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Claims for Patent: 4,430,343

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Claims for Patent: 4,430,343

Title: Benzimidazole derivatives, process for the preparation thereof and pharmaceutical composition containing the same
Abstract:Novel benzimidazole derivatives of the formula: ##STR1## wherein R.sup.1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and n is 2 or 3, or pharmaceutically acceptable acid addition salts thereof, which have excellent antihistaminic activities and are useful as antiallergics for various allergic diseases, and a process for the preparation thereof, and an antihistaminic composition containing the compound as an active ingredient.
Inventor(s): Iemura; Ryuichi (Kawanisi, JP), Kawashima; Tsuneo (Kobe, JP), Fukuda; Toshikazu (Osaka, JP), Ito; Keizo (Osaka, JP), Nose; Takashi (Nara, JP), Tsukamoto; Goro (Toyonaka, JP)
Assignee: Kanebo, Ltd. (Tokyo, JP)
Application Number:06/436,032
Patent Claims: 1. A benzimidazole derivative of the formula: ##STR20## wherein R.sup.1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof.

2. A compound according to claim 1 which is 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

3. A compound according to claim 1 which is 1-[2-(propargyloxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

4. A compound according to claim 1 which is 1-[2-(ethoxy)ethyl]-2-(1-piperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

5. A compound according to claim 1 which is 1-[2-(phenoxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

6. An antihistaminic composition, which comprises an effective amount of a benzimidazole derivative of the formula: ##STR21## wherein R.sup.1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof as an active ingredient in admixture with a conventional pharmaceutically acceptable carrier or diluent.

7. The composition according to claim 6, wherein the active ingredient is 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

8. The composition according to claim 6, wherein the active ingredient is 1-[2-(propargyloxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

9. The composition according to claim 6, wherein the active ingredient is 1-[2-(ethoxy)ethyl]-2-(1-piperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.

10. The composition according to claim 6, wherein the active ingredient is 1-[2-(phenoxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole or a pharmaceutically accetpable acid addition salt thereof.
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