HRP20120877T1 - Derivati sulfonil-kinolina - Google Patents

Derivati sulfonil-kinolina Download PDF

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HRP20120877T1
HRP20120877T1 HRP20120877AT HRP20120877T HRP20120877T1 HR P20120877 T1 HRP20120877 T1 HR P20120877T1 HR P20120877A T HRP20120877A T HR P20120877AT HR P20120877 T HRP20120877 T HR P20120877T HR P20120877 T1 HRP20120877 T1 HR P20120877T1
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Croatia
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fluoro
phenyl
quinoline
benzenesulfonyl
chloro
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HRP20120877AT
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János Galambos
György Keseru
Krisztina GÁL
Amrita Ágnes Bobok
Csaba WÉBER
Ibolya Prauda
Gábor András Wágner
Mónika VASTAG
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Richter Gedeon Nyrt.
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Priority claimed from HU0700417A external-priority patent/HU0700417D0/hu
Priority claimed from HU0800376A external-priority patent/HUP0800376A2/hu
Application filed by Richter Gedeon Nyrt. filed Critical Richter Gedeon Nyrt.
Publication of HRP20120877T1 publication Critical patent/HRP20120877T1/hr

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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having 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 with 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
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    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Quinoline Compounds (AREA)

Claims (6)

1. Spoj, naznačen time, da ima formulu (I): [image] gdje Ar1predstavlja fenil- ili tienil-skupinu, opcijski supstituiranu s jednim ili više supstituenata odabranih od sljedećih: vodik, fluor, klor, cijano, metil, metoksi; Ar2 predstavlja fenil, supstituiran s jednim ili više supstituenata odabranih od sljedećih: fluor, klor, cijano, metil, metoksi; R1, R2, R3i R4 međusobno neovisno predstavljaju jedan supstituent odabran od sljedećih: vodik, fluor, klor, cijano, metil, metoksi, hidroksi, trifluorometil, amino, metilamino, dimetilamino, aminometil, metilaminometil, dimetilaminometil, i/ili njegove soli i/ili njegovi hidrati i/ili solvati.
2. Spoj prema zahtjevu 1, naznačen time, da je odabran iz skupine koju čine: 4-(4-kloro-fenil)-3-(4-metil-benzensulfonil)-kinolin, 7-kloro-3-(4-kloro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 8-kloro-4-(3-kloro-fenil)-3-(3,4-dikloro-benzensulfonil)-kinolin, 7-fluoro-3-(4-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-7-fluoro-3-(4-metoksi-benzensulfonil)-kinolin, 7-fluoro-3-(4-metoksi-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 7-fluoro-3-(3-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 7-fluoro-3-(3-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3,4-dimetil-benzensulfonil)-7-fluoro-kinolin, 3-(3,4-dimetil-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,4-dimetil-benzensulfonil)-7-fluoro-4-(3-metoksi-fenil)-kinolin, 4-(3-kloro-fenil)-8-fluoro-3-(4-fluoro-benzensulfonil)-kinolin, 4-(4-kloro-fenil)-8-fluoro-3-(4-fluoro-benzensulfonil)-kinolin, 8-fluoro-3-(4-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 8-fluoro-3-(4-fluoro-benzensulfonil)-4-(3-metoksi-fenil)-kinolin, 4-(4-kloro-fenil)-6-fluoro-3-(4-metoksi-benzensulfonil)-kinolin, 4-(4-kloro-fenil)-3-(3,4-dimetil-benzensulfonil)-6-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3,5-difluoro-benzensulfonil)-7-fluoro-kinolin, 3-(3,5-difluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-3-(3-cijano-benzensulfonil)-7-fluoro-kinolin, 3-(3-cijano-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 7-fluoro-3-(4-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-7-fluoro-3-(3-fluoro-benzensulfonil)-kinolin, 4-(3-kloro-fenil)-7-fluoro-3-(3-metoksi-benzensulfonil)-kinolin, 7-fluoro-4-(4-fluoro-fenil)-3-(3-metoksi-benzensulfonil)-kinolin, 