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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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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.
RU2020113165A 2015-12-03 2016-12-01 Циклические пуриновые динуклеотиды в качестве модуляторов sting RU2020113165A (ru)

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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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