Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1991-12-10
1996-08-27
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
A61K 3155
Patent
active
055501249
ABSTRACT:
It is a purpose of this invention to provide a means of treating various central nervous system (CNS) injuries to prevent or minimize damage to the CNS. A novel use has been found for some previously known compounds which are inhibitory agonists of the peripheral-type BZ receptors.
It is another purpose of this invention to provide a means of speeding the recovery of tissue damaged through injury to the CNS. The above described inhibitory agonists of the peripheral-type BZ receptors are useful for this purpose, and provide an easily administrable medication.
Additionally, a means is provided for screening for new compounds which will act as inhibitory agonists of the peripheral-type BZ receptors and therefore which can be used for treating CNS injuries and for speeding the recovery of tissue damaged through such injuries.
REFERENCES:
patent: 3336295 (1967-08-01), Sternbach et al.
patent: 3880855 (1975-04-01), Juby et al.
patent: 4005099 (1977-01-01), Gall
patent: 4499094 (1985-02-01), Dubroeucq et al.
patent: 4997771 (1991-03-01), Barnett et al.
Baldessarini, R. J., "Drugs and the Treatment of Psychiatric Disorders," in: Goodman & Gilman's The Pharmacological Basis of Therapeutics, Pergamon Press, N.Y., pp. 383-435 (1990).
Benavides et al., "The quantification of brain lesions with an .omega..sub.3 site ligand: a critical analysis of animal models of cerebral ischaemia and neurodegeneration," Brain Res. 522:275-289 (1990).
Bourdiol et al., "Increase in .omega..sub.3 (peripheral type benzodiazepine) binding sites in the rat cortex and striatum after local injection of interleukin-1, tumour necrosis factor-.alpha.and lipopolysaccharide," Brain Res. 543:194-200 (1991).
Braestrup, C. and Squires, R. F., "Specific benzodiazepine receptors in rat brain characterized by high affinity [.sup.3 H ]diazepam binding", PNAS USA 74(9):3805-3809 (1977).
Drobinski et al., "Absence d'effet anti-isch emique d'qun antagoniste des r ecepteurs p eriph eques aux benzodiaz epines PK 11195," Therapie 44:263-267 (1989).
Krueger et al., "Purification, Cloning, and Expression of a Peripheral-Type Benzodiazepine Receptor," Adv. Biochem. Psychopharmacol. 46:1-13 (1990).
Mizoule et al., "Opposite Effects of Two Ligands for Peripheral Type Benzodiazepine Binding Sites, PK 11195 and R05-4864," Life Sci. 36:1059-1068 (1985).
Muller et al., in: The Benzodiazepine Receptor: Drug Acceptor Only or a Physiologically Relevant Part of our Central Nervous System?, Cambridge Univ. Press, pp. 32, 33, 75 and 76 (1987).
Pellow, S. and File, S. E., "Characteristics of an Atypical Benzodiazepine, Ro 5-4864," Neurosci. Behav. Rev. 8:405-413 (1984).
Rall, T. W., "Hypnotics and Sedatives; Ethanol", in: Goodman and Gilman's The Pharmacological Basis of Therapeutics, Chapter 17, Pergamon Press, N.Y., pp. 345-382 (1990).
Schoemaker et al., "Specific High-Affinity Binding Sites for [.sup.3 H]Ro 5-4864 in Rat Brain and Kidney," J. Pharmacol. Exp. Ther. 225(1): 61-69 (1983).
Skerritt et al., "Diazepam and its Anomalous .beta.-Chloro-derivative Ro 5-4864: Comparative Effects on Mouse Neurons in Cell Culture," Brain Res. 310:99-105 (1984).
Taupin et al., "Increase in IL-6, IL-1 and TNF levels in rat brain following traumatic lesion", J. Neuroimmunol. 42:177-186 (1993).
Wang et al., "Benzodiazepines that bind at peripheral sites inhibit cell proliferation," PNAS USA 81:753-756 (1984).
Wang et al., "Structural Requirements for the Binding of Benzodiazepines to Their Peripheral-Type Sites", Molec. Pharmacol. 25:349-351 (1984).
Demerl e-Pallardy et al., "Peripheral type benzodiazepine binding sites following transient forebrain ischemia in the rat: effect of neuroprotective drugs", Brain Res. 565:312-320 (Nov. 29, 1991).
Marana et al., "Cerebral Protection During Extracorporeal Circulation," Resuscitation 10:89-100 (1982).
"Differences in the mechanism of the antihypoxic action of benzodiazepine receptor agonists and muscimol," Biull Eksp Biol. Med. (USSR) 98(10):436-439 (1984).
Supplementary Partial European Search Report for EP 93 90 1476, issued Apr. 24, 1995. (6 pages).
Huff et al., Society for Neuroscience Abstracts, vol. 17, 1991.
Verrier et al., Aug. 1975, The Canadian Journal of Neurological Sciences, pp. 179-184.
Voll et al., Neurology 1991; 41:423-428.
Henley III Raymond
University of Southern California
LandOfFree
Use of peripheral-type benzodiazpine sites for treatment of CNS does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Use of peripheral-type benzodiazpine sites for treatment of CNS , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Use of peripheral-type benzodiazpine sites for treatment of CNS will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1056291