4-(4-kloro-fenil)-3-(3,4-dimetil-benzensulfonil)-7-fluoro-kinolin, 3-(3,4-dimetil-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-kloro-4-metoksi-benzensulfonil)-7-fluoro-kinolin, 3-(3-kloro-4-metoksi-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-kloro-4-metoksi-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-8-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 8-fluoro-3-(4-fluoro-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 4-(3-kloro-fenil)-8-fluoro-3-(4-metoksi-benzensulfonil)-kinolin, 4-(4-kloro-fenil)-8-fluoro-3-(4-metoksi-benzensulfonil)-kinolin, 8-fluoro-4-(4-fluoro-fenil)-3-(4-metoksi-benzensulfonil)-kinolin, 8-fluoro-3-(4-metoksi-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 8-fluoro-3-(4-metoksi-benzensulfonil)-4-(3-metoksi-fenil)-kinolin, 4-(3-kloro-fenil)-8-fluoro-3-(3-fluoro-benzensulfonil)-kinolin, 4-(4-kloro-fenil)-8-fluoro-3-(3-fluoro-benzensulfonil)-kinolin, 8-fluoro-3-(3-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 8-fluoro-3-(3-fluoro-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 8-fluoro-3-(3-fluoro-benzensulfonil)-4-(3-metoksi-fenil)-kinolin, 8-fluoro-3-(3-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-6-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-6-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-6-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-6-fluoro-3-(3-metoksi-benzensulfonil)-kinolin, 6-fluoro-4-(4-fluoro-fenil)-3-(3-metoksi-benzensulfonil)-kinolin, 3-(3-kloro-4-metoksi-benzensulfonil)-6-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3-kloro-4-metoksi-benzensulfonil)-6-fluoro-4-(3-metoksi-fenil)-kinolin, 4-(4-kloro-fenil)-7-fluoro-3-(4-fluoro-benzensulfonil)-kinolin, 3-(3,4-dimetil-benzensulfonil)-7-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3-kloro-4-metoksi-benzensulfonil)-4-(4-kloro-fenil)-6-fluoro-kinolin, 3-(3-kloro-4-metoksi-benzensulfonil)-6-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-7-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-7-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-7-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-kinolin, 7-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 7-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-7-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-7-fluoro-4-(3-metoksi-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-benzensulfonil)-7-fluoro-kinolin, 3-(3-cijano-benzensulfonil)-7-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-7-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3-kloro-4-metil-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-7-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-7-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-7-fluoro-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-7-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-8-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-8-fluoro-4-(3-metoksi-fenil)-kinolin, 4-(3-kloro-fenil)-8-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-kinolin, 4-(4-kloro-fenil)-8-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-kinolin, 8-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 8-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 8-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(3-metoksi-fenil)-kinolin, 8-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3,5-difluoro-benzensulfonil)-8-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3,5-difluoro-benzensulfonil)-8-fluoro-kinolin, 3-(3,5-difluoro-benzensulfonil)-8-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-8-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3,5-difluoro-benzensulfonil)-8-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-3-(3,4-difluoro-benzensulfonil)-8-fluoro-kinolin, 3-(3,4-difluoro-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-8-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-8-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-6-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-6-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-6-fluoro-4-(3-metoksi-fenil)-kinolin, 