- 专利标题: Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists
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申请号: US10537217申请日: 2003-11-28
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公开(公告)号: US20060135505A1公开(公告)日: 2006-06-22
- 发明人: Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
- 申请人: Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
- 申请人地址: DE Leverkusen 51368
- 专利权人: Bayer Healthcare AG
- 当前专利权人: Bayer Healthcare AG
- 当前专利权人地址: DE Leverkusen 51368
- 优先权: EP02027528.5 20021209
- 国际申请: PCT/EP03/13452 WO 20031128
- 主分类号: A61K31/445
- IPC分类号: A61K31/445 ; A61K31/40 ; A61K31/397 ; A61K31/17
摘要:
This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.