In vivo method of improving survival rate of brain neurons

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C435S115000, C435S116000, C435S117000, C435S118000, C435S113000, C514S018700, C514S019300, C514S706000, C514S708000, C514S709000, C514S710000, C514S712000, C514S713000, C562S553000, C562S556000, C562S557000, C562S433000, C424S570000

Reexamination Certificate

active

06239111

ABSTRACT:

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. In the human brain, several tens of billions of neurons form complicated neurological circuits in which the terminal of a neurite of a neuron transmits information at the junctional portion called a synapse by the mediation of a neurotransmitter. 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 certain compounds contained in garlic or preparations of processed garlic sulfur—amino acids having an allyl group and their analogs—inhibit decrease in brain neurons and promote branching of neurites, and therefore are useful as drugs for the treatment of 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.
Accordingly, the present invention provides the use in the manufacture of a preventive and therapeutic drug of brain diseases of a compound represented by the following formula:
CH
2
═CH—CH
2
—S(O)
n
—R  (1)
[wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group which is derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside.
The present invention also provides a method for the treatment of brain diseases characterized by administering an effective amount of the compound of formula (1), a glycoside thereof, or a salt of the compound or the glycoside.


REFERENCES:
patent: 3950387 (1976-04-01), Joullié et al.
Block B. “The Chemistry of Garlic and Onions” Sci. Am. 252, 114-119, 1985.

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