- 专利标题： MORPHINAN-DERIVATIVES FOR TREATING DIABETES AND RELATED DISORDERS
- 专利标题（中）： 佐治亚人
-
申请号： EP12756653.7申请日： 2012-08-22
-
公开(公告)号： EP2747754A1公开(公告)日： 2014-07-02
- 发明人: LAMMERT, Eckhard , MARQUARD, Jan , MEISSNER, Thomas
- 申请人： Heinrich-Heine-Universität Düsseldorf
- 申请人地址： Universitätsstrasse 1 40225 Düsseldorf DE
- 专利权人： Heinrich-Heine-Universität Düsseldorf
- 当前专利权人： Heinrich-Heine-Universität Düsseldorf
- 当前专利权人地址： Universitätsstrasse 1 40225 Düsseldorf DE
- 代理机构： Bülle, Jan
- 优先权： EP11006980 20110826; EP11010129 20111221
- 国际公布： WO2013029762 20130307
- 主分类号： A61K31/00
- IPC分类号： A61K31/00 ; A61K31/155 ; A61K31/485
摘要：
The invention relates to a morphinan-derivative that targets NMDA receptors on pancreatic islets and has the general formula (I) wherein R
1 is selected from -OH, -CO
2 H, -R
0 , -OR
0 , -OC(=O)R
0 , -OC(=O)OR
0 or -OC(=O)NHR
0 ; and R
2 is selected from -H, -R
0 , -C(=O)R
0 , -C(=O)OR
0 , -C(=O)NHR
0 or -C(=NH)-NH- C(=NH)-NH
2 ; wherein R
0 is in each case independently selected from -C
1 -C
6 -alkyl, - aryl, -heteroaryl, -C
1 -C
6 -alkyl-aryl or -C
1 -C
6 -alkyl-heteroaryl, in each case independently unsubstituted or substituted; or its physiologically acceptable salt and/or stereoisomer, including mixtures thereof in all ratios, for use in the treatment of a disease or condition, where the disease or condition is insulin-dependent diabetes mellitus, non-insulin-dependent diabetes mellitus, obesity, and/or diabetic nephropathy.
1 is selected from -OH, -CO
2 H, -R
0 , -OR
0 , -OC(=O)R
0 , -OC(=O)OR
0 or -OC(=O)NHR
0 ; and R
2 is selected from -H, -R
0 , -C(=O)R
0 , -C(=O)OR
0 , -C(=O)NHR
0 or -C(=NH)-NH- C(=NH)-NH
2 ; wherein R
0 is in each case independently selected from -C
1 -C
6 -alkyl, - aryl, -heteroaryl, -C
1 -C
6 -alkyl-aryl or -C
1 -C
6 -alkyl-heteroaryl, in each case independently unsubstituted or substituted; or its physiologically acceptable salt and/or stereoisomer, including mixtures thereof in all ratios, for use in the treatment of a disease or condition, where the disease or condition is insulin-dependent diabetes mellitus, non-insulin-dependent diabetes mellitus, obesity, and/or diabetic nephropathy.
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