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EP0016255A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Isoxazole derivative, preparation thereof and pharmaceutical compositions containing the same

Assignee: Zambon SpA
•
Filing: 1979-12-05
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Granted: —
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Expires: 1999-12-05
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Abstract

Abstract 1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethano endowed with therapeutic acitivity, in particular bronchodilating action is disclosed, as well as a method for preparing same from 3-bromo-5-isoxazolecarboxylic acid. Intermediate new compounds as well as pharmaceutical compositions containing the novel isoxazole derivative are also disclosed.

Inventors

  • 👤 Davide Della Bella
  • 👤 Dario Chiarino

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-26 16:33
CPC Classifications
C; C07; C07D; C07D261/00; C07D261/02; C07D261/06; C07D261/10; A; A61; A61P; A61P11/00; A61P11/08; A61P25/00; A61P25/02

Claims Analysis

Total Claims: 17
Claim 1
Independent Claim 1 words
1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethanol.
Claim 2
Dependent Claim 1 words
1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethanol.
Claim 3
Dependent Claim 61 words
A process for the preparation of 1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethanol, characterized in that (a) the 3-bromo-5-isoxazolecarboxylic acid is reacted with a chlorinating agent, (b) the obtained chloride of the 3-bromo-5-isoxazolecarboxylic-acid is converted into the corresponding ketone by reaction with a nucleofile alkylating aaent, followed by hydrolysis and decarboxylation, (c) the obtained ketone is brominated, reduced and (d) the obtained 1-(3-bromo-isoxazol-5-yl)-2-bromoethanol is treated with ter.butylamine.
Claim 4
Dependent Claim 61 words
A process for the preparation of 1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethanol, characterized in that (a) the 3-bromo-5-isoxazolecarboxylic acid is reacted with a chlorinating agent, (b) the obtained chloride of the 3-bromo-5-isoxazolecarboxylic-acid is converted into the corresponding ketone by reaction with a nucleofile alkylating aaent, followed by hydrolysis and decarboxylation, (c) the obtained ketone is brominated, reduced and (d) the obtained 1-(3-bromo-isoxazol-5-yl)-2-bromoethanol is treated with ter.butylamine.
Claim 5
Dependent Claim 24 words
A process according to claim 2, characterized in that the 1-(3-bromo-isoxazol-5-yl)-2-bromoethanol is first transformed into the 2-(3-bromo-isoxazol-5-yl)-oxi- rane and thereafter is treated with ter.butylamine.
Claim 6
Dependent Claim 1 words
3-Bromo-5-acetylisoxazole.
Claim 7
Dependent Claim 1 words
3-Bromo-5-acetylisoxazole.
Claim 8
Dependent Claim 1 words
3-Bromo-5-bromoacetyl-isoxazole.
Claim 9
Dependent Claim 1 words
3-Bromo-5-bromoacetyl-isoxazole.
Claim 10
Dependent Claim 1 words
1-(3-bromo-isoxazol-5-yl)-2-bromoethanol.
Claim 11
Dependent Claim 1 words
1-(3-bromo-isoxazol-5-yl)-2-bromoethanol.
Claim 12
Dependent Claim 1 words
2-(3-bromo-isoxazol-5-yl)-oxirane.
Claim 13
Dependent Claim 1 words
2-(3-bromo-isoxazol-5-yl)-oxirane.
Claim 14
Dependent Claim 7 words
The pharmaceutically acceptable salts of 1-(3-bro- mo-isoxazol-5-yl)-2-ter.butlaminoethanol.
Claim 15
Dependent Claim 7 words
The pharmaceutically acceptable salts of 1-(3-bro- mo-isoxazol-5-yl)-2-ter.butlaminoethanol.
Claim 16
Dependent Claim 18 words
The pharmaceutical compositions containing the 1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethanol or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim 18 words
The pharmaceutical compositions containing the 1-(3-bromo-isoxazol-5-yl)-2-ter.butylaminoethanol or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

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