Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-11-14
1997-04-29
Datlow, Philip I.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514183, 540470, A61K 31415, C07D40304
Patent
active
056249489
DESCRIPTION:
BRIEF SUMMARY
This is a National Stage Application under 35USC371 of International Application PCT/JP94/00787 filed May 16, 1994.
TECHNICAL FIELD
The present invention relates to novel 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds and pharmaceutically acceptable salts thereof being useful as therapeutic agents.
More particularly, the present invention relates to novel 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds represented by the formula: ##STR2## wherein X represents a hydrogen atom or a halogen atom; Y represents a covalent bond, a straight- or branched-chain alkylene group having 1 to 6 carbon atoms, or a straight- or branched-chain alkenylene group having 2 to 6 carbon atoms; R represents a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof.
BACKGROUND ART
Histamine H.sub.1 -receptor antagonists are widely employed in orally for the treatment of bronchial asthma, and it is reported that they often show systemic adverse actions such as sedation or arrhythmogenetic activity. Therefore, topical treatment using the antagonists has been attempted in order to avoid such adverse actions. However, the methods are unsuccessful because the antagonists have strong bronchia irritation when inhaled directly to the bronchia.
Thus, there remains a need for the development of histamine H.sub.1 -receptor antagonists which can be directly inhaled to the bronchia for the treatment of bronchial asthma with less irritation to bronchial tissues.
European Patent Application Unexamined Publication No. 5,318 discloses a benzimidazole compound represented by the formula: ##STR3## wherein Z represents a hydrogen atom or a fluorine atom; A represents a methoxy group, an ethoxy group, a 2-propenyloxy group, a hydroxy group, a methoxycarbonylmethyloxy group, an methoxycarbonylmethyloxy group, a cyanomethyloxy group, a methylthio group, a methanesulfonyl group, an amino group, a nitro group, a fluorine atom or a chlorine atom. In addition, of the above benzimidazole compounds, the compound represented by the formula: ##STR4## has been employed (general name: Astemizole) as oral histamine H.sub.1 -receptor antagonist. However, any topical formulation of this drug applied to the bronchia has not been acceptable in practice due to strong irritation to bronchial tissues.
The 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds of the present invention are novel compounds, and have not been disclosed or suggested in any prior literature.
DISCLOSURE OF THE INVENTION
The object of the present invention is to provide novel 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds and pharmaceutically acceptable salts thereof which are useful as therapeutic agents for the treatment of bronchial asthma by inhalation to the bronchia.
Another object of the present invention is to provide pharmaceutical composition containing a 1-(2-benzimidazolyl)-1,5-diazacyclooctane compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is effective for the treatment of bronchial asthma by inhalation to the bronchia.
A further object of the present invention is to provide the use of a 1-(2-benzimidazolyl)-1,5-diazacyclooctance compound or a pharmaceutically acceptable salt thereof for the manufacture of a pharmaceutical for the treatment of bronchial asthma.
Still further object of the present invention is to provide a method for the treatment of bronchial asthma, which comprises inhaling to the bronchia a therapeutically effective amount of a 1-(2-benzimidazolyl)-1,5-diazacyclooctane compound or a pharmaceutically acceptable salt thereof.
Other objects, feature and advantages of the present invention will become apparent from the following description of the invention.
The present invention provides novel 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds and pharmaceutically acceptable salts thereof which exhibit potent antihistaminic and antiallergic activities with less topical irritations, and particularly irritation to bronchial tissues.
REFERENCES:
patent: 4835161 (1989-05-01), Janssens et al.
patent: 4943580 (1990-07-01), Janssens et al.
patent: 4988689 (1991-01-01), Janssens et al.
patent: 5461059 (1995-10-01), Bonnet et al.
Isawa Hidetoshi
Momose Den-ichi
Nonaka Yoshinori
Satoh Masaaki
Takehana Yasuo
Datlow Philip I.
Kissei Pharmaceutical Co. Ltd.
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