are disclosed. In particular, the invention relates to the discovery of new opioid receptor ligands based on molecular dynamics simulations of conformational states of the &#x3bc; opioid receptor and the use of the identified opioid receptor ligands as analgesics, anti-diarrheal agents, and overdose reversal agents.

Ligands of the mu, kappa, and delta opioid receptors

Described herein are compounds of Formulae (I')-(II&#x2032;), compounds of Formulae (I)-(II) and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful for modulating opioid receptor activity. The provided compounds may have both agonistic and antagonistic effect on one or more opioid receptors. Methods of using the compounds for treating or managing pain are also described. 

Mitragynine analogs and uses thereof

Compounds of formula: in which Ris chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.

6-amido derivatives of 4,5A-epoxymorphinans for treatment of pain

6-amido derivatives of 4, 5-a epoxymorphinans for the treatment of pain

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Stamford, CT, United States of America

Susruta Majumdar