HRP20201263T1 - Natrijeva sol od n-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1h-pirazol-3-sulfonamida - Google Patents

Natrijeva sol od n-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1h-pirazol-3-sulfonamida Download PDF

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HRP20201263T1
HRP20201263T1 HRP20201263TT HRP20201263T HRP20201263T1 HR P20201263 T1 HRP20201263 T1 HR P20201263T1 HR P20201263T T HRP20201263T T HR P20201263TT HR P20201263 T HRP20201263 T HR P20201263T HR P20201263 T1 HRP20201263 T1 HR P20201263T1
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Croatia
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salt
indacen
hexahydro
pyrazole
carbamoyl
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HRP20201263TT
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English (en)
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David Miller
Angus Macleod
Susana Del Rio Gancedo
Samuel Alexander STRATFORD
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Inflazome Limited
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Publication of HRP20201263T1 publication Critical patent/HRP20201263T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (17)

1. Natrijeva sol od N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-l-izopropil-lH-pirazol-3-sulfonamida ili njezin hidrat ili solvat.
2. Sol sukladno zahtjevu 1, naznačena time što sol je mononatrijeva sol.
3. Sol sukladno zahtjevu 1 ili 2, naznačena time što je sol monohidrat.
4. Sol sukladno bilo kojem od zahtjeva 1 do 3, naznačena time što je sol kristalna.
5. Sol sukladno bilo kojem od zahtjeva 1 do 4, naznačena time što je sol kristalna mononatrijeva sol N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamid monohidrat.
6. Polimorfni oblik soli sukladno zahtjevu 5, ima XRPD spektar koji sadrži vrhove na: 4.3 ° 2θ, 8.7 ° 2θ i 20.6 ° 2θ, svih +0.2 ° 2θ.
7. Polimorfni oblik soli sukladno zahtjevu 5 ili 6, ima XRPD spektar u kojem 10 najintenzivnijih vrhova uključuje 5 ili više vrhova koji imaju vrijednost 2θ odabranu između: 4.3 ° 2θ, 6.2 ° 2θ, 6.7 ° 2θ, 7.3 ° 2θ, 8.7 ° 2θ, 9.0 ° 2θ, 12.1 ° 2θ, 15.8 ° 2θ, 16.5 ° 2θ, 18.0 ° 2θ, 18.1 ° 2θ, 20.6 ° 2θ, 21.6 ° 2θ, i 24.5 ° 2θ, svih +0.2 ° 2θ.
8. Postupak dobivanja natrijeve soli N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il) karbamoil)-1-izopropil-1H-pirazol-3-sulfonamida, koji sadrži: (a) kontaktiranje N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamida bez kiseline i izvora natrijevih iona u prisutnosti jednog ili više polarnih otapala da nastane mješavina; i (b) dobivanje krute natrijeve soli od N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il) karbamoil)-1-izopropil-1H-pirazol-3-sulfonamida iz mješavine.
9. Proces sukladno zahtjevu 8, naznačen time što jedno ili više polarnih otapala korištenih u koraku (a) sadrže vodu i polarno aprotično organsko otapalo.
10. Proces za pripremu kristalne mononatrijeve soli N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamid monohidrata u polimorfni oblik sukladno zahtjevu 6 ili 7, sadrži: (a) kontaktiranje N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamida bez kiseline i izvora natrijevih iona u prisutnosti vode i izborno polarno aprotično organsko otapalo da se dobije otopina; ili otapanje N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamid mononatrijeve soli u mješavini otapala koja sadrži vodu i, izborno polarno aprotično organsko otapalo da se dobije otopina; i (b) dobivanje kristalne mononatrijeve soli od N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamid monohidrata u polimorfni oblik sukladno zahtjevu 6 ili 7 iz otopine.
11. Proces sukladno zahtjevu 9 ili 10, naznačen time što polarno aprotično organsko otapalo korišteno u koraku (a) je aceton.
12. Proces sukladno bilo kojem od zahtjeva 8 do 11, naznačen time što natrijeva sol od N-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1H-pirazol-3-sulfonamida je dobivena u koraku (b) dodavanjem protuotapala.
13. Proces sukladno zahtjevu 12, naznačen time što protuotapalo je tert-butil metil eter.
14. Farmaceutski pripravak sadrži sol sukladno bilo kojem od zahtjeva 1 do 5, ili polimorfni oblik sukladno zahtjevu 6 ili 7, i farmaceutski prihvatljiv ekscipijent.
15. Sol sukladno bilo kojem od zahtjeva 1 do 5, ili polimorfni oblik sukladno zahtjevu 6 ili 7, ili farmaceutski pripravak iz zahtjeva 14, za uporabu u medicini.
16. Sol sukladno bilo kojem od zahtjeva 1 do 5, ili polimorfni oblik sukladno zahtjevu 6 ili 7, ili farmaceutski pripravak sukladno zahtjevu 14, za uporabu u liječenju ili sprječavanju bolesti, poremećaja ili stanja, pri čemu je bolest, poremećaj ili stanje odabrano između: (i) upale; (ii) auto-imunološke bolesti; (iii) raka; (iv) infekcije; (v) bolesti središnjeg živčanog sustava; (vi) metaboličke bolesti; (vii) kardiovaskularne bolesti; (viii) respiratorne bolesti; (ix) bolesti jetre; (x) bubrežne bolesti; (xi) očne bolesti; (xii) kožne bolesti; (xiii) stanje limfe; (xiv) psihološkog poremećaja; (xv) cijepljenja nasuprot bolesti domaćina; (xvi) alodnije; i (xvii) svake bolesti za koju je određeno da pojedinac ima zaraznu ili somatsku nečujnu mutaciju u NLRP3.
17. Sol sukladno bilo kojem od zahtjeva 1 do 5, ili polimorfni oblik sukladno zahtjevu 6 ili 7, ili farmaceutski pripravak sukladno zahtjevu 14, za uporabu u liječenju ili sprječavanju bolesti, poremećaja ili stanja, pri čemu je bolest, poremećaj ili stanje odabrano između: (i) periodičkih sindroma povezanih sa kriopirinom (CAPS); (ii) Muckle-Wells sindroma (MWS); (iii) obiteljskog autoinflamatornog sindroma (FCAS); (iv) višesistemske upalne bolesti neonatalnog nastanka (NOMID); (v) obiteljske mediteranske groznice (FMF); (vi) piogenog artritisa, pioderma gangrenosuma i sindroma akni (PAPA); (vii) hiperimunoglobulinemije D i sindroma periodične groznice (HIDS); (viii) faktor nekroze tumora (TNF) periodičkog sindroma povezanog s receptorima (TRAPS); (ix) sistemskog juvenilnog idiopatskog artritisa; (x) Stillove bolesti odrasle osobe (AOSD); (xi) relapsirajućeg polikondritisa; (xii) Schnitzlerovog sindroma; (xiii) Sweetovog sindroma; (xiv) Behcetove bolesti; (xv) sindroma anti-sintetaze; (xvi) nedostatka antagonista receptora interleukina 1 (DIRA); i (xvii) haploinsuficijencije A20 (HA20).
HRP20201263TT 2018-04-23 2020-08-11 Natrijeva sol od n-((1,2,3,5,6,7-heksahidro-s-indacen-4-il)karbamoil)-1-izopropil-1h-pirazol-3-sulfonamida HRP20201263T1 (hr)

