DK2178870T3 - Indole og indazole forbindelser som en inhibitor af cellulær nekrose - Google Patents

Indole og indazole forbindelser som en inhibitor af cellulær nekrose Download PDF

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DK2178870T3
DK2178870T3 DK08793298.4T DK08793298T DK2178870T3 DK 2178870 T3 DK2178870 T3 DK 2178870T3 DK 08793298 T DK08793298 T DK 08793298T DK 2178870 T3 DK2178870 T3 DK 2178870T3
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Prior art keywords
indol
phenyl
chloro
amine
methyl
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DK08793298.4T
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English (en)
Inventor
Soon Ha Kim
Hyoung Jin Kim
Sun Young Koo
Chul Woong Chung
Sung Bae Lee
Heui Sul Park
Seung Hyun Yoon
Hyo Shin Kwak
Dong Ook Seo
Eok Park
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Lg Chemical Ltd
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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Claims (39)

1. Indole forbindelser af følgende formel (1):
hvor n betegner et tal fra 1 til 3, m er 1, A repræsenterer phenyl, X repræsenterer C, R1 repræsenterer hydrogen, alkyl, -(CH2)rNR7R8 eller -(CH2)rC02H, hvor r betegner et tal fra 1 til 5, og R7 og R8 uafhængigt af hinanden repræsenterer hydrogen, alkyl eller alkylcarbonyl, eller kan sammen eventuelt danne en alkyl-erstattet alkylenkæde, hvor eventuelt en methylen erstattes af N-atom, R2 repræsenterer hydrogen, halogen, cyano, nitro, alkyl, alkoxy eller trialkylsilyl, repræsenterer -(CH2)PC02R7, -(CH2)pOR7, -(CH2)PNR7R8, -NHR10, -N(H)S(0)2R7, -NHC(0)R10, -(CH2)pS(0)2R7 eller (CH2)p-heterocyklus-R10, hvor p betegner et tal fra 0 til 3, heterocyklussen har 3-10 medlemmer og har 1-3 heteroatomer valgt blandt N, O og S, R7 og R8 er som defineret ovenfor, R10 repræsenterer hydrogen, oxo, alkylsulfonyl, alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl, alkoxy, alkyl eller heterocyklus med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O og S, R3 repræsenterer hydrogen, cyano, halogen, alkyl eller phenyl, eller repræsenterer -(CH2)n-heterocyclus eller -(CH2)n-aryl, hvor n betegner et tal fra 0 til 3, og heterocyklussen har 3-10 medlemmer og har 1 til 3 heteroatomer valgt blandt N, O og S, R4 repræsenterer -YR11, hvor Y repræsenterer en direkte binding eller -(CR7R8)pY’-, hvor p betegner et tal fra 0 til 3, R7 og R8 er som defineret ovenfor, Y’ er valgt blandt gruppen bestående af -O-, -S-, -NR12-, -NR12C(0)-, -C(O)-, -C(0)0-, - C(0)NR12-, -S(0)q- og -S(0)qNR12-, hvor R12 repræsenterer hydrogen, alkyl, aryl eller heteroaryl med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O og S, q betegner et tal fra 0 til 2, R11 er valgt blandt gruppen bestående af hydrogen, cyano, halogen, hydroxy, thiol, carboxy, alkyl og -(CH2)tB-R13, hvor t betegner et tal fra 0 til 3, B repræsenterer heterocyklus med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O og S, heteroaryl med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O og S eller aryl, R13 repræsenterer hydrogen, cyano, halogen, hydroxy, oxo, thiol, carboxy, carboxyalkyl, alkylcarbonyloxy, alkyl, alkoxy, alkylthio, alkylcarbonyl eller alkylsulfonyl, R5 repræsenterer hydrogen, alkyl, cycloalkyl, heterocyklus eller heterocyclylalkyl, hvor heterocyklussen har 3-10 medlemmer og har 1 til 3 heteroatomer valgt blandt N, O og S, R6 repræsenterer -(CR7R8)P-Z-D-W-R14, hvor Z repræsenterer en direkte binding, eller er valgt blandt gruppen bestående af -C(O)-, -C(0)0-, -C(0)NR12- og -S(0)y-, y betegner et tal fra 1 til 2, D repræsenterer en direkte binding, eller repræsenterer cycloalkyl, heteroaryl med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O og S, eller heterocyklus med 3-10 med 1 til 3 heteroatomer valgt blandt N, O og S, W repræsenterer en direkte binding, eller repræsenterer -NR7-, -C(O)-, -C(0)0-, -C(0)NR12-, -S(0)y-, - S(0)yNR12- eller -NR12S(0)y-, hvor R14 repræsenterer hydrogen, hydroxy, alkyl, alkoxy, heterocyklus med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O, heteroaryl med 3-10 medlemmer med 1 til 3 heteroatomer valgt blandt N, O og S, aryl eller aralkyl, R5 og R6 sammen repræsenterer alkylenkæde, hvor alkyl, alkoxy, aryl, cycloalkyl, heterocyklus og heteroaryl eventuelt kan erstattes, og erstatningerne er en eller flere valgt blandt gruppen bestående af hydroxy, halogen, nitril, amino, alkylamino, dialkylamino, carboxy, alkyl, alkoxy, carboxyalkyl, alkylcarbonyloxy, alkylthio, alkyloxycarbonyl, alkylaminocarbonyl, arylalkoxy og oxo og farmaceutisk acceptable salte eller optiske isomere deraf, forudsat at, forbindelsen af formlen (1) ikke er 2-phenyl-7-aminoindol.
