HYDROXY-TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES
    4.
    发明公开
    HYDROXY-TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES 有权
    羟基 - 四氢萘 - 萘酚衍生物

    公开(公告)号:EP1594836A1

    公开(公告)日:2005-11-16

    申请号:EP04708355.5

    申请日:2004-02-05

    摘要: This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VRl antagonist and are useful for the prophylaxis and treatment of diseases associated with VRl 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.

    摘要翻译: 本发明涉及可用作药物制剂活性成分的羟基 - 四氢 - 萘基脲衍生物及其盐。 本发明的羟基 - 四氢 - 萘基脲衍生物作为VR1拮抗剂具有极好的活性,并且可用于预防和治疗与VR1活性相关的疾病,特别是用于治疗尿失禁,急迫性尿失禁,膀胱过度活动症,慢性 疼痛,神经性疼痛,手术后疼痛,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,炎性病症,哮喘和COPD。

    2-NAPHTHAMIDE DERIVATIVES
    10.
    发明公开
    2-NAPHTHAMIDE DERIVATIVES 审中-公开
    2-萘酰胺衍生物

    公开(公告)号:EP1515941A1

    公开(公告)日:2005-03-23

    申请号:EP03735507.0

    申请日:2003-05-30

    CPC分类号: C07C235/66

    摘要: The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.

    摘要翻译: 本发明涉及可用作药物制剂活性成分的2-萘酰胺。 本发明的2-萘酰胺具有IP受体拮抗活性,可用于预防和治疗与IP受体活性有关的疾病。 这些疾病包括泌尿系统疾病或病症如下:膀胱出口梗阻,膀胱过度活动症,尿失禁,逼尿肌反射亢进,逼尿肌不稳定,膀胱容量减少,排尿频率,急迫性尿失禁,压力性尿失禁,膀胱高反应性,良性前列腺肥大(BPH ),前列腺炎,尿频,夜尿,尿急,骨盆过敏症,尿道炎,骨盆疼痛综合征,前列腺痛,膀胱炎或特发性膀胱过敏症。 本发明化合物还可用于治疗疼痛,包括但不限于炎症性疼痛,神经性疼痛,急性疼痛,慢性疼痛,牙齿疼痛,经前期疼痛,内脏疼痛,头痛等; 低血压; 血友病和出血; 和炎症,因为通过用IP受体拮抗剂治疗也可以缓解疾病。