4-(3-kloro-fenil)-6-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-kinolin, 6-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 6-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 6-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(3-metoksi-fenil)-kinolin, 6-fluoro-3-(3-fluoro-4-metil-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-benzensulfonil)-6-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3-cijano-benzensulfonil)-6-fluoro-kinolin, 3-(3-cijano-benzensulfonil)-6-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3-kloro-4-metil-benzensulfonil)-4-(3-kloro-fenil)-6-fluoro-kinolin, 3-(3-kloro-4-metil-benzensulfonil)-4-(4-kloro-fenil)-6-fluoro-kinolin, 3-(3-kloro-4-metil-benzensulfonil)-6-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-kloro-4-metil-benzensulfonil)-6-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3-kloro-4-metil-benzensulfonil)-6-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-6-fluoro-3-(3-metoksi-benzensulfonil)-kinolin, 6-fluoro-3-(3-metoksi-benzensulfonil)-4-(3-metoksi-fenil)-kinolin, 3-(3,4-dimetil-benzensulfonil)-6-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,4-dimetil-benzensulfonil)-6-fluoro-4-(4-metoksi-fenil)-kinolin, 3-(3,4-dimetil-benzensulfonil)-6-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-6-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-6-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-6-fluoro-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-6-fluoro-4-(3-metoksi-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-6-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-7-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-7-fluoro-kinolin, 4-(3-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-8-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3, 5-dikloro-benzensulfonil)-8-fluoro-kinolin, 4-(3-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-6-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-6-fluoro-kinolin, 6-fluoro-3-(4-metoksi-benzensulfonil)-4-(4-metoksi-fenil)-kinolin, 7-kloro-4-(4-kloro-fenil)-3-(3,5-difluoro-benzensulfonil)-kinolin, 7-kloro-4-(4-kloro-fenil)-3-(3,4-difluoro-benzensulfonil)-kinolin, 7-kloro-4-(4-kloro-fenil)-3-(3-cijano-benzensulfonil)-kinolin, 7-kloro-3-(3,5-dikloro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(4-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3,4-difluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, i 7-kloro-3-(3-cijano-5-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 6-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-7-fluoro-kinolin, 6-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-7-cijano-4-(2-fluoro-fenil)-kinolin, 7-kloro-3-(3,4-difluoro-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-8-fluoro-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 7-kloro-4-(4-kloro-fenil)-3-(3,4-difluoro-benzensulfonil)-8-fluoro-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-8-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3-cijano-4-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-5-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-8-fluoro-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-8-fluoro-4-(2-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-4-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-8-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-8-fluoro-4-(2-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-8-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-4-fluoro-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-4-fluoro-benzensulfonil)-kinolin, 3-(3-cijano-5-fluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3-cijano-4-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-4-(3,4-difluoro-fenil)-8-fluoro-kinolin, 7-kloro-3-(3-cijano-5-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 