RU2020108580A - Лекарственное соединение и способы его очистки - Google Patents

Лекарственное соединение и способы его очистки Download PDF

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RU2020108580A
RU2020108580A RU2020108580A RU2020108580A RU2020108580A RU 2020108580 A RU2020108580 A RU 2020108580A RU 2020108580 A RU2020108580 A RU 2020108580A RU 2020108580 A RU2020108580 A RU 2020108580A RU 2020108580 A RU2020108580 A RU 2020108580A
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composition
formula
compound
substituted
nucleotide
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RU2020108580A
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Раджашри ДЖОШИ-ХАНГАЛ
Нипун ДАВАР
Стефен Р. ПРЕБЕ
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Оцука Фармасьютикал Ко., Лтд.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/04Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7084Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/173Purine radicals with 2-deoxyribosyl as the saccharide radical
    • FMECHANICAL ENGINEERING; LIGHTING; HEATING; WEAPONS; BLASTING
    • F26DRYING
    • F26BDRYING SOLID MATERIALS OR OBJECTS BY REMOVING LIQUID THEREFROM
    • F26B5/00Drying solid materials or objects by processes not involving the application of heat
    • F26B5/04Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum
    • F26B5/06Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum the process involving freezing

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  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
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  • General Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (48)

1. Композиция, содержащая
a) соединение формулы
Figure 00000001
формула (1),
или его фармацевтически приемлемую соль,
где композиция содержит, по крайней мере, 95% соединения формулы (1); и
b) соединение на основе нуклеотида, которое не является соединением формулы (1).
2. Композиция по п.1, где соединение на основе нуклеотида представляет собой соединение формулы (2)
Figure 00000002
формула (2),
или его фармацевтически приемлемая соль, где R1 представляет собой гетероарил или карбамид, каждый из которых независимо замещен или не замещен; каждый R2 и R3 независимо представляет собой алкил, который замещен или не замещен; или водород; и R4 представляет собой водород или ацильную группу, каждая из которых независимо замещена или не замещена.
3. Композиция по п.2, где R1 представляет собой карбамид, который незамещен.
4. Композиция по п.2, где R1 представляет собой гетероарил.
5. Композиция по п.4, где R1 представляет собой 4-амино-2H-1λ2,3,5-триазин-2-он.
6. Композиция по п.2, где каждый R2 и R3 представляет собой замещенный алкил или водород.
7. Композиция по п.6, где R2 представляет собой H и R3 представляет собой метил, замещенный метокси.
8. Композиция по п.2, где R4 представляет собой водород.
9. Композиция по п.2, где R4 представляет собой ацильную группу.
10. Композиция по п.2, где соединение формулы (2) представляет собой
Figure 00000003
.
11. Композиция по п.2, где соединение формулы (2) представляет собой
Figure 00000004
.
12. Композиция по п.2, где соединение формулы (2) представляет собой
Figure 00000005
.
13. Композиция по п.2, где соединение формулы (2) представляет собой
Figure 00000006
.
14. Композиция по п.2, где соединение на основе нуклеотида представляет собой соединение формулы (3)
Figure 00000007
формула (3),
или его фармацевтически приемлемую соль, где R1 представляет собой гетероарил или карбамид, каждый из которых независимо замещен или не замещен.
15. Композиция по п.14, где R1 представляет собой гетероарил.
16. Композиция по п.15, где R1 представляет собой 4-амино-2H-1λ2,3,5-триазин-2-он.
17. Композиция по п.14, где R1 представляет собой карбамид, который замещен.
18. Композиция по п.14, где соединение формулы (3) представляет собой
Figure 00000008
.
19. Композиция по п.14, где соединение формулы (3) представляет собой
Figure 00000009
.
20. Композиция по п.1, где соединение на основе нуклеотида представляет собой соединение формулы (4)
Figure 00000010
формула (4),
или его фармацевтически приемлемую соль, где R1 представляет собой гетероарил, который замещен или не замещен; и R5 представляет собой гидрокси или нуклеотид.
21. Композиция по п.20, где R1 представляет собой гетероарил, который замещен.
22. Композиция по п.21, где R1 представляет собой 4-амино-2H-1λ2,3,5-триазин-2-он.
23. Композиция по п.21, где R1 представляет собой 2-амино-9λ2-пурин-6(1H)-он.
24. Композиция по п.20, где R5 представляет собой гидроксильную группу.
25. Композиция по п.20, где R5 представляет собой нуклеотид.
26. Композиция по п.25, где нуклеотид имеет формулу
Figure 00000011
.
27. Композиция по п.20, где соединение формулы (4) представляет собой
Figure 00000012
28. Композиция по п.20, где соединение формулы (4) представляет собой
Figure 00000013
.
RU2020108580A 2017-08-03 2018-08-02 Лекарственное соединение и способы его очистки RU2020108580A (ru)

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US201762540706P 2017-08-03 2017-08-03
US62/540,706 2017-08-03
PCT/IB2018/000992 WO2019025863A2 (en) 2017-08-03 2018-08-02 MEDICAMENT COMPOUND AND METHODS OF PURIFICATION

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US10858386B2 (en) 2020-12-08
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RU2020108580A3 (ru) 2022-01-27
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BR112020002280A2 (pt) 2020-07-28
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