基本信息:
- 专利标题： TETRAHYDRO-QUINOLINYLUREA DERIVATIVES
- 专利标题（中）：四氢喹啉衍生物
- 申请号：PCT/EP2004/012051 申请日：2004-10-26
- 公开(公告)号：WO2005044802A2 公开(公告)日：2005-05-19
- 发明人： BOUCHON, Axel , DIEDRICHS, Nicole , HERMANN, Achim , LUSTIG, Klemens , MEIER, Heinrich , PERNERSTORFER, Josef , REISSMÜLLER, Elke , MOGI, Muneto , FUJISHIMA, Hiroshi , TAJIMI, Masaomi , YAMAMOTO, Noriyuki
- 申请人： BAYER HEALTHCARE AG , BOUCHON, Axel , DIEDRICHS, Nicole , HERMANN, Achim , LUSTIG, Klemens , MEIER, Heinrich , PERNERSTORFER, Josef , REISSMÜLLER, Elke , MOGI, Muneto , FUJISHIMA, Hiroshi , TAJIMI, Masaomi , YAMAMOTO, Noriyuki
- 申请人地址： 51368 Leverkusen DE
- 专利权人： BAYER HEALTHCARE AG,BOUCHON, Axel,DIEDRICHS, Nicole,HERMANN, Achim,LUSTIG, Klemens,MEIER, Heinrich,PERNERSTORFER, Josef,REISSMÜLLER, Elke,MOGI, Muneto,FUJISHIMA, Hiroshi,TAJIMI, Masaomi,YAMAMOTO, Noriyuki
- 当前专利权人： BAYER HEALTHCARE AG,BOUCHON, Axel,DIEDRICHS, Nicole,HERMANN, Achim,LUSTIG, Klemens,MEIER, Heinrich,PERNERSTORFER, Josef,REISSMÜLLER, Elke,MOGI, Muneto,FUJISHIMA, Hiroshi,TAJIMI, Masaomi,YAMAMOTO, Noriyuki
- 当前专利权人地址： 51368 Leverkusen DE
- 代理机构： BAYER HEALTHCARE AG
- 优先权： EP03025575.6 20031108
- 主分类号： C07D215/00
- IPC分类号： C07D215/00
摘要：
This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-quinolinylurea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
摘要（中）：
本发明涉及可用作药物制剂活性成分的四氢 - 喹啉基脲衍生物及其盐。 本发明的四氢 - 喹啉基脲衍生物具有香草素受体（VR1）拮抗活性，可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗泌尿系统疾病或障碍，例如逼尿肌过度活动 膀胱过度活动），尿失禁，神经源性逼尿肌反应性（逼尿肌hyperflexia），特发性逼尿肌过度活动（逼尿肌不稳定），良性前列腺增生和下尿路症状; 慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风和炎性疾病如哮喘和慢性阻塞性肺（或气道）疾病（COPD）。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D215/00 | 杂环化合物，含喹啉或氢化喹啉环系 |