3-phenyl-pyridine-derivatives

US6225316A · 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 16, 2000
• Grant date: May 1, 2001
• Expiry date: Feb 16, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D213/81
• 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 or trifluoromethyl; PA1 R.sup.1 is hydrogen or halogen; or PA1 R and R.sup.1 may be together --CH.dbd.CH--CH.dbd.CH--; PA1 R.sup.2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; PA1 R.sup.3 is hydrogen, lower alkyl or form a cycloalkyl group; PA1 R.sup.4 is hydrogen, --N(R.sup.5).sub.2, --N(R.sup.5)S(O).sub.2 -lower alkyl, --N(R.sup.5)C(O)R.sup.5 or a cyclic tertiary amine of the group ##STR2## PA1 R.sup.5 is, independently from each other, hydrogen, C.sub.3-6 -cycloalkyl, benzyl or lower alkyl; PA1 R.sup.6 is hydrogen, hydroxy, lower alkyl, --N(R.sup.5)CO-lower alkyl, hydroxy-lower alkyl, cyano, --CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, PA1 X is --C(O)N(R.sup.5)--, --(CH.sub.2).sub.m O--, --(CH.sub.2).sub.m N(R.sup.5)--, --N(R.sup.5)C(O)--, or --N(R.sup.5)(CH.sub.2).sub.m --; PA1 n is 0-4; and PA1 m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.