Substituted guanidines and derivatives thereof as modulators of

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

514150, 514519, 514506, 514588, 514616, 514623, A61K 31155, A61K 3117, A61K 3116, A61K 31165

Patent

active

054038618

ABSTRACT:
Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

REFERENCES:
patent: 1422506 (1922-07-01), Weiss
patent: 1597233 (1926-08-01), Heuser
patent: 1642180 (1927-09-01), Scott
patent: 1672431 (1928-06-01), Schotte
patent: 1677235 (1928-07-01), Heuser
patent: 1756315 (1930-04-01), Ter Horst
patent: 1795738 (1931-03-01), Schotte
patent: 1850682 (1932-03-01), Meis
patent: 1915922 (1933-06-01), Christmann et al.
patent: 2145214 (1939-01-01), Jayne
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: 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'Italien
patent: 3681459 (1972-08-01), Hughes et al.
patent: 3769427 (1973-10-01), Hughes et al.
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: 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: 4891185 (1990-01-01), Goldin
patent: 4898978 (1990-02-01), Bergfeld 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.
Bean, B., Multiple Types of Calcium Channels in Heart Muscle and Neurons, Ann. N.Y. Acad. Sci. 560:334-345 (1989).
Bean, B., Classes of Calcium Channels in Vertebrate Cells, Annu. Rev. Physiol. 51:367-384 (1989).
Bent et al., Antiviral aminoguanidines compositions, Pesticides 74:63479m (1971).
Bhargava et al., Synthesis of some new N,N'-di-(substituted 2-benzothiazolyl) guanidines as antituberculars and CNS depressants, Chemical Abstracts 86:189787b (1977).
Campbell et al., Sigma Receptors Regulate Contractions of the Guinea Pig Ileum Logitudinal Muscle/Myenteric Plexus Preparation Elicited By Both . . . , Journal of Neuroscience 9(10):3380-3391 (1989).
Chernevskaya et al., NMDA receptor agonists selectively block N-type calcium channels in hippocampal neurons, Nature 349:418-420 (1991).
Choi, D., Cerebral Hypoxia: Some New Approaches and Unanswered Questions, Journal of Neuroscience 10(8):2493-2501 (1990).
Choi, D., Methods for Antagonizing Glutamate Neurotoxicity, Cerebrovascular and Brain Metabolism Reviews 2:105-147 (1990).
Choi, D., Glutamate Neurotoxicity and Diseases of the Nervous System, Neuron 1:623-634 (1988).
Dreyer et al., HIV-1 Coat Protein Neurotoxicity Prevented by Calcium Channel Antagonists, Science 248:364-367 (1990).
Durant et al., Biologically Active Guanidines and Related Compounds. II. Some Antiinflamatory Aminoguanidines, J. Med. Chem. 9:22-27 (1966).
Durant et al., The Histamine H2 Receptor Agonist Impromidine: Synthesis and Structure-Activity Considerations, J. Med. Chem. 28:1414-1422 (1985).
Fox et al., Kinetic and Pharmacological Properties Distinguishing Three Types of Calcium Currents in Chick Sensory Neurones, J. Physiol. 394:149-172 (1987).
Fox et al., Single-Channel Recordings of Three Types of Calcium Channels in Chick Sensory Neurones, J. Physiol. 394:173-200 (1987).
Geluk et al., Synthesis and Antiviral Properties of 1-Adamantylguanidine. A Modified Method for Preparing t-Alkylguanidines, J. Med. Chem. 12:712-715 (1969).
Ginsburg et al., Heterolytic reactions of polyfluorinated azoalkanes, Chem. Abstr. 4518 (1962).
Ginsburg et al., Polyfluoro Azo Compounds IV. Properties of Hexafluorohydrazomethane, Zhurnal Organicheskoi Khimii 7(11):2267-2270 (1971), Unverified Translation.
Godfraind et al., Increasing complexity revealed in regulation of Ca2+ antagonist receptor, Trends in Pharmacological Sciences 10(8):297-301 (1989).
Goldin, Stanley et al., Synthetic Neuroprotective Glutamate Release Blockers, Small Business Innovation Research Program Phase I Grant Application, funded Dec. 1991.
Heinisch, L., Darstellung neuer substituierter 1,2,4-Triazin-6-carbonsauren und 1,2,4-Triazin-6-yl-alkancarbonsauren, Journal f. prakt. Chemie 329:290-300 (1987).
Huisgen et al., Zur Bildung von 1.4-Dihydro-tetrazinen aus Nitriliminen; 1.4-Diphenyl-1-dihydro-1.2.4.5-tetrazin und isomere Verbindungen, Chem. Ber. 98:1476-1486 (1965).
Huisgen et al., 1,3-Dipolar cycloadditions. XVI. Formation of 1,4-dihydro-tetrazines from nitrilimines; 1,4-diphenyl-1,4-dihydro-1,2,4,5-tetrazine . . . , Chemical Abstracts 63:2975 (1965).
Kaneko et al., Anti-ischemic Effect of the Novel Anti-ischemic Agent 2-(4-(p-Fluorobenzoyl) piperidin-1-yl)-2'-acetonaphthone . . . , Arzneim. Forsch./Drug Res. 39(1):445-450 (1989).
Katragadda et al., Multiple Kinetically Distinguishable Components of 3H-Dopamine Release From Nerve Terminals, Soc. for Neurosci. Abstr. 16:64 (1990).
Kreutzberger et al., 2,2'-Azoimidazolbildung durch cyclische Acyloine, Arch. Pharmz, Ber. Duet. Pharm. Ges. 305:400-405 (1972).
Keana et al., Synthesis and characterization of a series of diarylguadines that are noncompetitive N-methyl-D-aspartate receptor antagonists . . . , Proc. Natl. Acad. Sci. USA 86:5631-5635 (1989).
Kroeger et al., 1,2,4-Triazoles. VI. Condensation of methyl-substituted aminoguanidines with aliphatic carborylic acids, Chemical Abstracts 60:9265 (1964).
Kroger et al., Die Kondensation methylsubstituierter Aminoguanidine mit aliphatischen Carbonsauren, Ber 97:396-404 (1964).
Langlais et al., Protective Effects of the Glutamate Antagonist MK-801 on Pyrithiamine-Induced Lesions and Amino Acid Changes in Rat Brain, J. Neuroscience 10(5):1664-1674 (1990).
Lemos et al., Two Types of Calcium Channels Coexist in Peptide-Releasing Vertebrate Nerve Terminals, Neuron 2:1419-1426 (1989).
Leung et al., Spider Toxins Selectively Block Calcium Currents in Drosophila, Neuron 3:767-772 (1989).
Malgouris et al., Riluzole, a Novel Antiglutamate, Prevents Memory Loss and Hippocampal Neuronal Damage in Ischemic Gerbils, J. Neuroscience 9(11):3720-3727 (1989).
Maryanoff et al., A Convenient Synthesis of Guanidines from Thioureas, J. Org. Chem. 51:1882-1884 (1986).
Meldrum, B., Protection Against Ischaemic Neuronal Damage by Drugs Acting on Excitatory Neuro-transmission, Cerebrovascular and Brain Metabolism Reviews 2:27-57 (1990).
Miura et al., Water-thinned ink compositions for writing an ink-jet printing, Chemical Abstracts 109:75454d (1988).
Plaitakis et al., Abnormal Gluta

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

Substituted guanidines and derivatives thereof as modulators of does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Substituted guanidines and derivatives thereof as modulators of , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted guanidines and derivatives thereof as modulators of will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2380981

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