DK3013826T3 - Krystallinske bromdomænehæmmere - Google Patents

Krystallinske bromdomænehæmmere Download PDF

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DK3013826T3
DK3013826T3 DK14745267.6T DK14745267T DK3013826T3 DK 3013826 T3 DK3013826 T3 DK 3013826T3 DK 14745267 T DK14745267 T DK 14745267T DK 3013826 T3 DK3013826 T3 DK 3013826T3
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crystal form
pyrrolo
difluorophenoxy
methyl
oxo
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Yuchuan Gong
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Abbvie Inc
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Claims (26)

1. Isoleret krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid, hvor krystal-formen har et pulverrøntgendiffraktionsmønster, der omfatter tre eller flere 20-topværdier ± 0,2 udvalgt fra gruppen, der består af: 6,2°, 9,0°, 12,3°, 12,6°, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
2. Isoleret krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1, hvor krystalformen har et pulverrøntgendiffraktionsmønster, der omfatter følgende 20-topværdier ± 0,2: 6,2°, 9,0°, 11,0°, 12,3°, 12,6°, 13,1°, 14,1°, 15,6°, 16,4°, 16,5°, 16,9°, 17,8°, 18,1°, 18,3°, 18,9°, 20,4°, 21,1°, 21,6°, 21,8°, 22,1°, 22,9°, 23,2°, 24,4°, 24,7°, 25,6°, 26,3°, 27,0° og 27,3°.
3. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter tre, fire, fem eller seks 20-topværdier ± 0,2 udvalgt fra gruppen, der består af 6,2°, 9,0°, 12,3°, 12,6, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
4. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter seks 20-topværdier ± 0,2 udvalgt fra gruppen, der består af 6,2°, 9,0°, 12,3°, 12,6°, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
5. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter fem 20-topværdier ± 0,2 udvalgt fra gruppen, der består af 6,2°, 9,0°, 12,3°, 12,6, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
6. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter fire 20-topværdier ± 0,2 udvalgt fra gruppen, der består af 6,2°, 9,0°, 12,3°, 12,6, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
7. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter tre 20-topværdier ± 0,2 udvalgt fra gruppen, der består af 6,2°, 9,0°, 12,3°, 12,6, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
8. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter følgende 20-topværdier ± 0,2: 6,2°, 9,0°, 12,3°, 12,6° og 15,6°.
9. Krystalform ifølge krav 1, der har et pulverrøntgendiffraktionsmønster, der omfatter følgende 20-topværdier ± 0,2: 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
10. Krystalform ifølge krav 2, der har et pulverrøntgendiffraktionsmønster, der omfatter topværdier ± 0,2 ved 20-positionerne 6,2°, 9,0°, 12,3°, 12,6°, 13,1°, 14,1°, 16,4°, 16,5°, 16,9°, 17,8°, 18,1°, 18,3° og 18,9°.
11. Krystalform ifølge krav 2, der har et pulverrøntgendiffraktionsmønster, der omfatter topværdier ± 0,2 ved 20-positionerne 6,2°, 9,0°, 12,3°, 12,6°, 13,1°, 14,1°, 18,1° og 18,9°.
12. Krystalform ifølge krav 2, der har et pulverrøntgendiffraktionsmønster, der omfatter topværdier ± 0,2 ved 20-positionerne 6,2°, 9,0°, 12,3°, 12,6°, 13,1° og 18,1°.
13. Krystalform ifølge krav 2, der har et pulverrøntgendiffraktionsmønster, der omfatter topværdier ± 0,2 ved 20-positionerne 9,0°, 12,3°, 12,6°, 13,1° og 18,1°.
14. Krystalform ifølge krav 1, der har en differentiel scanningskalorimetri-termogramendoterm på mellem 240 og 242 °C.
15. Krystalform ifølge krav 1, der har en differentiel scanningskalorimetri-termogramendoterm ved ca. 241 °C.
16. Farmaceutisk sammensætning, der omfatter en isoleret krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bærcmatcrialc.
17. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en fremgangsmåde til behandling af cancer hos en person, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det.
18. Farmaceutisk sammensætning til anvendelse ifølge krav 17, hvor canceren er udvalgt fra gruppen, der består af: akustikusneurom, akut leukæmi, akut lymfatisk leukæmi, akut myeloid leukæmi (monocytisk, myeloblastisk, adenokarcinom, angiosarkom, astrocytom, myelomonocytisk og promyelocytisk), akut T-celleleukæmi, basalcellekarcinom, galdevej skarcinom, blærecancer, hjernecancer, brystcancer, bronkogent karcinom, cervixcancer, kondrosarkom, chordom, choriokarcinom, kronisk leukæmi, kronisk lymfatisk leukæmi, kronisk myeloid (granulocytisk) leukæmi, kronisk myelogen leukæmi, coloncancer, kolorektal cancer, kraniofaryngiom, cystadenokarcinom, diffust storcellet B-cellelymfom, dysproliferative forandringer (dyspiasier og metaplasier), embryonalt karcinom, endometriecancer, endotelsarkom, ependymom, epitelkarcinom, erytroleukæmi, øsofaguscancer, østrogenreceptorpositiv brystcancer, essentiel trombocytæmi, Ewings tumor, fibrosarkom, follikellymfom, kimcelletestikelcancer, gliom, glioblastom, gliosarkom, heavy chain sygdom, hæmangioblastom, hepatom, hepatocellulær cancer, hormonufølsom prostatacancer, leiomyosarkom, leukæmi, liposarkom, lungecancer, lymfangioendoteliosarkom, lymfangiosarkom, lymfoblastisk leukæmi, lymfom (Hodgkins og non-Hodgkins), maligniteter og hyperproliferative forstyrrelser i blære, bryst, colon, lunge, ovarier, pankreas, prostata, hud og uterus, lymfoide maligniteter med udspring i T-celler eller B-celler, leukæmi, lymfom, medullært karcinom, mcdulloblastom, mclanom, mcningiom, mcsotcliom, multipelt myelom, myeloid leukæmi, myelom, myxosarkom, neuroblastom, NUT midtlinje karcinom (NMC), ikke-småcellet lungecancer, oligodendrogliom, oral cancer, osteogent sarkom, ovariecancer, pankreascancer, papillære adenokarcinomer, papillært karcinom, pinealom, polycythemia vera, prostatacancer, rectumcancer, renalcellekarcinom, retinoblastom, rhabdomyosarkom, sarkom, talgkirtelkarcinom, seminom, hudcancer, småcellet lungekarcinom, solide tumorer (karcinomer og sarkomer), småcellet lungecancer, ventikelcancer, pladeepitelkarcinom, synoviom, svedkirtelkarcinom, thyreoideacancer, Waldenstroms makroglobulinæmi, testikeltumorer, uteruscancer og Wilms' tumor.
