发明名称 Morphinoid derivatives as delta-opioid agonists and antagonists
摘要 Compounds of formula (I) in which R1 is hydrogen or alkyl; R2 is hydrogen or one or more alkyl groups; R3 is R1 or R1X-; wherein R1 is hydrogen or optionally substituted alkyl, aryl, arylalkyl, cycloalkyl or heterocyclyl and X is a linking group; and R4 is hydrogen or alkyl; with the proviso that when R4 is methyl and R3 is methyl or hydroxyethyl then R2 is not hydrogen. Are selective delta opioid receptor ligands and therefore of potential therapeutic utility as analgesics and antihyperalgesics for different pain conditions; immunosuppressants to prevent rejection in organ transplant and skin grafts; anti-allergic and anti-inflammatory agents; brain cell protectants; agents for treating drug and alcohol abuse, gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness and epilepsy.
申请公布号 AU2477202(A) 申请公布日期 2002.04.22
申请号 AU20020024772 申请日期 2001.10.05
申请人 GLAXOSMITHKLINE S.P.A. 发明人 GIULIO DONDIO;STEFANIA GAGLIARDI;DAVIDE GRAZIANI;LUCA FRANCESCO RAVEGLIA
分类号 C07D489/00;A61K31/496;A61K31/497;A61K31/506;A61P1/00;A61P1/12;A61P5/00;A61P9/00;A61P11/00;A61P25/00;A61P25/04;A61P25/08;A61P25/18;A61P25/30;A61P29/00;A61P31/00;A61P37/02;A61P37/08;A61P43/00;C07D491/22 主分类号 C07D489/00
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