Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-01-22
1995-02-14
Bond, Robert T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540575, 540470, 544398, 544399, 544400, 544402, 544403, 5483001, 564336, 564372, C07D24308, A61K 3155
Patent
active
053896300
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to novel diamine compounds and acid addition salts thereof and cerebral protective drugs containing the compounds or their salts, and more particularly to diamine compounds and acid addition salts thereof which have an excellent cerebral protective action and are useful as an drug for treating disorders of cerebral functions or preventing the progress of such disorders, and to cerebral protective drugs containing the diamine compounds or their acid addition salts.
BACKGROUND ART
Recent increase of the population of senior citizens has brought about the increased number of patients suffering from various functional disorders of the brain, typified by those accompanied by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders, and the like. These disorders are considered to be caused mainly from the decreased blood flow in the brain, hypoxia in the blood, metabolism disorders such as hypoglycemia.
Most of conventional drugs for treating these disorders have paid attention to the causes of the disorders to be treated, and have focused on the treatment of sequelae of cerebral ischemia, cerebrovascular dementia and the like. Such conventional drugs include drugs for improving cerebral circulation, drugs for improving cerebral metabolism, drugs for improving cerebral functions, drugs for inhibiting the platelet coagulation, which have already been clinically utilized. Recently, irrespective of the causes of the disorders, cerebral protective drugs have been proposed and have attracted attention as a drug for treating cerebral function disorders. They are designed to eliminate cerebral function disorders or preventing the progress of the disorders by protecting the brain from ischemia or hypoxia.
These drugs for treating cerebral function disorders, however, have only insufficient clinical effects, and do not show clear cerebral protective action when tested on animals under a condition of single dose oral administration, though most of them are designed to be useful for oral administration.
Accordingly, cerebral protective drugs which promise excellent clinical effect and are useful for oral administration have still been desired.
Under the above circumstances, the present inventors have conducted careful studies to solve the mentioned problems, and have found that the novel diamine compounds of formula (I) and their acid addition salts exhibit an excellent cerebral protective action, and this action is securely obtained even in the oral route administration. This invention was accomplished based on the above findings.
DISCLOSURE OF THE INVENTION
According to the present invention, there is provided diamine compounds represented by formula (I) and acid addition salts thereof: ##STR2## wherein R1, R2, R3, R4, R5 and R6 are the same or different from each other and represent individually a hydrogen atom, halogen atom, hydroxyl group, lower alkyl group, lower alkoxy group, lower acyloxy group, lower alkoxycarbonyloxy group, lower alkylsulfonyloxy group or an amino group, among which the lower alkyl group and lower alkoxy group may be substituted by a halogen atom or a phenyl group; R7 and R8 are the same or different from each other and represent individually a lower alkyl group, or the two bind to each other to represent an alkylene group having 1 to 4 carbon atoms; A and A' are the same or different from each other and represent individually a single bond, --O--, --NH--, --NHCO.fwdarw., --CONH.fwdarw., --NHCOO.fwdarw., --NHCONH--, --SO.sub.2 NH.fwdarw. or --COS.fwdarw. (here, the symbol `.fwdarw.` denotes a bond to Y or Y'), Y and Y' are the same or different from each other and represent a lower alkylene group or lower alkenylene group; and cerebral protective drugs containing them as an active component.
The compounds (I) according to the present invention have an excellent cerebral protective action, are very safe and exhibit their strong action even in the oral route administration, thus useful as a
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Kotelko et al., Chem. Abstract 71:38928n (1969).
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Burger, editor, Medicinal Chemistry, 3rd ed. (1970), part I pp. 74-75.
Noller, Chemistry of Organic Compounds, 2nd ed (1957), p. 272.
Journal of Pharmaceutical Sciences, 3 pgs., vol. 72, No. 3, Mar. 1983, Synthesis and Action on the Central Nervous System of Mescaline Analogues Containing Piperazine or Homopiperazine Rings Michael W. Majchrzak et al.
Kawamura Kiyoshi
Ohta Tomio
Sato Seiichi
Shimizu Sadahiro
Takahashi Yoshio
Bond Robert T.
Datlow Philip I.
Kowa Co. Ltd.
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