DK2532647T3 - Hidtil ukendte co-krystaller af agomelatin - Google Patents

Hidtil ukendte co-krystaller af agomelatin Download PDF

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DK2532647T3
DK2532647T3 DK12171231.9T DK12171231T DK2532647T3 DK 2532647 T3 DK2532647 T3 DK 2532647T3 DK 12171231 T DK12171231 T DK 12171231T DK 2532647 T3 DK2532647 T3 DK 2532647T3
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disorders
acid
crystal according
expressed
crystal
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Philippe Letellier
Michael Lynch
Jean-Manuel Pean
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Servier Lab
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Claims (19)

1. Co-krystal af agomelatin, kendetegnet ved, at den består af: agomelatin eller A/-[2-(7-methoxy-1-naphthyl)ethyl]acetamid med formlen (I)
og en organisk syre valgt blandt para-hydroxybenzoesyre, gallussyre, malonsyre, glutarsyre, glycolsyre og ketoglutarsyre.
2. Co-krystal ifølge krav 1, kendetegnet ved, at den modificerer den aktive bestanddels opløsningshastighed i forhold til krystalformen II.
3. Co-krystal ifølge et hvilket som helst af kravene 1 eller 2, kendetegnet ved, at den bibringer en modifikation af den aktive bestanddels opløsningshastighed i forhold til opløsningshastigheden for krystalformen II på mindst 25% under neutrale (pH 6,8) eller sure (HCI 0,01 N) betingelser.
4. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er N-[2-{7- methoxy-1-naphthyl)ethyl]acetamid / para-hydroxybenzoesyre (2/1), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 13,16°, 14,91°, 17,37°, 18,39°, 18,93°, 19,04°, 19,65°, 19,96°, 20,25°, 21,49°, 25,00° i sit røntgenpulverdiffraktionsdiagram.
5. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er A/-[2-(7- methoxy-1-naphthyl)ethyl]acetamid / para-hydroxybenzoesyre (1/2), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 9,50°, 12,28°, 14,00°, 15,76°, 16,18°, 16,62°, 17,56°, 18,15°, 19,96°, 21,00°, 21,30°, 22,00°, 22,97°, 23,55°, 23,76°, 24,44°, 26,09°, 26,82°, 28,42°, 28,71°, 29,85° i sit røntgenpulverdiffraktionsdiagram.
6. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er A/-[2-(7-methoxy-1-naphthyl)ethyl]acetamid / gallussyre (2/1), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 14,47°, 17,68°, 19,82°, 22,33°, 23,93° i sit røntgenpulverdiffraktionsdiagram.
7. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er A/-[2-(7-methoxy-1-naphthyl)ethyl]acetamid / malonsyre (1/1), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 10,47°, 11,95°, 14,78°, 16,05°, 22,32°, 24,50°, 25,05°, 25,24°, 27,38°, 27,91° i sit røntgenpulverdiffraktionsdiagram.
8. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er N-[2-(7-methoxy-1-naphthyl)ethyl]acetamid / glutarsyre (1/1), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 9,59°, 10,35°, 11,96°, 20,57°, 21,65°, 23,34° i sit røntgenpulverdiffraktionsdiagram.
9. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er N-[2-(7- methoxy-1-naphthyl)ethyl]acetamid / glycolsyre (1/1), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 10,29°, 14,11°, 14,23°, 17,98°, 18,83°, 19,51°, 20,61°, 23,96°, 24,39°, 26,44°, 28,11°, 29,52° i sit røntgenpulverdiffraktionsdiagram.
10. Co-krystal ifølge et hvilket som helst af kravene 1-3, som er N-[2-(7-methoxy-1-naphthyl)ethyl]acetamid / ketoglutarsyre (1/1), kendetegnet ved Bragg 2-theta-vinklerne (udtrykt i °±0,2) 15,36°, 16,34°, 16,54°, 19,24°, 23,57°, 23,90°, 24,41° i sit røntgenpulverdiffraktionsdiagram.