19. Fremgangsmåde til fremstilling af en farmaceutisk sammensætning, der omfatter N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH- pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid og et farmaceutisk acceptabelt bæremateriale, som omfatter: blanding af en isoleret krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid, hvor krystalformen har et pulverrøntgendiffraktionsmønster, der omfatter tre eller flere 20-topværdier + 0,2 udvalgt fra gruppen, der består af: 6,2°, 9,0°, 12,3°, 12,6°, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°, med et farmaceutisk acceptabelt bæremateriale.
20. Sammensætning, der omfatter mere end 90 % (vægt/vægt) krystalform II af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid, hvor krystalformen har et pulverrøntgendiffraktionsmønster, der omfatter tre eller flere 20-topværdier ± 0,2 udvalgt fra gruppen, der består af: 6,2°, 9,0°, 12,3°, 12,6°, 15,6°, 22,1°, 25,6°, 26,3°, 27,0° og 27,3°.
21. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4- difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en fremgangsmåde til behandling af en akut nyresygdom eller -tilstand hos en person, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det, hvor den akutte nyresygdom eller -tilstand er udvalgt fra gruppen, der består af: iskæmi/reperfusions-induceret nyresygdom, nyresygdom induceret af kardielt og større kirurgisk indgreb, nyresygdom induceret af perkutan koronar intervention, nyresygdom induceret af radioaktivt kontrastmiddel, sep sisinduceret nyresygdom, pneumoniinduceret nyresygdom og lægemiddeltoksicitetsinduceret nyresygdom.
22. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en fremgangsmåde til behandling af en kronisk nyresygdom eller -tilstand hos en person, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-cJpyridin-4-yl)phenylJethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det, hvor den kroniske nyresygdom eller -tilstand er udvalgt fra gruppen, der består af: diabetisk nefropati, hypertensiv nefropati, IIIV-relateret nefropati, glomerulonefritis, lupus nefritis, IgA-nefropati, fokal segmental glomerulosklerose, membranøs glomerulonefritis, minimal change sygdom, polycystisk nyresygdom og tubulær interstitiel nefritis.
23. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en fremgangsmåde til behandling af en sygdom eller tilstand hos en person, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det, hvor sygdommen eller tilstanden er udvalgt fra gruppen, der består af Addisons sygdom, akut urinsyregigt, ankyloserende spondylitis, astma, aterosklerose, Behcets sygdom, bulløse hudsygdomme, kardiel myopati, kardiel hypertrofi, kronisk obstruktiv lungesygdom (KOL), Crohns sygdom, dermatitis, eksem, kæmpecellearteritis, glomerulonefritis, hjertesvigt, hepatitis, hypofysitis, inflammatorisk tarmsygdom, Kawasakis sygdom, lupus nefritis, multipel sklerose, myocarditis, myositis, nefritis, organtransplantatafstødning, osteoarthritis, pankreatitis, pericarditis, polyarteritis nodosa, pneumonitis, primær biliær cirrose, psoriasis, psoriatisk arthritis, rheumatoid arthritis, scleritis, scleroserende cholangitis, sepsis, systemisk lupus erythematosus, Takayasus arteritis, toksisk shock, thyroiditis, type I-diabetes, ulcerativ colitis, uveitis, vitiligo, vasculitis og Wegeners granulomatose.
24. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-cJpyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en fremgangsmåde til behandling af erhvervet immundefektsyndrom (AIDS) hos en person, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det.
25. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en fremgangsmåde til behandling af et sygdom eller tilstand hos en person, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det, hvor sygdommen eller tilstanden er udvalgt fra gruppen, der består af: obesitas, dyslipidæmi, hyperkolesterolæmi, Alzheimers sygdom, metabolisk syndrom, hepatislc steatose, type Π-diabetes, insulinresistens, diabetisk retinopati og diabetisk neuropati.
26. Farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale til anvendelse i en præventionsmetode til en mand, som omfatter administrering af en terapeutisk effektiv mængde af en farmaceutisk sammensætning, der omfatter en krystalform af N-[4-(2,4-difluorphenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-lH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethansulfonamid ifølge krav 1 og mindst ét farmaceutisk acceptabelt bæremateriale, til en person, der har behov for det.
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