2. Forbindelserne ifølge krav 1, hvor n betegner et tal fra 1 til 3, m er 1, A repræsenterer phenyl, X repræsenterer C, R1 repræsenterer hydrogen, Ci-C6-alkyl eller -(CH2)rNR7R8, hvor r betegner et tal fra 2 til 3, og R7 og R8 uafhængigt af hinanden repræsenterer hydrogen eller Ci- C3-alkyl, eller sammen kan danne C2-C6-alkylenkæde, som eventuelt erstattes af Ci-C6-alkyl og en methylen eventuelt erstattes af N-atom, R2 repræsenterer hydrogen, halogen, Ci-C6-alkyl, -(CtypCChR7, -(CH2)pOR7, -(CH2)pNR7R8, -NHR10, -N(H)S(0)2R7, -NHC(0)R10, -(CH2)pS(0)2R7 eller -(CH2)P-heterocyklus-R10, p betegner et tal fra O til 3, R10 repræsenterer hydrogen, oxo, Ci-C6-alkylsulfonyl, Ci-C6-alkylcarbonyl, Ci-C6-alkyloxycarbonyl, Ci-C6-alkylaminocarbonyl, Ci-C6-alkoxy, Ci-C6-alkyl eller hydroxy-Ci-C6-alkyl, eller repræsenterer heterocyklus med 5~6 medlemmer som har 1 eller 2 nitrogenatomer som heteroatom, og eventuelt erstattes af Ci-C3-alkyl, R3 repræsenterer hydrogen, halogen eller Ci-C6-alkyl, repræsenterer phenyl eventuelt erstattet af Ci-C6-alkoxy, eller repræsenterer heterocyclyl-Ci-Cs-alkyl, hvor heterocyklussen har 5~6 medlemmer, har 1 eller 2 heteroatomer valgt blandt N og O, og erstattes eventuelt af 1 eller 2 oxogrupper, R4 repræsenterer -YR11, hvor Y repræsenterer en direkte binding eller -(CR7R8)PY’-, hvor Y’ er valgt blandt gruppen bestående af -O-, -C(O)-, -C(0)0-, -NHC(O)-, - NR12-, -C(0)NR12-, -S(0)q- og -S(0)qNR12-, R12 repræsenterer hydrogen eller Ci-C3-alkyl, q betegner et tal fra 0 til 2, R11 er valgt blandt gruppen bestående af hydrogen, halogen, hydroxy, thiol, carboxy, Ci-C6-alkyl, hydroxy-Ci-C6-alkyl og -(CH2)tB-R13, t betegner et tal fra 0 til 3, B repræsenterer C6-Cio-aryl, repræsenterer heterocyklus med 5~6 medlemmer med 1 eller 2 heteroatomer valgt blandt N, O og S, eller repræsenterer heteroaryl med 5~6 medlemmer med 1 eller 2 N-atomer, R13 repræsenterer hydrogen, halogen, hydroxy, oxo, thiol, carboxy, carboxy-Ci-C6-alkyl, Ci-Ce-alkylcarbonyloxy, Ci-C6-alkyl, C1-C6- alkoxy, Ci-Ce-alkylthio, Ci-C6-halogenoalkyl, Ci-Ce-alkylcarbonyl eller C1-C6- alkylsulfonyl, R5 repræsenterer hydrogen, Ci-Ce-alkyl, C3-C6-cycloalkyl, heterocyklus eller heterocyclyl-Ci-Ce-alkyl, hvor heterocyklussen er en ring med 3-8 medlemmer, som har 1 til 3 heteroatomer valgt blandt N og O, og erstattes eventuelt af 1 eller 2 oxogrupper, R6 repræsenterer -(CR7R8)P-Z-D-W-R14, Z repræsenterer en direkte binding, eller er valgt blandt gruppen bestående af -C(O)-, -C(0)0-, -C(0)NR12- og -S(0)y-, hvor y betegner et tal fra 1 til 2, D repræsenterer C4-C6-cycloalkyl, eller repræsenterer heterocyklus med 5-6 medlemmer, som har 1 eller 2 heteroatomer valgt blandt N, O og S, og eventuelt indeholder en oxogruppe, W repræsenterer en direkte binding, eller repræsenterer -NR7-. -C(O)-, -C(0)0-, -C(0)NR12-, -S(0)y-, -S(0)yNR12- eller -NR12S(0)y-, R14 repræsenterer hydrogen, hydroxy, Ci-C6-alkyl, hydroxy-Ci-C6-alkyl, carboxy-Ci-C6-alkyl, C6-Cio-aryl eller C6-Cio-ar-Ci-C6-alkyl, repræsenterer heterocyklus med 5-6 medlemmer, som har 1 til 3 heteroatomer valgt blandt N, O og S, og erstattes eventuelt af 1 eller 2 oxogrupper, eller repræsenterer heteroaryl med 5-6 medlemmer, som har 1 til 3 heteroatomer valgt blandt N, O og S, og erstattes eventuelt af Ci-C6-alkyl, eller R5 og R6 sammen repræsenterer C2-C6-alkylenkæde.
