Patent EP0123962A2 successfully refreshed from Google Patents.
EP0123962A2
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Benzimidazole derivative, process for the preparation thereof and pharmaceutical composition
Assignee: Kanebo Ltd
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Filing: 1984-04-06
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Granted: —
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Expires: 2004-04-06
Abstract
Abstract Novel benzimidazole derivatives of the formula:wherein R<sup>1</sup> is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R<sup>2</sup> 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
EP
Data Source
google_patents
Last Synchronized
2026-10-26 23:31
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: 14
Claim 1
Independent Claim
51 words
A benzimidazole derivative, of the formula: 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
51 words
A benzimidazole derivative, of the formula: 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-l-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-l-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
103 words
A process for preparing a benzimidazole derivative of the formula: wherein R 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, which comprises reacting a compound of the formula: wherein R 1 is as defined above, and X is a halogen atom, with a compound of the formula: wherein R 2 and n are as defined above, optionally converting the resulting compound into a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
103 words
A process for preparing a benzimidazole derivative of the formula: wherein R 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, which comprises reacting a compound of the formula: wherein R 1 is as defined above, and X is a halogen atom, with a compound of the formula: wherein R 2 and n are as defined above, optionally converting the resulting compound into a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
137 words
A process for preparing a benzimidazole derivative of the formula: wherein R 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, which comprises reacting a compound of the formula: wherein R 3 is a lower alkyl group, a lower hydroxyalkyl group or a protecting group which is easily removed by catalytic reduction or under an acidic or basic condition, and n is as defined above, with a compound of the formula: wherein R 1 is as defined above, and X is a halogen atom, optionally removing the protecting group and further optionally converting the resulting compound into a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
137 words
A process for preparing a benzimidazole derivative of the formula: wherein R 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, which comprises reacting a compound of the formula: wherein R 3 is a lower alkyl group, a lower hydroxyalkyl group or a protecting group which is easily removed by catalytic reduction or under an acidic or basic condition, and n is as defined above, with a compound of the formula: wherein R 1 is as defined above, and X is a halogen atom, optionally removing the protecting group and further optionally converting the resulting compound into a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
69 words
, An antihistaminic composition which comprises as an active ingredient a benzimidazole derivative of the formula: wherein R 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 11
Dependent Claim
69 words
, An antihistaminic composition which comprises as an active ingredient a benzimidazole derivative of the formula: wherein R 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 12
Dependent Claim
20 words
The composition according to claim 7, wherein the active ingredient is 1-(2-ethoxyethyl)-2-(4-methyl-1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 13
Dependent Claim
20 words
The composition according to claim 7, wherein the active ingredient is 1-(2-ethoxyethyl)-2-(1-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
Claim 14
Dependent Claim
20 words
The composition according to claim 7, wherein the active ingredient is 1-(2-propargyloxyethyl)-2-(4-methyl-l-piperazinyl)methylbenzimidazole or a pharmaceutically acceptable acid addition salt thereof.
References Cited (Backward Citations)
No citation records indexed.
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