DK1976509T3 - Ppar-modulatorer - Google Patents

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DK1976509T3
DK1976509T3 DK07804876T DK07804876T DK1976509T3 DK 1976509 T3 DK1976509 T3 DK 1976509T3 DK 07804876 T DK07804876 T DK 07804876T DK 07804876 T DK07804876 T DK 07804876T DK 1976509 T3 DK1976509 T3 DK 1976509T3
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derivative
ppar
phenyl
disease
treating
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Karsten Kristiansen
Prathama S Mainkar
Jean-Philippe Meyer
Sorensen Alexandra C O Evolva Sa Santana
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Evolva Sa
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Claims (15)

1. 1,3-dioxanderivat eller et farmaceutisk acceptabelt salt deraf til anvendelse i behandling af en peroxisom-proliferator aktiveret receptor (PPAR) responsiv sygdom eller tilstand valgt fra insulinresistens, diabetes, metabolisk syndrom, fedme, præ-diabetes, diabetes, dyslipidæmi, og sårheling, hvor derivatet er vist med formlen:
hvor A er en forgrenet eller lineær carbonkæde med 3 til 7 carbonatomer med op til 2 dobbeltbindinger; W er COOH, OH, NH2, SO3H, OSO3H, eller en aromatisk gruppe valgt fra gruppen bestående af phenyl, 1- eller 2-naphthyl, pyridin, furan, 2-methylpyridin og en dioxolan, hver eventuelt substitueret med COOH, OH eller NH2; Ar er en phenyl, 1-naphthyl, 2-naphthyl, eller en 5- eller 6-leddet heterocyklisk aromatisk gruppe eventuelt substitueret med hydroxy eller methoxy i ortho-, meta-og/eller para-stillingerne; og, Ra og Rb er uafhængigt hydrogen, 2-6C alkenyl, 1-8C alkyl eventuelt med op til tre halogensubstituenter, pentafluorphenyl, aryl eller aryl(l-4C)alkyl, hvilke aryl- eller aryl(l-4C)alkyl-substituenter eventuelt er substitueret med op til fem substituenter valgt fra halogeno, (l-6C)alkyl, forgrenet eller lineær (l-6C)alkoxy, (l-4C)alkylen-dioxy, trifluormethyl, cyano, nitro, hydroxyl, (2-6C)alkanoyloxy, (l-6C)alkylthio, (l-6C)alkansulphonyl, (l-6C)alkanoylamino og oxapolymethylen af 2 til 4 carbonatomer, eller Ra og Rb sammen danner polymethylen med 2 til 7 carbonatomer, eventuelt med en eller to (l-4C)alkylsubstituenter.
2. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 1, hvor A er en lineær carbonkæde med 3 til 7 carbonatomer, og W er COOH.
3. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 2, hvor carbonkæden omfatter en dobbeltbinding mellem C2-C3 eller C3-C4.
4. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge et hvilket som helst af de foregående krav, hvor Ar er en 2-OH- eller 2-OMe-substitueret phenyl- eller naphthylgruppe.
5. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge et hvilket som helst af de foregående krav, hvor Ra er H og Rb er en arylgruppe valgt fra gruppen bestående af phenyl, benzyl, 2- eller 3- eller 4-pyridin, furan, biphenyl 1-naphthyl og 2-naphthyl, hver eventuelt substitueret med halogen, OH, O-alkyl, amino, N-monoalkyl, N-dialkyl, nitroalkyl eller thioalkyl.
6. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 1, hvor forbindelsen er et 2,4-diphenyl-l,3-dioxanderivat med formel II eller et farmaceutisk acceptabelt salt deraf, hvor formel II er vist med:
hvor X er valgt fra fluor, chlor, brom, trifluormethyl, eventuelt substitueret phenyl, cyano, methoxy og nitro, eller phenyl-X-gruppen eventuelt kan være et substitueret chromenderivat; og Y og Z er individuelt hydrogen eller halogeno.
7. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 6, hvor grupperne ved stillingerne 2, 4 og 5 af dioxanringen i derivatet vist med formel II har cis-relativ stereokemi.
8. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 6 eller 7, hvor X er valgt fra 2-fluor, 2-chlor, 2-brom, 2-cyano, 2-trifluormethyl, 3-fluor, 3-chlor, 3-cyano, 3-nitro, 3-methoxy, 4-chlor, 4-cyano, 4-nitro og 4-methoxy; Y er hydrogen eller fluor; og Z er hydrogen.
9. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 8, hvor X er valgt fra 2-chlor, 3-chlor, 2-cyano, 4-cyano, 3-nitro og 4-nitro; og Y og Z er hydrogen.
10. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 8, hvor derivatet er er 4(Z)-6-(2-o-chlorphenyl-4-o-hydroxyphenyl-l,3-dioxan-cis-5-yl)hexensyre eller et farmaceutisk acceptabelt salt deraf.
11. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 1, hvor A er en forgrenet eller lineær carbonkæde med 3 til 7 carbonatomer med op til 2 dobbeltbindinger; W er COOH, OH, NH2, S03H, 0S03H, eller en aromatisk gruppe valgt fra gruppen bestående af phenyl, 1- eller 2-naphthyl, pyridin, furan, 2-methylpyridin og en dioxolan, hver eventuelt substitueret med COOH, OH eller NH2 Ar er phenyl, 1-naphthyl, 2-naphthyl, biphenyl (4-methoxyphenoxy)-phenyl, eller en 5-eller 6-leddet heterocyklisk aromatisk gruppe valgt fra substitueret eller ikke-substitueret 2-pyridin, 3-pyridin, thiophen, og furan, og, Ra er H og Rb er en arylgruppe eller en heterocykel eventuelt substitueret med tre forskellige substituenter valgt fra gruppen bestående af halogen, OH, O-alkyl, O-aryl, amino eller N-monoalkyl eller N-dialkyl eller N-monoaryl eller N-diaryl, nitro, thioalkyl eller oxo.
12. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 11, hvor A er er en fem-carbon-lineær kæde med en dobbeltbinding, W er COOH, Ar er phenyl substitueret i o-stillingen med OH eller OMe og Rb er en heterocykel eller en phenylgruppe substitueret med O-aryl.
13. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 11, hvor derivatet er 4(Z)-6-(2-[4-methoxyphenoxy-o-phenyl]-4-o-hydroxy-phenyl-l,3-dioxan-cis-5-yl)hexensyre eller et farmaceutisk acceptabelt salt deraf; eller derivatet er 4(Z)-6-(2-3-[6-chlor-4H-chromen-4-on ]-4-o-hydroxyphenyl-l,3-dioxan-cis-5-yl)hexensyre eller et farmaceutisk acceptabelt salt deraf.
14. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge et hvilket som helst af de foregående krav, hvor forbindelsen er til stede som et farmaceutisk acceptabelt salt valgt fra alkalimetal- og jordalkalimetalsalte, aluminium- og ammoniumsalte, og fra salte med organiske aminer og kvaternære baser der danner fysiologisk acceptable kationer.
15. Derivat til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand ifølge krav 1, hvor derivatet er valgt fra: 4(Z)-6-(2-[4-methoxyphenoxy-o-phenyl]-4-o-hydroxyphenyl-l,3-dioxan-cis-5-yl)hexensyre; 4(Z)-6-(2-[6-chlor-4H-chromen-4-on]-4-o-hydroxyphenyl-l,3-dioxan-cis-5-yl)hexensyre; (Z)-6-((2S,4S,5R)-2-(2-chlorphenyl)-4-(2-hydroxyphenyl)-l,3-dioxan-5-yl)hex-4-ensyre; (Z)-6-((2S,4S,5R)-2-(2,6-dichlorphenyl)-4-(2-methoxyphenyl)-l,3-dioxan-5-yl)hex-4-ensyre; (Z)-6-((2S,4S,5R)-4-(2-methoxy-phenyl)-2-(perfluorphenyl)-l,3-dioxan-5-yl)hex-4-ensyre; (E)-4-((2S,4S,5R)-2-(2-chlorphenyl)-4-(2-methoxyphenyl)-l,3-dioxan-5-yl)but-2-ensyre; (Z)-8-((2S,4S,5R)-2-(2-chlorphenyl)-4-(2-methoxyphenyl)-l,3-dioxan-5-yl)oct-6-ensyre; (Z)-8-((4S,5R)-4-(2-methoxyphenyl)-2,2-dimethyl-l,3-dioxan-5-yl)oct-6-ensyre; 8-((2S,4S,5R)-2-(2-chlor-phenyl)-4-(2-methoxyphenyl)-l,3-dioxan-5-yl)octansyre; og (Z)-7-((2S,4S,5R)-2-(2-chlorphenyl)-4-(2-methoxyphenyl)-l,3-dioxan-5-yl)hept-4-ensyre.
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