Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-03-15
1998-08-04
Morris, Patricia L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5462741, 5462744, A61K 31445, C07D40106, C07D40104
Patent
active
057894256
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to imidazolidinone derivatives with cholinergic activity (muscarine M.sub.1 activity) or pharmaceutically acceptable acid addition salts, processes for preparing them and therapeutics for senile dementia having them as effective components.
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.
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 particularly 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 imidazolidinone derivatives and their acid adducts have excellent cholinergic activity (muscarine M.sub.1 activity).
Namely, according to the invention, it has been found that imidazolidinone derivatives represented by a general formula (1) ##STR3## (wherein R denotes a lower alkyl group which may be substituted by halogen, cyclic alkyl group, or phenyl group, naphthyl group, 5-membered or 6-membered hetero ring and its benzene-condensed ring which may have one or more substituents, R.sup.1 and R.sup.2 denote identically or differently hydrogen atoms or lower alkyl groups, R.sup.3 denotes a formula ##STR4## (wherein R.sup.4 denotes a lower alkyl group which may be substituted by halogen, cyclic alkyl group, or phenyl group, naphthyl group, 5-membered or 6-membered hetero ring and its benzene-condensed ring which may have one or more substituents, q denotes 0 to 3, and R.sup.5 denotes a hydrogen atom or formula ##STR5## (wherein R.sup.6 and R.sup.7 denote identically or differently lower alkyl groups or may form a ring together with nitrogen atom (further may contain one hetero atom), m and n denote 0 to 3
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Journal of Organic Chemistry, vol. 26, No. 10, 4051-4057, Oct. 24, 1961, "The Rearrangement and Cyclization of Ethyl N-(Methylaminoalkyl) Carbanilates and 1,1-Dimethyl-3-Methylaminoalkyl--3-Phenylureas", W.B. Wright et al.
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Hirayama Takashi
Okazaki Kei
Takadoi Masanori
Takano Yasuo
Yamanishi Atsuhiro
Kyorin Pharmaceutical Co. Ltd.
Morris Patricia L.
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