Benzosulfone derivatives

US5990105A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Michael Bos · Montréal, CA
• Walter Hunkeler · Magden, CH
• Claus Riemer · Glückstadt, DE

Key dates

• Filing date: Jan 15, 1999
• Grant date: Nov 23, 1999
• Expiry date: Jan 15, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D239/38
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to novel compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen; PA0 R.sup.2 is hydrogen, trifluoromethyl or lower alkyl; PA0 R.sup.3 is hydrogen or amino; or PA0 R.sup.1 and R.sup.2 or R.sup.3 and R.sup.2 taken together are --CH.dbd.CH--CH.dbd.CH--; PA0 Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; PA0 R.sup.4, R.sup.5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group --NH(CH.sub.2).sub.n NR.sup.6 R.sup.7, --N(CH.sub.3)(CH.sub.2).sub.n NR.sup.6 R.sup.7, --NH(CH.sub.2).sub.n -morpholin-4-yl or --NH(CH.sub.2).sub.n OH; PA0 n is 2-4 PA0 R.sup.6 and R.sup.7 are each independently hydrogen or lower alkyl, and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.