| 摘要 |
The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CBi 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 RI is hydrogen, halo, trifluoromethyl, C 1-4alkyl, C1-4 alkyloxy-or C1-4 alkyloxycarbonyl; R2 is hydrogen, phenyl, C3-7 cycloalkyl or C1-6alkyl optionally substituted with Ar 1; R3 is hydrogen, hydroxyl or C1-6alkyl; 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 C1-6 alkyl.
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