3. Forbindelserne ifølge krav 2, hvor R1 repræsenterer hydrogen, Ci-C6-alkyl eller di(Ci-C3-alkyl)amino-C2-C3-alkyl.
4. Forbindelserne ifølge krav 3, hvor R1 repræsenterer hydrogen, methyl eller (dimethylamino)ethyl.
5. Forbindelserne ifølge krav 2, hvor R2 repræsenterer hydrogen, amino, halogen, Ci-C3-alkyl, carboxy, carboxy-Ci-C3-alkyl, Ci-C3-alkoxycarbonyl, C1-C3-alkoxycarbonyl-Ci-C3-alkyl, hydroxy-Ci-C3-alkyl, Ci-C3-alkoxy, -(CH2)PNR7R8, -NHR10, -N(H)S(0)2R7, -NHC(0)R10 eller -(CH2)P-heterocyklus-R10, hvor p, R7, R8 og R10 er defineret som i krav 2.
6. Forbindelserne ifølge krav 5, hvor R2 er valgt blandt gruppen af hydrogen, methyl, methoxy, fluoro, -NH2, -NHAc, -NHSChMe, -NHBOC, -NH(l-methyl-piperidin), l-oxo-2-hydroxy-ethyl, dimethylaminomethyl, hydroxymethyl, hydroxyethyl, carboxy, carboxymethyl, carboxyethyl, -CFh-(2-oxo)piperazin, -CFk-piperazin, -CH2-morpholin, -CH2-[l,l-dioxo-thiomorpholin-4- yl] og -CFh-[4-acetyl-piperazin-l-yl].
7. Forbindelserne ifølge krav 2, hvor R3 repræsenterer hydrogen, methyl eller bromo, repræsenterer phenyl eventuelt erstattet af Ci-C3-alkoxy, eller repræsenterer heterocyclyl-Ci-C3-alkyl, hvor heterocyklussen har 5~6 medlemmer, har 1 eller 2 heteroatomer valgt blandt N og O, og erstattes eventuelt af 1 eller 2 oxogrupper.
8. Forbindelserne ifølge krav 7, hvor R3 er valgt blandt gruppen bestående af hydrogen, methyl, bromo, phenyl, 4-MeO-phenyl, -CH2-(2-oxo-piperazin- 4-yl) og -CFb-(morpholin-4-yl).
9. Forbindelserne ifølge krav 2, hvor Y er valgt blandt gruppen bestående af en direkte binding, -O-, -C(O)-, -NH-, -CONH-, -SO2NH-, -NHC(O)-, -CH2CONH-, - CH2C(0)- og -CH2SO2-.
10. Forbindelserne ifølge krav 9, hvor Y er valgt blandt gruppen bestående af en direkte binding, -O-, -C(O)-, -CH2C(0)- og -NHC(O)-.
11. Forbindelserne ifølge krav 2, hvor R11 er valgt blandt gruppen bestående af hydrogen, halogen, hydroxy, Ci-Ce-alkyl og -(CFhltB-R13, hvor t, B og R13 er som defineret i krav 2.
12. Forbindelserne ifølge krav 11, hvor R11 er valgt blandt gruppen bestående af hydrogen, methyl, ethyl, phenyl, fluoro, chloro, hydroxy, 2-carboxy- pyrrolidin-l-yl, pyrrolidin-l-yl, 4-eddikesyre-1,3-thiazolin-2-yl, -CH2-(l,l-dioxo- thiomorpholin-4-yl) og -CH2-(2-oxopiperazin-4-yl).
13. Forbindelserne ifølge krav 2, hvor R5 repræsenterer hydrogen, Ci-C6-alkyl, C3-C6-cycloalk;yl, heterocyklus eller heterocyclyl-Ci-C6-alkyl, hvor heterocyklussen er en ring med 5~6 medlemmer, som har 1 til 2 heteroatomer valgt blandt N og O, og erstattes eventuelt af 1 eller 2 oxogrupper.
14. Forbindelserne ifølge krav 13, hvor R5 er valgt blandt gruppen bestående af hydrogen, methyl, cyclopentyl, tetrahydropyran-4-yl og CH2- (tetrahydropyran-4-yl).
