RU2018123797A - (S) -Isopropyl 2 - ({[(2R, 3R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -3-hydroxy-4,4-difluorotetrahydrofuran-2-yl ] methoxy} phenoxyphosphorylamino) propanoate, nucleoside inhibitor of HCV NS5B RNA polymerase, method for the preparation and use - Google Patents

(S) -Isopropyl 2 - ({[(2R, 3R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -3-hydroxy-4,4-difluorotetrahydrofuran-2-yl ] methoxy} phenoxyphosphorylamino) propanoate, nucleoside inhibitor of HCV NS5B RNA polymerase, method for the preparation and use Download PDF

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Publication number
RU2018123797A
RU2018123797A RU2018123797A RU2018123797A RU2018123797A RU 2018123797 A RU2018123797 A RU 2018123797A RU 2018123797 A RU2018123797 A RU 2018123797A RU 2018123797 A RU2018123797 A RU 2018123797A RU 2018123797 A RU2018123797 A RU 2018123797A
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Prior art keywords
compound
rna polymerase
hcv ns5b
ns5b rna
formula
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RU2018123797A
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Russian (ru)
Inventor
Олег Михайлович Корзинов
Александр Викторович Мелерзанов
Олег Дмитриевич Митькин
Алина Сергеевна Самарская
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Общество с ограниченной ответственностью "Институт клеточных и молекулярных технологий" (ООО "ИКМТ")
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Priority to RU2018123797A priority Critical patent/RU2018123797A/en
Publication of RU2018123797A publication Critical patent/RU2018123797A/en

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Claims (9)

1. Соединение (S)-изопропил 2-({[(2R,3R,5R)-5-(4-амино-2-оксопиримидин-1(2H)-ил)-3-гидрокси-4,4-дифтортетрагидрофуран-2-ил]метокси}феноксифосфориламино)пропионат формулы 1, представленное в виде смеси стереоизомеров по атому фосфора как аморфное стеклообразное вещество:1. The compound (S) -isopropyl 2 - ({[(2R, 3R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -3-hydroxy-4,4-difluorotetrahydrofuran- 2-yl] methoxy} phenoxyphosphorylamino) propionate of formula 1, presented as a mixture of stereoisomers at the phosphorus atom as an amorphous glassy substance:
Figure 00000001
Figure 00000001
 2. Способ получения соединения формулы 1 в аморфной форме, заключающийся во взаимодействии соединения формулы 2 с соединением формулы 32. A method of obtaining a compound of formula 1 in amorphous form, which consists in the interaction of the compounds of formula 2 with the compound of formula 3
Figure 00000002
Figure 00000003
Figure 00000002
Figure 00000003
 3. Активный компонент, обладающий свойствами нуклеозидных ингибиторов РНК-полимеразы HCV NS5B, представляющий собой соединения общей формулы в терапевтически эффективном количестве.3. An active component having the properties of nucleoside inhibitors of HCV NS5B RNA polymerase, which is a compound of the general formula in a therapeutically effective amount. 4. Способ ингибирования РНК-полимеразы HCV NS5B контактированием РНК-полимеразы HCV NS5B с соединением общей формулы 1 или его фармацевтически приемлемой солью.4. A method of inhibiting HCV NS5B RNA polymerase by contacting HCV NS5B RNA polymerase with a compound of general formula 1 or a pharmaceutically acceptable salt thereof. 5. Фармацевтическая композиция, обладающая свойствами ингибитора РНК-полимеразы HCV NS5B, пригодная для лечения и профилактики гепатита С, содержащая в терапевтически эффективном количестве соединение общей формулы 1 или активный компонент по п. 3.5. A pharmaceutical composition having the properties of an HCV NS5B RNA polymerase inhibitor, suitable for the treatment and prevention of hepatitis C, containing in a therapeutically effective amount a compound of general formula 1 or an active component according to claim 3. 6. Лекарственное средство для лечения и профилактики гепатита С, содержащее в эффективном количестве соединение общей формулы 1 или активный компонент по п. 3, или фармацевтическую композицию по п. 5.6. A drug for the treatment and prevention of hepatitis C, containing in an effective amount a compound of general formula 1 or the active component according to claim 3, or a pharmaceutical composition according to claim 5. 7. Способ профилактики и лечения заболевания, обусловленного вирусом гепатита С, введением в терапевтически эффективном количестве активного компонента по п. 3 или фармацевтической композиции по п. 5, или лекарственного средства по п. 6.7. A method for the prevention and treatment of a disease caused by hepatitis C virus, the introduction of a therapeutically effective amount of the active component according to p. 3 or the pharmaceutical composition according to p. 5, or a medicine according to p. 6.
RU2018123797A 2018-06-29 2018-06-29 (S) -Isopropyl 2 - ({[(2R, 3R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -3-hydroxy-4,4-difluorotetrahydrofuran-2-yl ] methoxy} phenoxyphosphorylamino) propanoate, nucleoside inhibitor of HCV NS5B RNA polymerase, method for the preparation and use RU2018123797A (en)

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RU2018123797A RU2018123797A (en) 2018-06-29 2018-06-29 (S) -Isopropyl 2 - ({[(2R, 3R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -3-hydroxy-4,4-difluorotetrahydrofuran-2-yl ] methoxy} phenoxyphosphorylamino) propanoate, nucleoside inhibitor of HCV NS5B RNA polymerase, method for the preparation and use

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RU2018123797A RU2018123797A (en) 2018-06-29 2018-06-29 (S) -Isopropyl 2 - ({[(2R, 3R, 5R) -5- (4-amino-2-oxopyrimidin-1 (2H) -yl) -3-hydroxy-4,4-difluorotetrahydrofuran-2-yl ] methoxy} phenoxyphosphorylamino) propanoate, nucleoside inhibitor of HCV NS5B RNA polymerase, method for the preparation and use

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