DK1551793T3 - Tetrafluorbenzylderivater og farmaceutisk sammensætning indeholdende disse til forebyggelse og behandling af akutte og kroniske neurodegenerative sygdomme i centralnervesystemet - Google Patents

Tetrafluorbenzylderivater og farmaceutisk sammensætning indeholdende disse til forebyggelse og behandling af akutte og kroniske neurodegenerative sygdomme i centralnervesystemet Download PDF

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DK1551793T3
DK1551793T3 DK03738707.3T DK03738707T DK1551793T3 DK 1551793 T3 DK1551793 T3 DK 1551793T3 DK 03738707 T DK03738707 T DK 03738707T DK 1551793 T3 DK1551793 T3 DK 1551793T3
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tetrafluoro
hydroxy
pharmaceutically acceptable
acceptable salt
salt according
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Byoung Joo Gwag
Sung Hwa Yoon
Ho Sang Moon
Eun Chan Park
Seok Joon Won
Young Ae Lee
Hae Un Lee
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Gnt Pharma Co Ltd
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    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
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    • C07C229/64—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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Claims (25)

1. Tetrafluorbenzylderivat repræsenteret ved følgende kemiske formel 1: Formel 1
hvor Ri, R2 og R3 er hydrogen eller halogen, R4 er hydroxy, alkyl, alkoxy, halogen, alkoxy substitueret med halogen, alkanoyloxy eller nitro, og R5 er carboxylsyre, carboxylsyreester substitueret med Ci-C4-alkyl, carboxyamid, sulfonsyre, halogen eller nitro; eller et farmaceutisk acceptabelt salt deraf.
2. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor Ri, R2 og R3 er halogen.
3. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1 eller 2, hvor Rlf R2 og R3 er F.
4. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor R4 er hydroxy, alkyl, alkoxy eller halogen.
5. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor R4 er hydroxy eller alkanoyloxy.
6. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor R4 er hydroxy.
7. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor R5 er carboxyl, carboxyamid, sulfonsyre eller halogen.
8. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor R5 er carboxyl.
9. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 1, hvor tetrafluorbenzylderivatet er 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 2-nitro-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 2-chlor-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 2-brom-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 2-hydroxy-5-(2,3,5,6-tetrafluor-4-methyl-benzylamino)-benzoesyTe, 2-methyl-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 2-methoxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-2-trifluormethoxy-benzoesyre, 2-nitro-4-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-phenol, 2-chlor-4-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-phenol, 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzamid, 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzensulfonsyre, methyl- 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoat, 2-ethanoyloxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, 2-propanoyloxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre, eller 2-cy clohexan-carbonyloxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzoesyre.
10. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 9, hvor tetrafluorbenzylderivatet er 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)benzoesyre.
11. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 9, hvor tetrafluorbenzylderivatet er 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)benzensulfonsyre.
12. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 9, hvor tetrafluorbenzylderivatet er 2-hydroxy-5-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)-benzamid.
13. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge krav 9, hvor tetrafluorbenzylderivatet er 2-chlor-4-(2,3,5,6-tetrafluor-4-trifluormethyl-benzylamino)phenol.
14. Farmaceutisk sammensætning omfattende et tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel.
15. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af epilepsi.
16. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af slagtilfælde.
17. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af traumatisk hjerneskade, traumatisk rygmarvsskade eller hydrocefali.
18. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af grøn stær, retinopati eller maculadegeneration.
19. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af stofafhængighed.
20. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af depression.
21. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af smerte.
22. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af encephalitis, meningitis, og/eller dissemineret sklerose.
23. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af neurodegenerative sygdomme udvalgt fra gruppen bestående af amyotrof lateral sklerose, Parkinsons sygdom, Huntingtons sygdom, Alzheimers sygdom og kombinationer deraf.
24. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af tromboemboli.
25. Tetrafluorbenzylderivat eller dets farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1 til 13 som virksom bestanddel til anvendelse i behandling og forebyggelse af hjertestop.
DK03738707.3T 2002-06-19 2003-06-19 Tetrafluorbenzylderivater og farmaceutisk sammensætning indeholdende disse til forebyggelse og behandling af akutte og kroniske neurodegenerative sygdomme i centralnervesystemet DK1551793T3 (da)

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KR20020034259 2002-06-19
PCT/KR2003/001205 WO2004000786A1 (en) 2002-06-19 2003-06-19 Tetrafluorobenzyl derivatives and pharmaceutical composition for preventing and treating acute and chronic neurodegenerative diseases in central nervous system containing the same

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EP (1) EP1551793B1 (da)
JP (1) JP4113957B2 (da)
KR (2) KR100545745B1 (da)
CN (2) CN1309703C (da)
AU (1) AU2003245070C1 (da)
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DK (1) DK1551793T3 (da)
ES (1) ES2568491T3 (da)
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