15. Forbindelserne ifølge krav 2, hvor Z repræsenterer en direkte binding, eller repræsenterer -C(O)-, -C(0)0-, -C(0)NH- eller -S(0)2-.
16. Forbindelserne ifølge krav 2, hvor D er valgt blandt gruppen bestående af cyclopentyl, cyclohexyl, pyrrolidin, tetrahydropyran, tetrahydrofuran og piperidin.
17. Forbindelserne ifølge krav 2, hvor W repræsenterer en direkte binding, eller repræsenterer -SO2-, -CO-, -C(0)0- eller -CONR12-, hvor R12 er som defineret i krav 2.
18. Forbindelserne ifølge krav 17, hvor W er valgt blandt gruppen bestående af -SO2-, -CO-, -C(0)0-, -CON(Me)- og -CONH-.
19. Forbindelserne ifølge krav 2, hvor R14 repræsenterer hydrogen, hydroxy, Ci-C6-alkyl, hydroxy-Ci-C6-alkyl, C6-Cio-aryl eller C6-Cio-ar-Ci-C3-alkyl, repræsenterer heterocyklus med 5~6 medlemmer, som har O eller S, og erstattes eventuelt af 1 eller 2 oxogrupper, eller repræsenterer heteroaryl med 5~6 medlemmer, som har 1 til 2 heteroatomer valgt blandt N, O og S, og erstattes eventuelt af Ci-C3-alkyl.
20. Forbindelserne ifølge krav 19, hvor R14 er valgt blandt gruppen bestående af hydrogen, hydroxy, methyl, ethyl, isobutyl, hydroxymethyl, hydroxyethyl, phenyl, benzyl, thiophen, tetrahydrofuran, tetrahydropyran, 1,1-dioxo-tetrahydro- thiopyran, furan, pyridin og 5 -methyl-pyridin.
21. Forbindelserne ifølge krav 2, hvor R5 og R6 sammen med N-atomet, som de er forbundet med, danner piperidin.
22. Forbindelserne ifølge krav 2, som er valgt blandt følgende: Cyclopentyl- [5-methyl-2-phenyl-1 H-indol-7-yl] -amin; 4- [(5-Chloro-2-phenyl-1 H-indol-7-yl)amino] -cyclohexan-1 -one; 7-(Cyclopentyl)amino-2-phenyl-lH-indole-5-carbonsyre ethyl ester; Cyclopentyl- [5-hydroxymethyl-2-phenyl-1 H-indol-7-yl] -amin; 7 - (Cyclopentyl) amino -2-phenyl-1 H-indole- 5-carbonsyre; 2-[7-(Cyclopentyl)amino-2-phenyl- lH-indol-5-yl]-eddikesyre ethyl ester; 2- [7 - (Cyclopentylamino) -2-phenyl-1 H-indol-5- yl] ethanol; 2- [7 - (Cyclopentyl)amino-2-phenyl-1 H-indol-5-yl] eddikesyre; 2-[2-Phenyl-7-(tetrahydropyran-4-yl)amino-lH-indol-5-yl]-eddikesyre; 2-[2-Phenyl-7-(l,l-dioxo-tetrahydro-thiopyran-4-yl)amino-lH-indol-5-yl]- eddikesyre; (Tetrahydropyran-4-yl)-[2-phenyl-5-( 1,1 -dioxo-thiomorpholin-4-yl)methyl- lH-indol-7-yl]amin; (Tetrahydropyran-4-yl)-[2-phenyl-5-(2-oxo-piperazin-4-yl)methyl-lH-indol-7- yl]amin; Cyclopentyl-[2-(3-fluoro)phenyl-5-(2-oxo-piperazin-4-yl)methyl-lH-indol-7-yl]amin; (Tetrahydropyran-4-yl)-[2-(4-methoxy)phenyl-5-(l,l-dioxo-thiomorpholin-4-yl)methyl -lH-indol-7-yl] amin; Cyclopentyl-[3,5-dimethyl-2-phenyl-lH-indol-7-yl]-amin; (Tetrahydropyran-4-yl)-(5-methyl-2-phenyl-lH-indol-7-yl)-amin; Cyclopentylmethyl-(5-methyl-2-phenyl-lH-indol-7-yl)-amin; (Tetrahydropyran-4-ylmethyl)-(5-methyl-2-phenyl-lH-indol-7-yl)-amin; (l-Methylpiperidin-4-yl)-(5-methyl-2-phenyl-lH-indol-7-yl)-amin; 1- [-4-[(5-Methyl-2-phenyl-lH-indol-7-yl)amino]piperidin-l-yl]ethanone; Cyclopentyl- (5 -chloro -2-phenyl-1 H-indol-7 -yl) - amin; Cyclohexyl- (5 -chloro -2-phenyl-1 H-indol-7 -yl) - amin; (Tetrahydropyran-4-yl)-(5-chloro-2-phenyl-lH-indol-7-yl)-amin; Cyclopentylmethyl-(5-chloro-2-phenyl-lH-indol-7-yl)-amin; (Tetrahydropyran-4-ylmethyl)-(5-chloro-2-phenyl-lH-indol-7-yl)-amin; (l-Benzylpyrrolidin-3-yl)-(5-chloro-2-phenyl-lH-indol-7-yl)-amin; (l-Methylpiperidin-4-yl)-(5-chloro-2-phenyl-lH-indol-7-yl)-amin; (l,4-Dioxaspiro[4.5]decan-8-yl)-(5-chloro-2-phenyl-lH-indol-7-yl)-amin; 2- [(5-Chloro-2-phenyl-lH-indol-7-yl)amino]propan-l,3-diol; (Tetrahydropyran-4-yl)-(5-methyl-2-phenyl-lH-indol-7-yl)-methyl-amin; (Tetrahydropyran-4-ylmethyl)-[2-phenyl-5-( 1, l-dioxo-thiomorpholin-4-yl)methyl- lH-i ndol-7-yl]amin; Di(tetrahydropyran-4-ylmethyl)-[2-phenyl-5-(l,l-dioxo-thiomorpholin-4-yl)methyl-lH -indol-7-yl] amin; Di(tetrahydropyran-4-yl)-[2-phenyl-5-(l,l-dioxo-thiomorpholin-4-yl)methyl-lH-indol-7-yl] amin; (1 -Methyl-piperidinemethyl-4-yl)- [5-fluoro-2-phenyl-1 H-indol-7-yl] amin; 2-[4-[(5-Fluoro-2-phenyl-lH-indol-7-yl)amino]piperidin-l-yl]ethanol; [l-(Tetrahydropyran-4-yl)piperidin-4-yl]-(5-fluoro-2-phenyl-lH-indol-7- yl)amin; (Tetrahydropyran-4-yl)-(5-phenoxy-2-phenyl-lH-indol-7-yl)-amin; (Tetrahydropyran-4-ylmethyl)-[2-phenyl-5-(2-oxo-piperazin-4-yl)methyl-lH-indol-7-yl ]amin; (Tetrahydropyran-4-yl)-[5-chloro-l-(2-diethylaminoethyl)-2-phenyl-lH-indol-7-yl]ami n; Dimethyl-(5-chloro-1 -methyl-2-phenyl- lH-indol-7-yl)amin; (Tetrahydropyran-4-yl)-(5-chloro-l-methyl-2-phenyl-lH-indol-7-yl)- methylamin; Cyclopentyl-(5-chloro-3-(morpholin-4-yl)methyl-2-phenyl-lH-indol-7-yl)-amin; (Tetrahydropyran-4-yl)-(5-chloro-3-(morpholin-4-yl)methyl-2-phenyl-lH- indol-7-yl)-amin; (Tetrahydropyran-4-yl)-(5-chloro-3-(2-oxo-piperazin-4-yl)methyl-2-phenyl-lH-indol-7 -yl)-amin; Cyclopentyl-(5-chloro-3-(2-oxo-piperazin-4-yl)methyl-2-phenyl-lH-indol-7-yl)-amin; (Tetrahydropyran-4-ylmethyl)-(5-chloro-3-(2-oxo-piperazin-4-yl)methyl-2-phenyl-lH-i ndol-7-yl)-amin; (Tetrahydropyran-4-yl)-(3-bromo-5-(l,l-dioxo-thiomorpholin-4-yl)methyl-2-phenyl-l H-indol-7-yl)-amin; Cyclopentyl-(3-bromo-5-(l,l-dioxo-thiomorpholin-4-yl)methyl-2-phenyl-lH- indol-7-yl)-amin; (Tetrahydropyran-4-ylmethyl)-(3-bromo-5-(l,l-dioxo-thiomorpholin-4-yl)methyl-2-ph enyl-1 H-indol-7 - yl) -amin; (Tetrahydropyran-4-yl)-(5-( 1, l-dioxo-thiomorpholin-4-yl)methyl-2-(3-fluorophenyl)-1 H-indol-7-yl)-amin; (3-Methylbutyl) - [5- (1,1 -dioxo-thiomorpholin-4-yl)methyl-2- (4-methoxyphenyl)-1 H-in dol-7-yl]-amin; t-Butyl N- [4- [5-chloro-7- (cyclopentylamino)-1 H-indol-2-yl]phenyl] carbamat; Cyclopentyl-[2-(4-aminophenyl)-5-chloro-lH-indol-7-yl]-amin; Cyclopentyl- {5-chloro-2- [4- (1 -methyl-piperidin-4-yl)aminophenyl] -1 H-indol-7-yl} -am in; N-[4-(5-chloro-7-cyclopentylamino-lH-indol-2-yl)-phenyl]-methanesulfonamid; Cyclopentyl- {5-(1,1 -dioxo-thiomorpholin-4-yl)methyl-2- [4- (acetyl)aminophenyl] -1 H-i