Agmatine, and polyaminoguanidine-bound heterocyclic compounds fo

Details Agmatine, and polyaminoguanidine-bound heterocyclic compounds fo Agmatine, and polyaminoguanidine-bound heterocyclic compounds fo

1996-04-16

2000-09-05

O'Sullivan, Peter

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514579, 514612, 514632, 514633, 514636, 514645, 514659, 514660, 514661, 514662, 564116, 564225, 564227, 564229, 564230, 564236, 564237, 564243, 564248, 564270, 564453, 564458, 564459, 564460, 564461, A61K 31155, A61K 31132, A61K 3115, A61K 31133

Patent

active

061143928

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 pharmaceutically acceptable salts and optically active isomers thereof.

REFERENCES:
patent: 4837218 (1989-06-01), Olney
patent: 5190976 (1993-03-01), Weber et al.
patent: 5262568 (1993-11-01), Weber et al.

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