摘要 |
The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CB<SUB>1 </SUB>modulators (known as antagonists or inverse agonists), useful in the treatment obesity, psychiatric and neurological disorders, as well as other diseases involving cannabinoid-CB<SUB>1 </SUB>neurotransmission (Current Opinion in Drug Discovery & Development 2004 7(4):498-506) the pharmaceutically acceptable acid addition salts and stereoisomeric forms thereof, wherein R<SUP>1 </SUP>is hydrogen, halo, trifluoromethyl, C<SUB>1-4</SUB>alkyl, C<SUB>1-4</SUB>alkyloxy- or C<SUB>1-4</SUB>alkyloxycarbonyl; R<SUP>2 </SUP>is hydrogen, phenyl, C<SUB>3-7</SUB>cycloalkyl or C<SUB>1-6</SUB>alkyl optionally substituted with Ar<SUP>1</SUP>; R<SUP>3 </SUP>is hydrogen, hydroxyl or C<SUB>1-6</SUB>alkyl; Ar<SUP>1 </SUP>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<SUB>1-6</SUB>alkyl;
|