Quinolein-2 (1H)-one derivatives as serotonin antagonists

US5958924A · kind A · utility

Assignee

• Synthelabo · FR

Inventors

• Gary MCCORT · Paris, FR
• Christian Hoornaert · Antony, FR
• Genevieve Dellac · Morangis, FR
• Michel Aletru · Antony, FR

Key dates

• Filing date: Feb 4, 1998
• Grant date: Sep 28, 1999
• Expiry date: Feb 4, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of formula (I) ##STR1## in which A represents a 4-(thieno3,2-c! pyridin-4-yl)-1-piperazinyl or 4-(4-fluorobenzoyl)-1-piperidyl group, R.sub.1 and R.sub.2 each represent, independently of one another, either a hydrogen or halogen atom, or an amino, hydroxyl, nitro, cyano, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, trifluoromethyl, trifluoromethoxy or --COOH group, a group --COOR.sub.4, a --CONH.sub.2 group or a group --CONHR.sub.4, --CONR.sub.4 R.sub.5, --SR.sub.4, --SO.sub.2 R.sub.4, --NHCOR.sub.4, --NHS0.sub.2 R.sub.4 or --N(R.sub.4).sub.2, where R.sub.4 and R.sub.5 are each a (C.sub.1 -C.sub.4)alkyl group, R.sub.3 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group, or a group --(CH.sub.2)OH, --(CH.sub.2).sub.p NH.sub.2, --(CH.sub.2).sub.n COOH, --(CH.sub.2).sub.n COOR.sub.4, --(CH.sub.2).sub.n CONH.sub.2, --(CH.sub.2).sub.n CONHOH, --(CH.sub.2).sub.p SH, --(CH.sub.2).sub.n SO.sub.3 H, --(CH.sub.2).sub.n SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHR.sub.4, --(CH.sub.2).sub.n SO.sub.2 NH.sub.4 R.sub.5, --(CH.sub.2).sub.n CONHR.sub.4, --(CH.sub.2).sub.n CONR.sub.4 R.sub.5, --(CH.sub.2).sub.p NHSO.sub.2 R.sub.4, --(CH.sub.2).sub.p NHCOR.sub.4…