4(5)-substituted imidazole derivatives as .alpha..sub.2 -adrenergic receptor blockers

US4933359A · kind A · utility

Assignee

• Farmos-yhtyma Oy · FI

Inventors

• Arja Karjalainen · Espoo, FI
• Arto Karjalainen · Oulu, FI

Key dates

• Filing date: May 14, 1987
• Grant date: Jun 12, 1990
• Expiry date: May 14, 2007

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D233/64
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention provides 4(5)-substituted imidazole derivatives of formula ##STR1## and their acid addition salts, in which either X is --CH.sub.2 -- and R.sub.1 is --CN, --COOH, COO(lower alkyl), --CHO, --CO(lower alkyl), lower alkyl or 3 or 5 carbon atoms, lower alkenyl, or lower (hydroxy alkyl) or X is ##STR2## --C(:CH--R)-- or --CH(CH.sub.2 R)--, where R is hydrogen or lower alkyl, and R.sub.1 is lower alkyl, and R.sub.3 and R.sub.4 are each hydrogen, methyl, ethyl, methoxy, or halogen, and novel intermediates and processes for their preparation. These compounds, in particular when R.sub.1 is lower alkyl, lower alkenyl, or lower (hydroxy alkyl), possess valuable pharmacological properties and are useful especially as selective .alpha..sub.2 -receptor antagonists.