Benzylidene-1,3-dihydro-indol-2-one derivatives a receptor tyrosine kinase inhibitors, particularly of Raf kinases

US6268391A · kind A · utility

Assignee

• Glaxo Wellcome Inc. · US

Inventors

• Scott Howard Dickerson · Chapel Hill, US
• Philip Anthony Harris · Raleigh, US
• Robert Neil Hunter, III · Boston, US
• David Kendall Jung · Durham, US
• Karen Elizabeth Lackey · Durham, US
• Robert W. McNutt, Jr. · Durham, US
• Michael Peel · Morrisville, US
• James Marvin Veal · Apex, US

Key dates

• Filing date: Apr 7, 2000
• Grant date: Jul 31, 2001
• Expiry date: Apr 7, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds of general formula (I) wherein: R.sup.1 is H or optionally joined with R.sup.2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R.sup.2 and R.sup.3 are independently H, HET, aryl, C.sub.1-12 aliphatic, CN, NO.sub.2, halogen, R.sup.10, --OR.sup.10, --SR.sup.10, --S(O)R.sup.10, --SO.sub.2 R.sup.10, --NR.sup.10 R.sup.11, --NR.sup.11 R.sup.12, --NR.sup.12 COR.sup.11, --NR.sup.12 CO.sub.2 R.sup.11, --NR.sup.12 CONR.sup.11 R.sup.12, --NO.sup.12 SO.sub.2 R.sup.11, --NR.sup.12 C(NR .sup.12)NHR.sup.11, --COR.sup.11, --CO.sub.2 R.sup.11, --CONR.sup.12 R.sup.11, --SO.sub.2 NR.sup.12 R.sup.11, --OCONR.sup.12 R.sup.11, C(NR.sup.12)NR.sup.12 R.sup.11, R.sup.6 and R.sup.7 are independently halogen, CN, NO.sub.2, --CONR.sup.10 R.sup.11, --SO.sub.2 NR.sup.10 R.sup.11, --NR.sup.10 R.sup.11, or --OR.sup.11, where R.sup.10 and R.sup.11 are as defined below; R.sup.8 is OH, NHSO.sub.2 R.sup.12 or NHCOCF.sub.3 ; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.