DK2970101T3 - Pro-drugs af fumarater og deres anvendelse i behandling af forskellige sygdomme - Google Patents

Pro-drugs af fumarater og deres anvendelse i behandling af forskellige sygdomme Download PDF

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DK2970101T3
DK2970101T3 DK14767892.4T DK14767892T DK2970101T3 DK 2970101 T3 DK2970101 T3 DK 2970101T3 DK 14767892 T DK14767892 T DK 14767892T DK 2970101 T3 DK2970101 T3 DK 2970101T3
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compound
substituted
unsubstituted
pharmaceutically acceptable
alkyl
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Tarek A Zeidan
Scott Duncan
Christopher P Hencken
Thomas Andrew Wynn
Carlos N Sanrame
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Alkermes Pharma Ireland Ltd
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/225Polycarboxylic acids
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    • A61K31/221Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
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Claims (15)

  1. 1. Forbindelse af formel (III), eller et farmaceutisk acceptabelt salt deraf: hvor:
    Ri er usubstitueret Ci-Ce alkyl; R6, R7, Rs og R9 er hver, uafhængigt, H, substitueret eller usubstitueret Ci-C6 alkyl, substitueret eller usubstitueret C2-C6 alkenyl, substitueret eller usubstitueret C2-C6 alkynyl eller C(O)ORa; Ra er H eller substitueret eller usubstitueret C1-C6 alkyl; m er 0, 1, 2, eller 3; t er 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10; og hver Rio er, uafhængigt, H, halogen, substitueret eller usubstitueret C1-C6 alkyl, substitueret eller usubstitueret C2-C6 alkenyl, substitueret eller usubstitueret C2-C6 alkynyl, substitueret eller usubstitueret C3-C10 carbocykel, substitueret eller usubstitueret heterocykel omfattende en eller to 5- eller 6-leddet ringe og 1-4 heteroatomer valgt fra N, O og S, eller substitueret eller usubstitueret heteroaryl omfattende en eller to 5- eller 6-leddet ringe og 1-4 heteroatomer valgt fra N, O og S; eller, alternativt, to Rio'er fastgjort til det samme kulstofatom, sammen med kulstofatomet til hvilket de er fastgjort, danner et carbonyl, substitueret eller usubstitueret C3-C10 carbocykel, substitueret eller usubstitueret heterocykel omfattende en eller to 5- eller 6-leddet ringe og 1-4 heteroatomer valgt fra N, O og S, eller substitueret eller usubstitueret heteroaryl omfattende en eller to 5- eller 6-leddet ringe og 1-4 heteroatomer valgt fra N, O og S; eller, alternativt, to Rio'er fastgjort til forskellige atomer, sammen med atomerne til hvilke de er fastgjort, danner et substitueret eller usubstitueret C3-C10 carbocykel, substitueret eller usubstitueret heterocykel omfattende en eller to 5- eller 6-leddet ringe og 1-4 heteroatomer valgt fra N, O og S, eller substitueret eller usubstitueret heteroaryl omfattende en eller to 5- eller 6-leddet ringe og 1-4 heteroatomer valgt fra N, O og S.
  2. 2. Forbindelsen ifølge krav 1, hvor Ri er methyl.
  3. 3. Forbindelsen ifølge krav 1 eller 2, hvor R6, R7, Rs og R9 er hver H.
  4. 4. Forbindelsen ifølge et hvilket som helst af de foregående krav, hvor m er 2 eller 3.
  5. 5. Forbindelsen ifølge et hvilket som helst af de foregående krav, hvor t er 0, 1, 2, 3, eller 4.
  6. 6. Forbindelsen ifølge et hvilket som helst af de foregående krav, hvor to Rio'er fastgjort til det samme kulstofatom, sammen med kulstofatomet til hvilket de er fastgjort, danner et carbonyl.
  7. 7. Forbindelsen ifølge krav 1, hvor forbindelsen er:
    eller et farmaceutisk acceptabelt salt deraf.
  8. 8. Forbindelsen ifølge krav 1, hvor forbindelsen er:
    eller et farmaceutisk acceptabelt salt deraf.
  9. 9. Forbindelsen ifølge krav 1, hvor forbindelsen er:
    eller et farmaceutisk acceptabelt salt deraf.
  10. 10. Forbindelsen ifølge krav 1, hvor forbindelsen er valgt fra gruppen bestående af:
    eller et farmaceutisk acceptabelt salt deraf.
  11. 11. Forbindelsen ifølge krav 1, hvor forbindelsen er valgt fra gruppen bestående af:
    eller et farmaceutisk acceptabelt salt deraf.
  12. 12. Farmaceutisk sammensætning omfattende: (i) forbindelse af formel (III), eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1-11; og (ii) en farmaceutisk acceptabel bærer.
  13. 13. Forbindelse af formel (III), et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1-11, eller en sammensætning ifølge krav 12, til anvendelse i behandling afen neurologisk sygdom.
  14. 14. Forbindelsen eller sammensætning til anvendelse ifølge krav 13, hvor den neurologiske sygdom er multipel sklerose.
  15. 15. Forbindelsen eller sammensætning til anvendelse ifølge krav 13, hvor den neurologiske sygdom er valgt fra relapserende-remitterende multipel sklerose, sekundær progressiv multipel sklerose, primær progressiv multipel sklerose, eller progressiv-relapserende multipel sklerose.
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