CANNABINOID RECEPTOR MODULATORS

• Main Authors: NIELSEN, PETER AADAL, LINGET, JEAN-MICHEL, BJURLING, EMELIE, HOEGBERG, THOMAS, ALMHOLT, DORTHE, RECEVEUR, JEAN MARIE, MURRAY, ANTHONY, NOERREGAARD, PIA KARINA
• Format: Patent
• Language: English; French
• Published: 18.06.2009
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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(R10)(R11)-*, -C(R10)(R11)-O-*, -C(R10)(R11)CH2-*, -C(R10)(R11)CH2-O-*, -CH2C(R10)(R11)-*, -CH2C(R10)(R11) -O-*. and -CH2-O-C(R10)(R11)-*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)aIkyI or (C1C3)fluoroalkyl; R4 is a radical of formula -(AIk1)P-(Q1)r (L)s -Q2 wherein p, r, s, AIk1, L, Q1 and Q2 are as specified; or R3 and R4 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-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, -NH2-, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen -F, -Cl, -Br, -CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and -OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.