ndol-7-yl}-amin; Dicyclopentyl-{5-(l,l-dioxo-thiomorpholin-4-yl)-2-[4-(acetyl)aminophenyl]-lH-indol- 7-yl}-amin; (Tetrahydropyran-4-yl)methyl-{5-(l,l-dioxo-thiomorpholin-4-yl)-2-[4-(acetyl)aminoph enyl] -1 H-indol-7-yl} -amin; Di(tetrahydropyran-4-yl)methyl-{ 5-(1, l-dioxo-thiomorpholin-4-yl)-2-[4-(acetyl)amino phenyl] - lH-indol-7-yl} -amin; (Tetrahydropyran-4-yl)-{5-(l,l-dioxo-thiomorpholin-4-yl)-2-[4-(acetyl)aminophenyl]- lH-indol-7-yl}-amin; (5-Methyl-2-phenyl-lH-indol-7-yl)-piperidin-4-yl-amin; [l-(Methanesulfonyl)piperidin-4-yl]-(5-methyl-2-phenyl-lH-indol-7-yl)-amin;
2-Hydroxy-1 -[4-(5-methyl-2-phenyl- lH-indol-7-yl)amino-piperidin-1 -yl]- ethanon; (5-Chloro-2-phenyl-lH-indol-7-yl)-piperidin-4-yl-amin; 4-(5-Chloro-2-phenyl-lH-indol-7-yl)amino-piperidin-l-yl-carbonsyre phenylamid; 1 - [4- (5-Chloro-2-phenyl-1 H-indol-7-yl)amino-piperidin-1 -yl] -2-dimethylamino-ethano n; [5-(1,1 -Dioxo-thiomorpholin-4-yl)methyl-2-phenyl- lH-indol-7-yl] -(piperidin-4-yl)met hyl-amin; (5-(1,1 -Dioxo-thiomorpholin-4-yl)methyl-2-phenyl-1 H-indol-7-yl)- (1 -methanesulfonyl -piperidin-4- yl)- amin; {4- [5- (1,1 -Dioxo-thiomorpholin-4-yl)methyl-2-phenyl-1 H-indol-7-yl] amino-piperidin-1 -yl} -(tetrahydrofuran-2-yl)-methanon; (5-Fluoro-2-phenyl-lH-indol-7-yl)-[l-(l,l-dioxo-tetrahydrothiopyran-4-yl)-piperidin-4 -yl]-amin; N-(5-Chloro-2-phenyl-lH-indol-7-yl)-N’,N’-dimethyl-cyclohexane-l,4- diamin; N-(5-Chloro-2-phenyl-lH-indol-7-yl)-N’-methyl-cyclohexane-l,4-diamin; 4-(5-Chloro-2-phenyl-lH-indol-7-yl)amino-cyclohexane-l-carbonsyre; 4-(5-Methyl-2-phenyl-lH-indol-7-yl)amino-cyclohexane-l-carbonsyre; 4-(5-Chloro-2-phenyl-lH-indol-7-yl)amino-cyclohexane-l-carbonsyre amid; 4-(5-Chloro-2-phenyl-lH-indol-7-yl)amino-cyclohexanecarbonsyre methylamid; (2-(5-Fluoro-2-phenyl-lH-indol-7-yl)amino-eddikesyre methyl ester; 2-(5-Fluoro-2-phenyl-lH-indol-7-yl)amino-eddikesyre; 2-(5-Phenoxy-2-phenyl-lH-indol-7-yl)amino-eddikesyre methyl ester; 2-[(5-Phenoxy-2-phenyl-lH-indol-7-yl)amino]-eddikesyre; 2-[(5-Phenoxy-2-phenyl-lH-indol-7-yl)amino]-propionsyre methyl ester; 2-(5-Phenoxy-2-phenyl-lH-indol-7-yl)amino-propionsyre; 2-(5-Chloro-2-phenyl-lH-indol-7-yl)amino-propionsyre; (5-Chloro-2-phenyl-lH-indol-7-yl)-pyridin-2-yl-amin; (5-Chloro-2-phenyl-lH-indol-7-yl)-5-methyl-pyridin-2-yl-amin; (2S)-l-(7-cyclopentylamino-2-phenyl-lH-indole-5-carbonyl)-pyrrolidine-2-carbonsyre methyl ester; (2S)-l-(7-cyclopentylamino-2-phenyl-lH-indole-5-carbonyl)-pyrrolidine-2-carbonsyre; (2S)-l-[2-phenyl-7-(tetrahydropyran-4-yl)amino-lH-indole-5-carbonyl]-pyrrolidin-2-ca rbonsyre; 2- (7 -Cyclopentylamino -2-phenyl-1 H-indol- 5 - yl] -1 -pyrrolidin-1 - yl-ethanon; Cyclopentyl-[2-phenyl-5-(2-pyrrolidin-l-yl-ethyl)-lH-indol-7-yl]-amin; 2-[(R)-2-(7-cyclopentylamino-2-phenyl-lH-indol-5-yl)-4,5-dihydro-thiazol-4-yl]-eddikesyre; 2- [(R)-2-(2-phenyl-7-(tetrahydropyran-4-yl)methylamino-lH-indol-5-yl)-4,5-dihydro-t