4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/06 (2006.01) A61K 31/415 (2006.01) A61P 9/00 (2006.01) A61P 25/04 (2006.01) C07D 231/08 (2006.01) C07D 401/04 (2006.01) C07D 409/04 (2006.01)

Patent

CA 2401832

The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent antagonists of the cannabis CB1-receptor. The compounds have general formula (I) wherein R and R1 are the same or different and represent phenyl, thienyl or pyridyl which groups may be substituted with 1, 2 or 3 substituents Y or R and/or R1 represent naphtyl, R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v), Bb represents sulfonyl or carbonyl, R3 represents benzyl, phenyl, thienyl or pyridyl which may be substituted with 1, 2 or 3 substituents Y or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphtyl.

La présente invention concerne un groupe de nouveaux dérivés de 4,5-dihydro-1H-pyrazole qui sont de puissants antagonistes du récepteur CB1 du cannabis. Les composés ont la formule générale (I) dans laquelle : R et R1 sont identiques ou différents et représentent phényle, thiényle ou pyridyle, ces groupes pouvant être substitués avec 1, 2 ou 3 substituants Y, ou R et/ou R1 représente naphtyle ; R2 représente hydrogène, hydroxy, alkoxy en C1-3, acétyloxy ou propionyloxy ; Aa représente l'un des groupes (i), (ii), (iii), (iv) ou (v) ; Bb représente sulfonyle ou carbonyle ; R3 représente benzyle, phényle, thiényle or pyridyle qui peuvent être substitués avec 1, 2 ou 3 substituants Y, ou R3 représente alkyle en C1-8 linéaire ou ramifié ou cycloalkyle en C3-8, ou R3 représente naphtyle.

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