公开(公告)号：EP2070926B1

公开(公告)日：2011-09-07

申请号：EP07816496.9

申请日：2007-09-30

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： HU, Lihong ,  YE, Jiming ,  LI, Jingya ,  JAMES, David, E ,  KRAEGEN, Edward, W ,  ZHANG, Hankun ,  CHENG, Zhe ,  LI, Jia

IPC分类号： C07D455/03 ,  A61K31/4375 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10

CPC分类号： C07D455/03

摘要： The present invention provides 13,13a-dihydroberberine derivatives as shown below, their physiologically acceptable salts, use and pharmaceutical composition comprising the said derivatives. The said 13,13a-dihydroberberine derivatives are glucose sorbefacient to muscle cells and have medical effects for improving glucose-tolerance and insulin-resistance, facilitating weight loss, relaxing fatty liver, etc, approved by tests to integer animals. The said compounds of the present invention can be used for treating diabetes mellitus, adiposity, fatty liver and their complications caused by insulin resistance.

公开(公告)号：EP2255816A1

公开(公告)日：2010-12-01

申请号：EP09708356.2

申请日：2009-01-14

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  The Garvan Institute Of Medical Research, Australia

发明人： YE, Yang ,  JAMES, David, E ,  TAN, Minjia ,  COONEY, Gregory, J ,  KE, Changqiang ,  KRAEGEN, Edward, W ,  CHEN, Tong ,  YE, Jiming ,  LI, Xiqiang

IPC分类号： A61K31/704 ,  A61K31/575 ,  A61P3/04 ,  A61P3/10

CPC分类号： A61K31/575 ,  A61K31/704

摘要： The present invention disclosed a medical use of cucurbitane triterpenoids represented by the following formula and isolated from Momordica charantia L. of Cucurbitaceae family in the preparation of medications for prevention and treatment of diabetes and obesity. The above cucurbitane triterpenoids may be acted as a glucose uptake stimulator, an agonist for the translocation of glucose transporter 4(GLUT4) to the cell membrane, and an activator of adenosine monophosphate-activated protein kinase (AMPK). They may have potential for the prevention and treatment of diabetes and obesity.

摘要翻译： 本发明游离缺失盘医疗使用由下式表示，并从葫芦科的苦瓜在药物用于预防和治疗糖尿病和肥胖的制备中分离葫芦三萜类化合物。 上述葫芦三萜类化合物可以充当葡萄糖摄取刺激物，以激动剂葡萄糖转运蛋白4（GLUT4）与细胞膜易位，以及磷酸腺苷活化蛋白激酶的激活剂（AMPK）。 他们可能有糖尿病和肥胖的预防和治疗潜力。

公开(公告)号：EP2255816B1

公开(公告)日：2016-03-30

申请号：EP09708356.2

申请日：2009-01-14

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  The Garvan Institute Of Medical Research, Australia

发明人： YE, Yang ,  JAMES, David, E ,  TAN, Minjia ,  COONEY, Gregory, J ,  KE, Changqiang ,  KRAEGEN, Edward, W ,  CHEN, Tong ,  YE, Jiming ,  LI, Xiqiang

IPC分类号： A61K31/704 ,  A61K31/575 ,  A61P3/04 ,  A61P3/10

CPC分类号： A61K31/575 ,  A61K31/704

公开(公告)号：EP2070926A1

公开(公告)日：2009-06-17

申请号：EP07816496.9

申请日：2007-09-30

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： HU, Lihong ,  YE, Jiming ,  LI, Jingya ,  JAMES, David, E ,  KRAEGEN, Edward, W ,  ZHANG, Hankun ,  CHENG, Zhe ,  LI, Jia

IPC分类号： C07D455/03 ,  A61K31/4375 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10

CPC分类号： C07D455/03

摘要： The present invention provides 13,13a-dihydroberberine derivatives or their physiologically acceptable salts represented by the following formula, pharmaceutical compositions comprising the same, and uses thereof. The 13,13a-dihydroberberine derivatives have an activity of promoting glucose absorption in muscle cells, and the whole animal tests show that the present compounds have effects on improving glucose-tolerance and insulin-resistance, facilitating weight loss, relieving fatty liver and the like. Thus, the present compounds can be used in treating diabetes mellitus, adiposity, fatty liver and complications thereof induced by insulin resistance.

摘要翻译： 本发明提供由下式表示的13,13a-二氢小檗碱衍生物或其生理学上可接受的盐，其包含其的药物组合物及其用途。 13,13a-二氢小檗碱衍生物具有促进肌肉细胞中葡萄糖吸收的活性，整个动物试验表明，本发明化合物具有改善葡萄糖耐量和胰岛素抵抗，促进体重减轻，缓解脂肪肝等作用 。 因此，本发明化合物可用于治疗由胰岛素抵抗引起的糖尿病，肥胖，脂肪肝及其并发症。