Urea derivatives as antagonists of the vanilloid receptor (vr1)

Details Urea derivatives as antagonists of the vanilloid receptor (vr1) Urea derivatives as antagonists of the vanilloid receptor (vr1)

C - Chemistry, Metallurgy

07

D

C07D 265/36 (2006.01) A61K 31/538 (2006.01) A61P 13/02 (2006.01) C07D 215/227 (2006.01)

Patent

CA 2563494

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

L'invention concerne des dérivés d'urée de formule générale (I) et des sels de ceux-ci qui sont utiles en tant qu'ingrédients actifs de préparations pharmaceutiques. Les dérivés d'urée de l'invention présente une excellente activité en tant qu'antagonistes du VR1 et sont utiles pour la prophylaxie et le traitement de maladies associées à l'activité du VR1, en particulier pour le traitement de troubles ou de maladies urologiques, de type hyperactivité vésicale (vessie hyperactive), incontinence urinaire, hyperactivité vésicale neurogène (hyperflexion vésicale), hyperactivité idiopathique (instabilité vésicale), hyperplasie prostatique bénigne, et symptômes des voies urinaires inférieures ; douleurs chroniques, douleurs neuropathiques, douleurs post-opératoires, douleurs dues à une polyarthrite rhumatoïde, névralgie, neuropathies, algésie, lésion nerveuse, ischémie, neurodégénération, accident vasculaire cérébral ; maladies respiratoires et troubles inflammatoires de type asthme, bronchopneumopathie chronique obstructive (COPD), rhume, toux, éternuements, bronchite de type aiguë et chronique, bronchiolite, rhinite, rhinite allergique, rhinite vasomotrice, mucosite, sinusite, allergie, troubles associés à des irritants exogènes de type fumée de tabac, brouillard de fumée, niveaux élevés de SO2 atmosphérique et de gaz nocifs sur le lieu de travail, hyperactivité des voies aériennes, intolérance aux produits laitiers, syndrome de Löffler, emphysème, mucoviscidose, bronchectasie, fibrose pulmonaire, pneumoconiose, collagénose avec manifestations vasculaires, maladie granulomateuse, laryngite, pharyngite, pneumonie, pleurésie, asthme persistent et bronchite asthmatique chronique. Dans ladite formule (I), n représente 0, 1, 2, 3, ou 4 ; X représente O, CH¿2?, S, or N(R?10¿) ; R?10¿ représentant hydrogène ou C¿1-6? alkyle.

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