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1. WO1992014713 - NOVEL CIMETIDINE POLYMORPH AND PROCESS FOR PREPARING SAME

Publication Number WO/1992/014713
Publication Date 03.09.1992
International Application No. PCT/HU1992/000007
International Filing Date 14.02.1992
Chapter 2 Demand Filed 14.09.1992
IPC
C07D 233/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
CPC
C07D 233/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
Applicants
  • RICHTER GEDEON VEGYÉSZETI GYÁR RT. [HU]/[HU] (AllExceptUS)
  • JESZENSZKY, Andor [HU]/[HU] (UsOnly)
  • VÉGH, Ferenc [HU]/[HU] (UsOnly)
  • BENCSIK, Péter [HU]/[HU] (UsOnly)
  • NAGY, László [HU]/[HU] (UsOnly)
  • HEGEDU^'S, Béla [HU]/[HU] (UsOnly)
  • GÖRÖG, Sándor [HU]/[HU] (UsOnly)
  • PAPNÉ SZIKLAI, Zsófia [HU]/[HU] (UsOnly)
  • HAHNÓCZY, Mariann [HU]/[HU] (UsOnly)
  • VERECKEI, László [HU]/[HU] (UsOnly)
  • KOZMA, Gézáné [HU]/[HU] (UsOnly)
  • KAPÁS, Margit [HU]/[HU] (UsOnly)
  • TÖRÖK, Éva [HU]/[HU] (UsOnly)
Inventors
  • JESZENSZKY, Andor
  • VÉGH, Ferenc
  • BENCSIK, Péter
  • NAGY, László
  • HEGEDU^'S, Béla
  • GÖRÖG, Sándor
  • PAPNÉ SZIKLAI, Zsófia
  • HAHNÓCZY, Mariann
  • VERECKEI, László
  • KOZMA, Gézáné
  • KAPÁS, Margit
  • TÖRÖK, Éva
Agents
  • DANUBIA
Priority Data
502/9115.02.1991HU
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL CIMETIDINE POLYMORPH AND PROCESS FOR PREPARING SAME
(FR) CIMETIDINE POLYMORPHE NOUVELLE ET PROCEDE D'ELABORATION
Abstract
(EN)
The invention relates to the novel polymorph modification 'E' of N-cyano-N'-methyl-N''{2-[(5-methyl-imidazol-4-yl)-methylthio]-ethyl}-guanidine (cimetidine 'E') characterized by infrared spectroscopical characteristics. According to the process of the invention cimetidine 'E' is prepared by accomplishing an aqueous system, which is supersaturated for N-cyano-N'-methyl-N''-{2-[(5-methylimidazol-4-il)-methylthio]-ethyl}-guanidine at a temperature below 30 °C and contains a water-miscible organic solvent in an amount of at most 40 % by volume, crystallizing the solution or emulsion optionally by adding an inoculating crystal, separating the crystals precipitated, drying them at a temperature below 20 °C or removing the water content of the crystals with an organic solvent and subsequently drying them. The novel modification 'E' of cimetidine shows better rheological and flowing properties in comparison to those of cimetidine 'A' and provides several advantages concerning pharmaceutical technology.
(FR)
L'invention a trait à une modification polymorphe nouvelle 'E' de N-cyano-N'-méthyl-N''{2-[(5-méthylimidazole-4-yl)-méthylthio]-éthyl}-guanidine (cimétidine 'E') se distinguant par ses caractéristiques spectroscopiques infrarouges. Selon le procédé de l'invention, la cimétidine 'E' est élaborée en réalisant un système aqueux, qui est sursaturé pour N-cyano-N'-méthyl-N''-{2-[(5-méthylimidazole-4-il)-méthylthio]-éthyl}-guanidine à une température inférieure à 30 °C et contient un solvant organique miscible dans l'eau dans une proportion d'au moins 40 % en volume, cristallisant la solution ou l'émulsion en ajoutant un cristal d'inoculation, en séparant les cristaux précipités, en les asséchant à une température inférieure à 20 °C ou en extrayant le contenu en eau des cristaux à l'aide d'un solvant organique puis en les asséchant. Cette nouvelle modification 'E' de cimétidine présente des caractéristiques rhéologiques et d'écoulement supérieures par rapport à celles de la cimétidine 'A' et offre plusieurs avantages aux techniques pharmaceutiques.
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