RU2021109549A - ИНГИБИТОРЫ α-АМИНО-β-КАРБОКСИМУКОНАТ ε-СЕМИАЛЬДЕГИД-ДЕКАРБОКСИЛАЗЫ - Google Patents

ИНГИБИТОРЫ α-АМИНО-β-КАРБОКСИМУКОНАТ ε-СЕМИАЛЬДЕГИД-ДЕКАРБОКСИЛАЗЫ Download PDF

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RU2021109549A
RU2021109549A RU2021109549A RU2021109549A RU2021109549A RU 2021109549 A RU2021109549 A RU 2021109549A RU 2021109549 A RU2021109549 A RU 2021109549A RU 2021109549 A RU2021109549 A RU 2021109549A RU 2021109549 A RU2021109549 A RU 2021109549A
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Роберто Пелличари
Йохан АУВЕРКС
Надия РАФФАЭЛЛИ
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Тес Фарма С.Р.Л.
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Claims (21)

  1. Соединение, представленное формулой (I)
  2. Figure 00000001
  3. или его фармацевтически приемлемая соль или таутомер,
  4. где в указанной формуле
  5. X представляет собой O, OH или Cl;
  6. L представляет собой -(CH2)mCH2CH2-, -(CH2)mY(CH2)p-, -(CH2)mC(O)(CH2)p-, -(CH2)mC(O)O(CH2)p-, -(CH2)mC(O)NR2(CH2)p- или -(CH2)mNR2C(O)(CH2)p;
  7. Y представляет собой O, N или S(O)q;
  8. R1 представляет собой (C6-C10)арил или гетероарил, где арил и гетероарил замещены Ra и Rb и, необязательно, замещены одним или несколькими Re;
  9. R2 представляет собой H или (C1-C6)алкил;
  10. один из Ra и Rb представляет собой водород, и другой представляет собой -(CH2)rCO2Rx, -OCH2CO2Rx, -(CH2)rтетразол, -(CH2)rоксадиазолон, -(CH2)rтетразолон, -(CH2)rтиадиазолол, -(CH2)rизоксазол-3-ол, -(CH2)rP(O)(OH)ORx, -(CH2)rS(O)2OH, -(CH2)rC(O)NHCN или -(CH2)rC(O)NHS(O)2алкил;
  11. Rc представляет собой H, (C1-C6)алкил, (C1-C6)галогеналкил, галоген, -CN, -ORx, CO2Rx или NO2;
  12. Rd представляет собой метил, необязательно замещенный 5-10-членный арил, необязательно замещенный 5- или 6-членный гетероарил или необязательно замещенный 5- или 6-членный карбоцикл;
  13. каждый Rx при каждом появлении представляет собой независимо водород или (C1-C6)алкил;
  14. каждый Re представляет собой независимо (C1-C6)алкил, (C2-C6)алкенил, (C2-C6)алкинил, галоген, -ORy, (C1-C6)галогеналкил, -NHRz, -OH или -CN;
  15. Rf представляет собой H или отсутствует;
  16. каждый Ry и Rz представляет собой независимо водород, (C1-C6)алкил или (C1-C6)галогеналкил;
  17. каждый m и p равен независимо 0, 1 или 2, где m+p <3;
  18. q равен 0, 1 или 2;
  19. r равен 0 или 1; и
  20. пунктирная линия представляет собой необязательную двойную связь;
  21. при условии, что Rc не является водородом или -CN, когда X представляет собой O, L представляет собой -SCH2-, и Rd представляет собой необязательно замещенный фенил, Rc не является (C1-C6)алкилом, когда X представляет собой O, L представляет собой -SCH2-, и Rd представляет собой метил, и что Rc не является -CN, когда X представляет собой O, L представляет собой -SCH2-, и Rd представляет собой 2-фурил.
RU2021109549A 2014-08-29 2015-08-28 ИНГИБИТОРЫ α-АМИНО-β-КАРБОКСИМУКОНАТ ε-СЕМИАЛЬДЕГИД-ДЕКАРБОКСИЛАЗЫ RU2021109549A (ru)

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TW202033516A (zh) * 2018-11-20 2020-09-16 義大利商Ｔｅｓ製藥（股份）責任有限公司 α-胺基-β-羧基己二烯二酸半醛去羧酶之抑制劑
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CN114409603B (zh) * 2022-01-20 2023-11-07 中国药科大学 一种嘧啶酮硫醚类化合物及其应用
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