RU2016148641A - Isopropyl N - [{[(1R) -2- (6-amino-9H-purin-9-yl) -1-methylethoxy] methyl} (1,3-benzothiazol-6-yl-hydroxy) phosphoryl] -L- alaninate fumarate as an antiviral drug - Tenofovir prodrugs - Google Patents

Isopropyl N - [{[(1R) -2- (6-amino-9H-purin-9-yl) -1-methylethoxy] methyl} (1,3-benzothiazol-6-yl-hydroxy) phosphoryl] -L- alaninate fumarate as an antiviral drug - Tenofovir prodrugs Download PDF

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Publication number
RU2016148641A
RU2016148641A RU2016148641A RU2016148641A RU2016148641A RU 2016148641 A RU2016148641 A RU 2016148641A RU 2016148641 A RU2016148641 A RU 2016148641A RU 2016148641 A RU2016148641 A RU 2016148641A RU 2016148641 A RU2016148641 A RU 2016148641A
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Prior art keywords
alaninate
methylethoxy
purin
benzothiazol
phosphoryl
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RU2016148641A
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Russian (ru)
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RU2665037C2 (en
RU2016148641A3 (en
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Андрей Владимирович Сизюхин
Михаил Айратович Шафеев
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Общество с ограниченной ответственностью "Вириом"
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings
    • C07F9/6541—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (8)

1. Соединение общей формулы 1:1. The compound of General formula 1:
Figure 00000001
Figure 00000001
 2. Фармацевтическая композиция, обладающая противовирусными свойствами по отношению к вирусам гепатита Б и ВИЧ, содержащая в качестве активного компонента соединение общей формулы 1 по пп. 1 в терапевтически эффективном количестве.2. A pharmaceutical composition having antiviral properties against hepatitis B and HIV viruses, containing, as an active component, a compound of general formula 1 according to claims. 1 in a therapeutically effective amount. 3. Фармацевтическая композиция по п. 2 для использования в форме таблеток, капсул или инъекций, помещенных в фармацевтически приемлемую упаковку.3. The pharmaceutical composition according to claim 2 for use in the form of tablets, capsules or injections, placed in a pharmaceutically acceptable package. 4. Способ лечения вирусного гепатита Б и ВИЧ, включающий введение указанному пациенту терапевтически эффективного количества соединения по пп. 1 или фармацевтической композиции по пп. 2 или 3.4. A method of treating viral hepatitis B and HIV, comprising administering to a specified patient a therapeutically effective amount of a compound according to claims. 1 or a pharmaceutical composition according to claims 2 or 3. 5. Способ получения соединения общей формулы 1 по п. 1, включающий постадийное проведение реакций по схеме 1 в подходящем растворителе или смеси растворителей5. A method for producing a compound of general formula 1 according to claim 1, comprising the stepwise carrying out of reactions according to scheme 1 in a suitable solvent or mixture of solvents
Figure 00000002
Figure 00000002
Figure 00000003
Figure 00000003
RU2016148641A 2016-12-12 2016-12-12 Isopropyl n-[{[(1r)-2-(6-amino-9h-purin-9-il)-1-methyletoxy]methyl} (1,3-benzotiazol-6-il-oxy)phosphoryl]-l-alaninate fumarat as an antiviral drug - prodrug of tenofovir RU2665037C2 (en)

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RU2016148641A RU2665037C2 (en) 2016-12-12 2016-12-12 Isopropyl n-[{[(1r)-2-(6-amino-9h-purin-9-il)-1-methyletoxy]methyl} (1,3-benzotiazol-6-il-oxy)phosphoryl]-l-alaninate fumarat as an antiviral drug - prodrug of tenofovir

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RU2016148641A RU2665037C2 (en) 2016-12-12 2016-12-12 Isopropyl n-[{[(1r)-2-(6-amino-9h-purin-9-il)-1-methyletoxy]methyl} (1,3-benzotiazol-6-il-oxy)phosphoryl]-l-alaninate fumarat as an antiviral drug - prodrug of tenofovir

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022180003A1 (en) * 2021-02-24 2022-09-01 F. Hoffmann-La Roche Ag Benzothiazolyl bicyclo[1.1.1]pentane derivatives for the treatment and prophylaxis of hepatitis b virus infection

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA81797C2 (en) * 2003-01-14 2008-02-11 Гилиад Сайенсиз, Инк. Pharmaceutical dosage of tenofovir disoproxil fumarate and emtricitabine for combination antiviral therapy
ES2532502T3 (en) * 2006-07-12 2015-03-27 Mylan Laboratories Limited Tenofovir preparation process

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022180003A1 (en) * 2021-02-24 2022-09-01 F. Hoffmann-La Roche Ag Benzothiazolyl bicyclo[1.1.1]pentane derivatives for the treatment and prophylaxis of hepatitis b virus infection

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