基本信息:
- 专利标题： SUBSTITUTED 2-PHENYL-BENZIMIDAZOLES AND THEIR USE AS PHARMACEUTICALS
- 专利标题（中）：取代的2-苯基苯并咪唑及其作为药物的用途
- 申请号：PCT/EP2007/008104 申请日：2007-09-18
- 公开(公告)号：WO2008037381A1 公开(公告)日：2008-04-03
- 发明人： ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
- 申请人： SANOFI-AVENTIS , ZOLLER, Gerhard , STROBEL, Hartmut , WILL, David, William , WOHLFART, Paulus
- 申请人地址： 174, avenue de France F-75013 Paris FR
- 专利权人： SANOFI-AVENTIS,ZOLLER, Gerhard,STROBEL, Hartmut,WILL, David, William,WOHLFART, Paulus
- 当前专利权人： SANOFI-AVENTIS,ZOLLER, Gerhard,STROBEL, Hartmut,WILL, David, William,WOHLFART, Paulus
- 当前专利权人地址： 174, avenue de France F-75013 Paris FR
- 代理机构： KUJATH, Eckard
- 优先权： EP06020654.7 20060930
- 主分类号： C07D235/18
- IPC分类号： C07D235/18 ; C07D413/04 ; A61K31/4184 ; A61K31/4245 ; A61P9/00
摘要：
The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula (I), in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula(I) upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula (I), to pharmaceutical compositions comprising them, and to the use of compounds of the formula (I) for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
摘要（中）：
本发明涉及式（I）的2-苯基 - 苯并咪唑的衍生物，其中X，R，R 1至R 3和n具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录 并且是有价值的药理活性化合物。 具体地，式（I）化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下使用。 本发明还涉及制备式（I）化合物，包含它们的药物组合物的方法，以及式（I）化合物在制备用于刺激内皮细胞表达的药物中的应用 NO合成酶或用于治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心脏功能不全等各种疾病。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D235/00 | 杂环化合物，含1,3-二唑或氢化1,3-二唑环、与其他环稠合 |
| --------C07D235/02 | .与碳环或碳环系稠合 |
| ----------C07D235/04 | ..苯并咪唑；氢化苯并咪唑 |
| ------------C07D235/18 | ...有芳基直接连在位置2 |