hiazol-4-yl] -eddikesyre; 3- (7-Cyclopentylamino-5-chloro-lH-indol-2-yl)-benzoesyre methyl ester; 3- (7-Cyclopentylamino-5-chloro-lH-indol-2-yl)-benzoesyre; [3-(5-Chloro-7-cyclopentylamino-lH-indol-2-yl)-phenyl]-methanol; {3-[5-Chloro-7-(tetrahydropyran-4-yl)amino-lH-indol-2-yl]-phenyl}-methanol; 2- {3 - [5 -Chloro-7- (tetrahydropyran-4- ylmethyl)amino-1 H-indol-2- yl] -phenyl} -eddikesy re; 2-[3-(5-Chloro-7-cyclopentylamino-l-H-indol-2-yl)-phenyl]-eddikesyre; 2-{3-[5-Chloro-7-(tetrahydropyran-4-yl)amino-lH-indol-2-yl]-phenyl}-eddikesyre; 2-{3-[5-Chloro-7-(tetrahydropyran-4-ylmethyl)amino-lH-indol-2-yl]-phenyl}-eddikesy re methyl ester; 2-[3-(5-Chloro-7-cyclopentylamino-lH-indol-2-yl)-phenyl]-eddikesyre methyl ester; 2-{3-[5-Chloro-7-(tetrahydropyran-4-yl)amino)-lH-indol-2-yl]-phenyl}-eddikesyre methyl ester; [2-(5-Chloro-7-cyclopentylamino-lH-indol-2-yl)-phenyl]-methanol; 2-(5-Chloro-7-cyclopentylamino-lH-indol-2-yl)-benzoesyre; 2-(5-Chloro-7-cyclopentylamino-1 H-indol-2-yl)-benzoesyre methyl ester; [4-(5-Chloro-7-cyclopentylamino-lH-indol-2-yl)-phenyl]-methanol; 2-{4-[5-Chloro-7-(tetrahydropyran-4-yl)amino-lH-indol-2-yl]phenyl}-ethanol; 4- (5-Chloro-7-cyclopentylamino-lH-indol-2-yl)-benzoesyre; 2- {4- [5-Chloro-7-(tetrahydropyran-4-ylmethyl)amino-1 H-indol-2-yl]phenyl} -eddikesyre; 2-[4-(5-Chloro-7-cyclopentylamino-lH-indol-2-yl)phenyl]-eddikesyre; 2- {4- [5-Chloro-7-(tetrahydropyran-4-yl)amino- lH-indol-2-yl]phenyl} -eddikesyre; 4-(5-Chloro-7-cyclopentylamino-1 H-indol-2-yl)benzoesyre methyl ester; 4-(7-Cyclopentylamino-5-methyl-1 H-indol-2-yl)benzoesyre methyl ester; 2- {4- [5-Chloro-7-(tetrahydropyran-4-ylmethyl)amino-1 H-indol-2-yl]phenyl} -eddikesyr e methyl ester; 2-[4-(5-Chloro-7-cyclopentylamino- lH-indol-2-yl)phenyl]eddikesyre methyl ester; 2- {4- [5-Chloro-7-(tetrahydropyran-4-yl)amino- lH-indol-2-yl]phenyl} -eddikesyre methyl ester; [5-Chloro-2-(3-dimethylaminomethylphenyl)-lH-indol-7-yl]-(tetrahydropyran-4-yl)-a min; [5-Chloro-2-(3-morpholin-4-ylmethylphenyl)-lH-indol-7-yl]-(tetrahydropyran-4-yl)-a min; [5-Chloro-2-(3-pyrrolidin-4-ylmethylphenyl)-lH-indol-7-yl]-(tetrahydropyran-4-yl)-am in; 1 - {4- [3-(5-Chloro-7-tetrahydropyran-4-ylamino-1 H-indol-2-yl)-benzyl]-piperazin-1 -yl }-ethanon; {5-Chloro-2-[3-(2-oxo-piperazin-4-yl)ethylphenyl]-lH-indol-7-yl}-(tetrahydropyran-4- yl)-amin; {5-Chloro-2-[3-(l,l-dioxo-thiomorpholin-4-yl)ethylphenyl]-lH-indol-7-yl}-(tetrahydro pyran-4-yl)-amin; og (Tetrahydropyran-4-yl)-[3-bromo-5-(morpholin-4-yl)methyl-2-phenyl-lH-indol- 7-yl]-amin.
23. En sammensætning til anvendelse ved forebyggelse eller behandling af nekrose- og nekroseassocierede sygdomme, som omfatter terapeutisk effektiv mængde af forbindelser af formlen (1), farmaceutisk acceptable salte eller optiske isomere deraf som defineret i krav 1 som en aktiv ingrediens sammen med farmaceutisk acceptable bærer eller fortyndere.
