Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-09-08
1997-03-04
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514294, 514411, A61K 31505, A61K 3144, A61K 3140
Patent
active
056079389
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a new use of a compound having 5-HT antagonism.
More particularly, the present invention relates to a new use of a compound having 5-HT antagonism (hereinafter referred to as "5-HT antagonist") such as 5-HT.sub.1 antagonism, 5-HT.sub.2 antagonism and 5-HT.sub.3 antagonism, especially 5-HT.sub.3 antagonism for treating or preventing cerebrovascular diseases.
DISCLOSURE OF THE INVENTION
One object of the present invention is to provide a therapeutic or preventive agent of cerebrovascular diseases which comprises a 5-HT antagonist as an active ingredient.
Another object of the present invention is to provide a new use of a 5-HT antagonist as a therapeutic or preventive agent for cerebrovascular diseases.
Other object of the present invention is to provide a pharmaceutical composition for treating or preventing cerebrovascular diseases comprising a 5-HT antagonist, as an active ingredient, in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Further object of the present invention is to provide a new use of a 5-HT antagonist for manufacturing a medicament for treating or preventing cerebrovascular diseases and conditions such as cerebral infarction, cerebrovascular dementia, and the like.
Still further object of the present invention is to provide a method for treating or preventing cerebrovascular diseases and conditions as mentioned above which comprises administering an effective amount of a 5-HT antagonist to a host such as animals, e.g. mammals including human.
It is known that 5-HT antagonists are of use for treating or preventing central nervous system (CNS) disorders such as psychosis (e.g. schizophrenia, mania, etc.), anxiety, and depression; pains or aches such as headaches (e.g. migraine, cluster headaches, vascular headaches, etc.), and neuralgia (e.g. trigeminal neuralgia, etc.); gastrointestinal disorders such as symptoms of gastrointestinal dysfunction such as occur with, for example, dyspepsia, pectic ulcer, reflux oesophagitis and flatulence, and irritable bowel syndrome (IBS); nausea or vomiting, each of which may be associated with cancer therapy; motion sickness; and the like.
The inventors of the present invention extensively investigated various effects of the 5-HT antagonists, and during such investigations, it has been found that the 5-HT antagonists are further of use for treating or preventing cerebrovascular diseases. This finding is really new and is not expectable at all for a person skilled in this field.
The 5-HT antagonist used in the present invention can be represented by the following general formulae: ##STR2##
wherein R.sup.1 is hydrogen, lower alkyl, lower alkenyl or N,N-di(lower)alkylaminomethyl, substituent(s), and ##STR3## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined above, or a pharmaceutically acceptable salt thereof, and ##STR4##
wherein R.sup.6, R.sup.7 and R.sup.8 are each hydrogen lower alkyl, lower alkenyl, aryl or ar(lower)alkyl,
In the compounds of the formulae (I), (II) and (III), a suitable pharmaceutically acceptable salt of these compounds includes conventional one such as acid addition salt with an organic or inorganic acid (e.g. hydrochloride, sulfate, formate, acetate, etc.), or a salt with a base such as alkali metal salt (e.g. sodium salt, potassium salt, etc.), alkaline earth metal salt (e.g. calcium salt, etc.), organic basic salt (e.g. cyclohexylamine salt, etc.), and the like.
The most preferred embodiment of the 5-HT antagonist used in the present invention is as follows. -7-[(5-methyl-1H-imidazol-4-yl)-methyl]pyrido[1,2-a]indol-6(7H)-one or its hydrochloride salt; methyl]-4H-carbazol-4-one or its hydrochloride and/or its hydrate; and ndol-1(2H)-one or its hydrochloride.
The compounds of the general formulae (I), (II) and (III), and the specific compounds mentioned above are known compounds, and the methods for preparation thereof are described, for example, in the following publications, or they can be prepared by a conven
Katsuta Kiyotaka
Nakanishi Hajime
Takamatsu Hiroyuki
Ueda Yoshiko
Yoshida Keizo
Fujisawa Pharmaceutical Co. Ltd.
Jordan Kimberly
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