UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1)

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(R<10>), Wherein R<10> respresents hydrogen or C1-6 alkyl