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1. WO2001043738 - METHOD FOR DETECTING NUCLEOTIDE SYNTHESIS INHIBITORS HAVING FEWER SIDE EFFECTS

Publication Number WO/2001/043738
Publication Date 21.06.2001
International Application No. PCT/EP2000/012043
International Filing Date 30.11.2000
Chapter 2 Demand Filed 03.07.2001
IPC
A61K 31/275 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
275Nitriles; Isonitriles
G01N 33/50 2006.1
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48Biological material, e.g. blood, urine; Haemocytometers
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
CPC
A61K 31/275
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
275Nitriles; Isonitriles
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
G01N 33/5088
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
48Biological material, e.g. blood, urine
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
5005involving human or animal cells
5008for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
5082Supracellular entities, e.g. tissue, organisms
5088of vertebrates
Applicants
  • AVENTIS PHARMA DEUTSCHLAND GMBH [DE]/[DE]
  • LINDNER, Jürgen (JP)
  • HAASE, Burkhard (JP)
Inventors
  • LINDNER, Jürgen
  • HAASE, Burkhard
Priority Data
199 60 443.615.12.1999DE
Publication Language German (de)
Filing Language German (DE)
Designated States
Title
(DE) VERFAHREN ZUR AUFFINDUNG VON NUKLEOTIDSYNTHESEINHIBITOREN MIT WENIGER NEBENWIRKUNGEN
(EN) METHOD FOR DETECTING NUCLEOTIDE SYNTHESIS INHIBITORS HAVING FEWER SIDE EFFECTS
(FR) PROCEDE DE DETECTION D'INHIBITEURS DE SYNTHESE NUCLEOTIDIQUE AYANT MOINS D'EFFETS SECONDAIRES
Abstract
(DE) Die Erfindung betrifft ein Verfahren zum Auffinden von Nukleotidsyntheseinhibitoren, die ein besseres therapeutisches Fenster aufweisen, worin man den Nukleotidsyntheseinhibitor einem für die human Situation relevanten Säugetier in einer wirksamen Dosis appliziert, die Konzentration des Nukleotidsyntheseinhibitors im Blut des Säugetiers feststellt und bestimmt, ob der Nukleotidsyntheseinhibitor eine Halbwertzeit aufweist, die kürzer als die von N-(4-Trifluormethylphenyl)-2-cyan-3-hydroxy-crotonsäureamid ist.
(EN) The invention relates to a method for detecting nucleotide synthesis inhibitors, which have an improved therapeutic window, wherein the nucleotide synthesis inhibitor is administered to a mammal in an effective dosage. Said mammal can be used as a model for humans. The concentration of the nucleotide synthesis inhibitor is determined in the blood of the mammal. The half-life of said nucleotide synthesis inhibitor is measured in order to determine whether said half-life is shorter than the half-life of N-(4-trifluoromethylphenyl)-2-cyan-3-hydroxy-crotonic acid amide.
(FR) La présente invention concerne un procédé permettant de détecter des inhibiteurs de synthèse nucléotidique qui présentent une meilleure ouverture thérapeutique. Dans ledit procédé, une dose efficace de l'inhibiteur de synthèse nucléotidique est appliquée à un mammifère de situation proche de celle de l'être humain, la concentration de l'inhibiteur de synthèse nucléotidique dans le sang du mammifère est détectée et l'on détermine si l'inhibiteur de synthèse nucléotidique a une demi-vie inférieure à celle de l'amide de l'acide crotonique N-(4-trifluorométhylphényl)-2-cyan-3-hydroxy.
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