Agmatine, and polyaminoguanidine-bound heterocyclic compounds for neurotrauma and neurodegenerative diseases

US6114392A · kind A · utility

Inventors

• Gad Gilad · Givatayim, IL
• Varda Gilad · Givatayim, IL

Key dates

• Filing date: Apr 16, 1996
• Grant date: Sep 5, 2000
• Expiry date: Apr 16, 2016

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/155
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia). The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.sub.6, and R.sub.7 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, or halogeno; and phar…