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1. WO1996002533 - NOVEL 6- AND 6,8-SUBSTITUTED 1-[4-(1H-1,2,4-TRIAZOL-1-YL METHYL) PHENYL] QUINOLONE CARBOXYLIC ACIDS

Publication Number WO/1996/002533
Publication Date 01.02.1996
International Application No. PCT/EP1995/002644
International Filing Date 07.07.1995
Chapter 2 Demand Filed 12.02.1996
IPC
C07D 521/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
521Heterocyclic compounds containing unspecified hetero rings
CPC
C07D 231/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
12with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/56
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
56with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 249/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
Applicants
  • BAYER AKTIENGESELLSCHAFT [DE/DE]; D-51368 Leverkusen, DE (AllExceptUS)
  • BENDER, Wolfgang [DE/DE]; DE (UsOnly)
  • RÖBEN, Wolfgang [DE/DE]; DE (UsOnly)
  • PAESSENS, Arnold [DE/DE]; DE (UsOnly)
  • BARTEL, Stephan [DE/DE]; DE (UsOnly)
Inventors
  • BENDER, Wolfgang; DE
  • RÖBEN, Wolfgang; DE
  • PAESSENS, Arnold; DE
  • BARTEL, Stephan; DE
Common Representative
  • BAYER AKTIENGESELLSCHAFT; D-51368 Leverkusen, DE
Priority Data
P 44 25 648.520.07.1994DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) NEUE 6 UND 6,8-SUBSTITUIERTE 1-[4-(1H-1,2,4-TRIAZOL-1-YL-METHYL)PHENYL] CHINOLONCARBONSÄUREN
(EN) NOVEL 6- AND 6,8-SUBSTITUTED 1-[4-(1H-1,2,4-TRIAZOL-1-YL METHYL) PHENYL] QUINOLONE CARBOXYLIC ACIDS
(FR) NOUVEAUX ACIDES 1-[4-(1H-1,2,4-TRIAZOL-1-YL-METHYL)PHENYL]QUINOLONE-CARBOXYLIQUES SUBSTITUES EN 6 ET 6,8
Abstract
(DE)
6- und 6,8-substituierte 1-[4-(1H-1,2,4-triazol-1-yl-methyl)phenyl] Chinoloncarbonsäuren der allgemeinen Formel (I), in welcher A für Wasserstoff oder Methyl steht, R1 für Phenyl, Naphthyl, Pyridyl, Pyrimidyl oder Pyrazinyl steht, die gegebenenfalls bis zu 3-fach gleich oder verschieden durch Nitro, Trifluormethyl, Halogen, Cyano, Hydroxy oder durch geradkettiges oder verzweigtes Alkyl, Acyl, Alkoxy oder Alkylthio mit jeweils bis zu 8 Kohlenstoffatomen substituiert sind, R2 für Wasserstoff, Fluor oder Chlor steht, Verfahren zu ihrer Herstellung, sowie ihre Verwendung als Arzneimittel, insbesondere als antivirale Mittel.
(EN)
The invention pertains to 6- and 6,8-substituted 1-[4-(1H-1,2,4-triazol-1-yl methyl) phenyl] quinolone carboxylic acids of general formula (I), in which A is hydrogen or methyl, R1 is phenyl, naphthyl, pyridyl, pyrimidyl or pyrazinyl, optionally substituted up to three times, alike or differently, by nitro, trifluoromethyl, halogen, cyano, hydroxy or by straight-chain or branched alkyl, acyl, alkoxy or alkylthio with up to 8 carbon atoms in each case, and R2 is hydrogen, fluorine or chlorine. The invention also pertains to methods for preparing them as well as their use as drugs, especially as antiviral agents.
(FR)
L'invention concerne des acides 1-[4-(1H-1,2,4-triazol-1-yl-méthyl)phényl]quinolone-carboxyliques substitués en 6 et 6,8 de la formule générale (I) dans laquelle A désigne hydrogène ou méthyle, R1 désigne phényle, naphtyle, pyridyle, pyrimidyle ou pyrazinyle, éventuellement substitués jusqu'à 3 fois de manière identique ou différente par nitro, trifluorométhyle, halogène, cyano, hydroxy ou par alkyle, acyle, alcoxy ou alkylthio linéaire ou ramifié et comportant chacun jusqu'à 8 atomes de carbone, R2 désigne hydrogène, fluor ou chlore. L'invention concerne des procédés permettant de les préparer, ainsi que leur utilisation comme médicaments, notamment comme agents antiviraux.
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