Optically active imidazolidinone derivatives and processes for p

Details Optically active imidazolidinone derivatives and processes for p Optically active imidazolidinone derivatives and processes for p

1996-03-15

1998-03-10

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546210, A61K 31445, C07D40104

Patent

active

057261881

DESCRIPTION:

BRIEF SUMMARY
SPECIFICATION

This application is a 371 of PCT/JP94/01505 filed Sep. 12, 1994.
1. Technical Field
The present invention relates to optically active imidazolidinone derivatives with cholinergic activity (muscarine M.sub.1 activity) or pharmaceutically acceptable acid addition salts, processes for preparing them and therapeutic drugs for senile dementia having them as effective components.
2. Background Techniques
In recent years, as the average span of life becomes long, the senile dementia such as Alzheimer type senile dementia has posed a significant problem both medically and socially.
The patients of dementia show symptom such as loss of intellectual ability, disturbance of memory, disturbance of abstract thinking, verbal aphasia, apraxia, disorientation, etc. and the disorder of basic functions lies in the disturbance of the formation of memory or the expressive ability of retained memory. Until today, however, there have been almost no medicaments that can treat this effectively, hence immediate development of therapeutic drugs is desired.
It is said that the disturbances of learning and memory in the patients of dementia (in particular, senile dementia and Arzheimer type senile dementia) are particularly associated with the decrease in central cholinergic function. Hence, such compounds that have this central cholinergic function, that is, the functional activity of acetylcholine being a nerve transmitter can be used for the treatment of patients of dementia (Science, 217, 408 (1982): R. I. Bartus et al.).
It is said that, among the degenerative diseases of nerve due to decreased central cholinergic function, the core symptoms relating particularly to the disturbances of memory, recognition, etc. are due to the decreased function of central cholinergic nerve and conventionally, for improving these core symptoms, administration of acetylcholinesterase inhibitor such as physostigmine, administration of acetylcholine precursors such as choline and lecithin, administration of drugs acting on the cholinergic receptor such as arecoline, and the like have been attempted (e.g. Dementia, 1, 188 (1987) etc.). All of these attempts however have many problematic points that they are ineffective in the therapy, that, even if slight effect may be developed, adverse effect is strong or the therapeutic range is narrow, and the like.
Moreover, the optically active imidazolidinone derivatives of the invention are not described in the literatures, but, for compounds relat.ing to racemic form, there is U.S. Pat. No. 3,459,757 (Aug. 5, 1969) showing a following general formula. ##STR1## (wherein R and R.sup.1 denote hydrogen atoms, halogen atoms, lower alkyl groups, lower alkoxy groups or trifluoromethyl groups, A and B denote hydrogen atoms or lower alkyl groups, Y denotes an oxygen atom or sulfur atom, m denotes 0 to 1, and n denotes 0 to 2).
In this patent, however, a description that the compounds are effective for the CNS depressant properties, muscle relaxant, etc. at a level of nontoxicity can be found, but there is no description at all that they have muscarine (M.sub.1) activity.
In addition, a compound represented by a following formula ##STR2## is described in the example, but this compound is of racemic form and there is no sign at all that it was developed as a medicinal drug.
The purpose of the invention is to provide the therapeutic drugs for senile dementia which activate the central cholinergic function of the patients of dementia (in particular, senile dementia and Arzheimer type senile dementia) and which are effective for the therapy of the disturbance of memory and having high safety, taking the present status of the patients of dementia aforementioned into consideration.


DISCLOSURE OF THE INVENTION

As a result of diligent studies searching for the therapeutics articularly for the disturbance of memory among various symptoms of dementia for the purpose of developing novel therapeutics for senile dementia, the inventors have found that the inventive optically active imidazolidinone derivatives and

REFERENCES:
patent: 3196152 (1965-07-01), Wright et al.
patent: 3355457 (1967-11-01), Wright et al.
patent: 3459757 (1969-08-01), Wright, Jr.
patent: 4011238 (1977-03-01), Fontanella et al.
patent: 5300515 (1994-04-01), Takano et al.
patent: 5401750 (1995-03-01), Varasi et al.

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