3-(3-cijano-benzensulfonil)-8-fluoro-4-(4-fluoro-fenil)-kinolin, 3-(3,5-dikloro-benzensulfonil)-8-fluoro-4-(2-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-7-fluoro-4-(2-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-3-(3-cijano-benzensulfonil)-8-fluoro-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-S-fluoro-benzensulfonil)-kinolin, 7-kloro-3-(3-cijano-benzensulfonil)-4-(2-fluoro-fenil)-kinolin, 3-(3-cijano-5-fluoro-benzensulfonil)-7-fluoro-4-(3-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(3-kloro-fenil)-8-fluoro-kinolin, 3-(3-cijano-benzensulfonil)-7-fluoro-4-(2-fluoro-fenil)-kinolin, 3-(3-cijano-5-fluoro-benzensulfonil)-4-(3,4-difluoro-fenil)-7-fluoro-kinolin, 3-(3-cijano-4-fluoro-benzensulfonil)-4-(3,4-dikloro-fenil)-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(2-fluoro-fenil)-kinolin, 7-kloro-3-(3-cijano-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-4-fluoro-benzensulfonil)-7-fluoro-kinolin, 3-(3,4-difluoro-benzensulfonil)-4-(3,5-difluoro-fenil)-8-fluoro-kinolin, 3-(3,4-difluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-4-(3,4-difluoro-fenil)-8-fluoro-kinolin, 3-(3,5-dikloro-benzensulfonil)-4-(3,4-difluoro-fenil)-7-fluoro-kinolin, 3-(3,4-difluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 7-kloro-3-(3-cijano-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-kloro-4-(3-kloro-fenil)-3-(3-cijano-4-fluoro-benzensulfonil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-8-fluoro-4-(2-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-5-fluoro-benzensulfonil)-7-fluoro-kinolin, 3-(3-cijano-benzensulfonil)-4-(3,5-difluoro-fenil)-7-fluoro-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-benzensulfonil)-8-fluoro-kinolin, 4-(4-kloro-fenil)-3-(3,4-difluoro-benzensulfonil)-7-fluoro-kinolin, 7-kloro-3-(3,4-dikloro-benzensulfonil)-4-(3,4-difluoro-fenil)-kinolin, 3-(3,5-dicijano-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3-kloro-5-fluoro-benzensulfonil)-4-(3-kloro-fenil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-4-(3,4-difluoro-fenil)-7-fluoro-kinolin, 7-kloro-4-(3-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-8-fluoro-kinolin, 7-kloro-4-(3-kloro-fenil)-3-(3-cijano-benzensulfonil)-8-fluoro-kinolin, 7-kloro-4-(3-kloro-fenil)-3-(3-cijano-benzensulfonil)-kinolin, 7-kloro-3-(3,5-dikloro-benzensulfonil)-4-(2-fluoro-fenil)-kinolin, 3-(3,5-dicijano-benzensulfonil)-4-(3,4-difluoro-fenil)-7-fluoro-kinolin, 3-(3,5-dikloro-benzensulfonil)-7-fluoro-4-(2-fluoro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(3-kloro-fenil)-7-fluoro-kinolin, 4-(3-kloro-fenil)-3-(3,4-difluoro-benzensulfonil)-8-fluoro-kinolin, 4-(3,4-dikloro-fenil)-3-(3,4-difluoro-benzensulfonil)-kinolin, 3-(3,4-difluoro-benzensulfonil)-7-fluoro-4-(2-fluoro-fenil)-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(3,5-difluoro-fenil)-kinolin, 7-kloro-4-(3-kloro-fenil)-3-(3,5-dikloro-benzensulfonil)-kinolin, 7-amino-3-(3,4-difluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, 4-(3-kloro-fenil)-3-(3-cijano-benzensulfonil)-kinolin, 3-(3-cijano-5-fluoro-benzensulfonil)-4-(3,4-difluoro-fenil)-kinolin, 3-(3-cijano-S-fluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 4-(4-kloro-fenil)-3-(3-cijano-5-fluoro-benzensulfonil)-7-fluoro-kinolin, 7-kloro-3-(3-kloro-5-fluoro-benzensulfonil)-4-(4-kloro-fenil)-kinolin, 7-kloro-3-(3-kloro-5-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 3-(3-kloro-5-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 3-(3-kloro-5-fluoro-benzensulfonil)-4-(4-kloro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-7-fluoro-kinolin, 3-(3-kloro-4-fluoro-benzensulfonil)-7-fluoro-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-kloro-3-(3-kloro-4-fluoro-benzensulfonil)-4-(4-kloro-fenil)-kinolin, 7-amino-3-(3-kloro-5-fluoro-benzensulfonil)-4-(4-fluoro-fenil)-kinolin, 7-amino-3-(3-kloro-5-fluoro-benzensulfonil)-4-(3-fluoro-fenil)-kinolin, i/ili njegove soli i/ili njegovi hidrati i/ili solvati.
