abstract |
Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R 10 )(R 11 )—*, —C(R 10 )(R 11 )—O—*, —C(R 10 )(R 11 )CH 2 —*, —C(R 10 )(R 11 )CH 2 —O—*, —CH 2 C(R 10 )(R 11 )—*, —CH 2 C(R 10 )(R 11 )—O—*. and —CH 2 —O—C(R 10 )(R 11 )—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R 3 is hydrogen, (C 1 -C)alkyl or (C 1 C 3 )fluoroalkyl; R 4 is a radical of formula -(Alk 1 ) p -(Q 1 ) r (L) s -Q 2 wherein p, r, s, Alk 1 , L, Q 1 and Q 2 are as specified; or R 3 and R 4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L) s -Q 2 wherein s, L and Q 2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH 2 —, or mono- or di-(C 1 C 3 )alkylamino; R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C 1 -C 3 )alkyl, (C 1 C 3 )fluoroalkyl, cyclopropyl, and —OR 9 ; R 10 is hydrogen, (C 1 C 3 )alkyl, hydroxyl or NH 2 , and R 11 is hydrogen or (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring. |