Bisbiguanide compounds

US4670592A · kind A · utility

Assignee

• IMPERIAL CHEMICAL INDUSTRIES LIMITED · GB

Inventors

• Murdoch Allan Eakin · Macclesfield, GB
• Philip N. Edwards · Bramhall, GB
• Michael S. Large · Stafford, GB

Key dates

• Filing date: May 7, 1984
• Grant date: Jun 2, 1987
• Expiry date: May 7, 2004

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61Q11/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A bisbiguanide compound of the formula: EQU R.sup.1 R.sup.2 N.C(:NR.sup.6)NH.C(:NH)NH.CH.sub.2 X-- --(CH.sub.2).sub.3 NH.C(:NH)NH.C(:NR.sup.7)NR.sup.3 R.sup.4 V or a tautomer thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 2-16C alkoxyalkyl radical, a 3-12C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, or an optionally substituted phenyl or phenyl(1-4C alkyl) radical, or R.sup.1 and R.sup.2 and the nitrogen atom to which they are attached, or R.sup.3 and R.sup.4 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical each of which may bear 1-3C alkyl substituents; each of R.sup.6 and R.sup.7, which may be the same or different, is hydrogen or a 1-8C alkyl radical; and X is a substituted ethylene or ethylidene radical of the formula: EQU --CH.sub.2 CH(YR.sup.5)-- VI or EQU --CH(CH.sub.2 YR.sup.5)-- VII reading from left to right in formula V above, wherein Y is an oxygen or sulphur atom and R.sup.5 is a 1-…