3. Postupak pripravljanja spoja formule (I): [image] gdje su Ar1, Ar2, R1, R2, R3 i R4određeni u zahtjevu 1, i/ili njegovih soli i/ili hidrata i/ili solvata, naznačen time, da obuhvaća sljedeće korake: a. a1. reakcija spoja formule (II): [image] gdje su R1, R2, R3 i R4 određeni kao gore za spoj formule (I), sa spojem formule (III): Ar1-S-M+(III) gdje je Ar1određen kao gore za spojeve formule (I), M je odabran od alkalijskih metala ili zemno-alkalijskih metala, kako bi se dobio spoj formule (IV): [image] gdje su Ar1, R1, R2, R3 i R4određeni kao gore za spojeve formule (I), nakon toga oksidiranje spoja formule (IV) za dobivanje spoja formule (V): [image] gdje su Ar1, R1, R2, R3 i R4 određeni kao gore za spojeve formule (I), nakon toga oksidiranje spoja formule (V) za dobivanje spoja formule (VI): [image] gdje su Ar1, R1, R2, R3 i R4 određeni kao gore za spojeve formule (I), ili a2. reakcija spoja formule (IX): Ar1-SO2Na (IX) gdje je Ar1 određen kao gore za spojeve formule (I), s esterima α-halogen-octene kiseline formule (X): Hlg-CH2-COOR5(X) gdje Hlg je halogen, a R5 je etil- ili metil-skupina, za dobivanje spoja formule (XI): Ar1-SO2-CH2-COOR5(XI) gdje Ar1 je određen kao gore za spoj formule (I), a R5je određen kao gore za spojeve formule (X), nakon toga reakcija spoja formule (XI) s trialkil ortoformiatom formule (XII): CH(OR6)3(XII) gdje R6 je etil- ili metil-skupina, za dobivanje spoja formule (XIII): [image] gdje Ar1 je određen kao gore za spoj formule (I), R5je određen kao gore za spojeve formule (X), a R6je određen kao gore za spojeve formule (XII), nakon toga reakcija spoja formule (XIII) s derivatom anilina formule (XIV): [image] gdje su R1, R2, R3 i R4 određeni kao gore za spoj formule (I), za dobivanje spoja formule (VI): [image] gdje su Ar1, R1, R2, R3 i R4 određeni kao gore za spoj formule (I), nakon toga pretvaranje spoja formule (VI) u spoj formule (VII): [image] gdje su Ar1, R1, R2, R3 i R4 određeni kao gore za spojeve formule (I), X je odabran od sljedećih skupina: kloro, bromo, benzensulfoniloksi, 4-fluoro-benzensulfoniloksi, 4-metil-benzensulfoniloksi, metansulfoniloksi ili trifluorometansulfoniloksi, nakon toga reakcija dobivenog spoja formule (VII) s derivatom borne kiseline formule (VIII): Ar2-B(OH)2(VIII) gdje je Ar2 određen kao gore za spoj formule (I), u prisutnosti baze i katalizatora u otapalu, te nakon toga opcijski tvorba soli i/ili hidrata i/ili solvata spojeva formule (I), ili b. pretvaranje spoja formule formule (I), gdje su Ar1, Ar2, R1, R2, R3 i R4 određeni gore za spoj formule (I), u različite spojeve formule (I), gdje su Ar1, Ar2, R1, R2, R3 i R4određeni gore za spoj formule (I), te nakon toga opcijski tvorba soli i/ili hidrata i/ili solvata spojeva formule (I).
4. Farmaceutska formulacija, naznačena time, da sadrži terapeutski učinkovitu količnu spoja formule (I) određenog u zahtjevu 1, i/ili njegovih fiziološki prihvatljivih soli i/ili hidrata i/ili solvata u sastavu s jednim ili više fiziološki prihvatljivih razrjeđivača, pomoćnih sredstava i/ili inertnih nosača.
5. Farmaceutska formulacija prema zahtjevu 4, naznačena time, da se upotrebljava u postupku prevencije i/ili liječenja poremećaja odabranog od sljedećih: psihijatrijski poremećaji, neurološki poremećaji, kronični i akutni bolovi, neuromuskularna disfunkcija donjeg urinarnog trakta, gastrointestinalna refluksna bolest, sindrom osjetljivog mjehura, zlouporaba loših tvari i odvikavanje od uzimanja loših tvari.
6. Spoj formule (I) prema zahtjevima 1 ili 2 i/ili njegove fiziološki prihvatljive soli i/ili hidrati i/ili solvati, naznačen time, da se upotrebljava u postupku prevencije i/ili liječenja poremećaja odabranog od sljedećih: psihijatrijski poremećaji, neurološki poremećaji, kronični i akutni bolovi, neuromuskularna disfunkcija donjeg urinarnog trakta, gastrointestinalna refluksna bolest, sindrom osjetljivih crijeva, zlouporaba loših tvari i odvikavanje od uzimanja loših tvari.
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CU20090219A7 (es) 2011-10-14
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