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1. WO1990014337 - DIVALENT METAL SALTS OF INDOMETHACIN

Publication Number WO/1990/014337
Publication Date 29.11.1990
International Application No. PCT/AU1990/000209
International Filing Date 21.05.1990
Chapter 2 Demand Filed 08.11.1990
IPC
C07D 209/28 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
26with an acyl radical attached to the ring nitrogen atom
281-(4-Chlorobenzoyl)-2-methyl- indolyl-3-acetic acid, substituted in position 5 by an oxygen or nitrogen atom; Esters thereof
CPC
C07D 209/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
26with an acyl radical attached to the ring nitrogen atom
281-(4-Chlorobenzoyl)-2-methyl-indolyl-3-acetic acid, substituted in position 5 by an oxygen or nitrogen atom; Esters thereof
Applicants
  • BIOCHEMICAL VETERINARY RESEARCH [AU]/[AU] (AllExceptUS)
  • REGTOP, Hubertus, Leonardus [AU]/[AU] (UsOnly)
  • BIFFIN, John, Raymond [AU]/[AU] (UsOnly)
Inventors
  • REGTOP, Hubertus, Leonardus
  • BIFFIN, John, Raymond
Agents
  • SPRUSON & FERGUSON
Priority Data
PJ 432822.05.1989AU
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DIVALENT METAL SALTS OF INDOMETHACIN
(FR) SELS METALLIQUES DIVALENTS D'INDOMETHACINE
Abstract
(EN)
The present invention provides a method for the treatment of infllammation and pain in a mammal requiring such treatment, comprising administering to said mammal an anti-inflammatory and analgesically effective amount of an indomethacin salt of a divalent metal capable of forming a stable complex with indomethacin, or of a pharmaceutical composition comprising said indomethacin salt together with a pharmaceutically acceptable carrier, diluent and/or excipient. The present invention also provides a process for the preparation of an indomethacin salt of a divalent metal capable of forming a stable complex with indomethacin comprising forming a solution by dissolving indomethacin and a salt of said divalent metal in a tertiary amide or cyclic tertiary amide, adding a C1-4 alkanol or C3-6 ketone to the solution to precipitate the indomethacin metal salt and separating the indomethacin metal salt precipitate from the solution. The present invention still further provides a pharmaceutical composition for alleviating inflammation and pain comprising an anti-inflammatory and analgesically effective amount of salts of indomethacin produced by the process of the invention together with a pharmaceutically acceptable carrier, diluent and/or excipient.
(FR)
Le procédé décrit, qui sert à traiter les inflammations et les douleurs chez un mammifère nécessitant un tel traitement, consiste à administrer au mammifère une quantité anti-inflammatoire et analgésiquement efficace d'un sel d'indométhacine d'un métal divalent capable de former un complexe stable avec l'indométhacine, ou d'une composition pharmaceutique comprenant ce sel d'indométhacine conjointement avec un véhicule, un diluant et/ou un excipient pharmaceutiquement acceptables. L'invention se rapporte également à un procédé de préparation d'un sel d'indométhacine d'un métal divalent capable de former un complexe stable avec l'indométhacine, ce procédé consistant à former une solution en dissolvant l'indométhacine et un sel de ce métal divalent dans un amide tertiaire ou un amide tertiaire cyclique, à ajouter un alcanol de 1 à 4 atomes de carbones ou une cétone de 3 à 6 atomes de carbone dans la solution, afin de précipiter le sel métallique d'indométhacine, puis à séparer le précipité de sel métallique d'indométhacine de la solution. L'invention se rapporte en outre à une composition pharmaceutique de soulagement des inflammations et des douleurs, qui comprend une quantité anti-inflammatoire et analgésiquement efficace de sels d'indométhacine produits par le procédé de la présente invention conjointement avec un véhicule, un diluant et/ou un excipient pharmaceutiquement acceptables.
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