US4603130A
Expired / Lapsed
US
⏱️ 0.0 years remaining
1-substituted-2-(piperazinyl or homopiperazinyl)-benzimidazole compounds and pharmaceutical composition
Assignee: Kanebo Ltd
•
Filing: 1984-03-28
•
Granted: 1986-07-29
•
Expires: 2004-03-28
Abstract
Abstract Novel benzimidazole derivatives of the formula: <IMAGE> wherein R1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof, which have potent antihistaminic activity with less toxicity and hence are useful as an antihistaminics, and a process for the preparation of the compounds, and a pharmaceutical composition useful as antihistaminics containing the compound as an essential 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 10:50
CPC Classifications
C; C07; C07D; C07D235/00; C07D235/02; C07D235/04; C07D235/06; C07D235/14; A; A61; A61P; A61P43/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
52 words
A benzimidazole compound of the formula ##STR16## wherein R 1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R 2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
52 words
A benzimidazole compound of the formula ##STR16## wherein R 1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R 2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
17 words
The compound according to claim 1, which is 1-(2-ethoxyethyl)-2-(4-methyl-1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
17 words
The compound according to claim 1, which is 1-(2-ethoxyethyl)-2-(1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
17 words
The compound according to claim 1, which is 1-(2-propargyloxyethyl)-2-(4-methyl-1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
75 words
An antihistaminic composition which comprises as an active ingredient an antihistaminically effective amount of a benzimidazole compound of the formula: ##STR17## wherein R 1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R 2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof in admixture with a pharmaceutically acceptable carrier or diluent.
Claim 7
Dependent Claim
75 words
An antihistaminic composition which comprises as an active ingredient an antihistaminically effective amount of a benzimidazole compound of the formula: ##STR17## wherein R 1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R 2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof in admixture with a pharmaceutically acceptable carrier or diluent.
Claim 8
Dependent Claim
20 words
The composition according to claim 5, wherein the active ingredient is 1-(2-ethoxyethyl)-2-(4-methyl-1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
20 words
The composition according to claim 5, wherein the active ingredient is 1-(2-ethoxyethyl)-2-(1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
20 words
The composition acording to claim 5, wherein the active ingredient is 1-(2-propargyloxyethyl)-2-(4-methyl-1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
References Cited (Backward Citations)
US3423413A
Cited
GB1216381A
Cited
US3658822A
Cited
US3794651A
Cited
US4011322A
Cited
US4029789A
Cited
US4093726A
Cited
US4179505A
Cited
US4459296A
Cited
US4430343A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-07-28 | 1990-01-27 | 1990-07-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-07-28 | 1994-01-27 | 1994-07-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-07-28 | 1998-01-27 | 1998-07-29 | $7700.00 | Window Closed / Lapsed |