11. Fremgangsmåde til opnåelse af co-krystallen ifølge et hvilket som helst af kravene 1-11, kendetegnet ved, at: - de to bestanddele blandes i et organisk opløsningsmiddel i de ønskede andele (1 ækvivalent agomelatin til 0,25-4 molækvivalenter organisk syre); - den opnåede opløsning omrøres og eventuelt opvarmes til en temperatur, som højst er lig med det valgte opløsningsmiddels kogepunkt; - mediet afkøles under omrøring, og co-krystallen udfældes naturligt eller efter overførsel til et andet opløsningsmiddel; - det opnåede bundfald frafiltreres og tørres.
12. Fremgangsmåde til fremstilling af co-krystallen ifølge et hvilket som helst af kravene 1-10, kendetegnet ved, at de to bestanddele formales sammen.
13. Fremgangsmåde til fremstilling af co-krystallen ifølge et hvilket som helst af kravene 1-10, kendetegnet ved, at de to bestanddele blandes i et organisk eller vandigt-organisk opløsningsmiddel og derpå nedfryses og tørres ved mellem -40°C og -60°C.
14. Fremgangsmåde til fremstilling af co-krystallen ifølge et hvilket som helst af kravene 1-10, kendetegnet ved, at pulverne af agomelatin og den pågældende syre blandes i en blander, hvorefter blandingen ekstruderes ved dobbeltsnekke-ekstrudering uden dyse for at opnå et fast granulært produkt direkte ved ekstruderens udløb.
15. Farmaceutiske sammensætninger, der som aktiv bestanddel indeholder en co-krystal ifølge et hvilket som helst af kravene 1-10 i kombination med en eller flere inerte, ikke-toksiske og farmaceutisk acceptable bærere.
16. Farmaceutiske sammensætninger ifølge krav 15, som er egnede til fremstilling af lægemidler til behandling af forstyrrelser i det melatoninerge system.
17. Farmaceutiske sammensætninger ifølge krav 15, som er egnede til fremstilling af lægemidler til behandling af stress, søvnforstyrrelser, angstlidelser og navnlig generaliseret angst, obsessive-kompulsive forstyrrelser, stemningsforstyrrelser og navnlig bipolare lidelser, egentlig depression, sæsonbetinget depression, kardiovaskulære patologier, patologier i fordøjelsessystemet, insomni og træthed forårsaget af jetlag, skizofreni, panikanfald, melankoli, appetitforstyrrelser, obesitas, insomni, smerter, psykotiske lidelser, epilepsi, diabetes, Parkinsons sygdom, senildemens, forskellige lidelser relateret til normal eller patologisk aldring, migræne, hukommelsestab, Alzheimers sygdom, samt ved forstyrrelser i det cerebrale kredsløb og ved seksuelle dysfunktioner, som ovulationshæmmere og immunmodulatorer, og ved behandling af cancere.
18. Co-krystal ifølge et hvilket som helst af kravene 1-10 til behandling af forstyrrelser i det melatoninerge system.
19. Co-krystal ifølge et hvilket som helst af kravene 1-10 til behandling af stress, søvnforstyrrelser, angstlidelser og navnlig generaliseret angst, obsessive-kompulsive forstyrrelser, stemningsforstyrrelser og navnlig bipolare lidelser, egentlig depression, sæsonbetinget depression, kardiovaskulære patologier, patologier i fordøjelsessystemet, insomni og træthed forårsaget af jetlag, skizofreni, panikanfald, melankoli, appetitforstyrrelser, obesitas, insomni, smerter, psykotiske lidelser, epilepsi, diabetes, Parkinsons sygdom, senildemens, forskellige lidelser relateret til normal eller patologisk aldring, migræne, hukommelsestab, Alzheimers sygdom, samt ved forstyrrelser i det cerebrale kredsløb og ved seksuelle dysfunktioner, som ovulationshæmmere og immunmodulatorer, og ved behandling af cancere.
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