US4430343A
Expired / Lapsed
US
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Benzimidazole derivatives, process for the preparation thereof and pharmaceutical composition containing the same
Assignee: Akzo Nobel NV
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Filing: 1982-10-22
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Granted: 1984-02-07
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Expires: 2002-10-22
Abstract
Abstract Novel benzimidazole derivatives of the formula: <IMAGE> (I) wherein R1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R2 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.
Inventors
- 👤 Ryuichi Iemura
- 👤 Tsuneo Kawashima
- 👤 Toshikazu Fukuda
- 👤 Keizo Ito
- 👤 Takashi Nose
- 👤 Goro Tsukamoto
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 23:19
CPC Classifications
C; C07; C07D; C07D235/00; C07D235/02; C07D235/04; C07D235/24; A; A61; A61P; A61P37/00; A61P37/08; A61P43/00; C07D235/30; C07D403/00; C07D403/02; C07D403/04; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
56 words
A benzimidazole derivative of the formula: ##STR20## wherein R 1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R 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.
Claim 2
Dependent Claim
56 words
A benzimidazole derivative of the formula: ##STR20## wherein R 1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R 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.
Claim 3
Dependent Claim
17 words
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.
Claim 4
Dependent Claim
17 words
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.
Claim 5
Dependent Claim
17 words
A compound according to claim 1 which is 1-[2-(ethoxy)ethyl]-2-(1-piperazinyl)benzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
17 words
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.
Claim 7
Dependent Claim
79 words
An antihistaminic composition, which comprises an effective amount of a benzimidazole derivative of the formula: ##STR21## wherein R 1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R 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.
Claim 8
Dependent Claim
79 words
An antihistaminic composition, which comprises an effective amount of a benzimidazole derivative of the formula: ##STR21## wherein R 1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R 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.
Claim 9
Dependent Claim
20 words
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.
Claim 10
Dependent Claim
20 words
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.
Claim 11
Dependent Claim
20 words
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.
Claim 12
Dependent Claim
20 words
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.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-02-06 | 1987-08-08 | 1988-02-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-02-06 | 1991-08-08 | 1992-02-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-02-06 | 1995-08-08 | 1996-02-07 | $7700.00 | Window Closed / Lapsed |