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GBGB1806578.9A GB201806578D0 (en) 2018-04-23 2018-04-23 Novel compound
PCT/EP2019/060311 WO2019206871A1 (en) 2018-04-23 2019-04-23 A sodium salt of n-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1 -isopropyl-1 h-pyrazole-3-sulfonamide
EP19721230.1A EP3606909B1 (en) 2018-04-23 2019-04-23 A sodium salt of n-((1,2,3,5,6,7-hexahydro-s-indacen-4 -yl)carbamoyl)-1-isopropyl-1h-pyrazole-3-sulfonamide

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AR (1) AR114827A1 (hr)
AU (1) AU2019257973A1 (hr)
BR (1) BR112020021650A2 (hr)
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WO2019008029A1 (en) 2017-07-07 2019-01-10 Inflazome Limited SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3
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GB201817038D0 (en) 2018-10-19 2018-12-05 Inflazome Ltd Novel processes
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ES2811228T3 (es) 2021-03-11
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EP3722281A1 (en) 2020-10-14
AU2019257973A1 (en) 2020-11-19
MD3606909T2 (ro) 2020-08-31
EP3606909A1 (en) 2020-02-12
CY1123260T1 (el) 2021-12-31
JP2021522195A (ja) 2021-08-30
PL3606909T3 (pl) 2020-11-16
CN112020495B (zh) 2024-05-17
SI3606909T1 (sl) 2020-09-30
LT3606909T (lt) 2020-10-12
UY38186A (es) 2019-11-29
AR114827A1 (es) 2020-10-21
US10973803B2 (en) 2021-04-13
TW201943704A (zh) 2019-11-16
EP3606909B1 (en) 2020-05-27
CA3097832A1 (en) 2019-10-31
MX2020011196A (es) 2020-11-13
GB201806578D0 (en) 2018-06-06
ME03822B (me) 2021-04-20
RS60646B1 (sr) 2020-09-30
MA48051B1 (fr) 2020-08-31
PT3606909T (pt) 2020-07-09
DK3606909T3 (da) 2020-08-24
US20210315862A1 (en) 2021-10-14
US20200237723A1 (en) 2020-07-30
JP7382958B2 (ja) 2023-11-17
MA51082A (fr) 2021-05-19
KR20210005589A (ko) 2021-01-14
CN112020495A (zh) 2020-12-01
BR112020021650A2 (pt) 2021-01-26

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