TETRAHYDRO-QUINOLINYLUREA DERIVATIVES
    1.
    发明公开
    TETRAHYDRO-QUINOLINYLUREA DERIVATIVES 有权
    四氢呋喃 - 喹啉类衍生物

    公开(公告)号:EP1685112A2

    公开(公告)日:2006-08-02

    申请号:EP04790836.3

    申请日:2004-10-26

    IPC分类号: C07D215/00

    CPC分类号: C07D215/38

    摘要: This invention relates to tetrahydro quinolinylurea derivatives (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-quinolinylurea ueri votive (J.) of the present invention has vanilloid receptor (VRl) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VRl 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), beniyn proscatic 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).

    摘要翻译: 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(Ⅰ)及其盐。 本发明的四氢喹啉基尿酸还原剂(J.)具有类香草素受体(VR1)拮抗活性,并且可用于预防和治疗与VR1活性相关的疾病,特别是用于治疗泌尿科疾病或病症, 如逼尿肌过度活动(膀胱活动过度),尿失禁,神经原性逼尿肌过度活动(逼尿肌反射过度),特发性逼尿肌过度活动(逼尿肌不稳定),beniyn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,中风和炎症如哮喘和慢性阻塞性肺(气道)疾病(COPD)。

    BICYCLIC AMIDE, CARBAMATE OR UREA DERIVATIVES AS VANILLOID RECEPTOR MODULATORS
    6.
    发明授权
    BICYCLIC AMIDE, CARBAMATE OR UREA DERIVATIVES AS VANILLOID RECEPTOR MODULATORS 有权
    双酚A胺,卡巴胺 - 硬脂酸盐

    公开(公告)号:EP1687262B1

    公开(公告)日:2008-11-19

    申请号:EP04790835.5

    申请日:2004-10-26

    摘要: This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea 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).

    摘要翻译: 本发明涉及可用作药物制剂活性成分的双环酰胺,氨基甲酸酯或脲衍生物及其盐。 本发明的双环酰胺,氨基甲酸酯或脲衍生物具有香草素受体(VR1)拮抗活性,并且可用于预防和治疗与VR1活性相关的疾病,特别是用于治疗泌尿系统疾病或病症,例如 逼尿肌过度活动症(膀胱过度活动症),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,中风和炎症性疾病如哮喘和慢性阻塞性肺部(或气道)疾病(COPD)。

    UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1)
    8.
    发明公开
    UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1) 审中-公开
    脲衍生物AS香草素拮抗剂(VR1)

    公开(公告)号:EP1740557A1

    公开(公告)日:2007-01-10

    申请号:EP05716548.2

    申请日:2005-04-07

    CPC分类号: C07D265/36 C07D215/227

    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