Compound and method for modulating opioid receptor activity

Patent metadata

Field	Value
Publication number	US-9045526-B2
Application number	US-201214128800-A
Country	US
Kind code	B2
Filing date	Jun 22, 2012
Priority date	Jun 23, 2011
Publication date	Jun 2, 2015
Grant date	Jun 2, 2015

Abstract

The invention provides a compound of formula (I), wherein R 1 is H, C(NH)NH 2 , an amino acid, or a peptide; X is OH, NH 2 , NHR 2 , NR 2 R 3 , an amino acid, or a peptide; R 2 and R 3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R 4 and R 5 is independently H or CH 3 ; Z is 2-amino-2,3-dihydro-1H-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1H-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that X is not NH 2 when R 1 is H, R 4 is H, R 5 is CH 3 , Z is Aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided.

First claim

What is claimed:

1. A compound having a structure of formula (I):

wherein
R 1 is H, C(NH)NH 2 , an amino acid, or a peptide;
X is OH, NH 2 , NHR 2 , NR 2 R 3 , an amino acid, or a peptide;
R 2 and R 3 are the same or different and selected from alkyl, alkylenearyl, or alkyleneheteroaryl;
each R 4 and R 5 is independently H or CH 3 ;
Z is an amino acid select…

Assignees

• Mosberg Henry I
• Univ Michigan

Inventors

• Mosberg Henry I

Classifications

• A61P29/00

  Human Necessities · mapped topic

• A61P23/00

  Human Necessities · mapped topic

• A61K45/06

  Human Necessities · mapped topic

• A61K38/00

  Human Necessities · mapped topic

• C07K5/1016 Primary

  Chemistry & Metallurgy · mapped topic