RU2020113165A - Циклические пуриновые динуклеотиды в качестве модуляторов sting - Google Patents

Циклические пуриновые динуклеотиды в качестве модуляторов sting Download PDF

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RU2020113165A
RU2020113165A RU2020113165A RU2020113165A RU2020113165A RU 2020113165 A RU2020113165 A RU 2020113165A RU 2020113165 A RU2020113165 A RU 2020113165A RU 2020113165 A RU2020113165 A RU 2020113165A RU 2020113165 A RU2020113165 A RU 2020113165A
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cyclic purine
purine dinucleotides
sting modulators
represent
sting
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Джерри Лерой Адамс
Кевин Дж. Даффи
Ицянь Лянь
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Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
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    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/555—Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511—Organic adjuvants

Claims (13)

  1. Соединение формулы (I)
  2. Figure 00000001
    ,
  3. где Y1 и Y2 независимо представляют собой CH2 или O;
  4. X1 и X2 независимо представляют собой S или O;
  5. R1 представляет собой OH, и R2 представляет собой NH2, или R1 представляет собой NH2, и R2 представляет собой H;
  6. R3 представляет собой OH, и R4 представляет собой NH2, или R3 представляет собой NH2, и R4 представляет собой H;
  7. R5 выбирают из: F, OH и OC(O)R7;
  8. R6 выбирают из: F, OH и OC(O)R7;
  9. при условии: если ни R5, ни R6 не представляют собой F, то, по меньшей мере, один из Y1 и Y2 представляет собой CH2; и
  10. R8 и R9 независимо выбирают из: H, CH2OC(O)R7 , CH2OCO2R7, CH2CH2SC(O)R7 и CH2CH2SSCH2R7;
  11. при условии: если X1 и X2 оба представляют собой O, то, по меньшей мере, один из R8 и R9 не представляет собой H;
  12. где R7 выбирают из: арила, гетероарила, гетероциклоалкила, циклоалкила, C1-20алкила и C1-20алкила, замещенного 1-5 заместителями, независимо выбранными из: арила, циклоалкила, гидрокси и F;
  13. или его фармацевтически приемлемая соль.
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US201662299704P 2016-02-25 2016-02-25
US62/299,704 2016-02-25
US201662327579P 2016-04-26 2016-04-26
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