BENZOTRIAZOLE DERIVATIVES AS CANNABINOID RECEPTOR ANTAGONISTS

摘要

The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CB_i modulators (known as antagonists or inverse agonists), useful in the treatment obesity, psychiatric and neurological disorders, as well as other diseases involving cannabinoid-CB₁ neurotransmission (Current Opinion in Drug Discovery & Development 2004 7(4):498-506) the pharmaceutically acceptable acid addition salts and stereoisomeric forms thereof, wherein R^I is hydrogen, halo, trifluoromethyl, C_1-4alkyl, C_1-4 alkyloxy- or C_1-4 alkyloxycarbonyl; R² is hydrogen, phenyl, C_3-7cycloalkyl or C_1-6alkyl optionally substituted with Ar¹; R³ is hydrogen, hydroxyl or C_1-6alkyl; Ar¹ is phenyl or phenyl substituted with up to three halo substituents; and Het represents a monocyclic 5 or 6 membered partially saturated or aromatic heterocycle selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, pyrimidinyl, pyridinyl, pyrazinyl, triazinyl, pyridazinyl, 2H-pyranyl or 4H-pyranyl wherein said heterocycle is optionally substituted with C_1-6alkyl.