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1. WO1996002511 - NOVEL N¿1? DIVERSE 6-FLUORINE-8-DIFLUOROMETHOXY SUBSTITUTED QUINOLONE CARBOXYLIC ACIDS

Publication Number WO/1996/002511
Publication Date 01.02.1996
International Application No. PCT/EP1995/002645
International Filing Date 07.07.1995
Chapter 2 Demand Filed 12.02.1996
IPC
C07D 215/56 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
54attached in position 3
56with oxygen atoms in position 4
C07D 521/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
521Heterocyclic compounds containing unspecified hetero rings
CPC
C07D 215/56
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
54attached in position 3
56with oxygen atoms in position 4
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
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of bulk chemicals
55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • BAYER AKTIENGESELLSCHAFT [DE]/[DE] (AllExceptUS)
  • BENDER, Wolfgang [DE]/[DE] (UsOnly)
  • RÖBEN, Wolfgang [DE]/[DE] (UsOnly)
  • PAESSENS, Arnold [DE]/[DE] (UsOnly)
  • BARTEL, Stephan [DE]/[DE] (UsOnly)
Inventors
  • BENDER, Wolfgang
  • RÖBEN, Wolfgang
  • PAESSENS, Arnold
  • BARTEL, Stephan
Common Representative
  • BAYER AKTIENGESELLSCHAFT
Priority Data
P 44 25 659.020.07.1994DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) NEUE N1-DIVERSE 6-FLUOR-8-DIFLUORMETHOXY SUBSTITUIERTE CHINOLONCARBONSÄUREN
(EN) NOVEL N1 DIVERSE 6-FLUORINE-8-DIFLUOROMETHOXY SUBSTITUTED QUINOLONE CARBOXYLIC ACIDS
(FR) NOUVEAUX ACIDES CARBOXYLIQUES DE QUINOLONE A DIVERS N1 SUBSTITUES PAR 6-FLUORO-8-DIFLUOROMETHOXY
Abstract
(DE)
N1-diverse 6-Fluoro-8-difluormethoxy substituierte Chinoloncarbonsäuren der allgemeinen Formel (I), in welcher A für Wasserstoff oder Methyl steht, R1 für Phenyl, 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 oder für geradkettiges oder verzweigtes Alkyl mit bis zu 6 Kohlenstoffatomen steht, D oder E für Wasserstoff steht und D für Morpholino steht oder E für einen Rest der Formel -CH2-L steht, worin L Morpholino, oder einen über N-gebundenen 5-gliedrigen Heteroaromaten mit bis zu 3 weiteren Stickstoffatomen bedeutet, oder eine Gruppe der Formel -NR3R4 bedeutet, worin R3 und R4 gleich oder verschieden sind, und Wasserstoff, geradkettiges oder verzweigtes Alkyl mit bis zu 6 Kohlenstoffatomen oder eine Aminoschutzgruppe bedeuten, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel, insbesondere als antivirale Mittel.
(EN)
N1 diverse 6-fluorine-8-difluoromethoxy substituted quinolone carboxylic acids of the general formula (I) in which A is hydrogen or methyl, R1 is phenyl, pyridyl, pyrimidyl or pyrazinyl, which may be substituted up to triply, equally or differently, by nitro, trifluoromethyl, halogen, cyano, hydroxy or by straight-chained or branched alkyl, acyl, alkoxy or alkylthio with up to 8 carbon atoms, R2 is hydrogen or a straight-chained or branched alkyl with up to 6 carbon atoms, D or E is hydrogen and D is morpholino or E is a radical of the formula -CH2-L, in which L is morpholino or a 5-membered heteroaromatic bonded via N with up to 3 further nitrogen atoms or a group of the formula NR3R4, in which R3 and R4 are the same or different and are hydrogen, straight-chained or branched alkyl with up to 6 carbon atoms or an amino protective group, process for their production and their use as medicaments, especially antiviral agents.
(FR)
L'invention concerne de nouveaux acides carboxyliques de quinolone à divers N1 substitués par 6-fluoro-8-difluorométhoxy de la formule (I), dans laquelle A désigne hydrogène ou méthyle, R1 désigne phényle, pyridyle, pyrimidyle ou pyrazinyle, éventuellement substitués jusqu'à trois fois de manière identique ou différente par nitro, trifluorométhyle, halogène, cyano, hydroxy ou par alkyle, acyle, alcoxy ou alkylthio linéaire ou ramifié, comportant chacun jusqu'à 8 atomes de carbone, R2 désigne hydrogène ou alkyle linéaire ou ramifié ayant jusqu'à 6 atomes de carbone, D ou E désigne hydrogène et D désigne morpholino ou E désigne un reste de la formule -CH2-L, dans laquelle L désigne morpholino ou un hétéro-aromatique à 5 chaînons lié en N et comportant jusqu'à 3 autres atomes d'azote ou un groupe de la formule -NR3R4, dans laquelle R3 et R4 sont identiques ou différents et désignent hydrogène, alkyle linéaire ou ramifié ayant jusqu'à 6 atomes de carbone ou un groupe protecteur amino. L'invention concerne des procédés permettant de les préparer, ainsi que leur utilisation comme médicaments, notamment comme agents antiviraux.
Also published as
Latest bibliographic data on file with the International Bureau