1,3,8-triazaspiro[4,5]decan-4-one derivatives

US6071925A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Geo Adam · Schopfheim, DE
• Andrea Cesura · Nyon, CH
• Guido Galley · Rheinfelden (Baden), DE
• François Jenck · Riedisheim, FR
• Frederick Monsma · Baltimore, US
• Stephan Rover · Weil am Rhein, DE
• Jurgen Wichmann · Steinen, DE

Key dates

• Filing date: Jan 20, 1998
• Grant date: Jun 6, 2000
• Expiry date: Jan 20, 2018

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, lower alkoxy or halogen; PA0 R.sup.3 is phenyl, which is unsubstituted or substituted by lower alkyl, CF.sub.3, lower alkoxy or halogen; PA0 R.sup.4 is hydrogen, lower alkyl, lower alkenyl, --C(O)-lower alkyl, --C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylene-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF.sub.3, phenyl or benzyl, PA0 R.sup.5 and R.sup.6 are each independently hydrogen, phenyl, lower alkyl or di-lower alkyl or R.sup.5 and R.sup.6 together with the carbon atoms to which they are bound form a phenyl ring, or PA0 R.sup.5 and one of R.sup.1 or R.sup.2 together with the carbon atoms to which they are bound form a saturated or unsaturated 6 membered ring, PA0 A is a 4-7 membered saturated ring, their racemates and the enantiomers thereof, and the pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.