Tri-and tetra-substituted guanidines and their use as excitatory

Details Tri-and tetra-substituted guanidines and their use as excitatory Tri-and tetra-substituted guanidines and their use as excitatory

1995-06-06

1998-06-16

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...

514183, 514457, 549288, 552 8, 564230, 564237, 564238, 564239, 564240, A61K 31155, A61K 31655, A61K 3137, C07C27918

Patent

active

057671621

ABSTRACT:
Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, 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: 1730388 (1929-10-01), Scott
patent: 1756315 (1930-04-01), terHorst
patent: 1795398 (1931-03-01), Schotte
patent: 1850682 (1932-03-01), Meiss
patent: 1915922 (1933-06-01), Christmann et al.
patent: 2145214 (1939-01-01), Jayne, Jr.
patent: 2254009 (1941-08-01), Hechenbleikner
patent: 2274476 (1942-02-01), Hechenbleikner
patent: 2289541 (1942-07-01), Ericks et al.
patent: 2362915 (1944-11-01), MacGregor
patent: 2633474 (1953-03-01), Beaver
patent: 2704710 (1955-03-01), Sprung
patent: 3117994 (1964-01-01), McKay et al.
patent: 3140231 (1964-07-01), Luskin et al.
patent: 3159676 (1964-12-01), Spickett et al.
patent: 3168562 (1965-02-01), Walton et al.
patent: 3228975 (1966-01-01), Abraham et al.
patent: 3248426 (1966-04-01), Dvornik
patent: 3252861 (1966-05-01), Mull
patent: 3270054 (1966-08-01), Gagneux et al.
patent: 3283003 (1966-11-01), Jack et al.
patent: 3301755 (1967-01-01), Mull
patent: 3320229 (1967-05-01), Szabo et al.
patent: 3391189 (1968-07-01), Mull
patent: 3409669 (1968-11-01), Dyke
patent: 3479437 (1969-11-01), Szabo et al.
patent: 3547951 (1970-12-01), Hardie et al.
patent: 3639477 (1972-02-01), L'ltalien
patent: 3681459 (1972-08-01), Hughes et al.
patent: 3769427 (1973-10-01), Hughes et al.
patent: 3784643 (1974-01-01), Suh et al.
patent: 3795533 (1974-03-01), Gauri
patent: 3803324 (1974-04-01), Winter et al.
patent: 3804898 (1974-04-01), Panneman
patent: 3908013 (1975-09-01), Hughes et al.
patent: 3949089 (1976-04-01), Maxwell et al.
patent: 3968243 (1976-07-01), Maxwell et al.
patent: 3976643 (1976-08-01), Diamond et al.
patent: 3976787 (1976-08-01), Hughes et al.
patent: 4007181 (1977-02-01), DuCharme et al.
patent: 4014934 (1977-03-01), Hughes et al.
patent: 4051256 (1977-09-01), Swallow
patent: 4052455 (1977-10-01), Matier et al.
patent: 4060640 (1977-11-01), Kodama et al.
patent: 4109014 (1978-08-01), Liu et al.
patent: 4130663 (1978-12-01), Matier et al.
patent: 4161541 (1979-07-01), Rasmussen
patent: 4169154 (1979-09-01), Cohen et al.
patent: 4393077 (1983-07-01), Douglas et al.
patent: 4471137 (1984-09-01), Barton et al.
patent: 4709094 (1987-11-01), Weber et al.
patent: 4742054 (1988-05-01), Naftchi
patent: 4837218 (1989-06-01), Olney
patent: 4898978 (1990-02-01), Bergfield et al.
patent: 4906779 (1990-03-01), Weber et al.
patent: 5093525 (1992-03-01), Weber et al.
patent: 5190976 (1993-03-01), Weber et al.
patent: 5262568 (1993-11-01), Weber et al.
patent: 5298657 (1994-03-01), Durant
patent: 5308869 (1994-05-01), Keana et al.
patent: 5312840 (1994-05-01), Keana et al.
patent: 5336689 (1994-08-01), Weber et al.
patent: 5385946 (1995-01-01), Keana et al.
D. Lloyd et al., Tetrahedron, 33:1379-1389 (1977).
H. Shimazu et al., Chemical Abstracts, 111(2):16337m (1989).
T. Tada et al., Chemical Abstracts, 104(24):208252g (1986).
L. Kiselev et al., Chemical Abstracts, 91(21):175291b (1979).
A. Heesing et al., Chemical Abstracts, 64(1):15776h (1966).
K. Akiba et al., Bull. Chem. Soc. Jap., 47(4):935-934 (1974).
Database Rtecs, "National Institute of Occupational Safety and Health", RTECS No. MF735000.
J. Keana et al., Proc. Natl. Acad. Sci., 86:5631-5635 (1989).
S. Siddiqui et al., Pakistan Journal of Scientific and Industrial Res., 30(3):163-181 (1987).
E. Maida et al., Wiener Klinische Wochenschrift, 90(2):43-48 (1978).
C. Chavkin et al., Advances in the Biosciences, 75:407-410 (1989).
P.N. Bhargava et al., Chemical Abstracts, 86:598, 189787b (1977).
H.W. Geluk et al., J. Med. Chem., 12:712-715 (1969).
M.W. Scherz et al., J. Med. Chem., 33:2421-2429 (1990).
A.A. Stolyarchuk et al., Chemical Abstracts, 86:522-523, 121071h (1977).
T.J.R. Weakley et al., Acta. Cryst., 46:2234-2236 (1990).
J.T. Adams et al., Eur. J. Pharm., 142:61-71 (1987).
B.G. Campbell et al., J. Neurosci., 9:3380-3391 (1989).
G.J. Durant et al., J. Med. Chem., 28:1414-1422 (1985).
M.P. Kavanaugh et al., Proc. Natl. Acad. Sci. USA, 85:2844-2848 (1988).
B. Tester et al., Society for Neuroscience, 19th Annual Meeting, 983, 396.17 (1989).
E. Weber et al., Proc. Natl. Acad. Sci. USA, 83:8784-8788 (1986).
C.A. Maryanoff et al., J. Org. Chem., 51:1882-1884 (1986).
S.R. Safir et al., J. Org. Chem., 13:924-932 (1948).
F.R. Sharp et al., Society for Neuroscience Abstr., 18, Abstr. No. 482.3 (1992).
B. Clement et al., Xenobiotica, 23(2):155-167 (1993).
Kiselev et al., Chemical Abstracts, vol. 66 (1967).
Durant et al., J. Med. Chem. 9:22-27 (1966).
Ginsburg et al., Chemical Abstracts, 4518 (1962).
S. Goldin et al., Synthetic Neuroprotective Glutamate Release Blockers, Small Business Innovation Research Program Phase I Grant Application, funded Dec. 1991.
Kroger et al., Ber., 97:396-404 (1964).
Miura et al., Chem. Abstr., 109:75455d (1988).
Podrebarac et al., J. Med. Chem., 6:283-288 (1963).
Prasad et al., Can. J. Chem., 45:2247-2252 (1967).
Vasilev et al., Chemical Abstract, 93:1500095u (1980).
Ahmad et al., Chemical Abstract, 108:221382 (1988).
Doull et al., A Survey of Compounds for Radiation Protection (USAF Radiation Laboratory), 1962.

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