发明名称 |
Mixed ORL1/[mu] agonists for treating pain |
摘要 |
<p>Use of compounds (I), which exhibit an affinity for the mu -opioid-receptor of at least 100 nM (K i value for human) and an affinity for opioid receptor-like (ORL)-1-receptor, is claimed, where the ratio of the affinities ORL1/mu defined as 1/[K i(ORL1)/K i(mu )] is 1:10 to 30:1, for the production of a medicament and to treat: diabetic neuropathy; narcosis or analgesia during narcosis; pain in patients over 60 years and in patients with increased addictive potential and postoperative pain. An independent claim is included for use of a mu -agonist (II), which is selective as an ORL1/mu defined as 1/[K i(ORL1)/K i(mu )] 1:10, and a ORL1-agonist, which is selective as ORL1/mu defined as 1/[K i(ORL1)/K i(mu )] in a ratio of 30:1 in a mixture, which exhibits the characteristics of the compounds, for the manufacture of medicaments to treat pain. ACTIVITY : Neuroprotective; Analgesic. MECHANISM OF ACTION : Opioid receptor-like-1/mu -agonist.</p> |
申请公布号 |
EP2206498(B1) |
申请公布日期 |
2012.01.25 |
申请号 |
EP20100003202 |
申请日期 |
2007.09.26 |
申请人 |
GRUENENTHAL GMBH |
发明人 |
LINZ, KLAUS, DR.;KOEGEL, BABETTE-YVONNE, DR.;SCHROEDER, WOLFGANG, DR.;CHRISTOPH, THOMAS, DR.;DE VRY, JEAN, DR.;FRIDERICHS, ELMAR |
分类号 |
A61K31/407;A61K31/438;A61P25/04 |
主分类号 |
A61K31/407 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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