Modulators of CB1 receptors

US8148404B2 · kind B2 · utility

Assignee

• 7TM Pharma A/S · DK

Inventors

• Martin Cooper · Loughborough, GB
• Jean-Marie Receveur · Montpellier, FR
• Thomas Hoegberg · Hørsholm, DK
• Peter Aadal Nielsen · Oxie, SE
• Jean-Michel Linget · Hørsholm, DK
• Pia Karina Noeregaard · Hørsholm, DK
• Anthony Murray · Hellerup, DK
• Emelie Bjurling · Hørsholm, DK

Key dates

• Filing date: Dec 17, 2007
• Grant date: Apr 3, 2012
• Expiry date: Feb 21, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B1 is —CO—, -0-, —S—, —SO—, —SO2—, —CH2—, —CHCH3—, —CHOH— or —NR7—; or (iii) a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(…