39825-33-7Relevant articles and documents
Preparation methods of tenofovir alafenamide fumarate isomer impurities
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Paragraph 0093; 0095, (2020/07/13)
The invention discloses preparation methods of tenofovir alafenamide fumarate isomer impurities, which comprise preparation methods of four isomer impurities, specifically, preparation methods of 9-{(R)-2-[((R)-{[(R)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine, 9-{(R)-2-[((R)-{[(S)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine, 9-{(R)-2-[((S)-{[(R)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine and 9-{(S)-2-[((R)-{[(R)-1-(isopropoxycarbonyl) ethyl] amino}-phenoxy phosphoryl) methoxy] propyl} adenine. The preparation methods of tenofovir alafenamide fumarate isomer impurities have the beneficial effects that the methods are simple and easy to implement, raw materials are easy to obtain, conditions are mild, cost is low, production is facilitated, and meanwhile the obtained isomer impurity has important significance in preparing high-purity tenofovir alafenamide fumarate.
Antiviral novel nucleoside reverse transcriptase inhibitors
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Paragraph 0317; 0318; 0320; 0321; 0322, (2019/02/25)
The invention relates to compounds of antiviral novel nucleoside reverse transcriptase inhibitors, pharmaceutical compositions containing the compounds, and preparation and use of the compounds, and particularly discloses fused pyrimidine compounds shown in formula (I) and the pharmaceutical compositions containing the compounds, pharmaceutically acceptable salts, stereoisomers, solvates, hydrates, crystal forms, prodrugs or isotope derivatives. The compounds can be used for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV). The formula (I) is shown in the specification.
Tenofovir diester compounds and salts thereof, preparation method and medicine application of compounds
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Paragraph 0056-0063, (2019/03/24)
The invention discloses tenofovir diester compounds (Ia) as well as salts of the compounds, diastereoisomers (Ib) of the compounds and salts of (Ib). The invention also discloses a preparation methodand pharmaceutical composition containing the compounds. Tests prove that the compounds have activity of inhibiting HIV-1/HBV replication, and meanwhile, the compounds have the advantages of higher lipid solubility, higher bioavailability, higher activity, lower toxicity and the like than existing TDF (tenofovir disoproxil fumarate) and TAF (tenofovir alafenamide fumarate) medicines for treating AIDS. Experiments also prove that the compounds have activity of inhibiting HBV replication and can be applied to development of medicines for treating AIDS or hepatitis B.
Puerarin derivative and preparation method and application thereof
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Paragraph 0066; 0067, (2019/04/06)
The invention relates to a puerarin derivative and a preparation method and an application thereof. The puerarin derivative is prepared through six steps of reactions by taking puerarin and L-alanineisopropyl ester hydrochloride as main raw materials. The puerarin derivative not only has good water solubility, but also has good anti-platelet aggregation action and can be used for preparing anti-platelet aggregation drugs. In addition, the reaction conditions of the reactions for preparing the puerarin derivative are mild, and the synthetic method is simple.
HCV POLYMERASE INHIBITORS
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Page/Page column 76; 77, (2020/02/14)
The invention provides compounds of the formula:wherein B is a nucleobase selected from the groups (a) to (d):and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
COMBINATION THERAPY COMPRISING TENOFOVIR ALAFENAMIDE HEMIFUMARATE AND COBICISTAT FOR USE IN THE TREATMENT OF VIRAL INFECTIONS
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Paragraph 0296; 0297, (2017/08/01)
The use of the hemifumarate form of {9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine} (tenofovir alafenamide hemifumarate) in combination with cobicistat is disclosed. In addition, the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and elvitegravir, and the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and darunavir, are disclosed.
DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
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Page/Page column 47, (2016/03/22)
The invention provides compounds of formula (I), wherein: R1 is OR11, or NR5R5'; R2 is H or F; R5 is H, C1-C6alkyl, OH, C(=O)R6, O(C=O)R6 or O(C=O)OR6; R5′ is H or C1-C6alkyl; R6 is C1-C6alkyl or C3-C7cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.
HCV POLYMERASE INHIBITORS
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Page/Page column 66, (2015/05/05)
The invention provides compounds of the formula (I) wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
AN IMPROVED PROCESS FOR THE PREPARATION OF TENOFOVIR ALAFENAMIDE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Page/Page column 18, (2015/04/15)
The present invention provides an improved process for the preparation of Tenofovir alafenamide or pharmaceutically acceptable salts thereof in high yield and purity. Also provided is a process for the separation of diastereomers of Tenofovir alafenamide by simulated moving bed chromatography or preparative high performance liquid chromatography.
HCV POLYMERASE INHIBITORS
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Page/Page column 64, (2015/03/28)
The invention provides compounds of the formula:(I) wherein B is a nucleobase selected from the groups (a) to (d) and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.