Inhibitors of isoprenyl transferase

US6265603A · kind A · utility

Assignee

• Eisai Inc. · JP

Inventors

• Michael Lewis · Andover, US
• Ana Maria Garcia · Belmont, US
• James J. Kowalczyk · Andover, US
• Hu Yang · Manvel, US
• Eric Schwartz · Lynnfield, US

Key dates

• Filing date: Apr 1, 1999
• Grant date: Jul 24, 2001
• Expiry date: Apr 1, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D307/52
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Peptidomimetic isoprenyl transferase inhibitors R6SCHR1'CHR1WCHR2YC(:X)NR3CHR5COR4 wherein R1=OH, H, alkyl, amino group or R1 and R6 together form a heterocyclic ring; R1'=H, alkyl, aryl; R2=H, alkyl, arylalkyl, heteroarylalkyl; R3=H, alkyl, arylalkyl; R4=OH, alkoxy, amino group; R5=natural amino acid residue or D--E--F, where D is alkyl or alkenyl, E is O, S, N, or null, F is H, alkyl, aryl, carboxy amino, etc.; R6=H, alkyl, acyl, etc.; W=alkyl, alkenyl; X=O, S, Y is M--O--P, where M is C0-6 alkyl, O is oxygen-C0-4 alkyl, P is(un)substituted C6-20 aryl are disclosed.