Pyrazolone derivatives as MCP-1 antagonists

US6011052A · kind A · utility

Assignee

• WARNER-LAMBERT COMPANY LLC · US

Inventors

• Janak Khimchand Padia · Germantown, US
• Bruce D. Roth · Ann Arbor, US
• John Strode · Ann Arbor, US
• Bharat Kalidas Trivedi · Farmington Hills, US

Key dates

• Filing date: Apr 25, 1997
• Grant date: Jan 4, 2000
• Expiry date: Apr 25, 2017

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D231/50
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Pyrazolone derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammatory diseases or conditions, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## where: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 can be independently H, PA0 C.sub.1-20 alkyl, PA0 C.sub.5-7 cycloalkyl, PA0 --(CH.sub.2).sub.n NR.sub.6 R.sub.7 PA0 --(CH.sub.2).sub.0-6 CONR.sub.6 R.sub.7, PA0 --(CH.sub.2).sub.n OH or PA0 --(CH.sub.2).sub.0-6 CO.sub.2 R.sub.11, PA0 biphenyl, PA0 aryl of from 6 to 10 carbon atoms, or PA0 aryl of from 6 to 10 carbon atoms substituted up to 3 times by halogen, --CN, lower alkyl of from 1-4 carbon atoms, --OH, nitro, --SO.sub.2 H, SO.sub.2 lower alkyl, PA1 --SO.sub.2 NR.sub.6 R.sub.7 lower alkoxy PA1 --C0.sub.2 R.sub.11, PA1 --CONR.sub.6 R.sub.7, PA1 --NR.sub.6 R.sub.7 or CH.sub.2 OH.