Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-01-07
1993-03-30
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514365, 514422, 514423, 544132, 544133, 546208, 546209, 548200, 548518, 548540, A61K 3140, A61K 3141, C07D27704, C07D20704
Patent
active
051984504
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to novel phenylalkanoylamine derivatives which are useful as medicines for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, and memory disturbance, and to a process for preparing the same.
DESCRIPTION OF THE BACKGROUND ART
Senile dementia caused by such cerebral disorders as cerebrovascular disorder, cerebral circulation disorder, cerebral metabolism disorder, and memory disturbance has become a social problem in the society with prolonged life-span. A number of drugs for the treatment or prevention of these diseases, including cerebral vasodilators, cerebral metabolism accelerators, and the like, are clinically used.
None of these medicines, however, exhibit sufficient effects on the treatment of diseases such as cerebrovascular disorder sequelae, or the like.
Cerebral tissues of mammals rely upon aerobic glycolysis for the energy to maintain their functional activity. For this reason, a constant supply of a large amount of oxygen and glucose to brain tissues is necessary. It is a clinical knowledge that a decreased oxygen supply to brain tissues caused by circulation disorder, or the like remarkably lowers the brain cell functions. The continued decrease in oxygen supply to brain tissues extremely lowers brain cell functions. Interruption of oxygen supply (for several minutes) is known to completely inactivate physiological functions of brain cells and to cause irreversible organic disorders [J. Cereb. Blood Flow Metab. 9, 2-19, (1989]. In view of this, pharmacological experiments using hypoxia induction methods have long been carried out. A great attention to the problems concerning cerebral ischemia in recent years has led to the investigations about the cause of cerebral functional disorder or cerebral tissue disorder. The studies involving biochemistry, blood circulation dynamics, and electrophysiology resulted in the evidenced utility of hypoxia induction methods [Arch. Int. Pharmacodyn. 286, 299-307 (1987)]. Drugs protecting the brain from the induced hypoxia have been recognized as possessing more excellent effects on the improvement in cerebral circulation and cerebral metabolism, as well as on the prevention of amnesia than conventional drugs for improving cerebral circulation.
In view of this situation, the present inventors have undertaken extensive studies in order to develop a more excellent medicine for improving cerebral circulation and metabolism as well as for preventing amnesia. As a result, the inventors have found that phenylalkanoylamine derivatives represented by the following formula (I) exhibited excellent anti-hypoxic and anti-amnesic activities, and are pharmacologically useful. Such findings have led to the completion of this invention.
DISCLOSURE OF THE INVENTION
An object of this invention is to provide an agent for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance comprising as an effective component a phenylalkanoylamine derivative represented by the following formula (I), ##STR3## wherein A represents a 1,3-thiazolidin-3-yl group, a 1,2,3,6-tetrahydropyridin-1-yl group, a morpholino group, a thiomorpholin-4-yl group, or a 3-pyrrolin-1-yl group, R.sup.1 and R.sup.2, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, or a guanidino group, or a group ##STR4## (wherein R.sup.3 and R.sup.4 independently represent a lower alkyl group or form in combination 5- or 6-membered heterocyclic group), and n represents an integer of 2-6, or a salt thereof.
Among the compounds represented by the formula (I those represented by the following formula (I') are novel compounds. Accordingly, it is another object of this invention to provide phenylalkanoylamine derivatives represented by the following formula (I'), ##STR5## wherein A' represents a 1,3-thiazolidin-3-yl group, a 1,2,3,6-tetrahydropyridin-1-yl group, a morpholino group, a thiomorpholin-4-y
REFERENCES:
Mukaiyama et al., (Chemical Abstract), 92(1), 1979, #6522t.
Mukaiyama et al., (Chemical Abstract), 91(23), 1979, #192996c.
Chemical Abstracts, 63:9885h (1965) (Michael Sy & Georges Andre Thiault), Bull. Soc. Chim. France, 1965 (5), 1309-1315 (Fr).
Chemical Abstracts, 82, 1, 82(1):3917h, (1975), (Cont. Rech. Clin-Midy, Montpellier, Fr.), Krausj. F., et al., Arjneim.--Forsch. 1974, 24(9a), 1360-1364 (Fr.).
Aotsuka Tomoji
Kato Hisayoshi
Miura Naoyoshi
Morita Hikaru
Nakata Noaki
Gupta Y. N.
Shah Mukund J.
Zeria Pharmaceutical Co. Ltd.
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