Piperizine-4-phenyl derivatives as inhibitors of the interaction between mdm2 and p 53

US6770627B1 · kind B1 · utility

Assignee

• ASTRAZENECA AB · SE

Inventors

• Richard Wa Luke · Macclesfield, GB
• Philip J Jewsbury · Grafton, GB
• Ronald Cotton · Gosport, GB

Key dates

• Filing date: Mar 7, 2001
• Grant date: Aug 3, 2004
• Expiry date: Mar 7, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K5/0815
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A compound of formula (1), wherein: R5 is hydrogen, C1-4alkyl, R6CH2— or R6C(O)—; R6 is aryl, heteroaryl, heterocyclyl, aminoC3-6alkyl, N-(C1-4alkyl)aminoC3-6alkyl, NN-(diC1-4alkyl)aminoC3-6alkyl, or R7; wherein the aryl, heteroaryl or heterocyclyl rings may be optionally substituted with up to three substituents independently selected from nitro, C1-4alkyl, C1-4alkoxy, halo, (C1-4alkyl)sulfanyl, C1-4alkoxycarbonyl, N-(C1-4alkyl)carbamoyl, NN-(diC1-4alkyl)carbamoyl, N-(C1-4alkyl)amino or NN-(diC1-4alkyl)amino; wherein R7 is either a group or formula (2) or formula (3); and wherein L1, L2, L3, L4, R1, R2, R3, R4, R8, R9, R10, R11, R12, R13, A1, n, p, q, r and s are as defined herein. The compounds of formula (1) inhibit the interactions between MDM2 and p53 and may be useful in the treatment of cancers.