Biphenyl derivatives

US6291465A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Michael Bos · Montréal, CA
• Guido Galley · Rheinfelden (Baden), DE
• Thierry Godel · Basel, CH
• Torsten Hoffmann · Weil am Rhein, DE
• Walter Hunkeler · Magden, CH
• Patrick Schnider · Bottmingen, CH
• Heinz Stadler · Basel, CH

Key dates

• Filing date: Feb 25, 2000
• Grant date: Sep 18, 2001
• Expiry date: Feb 25, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C235/42
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of the formula ##STR1## wherein PA1 R is hydrogen, lower alkyl, lower alkoxy halogen, amino, --N(R.sup.6).sub.2 or trifluoromethyl; PA1 R.sup.1 is hydrogen lower alkoxy or halogen, PA1 R and R.sup.1 may be together --CH.dbd.CH--CH.dbd.CH--; PA1 R.sup.2 is halogen, lower alkyl or trifluoromethyl; PA1 R.sup.3 is hydrogen or lower alkyl; PA1 R.sup.4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; PA1 R.sup.5 is hydrogen, nitro, amino or --N(R.sup.6).sub.2 ; PA1 R.sup.6 is hydrogen or lower alkyl, PA1 X is --C(O)N(R.sup.6)--, --(CH.sub.2).sub.n O--, (CH.sub.2).sub.n N(R.sup.6)--, --N(R.sup.6)C(O)-- or --N(R.sup.6)(CH.sub.2).sub.n --; and PA1 n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.