发明名称 |
Compound and method for modulating opioid receptor activity |
摘要 |
The invention provides a compound of formula (I), wherein R1 is H, C(NH)NH2, an amino acid, or a peptide; X is OH, NH2, NHR2, NR2R3, an amino acid, or a peptide; R2 and R3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R4 and R5 is independently H or CH3; 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 NH2 when R1 is H, R4 is H, R5 is CH3, 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.; |
申请公布号 |
US9045526(B2) |
申请公布日期 |
2015.06.02 |
申请号 |
US201214128800 |
申请日期 |
2012.06.22 |
申请人 |
THE REGENTS OF THE UNIVERSITY OF MICHIGAN |
发明人 |
Mosberg Henry I. |
分类号 |
A61K38/00;A61P23/00;C07K5/107;C07K7/06;A61K38/07;A61K45/06 |
主分类号 |
A61K38/00 |
代理机构 |
Marshall, Gerstein & Borun LLP |
代理人 |
Marshall, Gerstein & Borun LLP |
主权项 |
1. A compound having a structure of formula (I):wherein
R1 is H, C(NH)NH2, an amino acid, or a peptide; X is OH, NH2, NHR2, NR2R3, an amino acid, or a peptide; R2 and R3 are the same or different and selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R4 and R5 is independently H or CH3; Z is an amino acid selected from the group consisting of 2-amino-2,3-dihydro-1H-indene-2-carboxylic acid (Aci); 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid (Atc); 6-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine (Cha); cyclohexylglycine (Chg); homophenylalanine (Hfe); 1-naphthylalanine (1-Nal); 2-naphthylalanine (2-Nal); 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic); and octahydro-1H-indole-2-carboxylic acid (Oic); n is 0, 1, 2, 3, or 4;with the proviso that X is not NH2 when R1 is H, each R4 is H, each R5 is CH3, Z is Aci, and n is 2;or a pharmaceutically acceptable salt, ester or solvate thereof. |
地址 |
Ann Arbor MI US |