Invention Grant
- Patent Title: Compound and method for modulating opioid receptor activity
- Patent Title (中): 调节阿片受体活性的化合物和方法
-
Application No.: US14128800Application Date: 2012-06-22
-
Publication No.: US09045526B2Publication Date: 2015-06-02
- Inventor: Henry I. Mosberg
- Applicant: Henry I. Mosberg
- Applicant Address: US MI Ann Arbor
- Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
- Current Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
- Current Assignee Address: US MI Ann Arbor
- Agency: Marshall, Gerstein & Borun LLP
- International Application: PCT/US2012/043819 WO 20120622
- International Announcement: WO2012/178063 WO 20121227
- Main IPC: A61K38/00
- IPC: A61K38/00 ; A61P23/00 ; C07K5/107 ; C07K7/06 ; A61K38/07 ; A61K45/06

Abstract:
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.
Public/Granted literature
- US20140154272A1 COMPOUND AND METHOD FOR MODULATING OPIOID RECEPTOR ACTIVITY Public/Granted day:2014-06-05
Information query
IPC分类: