Quinazolinone derivatives useful as vanilloid antagonists

摘要

The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.;

主权项

1. A method for modulating vanilloid receptor 1 activity, comprising administering to a mammal in need thereof a therapeutically effective amount of a quinazolinone compound of the formula (Ia) wherein R1 is C2-C6alkyl, (C1-C6alkyl)C1-C6alkyl, di-(C1-C6alkyl)C1-C6alkyl, or C3-C6cycloalkyl; each R2, independently, is halogen, C1-C6alkyl, halogen-substituted C1-C6alkyl, hydroxyC1-C6alkyl, cyano or a group —C(═O)—R2a, where R2a is C1-C6alkyl; R3 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, hydroxy, hydroxy-substituted C1-C6alkyl, C1-C6alkoxy, C3-C6cycloalkyl, cyano, —C(C═O)H, phenyl, (C3-C6cycloalkyl)C1-C6alkoxy, (C1-C6alkoxycarbonylamino)C1-C6alkoxy or (C1-C6alkylcarbonylamino)C1-C6alkoxy; R4 is hydroxy, esterified hydroxy, etherified hydroxy, a group or a group where R4a is halogen-substituted C1-C6alkyl, or a group where R4b is benzyl or phenylethyl; and m is 1 or 2, in free base form or in pharmaceutically acceptable salt form.