Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-01-09
1999-10-05
MacMillan, Keith D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514460, A61K 3144, A61K 3135
Patent
active
059624809
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a drug for ameliorating brain diseases, and more particularly to a drug for ameliorating brain diseases useful for the prevention and treatment of cerebral function disorders, such as dementia, caused by degeneration and sloughing of brain neurons.
BACKGROUND ART
In recent years, among intrinsic diseases that occur as age increases, brain diseases led by Alzheimer's disease have come to be great social problems. The human brain contains several tens of billions of neurons. The terminal portions of neurites of the neurons transmit information from one to another at junctional portions called synapses by the mediation of a neurotransmitter, forming complicated neurological circuits. Almost all brain disorders are considered to be caused by the destruction of neurological circuits due to degeneration or sloughing of neurons. As is widely accepted, neurons that have matured can no longer undergo cell division. Therefore, needless to say, damage to neurons considerably affects maintenance of brain functions.
Recently, substances that participate in differentiation and growth of nerve tissue have been searched for in the living body, and several in vivo hormones have already been clarified to be active substances.
However, it has been pointed out that these hormones disturb the in vivo hormone balance when used at a concentration where they exhibits their activity on neurons, and therefore in actual use they are problematic for administration. In view of the foregoing, there is a strong need for the development of extracorporeally derived pharmaceuticals that are effective in the prevention of damage to neurons, particularly prevention or treatment of degeneration and sloughing of neurons.
Accordingly, the object of the present invention is to provide a drug for treating brain diseases, which drug enables prevention or treatment of dementia and similar diseases caused by degeneration or sloughing of neurons.
DISCLOSURE OF THE INVENTION
The present inventors have conducted a screening of a wide variety of compounds originating from plants, and have discovered that a compound having a gamma-pyrone ring--which is known to be so-called stress compounds produced when garlic undergoes certain stress--and their analogs inhibit decrease in brain neurons and promote branching of neurites, and therefore are useful as drugs for ameliorating brain diseases such as dementia caused in association with degeneration and sloughing of brain neurons. The present invention has been accomplished based on this finding.
Specifically, the present invention provides a compound for ameliorating brain diseases comprising as the active ingredient a compound represented by the following formula (1): ##STR2## alkoxyl group, or a lower alkyl group; each of R.sup.2 and R.sup.3 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a lower alkenyl group, a phenyl group, a substituted phenyl group, a styryl group, or a substituted styryl group; and X represents an oxygen atom or a nitrogen atom which may be substituted by a lower alkyl group! or a salt thereof.
The present invention also provides a composition for ameliorating brain diseases, which composition contains a compound represented by the above formula (1) or a salt thereof and a pharmaceutically acceptable carrier.
The present invention also provides use, in the manufacture of a therapeutic drug of brain diseases, of a compound represented by the above formula (1) or a salt thereof.
The present invention also provides a method for ameliorating brain diseases, characterized by administering to a patient an effective amount of the compound of formula (1) or a salt thereof.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows the branching promotion effect of compound (1) on neurites; and
FIG. 2 shows the branching promotion effect of compound (3) on neurites.
BEST MODE FOR CARRYING OUT THE INVENTION
The active ingredient of the drug of the present invention for ameliorating brain diseases is a compound re
REFERENCES:
Database Chemical Abstracts on STN, Kodera et al, AN 1990:73738, "Allixin, a stress compound from garlic", Chem. Pharm. Bull. (1989), 37(6), 1656-8, Jan. 1990.
Database CHemical Abtracts on STN, AN 1990:191529, Nishino et al, "Antitumor-promoting activity of allixin . . . ", Cancer J. (Jan. 1990), 3(1), 20-1.
Database Chemical Abstracts on STN, Yamasaki et al, AN 1991:574254, "Effect of Allixin, a phytoalxin produced by garlic, on mutagenesis, DNA-binging and metabolism of aflatoxin B1", Cancer Lett. (Shannon, Irel.) (Jan. 1991), 59(2), 89-94.
Database Chemical Abstracts on STN, AN 1983:124508, "Hydroxypyranones as antioxidants for oils and fats", Jpn. Kokai Tokkyo Koho, JP 57137394, Aug. 24, 1982.
Database Chemical Abstracts on STN, AN 1992:207843, Yamamoto, "Pharmaceuticals containing allomaltol for treatment of pigmentation disorders", Jpn. Kokai Tokkyo Koho, 5 pp., JP 04036217, Feb. 6, 1992.
Matsuura Hiromichi
Moriguchi Toru
Saito Hiroshi
MacMillan Keith D.
Wakunaga Pharmaceutical Co., Ltd.
LandOfFree
Drug for ameliorating brain diseases does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Drug for ameliorating brain diseases, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Drug for ameliorating brain diseases will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1171853