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EP0034474A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Substituted imidazoles, their preparation and pharmaceutical compositions containing the same

Assignee: Farmos Yhtyma Oy
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Filing: 1981-02-12
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Granted: —
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Expires: 2001-02-12
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Abstract

Abstract The invention provides compounds of the formula: wherein each of R 1 , R 2 and R 3 , which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R 4 is hydrogen or alkyl of 1 to 7 carbon atoms; and n is 0-3; and their non-toxic pharmaceutically acceptable acid addition salts. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, e.g. as anti-hypertensive, β-blocking and anti-thrombotic agents. Furthermore the compounds have remarkable antimicrobial activity. The compounds may be made by a variety of methods and may be incorporated in pharmaceutical compositions also comprising a compatible pharmaceutically acceptable carrier.

Inventors

  • 👤 Arto Johannes Karjalaynen
  • 👤 Kauko Oiva Antero Kurkela

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-30 19:31
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/56; A; A61; A61P; A61P25/00; A61P25/02; A61P31/00; A61P31/04; A61P7/00; A61P7/02; A61P7/10; A61P9/00; A61P9/12; C07D233/64; C07D263/00; C07D263/02; C07D263/30; C07D263/32

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 102 words
A process for the preparation of a substituted imidazole derivative of the formula: wherein each of R 1 , R 2 and R 3 , which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R 4 is hydrogen or an alkyl radical of 1 to 7 carbon atoms; and n is an integer from 0-3, or a non-toxic pharmaceutically acceptable acid addition salt thereof, which comprises dehydration of a compound of the formula: wherein R 1 , R 2' R 3 and R 4 are as defined above and n is 1-4.
Claim 2
Dependent Claim 102 words
A process for the preparation of a substituted imidazole derivative of the formula: wherein each of R 1 , R 2 and R 3 , which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R 4 is hydrogen or an alkyl radical of 1 to 7 carbon atoms; and n is an integer from 0-3, or a non-toxic pharmaceutically acceptable acid addition salt thereof, which comprises dehydration of a compound of the formula: wherein R 1 , R 2' R 3 and R 4 are as defined above and n is 1-4.
Claim 3
Dependent Claim 72 words
A process for the preparation of a substituted imidazole derivative of the formula I as defined in claim 1 or a non-toxic pharmaceutically acceptable acid addition salt thereof which comprises reacting an imidazole aldehyde of the formula wherein R 4 is as defined in claim 1, with an aralkylidenetriphenyl phosporane of the formula wherein R 1 , R 2 and R 3 are as defined in claim 1 and n is 0-3.
Claim 4
Dependent Claim 84 words
A process for the preparation of a substituted imidazole derivative of the formula I as defined in claim 1 or a non-toxic pharmaceutically acceptable acid addition salt thereof which comprises reacting a compound of the formula wherein R 1 , R 2 and R 3 are as defined in claim 1, X is a halogen atom or hydroxy, R 4 is hydrogen or methyl and n is 0-3, with a reagent capable of converting said starting material to the corresponding imidazole of formula (I).
Claim 5
Dependent Claim 13 words
A process according to claim 3, in which the said reagent is formamide.
Claim 6
Dependent Claim 21 words
A process according to claim 1 wherein the dehydration is performed by refluxing the said compound with an appropriate acidic solution.
Claim 7
Dependent Claim 23 words
A process according to claim 1 wherein the dehydration of the said compound is performed by heating it with anhydrous potassium hydrogen sulfate.

References Cited (Backward Citations)

US3050520A Cited

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