24. Sammensætning til anvendelse ifølge krav 23, hvor nekrose- og nekroseassocierede sygdomme er valgt blandt gruppen bestående af akut/kronisk leversygdom, neurodegenerative sygdomme, iskæmiske sygdomme, diabetes, pankreatitis, bakteriel/viral sepsis, nekrotiserende procolitis, cystisk fibrose, rheumatoid arthritis, degenerative arthritis, nefropati, bakteriel infektion, viral infektion, multipel sklerose, leukæmi, lymfom, neonatal åndedrætsbesværsyndrom, asfyksi, tuberkulose, endometriose, angiasthenia, psoriasis, frostknuder, komplikationer ved steroidbehandling, koldbrand, liggesår, hæmoglobinuri, sæde, hypertermi, Crohns sygdom, cøliaki, rumsyndrom, rygmarvsskader, glomerulonefritis, muskelsvind, nedarvede stofskiftesygdomme, mykoplasmasygdomme, miltbrand, Andersens sygdom, arvelig mitokondrial sygdom, phenylketonuri, placental infarkt, syfilis og aseptisk nekrose.
25. Sammensætningen til anvendelse ifølge krav 23, hvor nekrose- og nekroseassocierede sygdomme er forårsaget ved medikamenter og giftige substanser og er valgt blandt gruppen bestående af nekrose associeret med alkoholisme, udsættelse for, eller administration eller egen-administration af, kokain, medikamenter, antibiotika, kræftbekæmpende midler, adriamycin, puromycin, bleomycin, NSAID, cyclosporin, kemiske giftstoffer, giftgas, landbrugskemikalier, rungmetaller eller skader på grund af udsættelse for radioaktivitet/UV og associeret nekrose deraf.
26. Sammensætningen til anvendelse ifølge krav 24, som er til leverbeskyttelse, funktionel forbedring af lever og forebyggelse eller behandling af leversygdomme.
27. Sammensætningen til anvendelse ifølge krav 26, hvor leversygdommen er valgt blandt gruppen bestående af levertransplantation, alkoholisk eller ikke-alkoholisk fedtlever, leverfibrose, hepatocirrhoisis og hepatitis forårsaget af virus eller medikamenter.
28. Sammensætningen til anvendelse ifølge krav 26, hvor leversygdommen er alkoholisk akut/kronisk leversygdom.
29. Sammensætningen til anvendelse ifølge krav 26, hvor leversygdommen er fedtsyrepåvirket fedtlever eller akut/kronisk leversygdom afledet af fedtlever.
30. Sammensætningen til anvendelse ifølge krav 26, hvor leversygdommen skyldes radioaktive oxygenarter (ROS).
31. Sammensætningen til anvendelse ifølge krav 26, hvor leversygdommen skyldes tungmetaller.
32. Sammensætningen til anvendelse ifølge krav 23, som co-administreres med profylatiske eller terapeutiske midler for medikamentafledt nekrose og nekroseassocierede sygdomme.
33. Sammensætningen til anvendelse ifølge krav 32, hvor de profylaktiske eller terapeutiske midler for medikamentafledt nekrose og nekroseassocierede sygdomme er valgt blandt gruppen bestående af antibiotika, kræftbekæmpende midler, anti-virale midler, infektionsbekæmpende midler, antiinflammatoriske midler, antikoaguleringsmidler, lipidforbedrende midler, celledødsinhibitorer, anti-hypertensive midler, anti-diabetiske/fedmebekæmpende midler, terapeutiske midler, terapeutiske midler for hjerte-kar-sygdomme, terapeutiske midler for neurodegenerative sygdomme, antiældningsmidler og terapeutiske midler for metaboliske sygdomme.
34. Sammensætningen til anvendelse ifølge krav 26, som co-administreres med midler valgt blandt gruppen bestående af hepatocyt regenererende promotorer, funktionelle adjuvanter for lever, anti-virale midler, immunosuppressiver og fibroseinhibitorer.
35. Sammensætningen til anvendelse ifølge krav 24, hvor den neurodegenerative sygdom er demens, Parkinsons sygdom eller Huntingtons sygdom.
36. Sammensætningen til anvendelse ifølge krav 24, hvor den iskæmiske sygdom er hjertesygdom, reperfusionsskade, iskæmisk infarkt eller iskæmisk skade.
37. Sammensætningen til anvendelse ifølge krav 24, hvor diabetes forårsages af celleødelæggende substanser i bugspytkirtlen, diabetiske komplikationer eller diabetisk vaskulær sygdom.
38. Sammensætningen til anvendelse ifølge krav 37, hvor diabetes skyldes virus, hyperglykæmi, fedtsyre, diæt, giftstoffer eller streptozotocin.
39. En metode til klargøring af en sammensætning til anvendelse ved forebyggelse eller behandling af nekrose- og nekroseassocierede sygdomme, som omfatter trinnet at blande forbindelser af formlen (1), farmaceutisk acceptable salte eller optiske isomere deraf som defineret i krav 1 som en aktiv ingrediens sammen med farmaceutisk acceptable bærer.
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