发明公开
- 专利标题: UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1)
- 专利标题(中): 脲衍生物AS香草素拮抗剂(VR1)
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申请号: EP05716548.2申请日: 2005-04-07
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公开(公告)号: EP1740557A1公开(公告)日: 2007-01-10
- 发明人: FUJISHIMA, Hiroshi , MOGI, Muneto , YUASA, Hiroaki , TAIJIMI, Masaomi , YAMAMOTO, Noriyuki , HAYASHI, Fumihiko , TSUKIMI, Yasuhiro , GUPTA, Jang
- 申请人: Bayer HealthCare AG
- 申请人地址: 51368 Leverkusen DE
- 专利权人: Bayer HealthCare AG
- 当前专利权人: Bayer HealthCare AG
- 当前专利权人地址: 51368 Leverkusen DE
- 优先权: EP04009274 20040420
- 国际公布: WO2005103018 20051103
- 主分类号: C07D265/36
- IPC分类号: C07D265/36 ; C07D215/227 ; A61K31/538 ; A61P13/02
摘要:
This invention relates to urea derivatives according to general formula I and salts thereof which are useful as active ingredients of pharmaceutical preparations. The urea 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 urological disorder or disease, 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 respiratory diseases and inflammatory disorders such as asthma, chronic obstructive pulmonary (or airways) disease (COPD), common cold, cough, sneeze, bronchitis including acute and chronic bronchitis, bronchiolitis, rhinitis, allergic rhinitis, vasomotor rhinitis, mucositis, sinusitis, allergy, disorders associated with exogenous irritants such as tobacco smoke, smog, high levels of atmospheric SO2 and noxious gases in the workplace, and airways hyperreactivity, milk product intolerance, Loffler's pneumonia, emphysema, cystic fibrosis, bronchiectasis, pulmonary fibrosis, pneumoconiosis, collagen vascular disease, granulomatous disease, laryngitis, pharyngitis, pneumonia, pleuritis, persistent asthma and chronic asthmatic bronchitis. Formula I Wherein n represents 0, 1, 2, 3, or 4; X represents O, CH2, S, or N(R10), Wherein R10 respresents hydrogen or C1-6 alkyl
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