Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-05-08
1998-07-07
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546144, C07D21704, A61K 3146
Patent
active
057769451
DESCRIPTION:
BRIEF SUMMARY
This is a 371 Application of PCT/JP96/02030, filed Mar. 18, 1997.
TECHNICAL FIELD
The present invention relates to a 4a-aryldecahydroisoquinoline compound and a pharmacologically acceptable salt thereof, and also relates to a medicine, a cerebral cytoprotective agent, an analgesic, and an antitussive, each of which contains the foregoing compound or salt as an active ingredient.
BACKGROUND ART
Recently, cases of various cerebrovascular diseases have increased with the arrival of an aging society. Cerebrovascular diseases are considered to be caused by aging, hypertension, arterial sclerosis, hyper lipidemia, and the like, and are generally called as stroke. However, cerebral functional damage due to head trauma and the like are occasionally included in the cerebrovascular diseases in a broad sense.
Stroke is roughly divided into infarctional diseases and hemorrhagic diseases such that the former includes cerebral infarction (cerebral thrombosis and cerebral embolus) and the latter includes cerebral hemorrhage and subarachnoid hemorrhage. These diseases cause supply shortages of glucose, oxygen, and the like, which are the energy source of cerebral neurocytes; thus cerebral edema or infarction consequently occurs, resulting in death of the cerebral neurocytes positioned in and around the ischemic areas. As a result, various aftereffects such as cerebrovascular dementia occur, and together with Alzheimer-type senile dementia and the like, they appear as medically and socially serious problems at present.
Conventionally, medicines developed to be applied for improvement in psychoneurotic symptoms associated with the above cerebrovascular diseases and senile dementia mainly take effect through promoting supply of glucose, oxygen, etc. to ischemic areas by increasing the blood flow to the brain, and based on these functional mechanisms, they are called by ambiguous names such as agents for improving cerebral circulation, activators for cerebral metabolism, and agents for improving cerebral functions. However, almost all of these medicines are aimed at improving the above aftereffects and are regarded to be effective for improving peripheral symptoms such as volition disorder, emotional disorder, and abnormal behavior; meanwhile their effectiveness on core symptoms of dementia such as memory disorder(s) is considered to be doubtful by many people. Anyway, these medicines are almost ineffective for cerebral neurocytes damaged by cerebrovascular disorder and, up to the present, almost no medicine has been found which is effective for this damage. In particular, treatment of the acute stage which is within 24 hours from the onset of cerebrovascular diseases is regarded to be important, and development of a cerebral cytoprotective agent which has reliable protective effects and which can be used in a safe and easy way is in demand under present conditions.
Meanwhile, analgesics which exhibit their effect by affecting the central nervous system and which are represented by morphines and the like are frequently used at present because of their strong analgesic action, however strict management is required in using these medicines since they have severe adverse effect including dependence, respiratory supression and smooth muscle deppressomotor (constipation). Therefore, central analgesics have been in demand which are highly effective and which can be used with relief. In addition, codeine and dextromethorphan which are known as strong central antitussives are generally used for not only prescription medicines but also a component of commercially available cold medicines, and these medicines fundamentally have similar severe adverse effect. In particular, abuse of antitussives containing codeine and psychogenesis of dextromethorphan are serious, and development of safer and stronger central antitussives has been expected.
DISCLOSURE OF THE INVENTION
As a result of in depth study conducted for solving the above problems, inventors of the present invention have found that a 4a-aryldecahydroisoquinoline compound
REFERENCES:
patent: 4301290 (1981-11-01), Pfaffli et al.
Endo Takashi
Imamura Yoshifumi
Nagase Hiroshi
Ohno Hiroshi
Davis Zinna Northington
Toray Industries Inc.
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