4-phenyl-pyrimidine derivatives

US6274588A · 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: May 22, 2000
• Grant date: Aug 14, 2001
• Expiry date: May 22, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention provides compounds of the formula ##STR1## wherein PA1 R.sup.1 is hydrogen or halogen; PA1 R.sup.2 is hydrogen, halogen, lower alkyl or lower alkoxy; PA1 R.sup.1 and R.sup.2 may together be --CH.dbd.CH--CH.dbd.CH--, wherein R1 and R.sup.2 together with the two carbon ring atoms to which they are attached form a fused ring; PA1 R.sup.3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; PA1 R.sup.4 /R.sup.4' are each independently hydrogen or lower alkyl; PA1 R.sup.5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, --(CH.sub.2).sub.n -piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, --(CH.sub.2).sub.n -morpholinyl, --(CH.sub.2).sub.n -piperidinyl, --(CH.sub.2).sub.n+1 -imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, --NH--(CH.sub.2).sub.n+1 N(R.sup.4").sub.2, --(CH.sub.2).sub.n+1 N(R.sup.4").sub.2, --O--(CH.sub.2).sub.n+1 -morpholinyl, --O--(CH.sub.2).sub.n+1 -piperidinyl or --O--(CH.sub.2).sub.n+1 N(R.sup.4").sub.2, wherein R.sup.4" is hydrogen or lower alkyl; and PA1 n is 0-2; PA1 X is --C(O)N(R.sup.4")-- or…