Benzotriazole derivatives as cannabinoid receptor antagonists

Details Benzotriazole derivatives as cannabinoid receptor antagonists Benzotriazole derivatives as cannabinoid receptor antagonists

A - Human Necessities

61

K

A61K 31/4192 (2006.01) A61P 3/04 (2006.01) C07D 403/06 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2600052

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, C1-4alkyl, C1-4 alkyloxy- or C1-4 alkyloxycarbonyl; R2 is hydrogen, phenyl, C3- 7cycloalkyl or C1-6alkyl optionally substituted with Ar1; 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 C1-6alkyl.

La présente invention concerne un groupe de dérivés de benzotriazole, infra qui sont de puissant modulateurs cannabinoïdes-CBi (communément appelés antagonistes ou agonistes inverses), utilisés dans le traitement de l'obésité, des troubles psychiatriques et neurologiques et d'autres maladies impliquant la neurotransmission cannabidoïde-CB1 (selon Current Opinion in Drug Discovery & Development 2004 7(4):498-506), leurs sels d'addition acide pharmaceutiquement acceptables et leurs formes stéréoisomères. R1 désigne hydrogène, halo, trifluorométhyle, alkyle C1-4, alkyloxy C1-4 ou alkyloxycarbonyle C1-4; R2 désigne hydrogène, phényle, cycloalkyle C3-7 ou alkyle C1-6 éventuellement substitué par Ar1; R3 désigne hydrogène, hydroxyle ou alkyle C1-6; Ar1 désigne phényle ou phényle substitué par jusqu'à trois substituants halo; et Het désigne un hétérocycle monocyclique à 5 ou 6 membres partiellement saturé ou aromatique sélectionné dans le groupe furanyle, thiényle, pyrrolyle, oxazolyle, thiazolyle, imidazolyle, pyrazolyle, isoxazolyle, isothiazolyle, oxadiazolyle, triazolyle, thiadiazolyle, pyrimidinyle, pyridinyle, pyrazinyle, triazinyle, pyridazinyle, 2H-pyranyle ou 4H-pyranyle, ledit hétérocycle étant éventuellement substitué par alkyle C1-6.

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