N,N'-disubstituted guanidines and their use as excitatory amino

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

564239, C07C27700

Patent

active

050935259

ABSTRACT:
Disubstituted guanidines, e.g., bis-1,3-(o-isopropylphenyl)guanidine, bis-1,3-(m-isopropylphenyl)guanidine, bis-1,3-(1-naphthyl)guanidine, bis-1,3-(m-methoxyphenyl)guanidine, N-(1-naphthyl)-N'-(o-iodophenyl)-guanidine, N-(1-naphthyl)-N'-(m-ethylphenyl)guanidine, and N-(1-napthyl)-N'-(o-isoproylphenyl) guanidine, exhibit a high binding affinity to phencyclidine (PCP) receptors. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors of glutamate-induced responses generated via the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal chord ischemia, brain or spinal cord trauma, as well as being useful for the treatmnet of epilepsy, Alzheimer's disease, Amyotrophic Laterla Scherosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

REFERENCES:
patent: 1422506 (1922-07-01), Weiss
patent: 1597233 (1926-08-01), Heuser et al.
patent: 1642180 (1927-09-01), Scott
patent: 1672431 (1928-06-01), Schotte
patent: 1677235 (1928-07-01), Heuser
patent: 2362915 (1944-11-01), Hutchinson et al.
patent: 2633474 (1953-03-01), Beaver
patent: 3320229 (1967-05-01), Szabo et al.
patent: 3479437 (1969-11-01), Szabo et al.
patent: 3976643 (1976-08-01), Diamond et al.
patent: 4709094 (1990-03-01), Weber et al.
patent: 4906779 (1990-03-01), Weber et al.
Keana, J. F. W. et al., Proc. Natl. Acad. Sci. (U.S.A.) 86 5631-5635 (1989).
Galvin et al., Biol. Abstr. 69: 52486 (1980).
Hall et al., Biol. Abstr. 70: 39405 (1980).
Kranz et al., Biol. Abstr. 70: 80555 (1980).
International Search Report for PCT/US91/01448.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

N,N'-disubstituted guanidines and their use as excitatory amino does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with N,N'-disubstituted guanidines and their use as excitatory amino , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and N,N'-disubstituted guanidines and their use as excitatory amino will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-273675

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.