- Prodrugs of baloxvir and derivatives thereof and preparation method and application of prodrugs
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The present invention provides a compound having a structure represented by formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof, where X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, (R9) m in the formula (I) are defined as in the description and claims of the present invention. The compound is a prodrug of baloxavir and a derivative thereof, and the bioavailability of the compound is greatly improved compared with the bioavailability of the existing baloxavir marboxil. The compound is better than Baloxavir marboxil in the aspects of reducing the dosage, reducing the side effect of the medicine and improving the medicine effect, and can be used as a medicine for treating and/or preventing influenza virus infectious diseases.
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Paragraph 0047-0050
(2021/05/05)
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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The present invention provides a compound of formula (II): an inhibitor of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases. Its prodrugs are disclosed.
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Page/Page column 105; 106; 107
(2019/07/20)
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- Preparation method of liconazole sulfate and intermediate thereof (by machine translation)
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The preparation method disclosed by the invention has, the advantages that the preparation process efficiency of the idazooconazole sulfate and the. intermediate thereof is higher by no need C2 for column A4 chromatography and purification . and the method disclosed by, the invention only needs. to be subjected to deprotecting A4 and ion exchange by simple purification. (by machine translation)
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- Preparation method of [N-methyl-pyridine-2-yl] carbamate-1-ethyl chloride
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The invention relates to a preparation method of [N-methyl-N-3-((tert-butoxycarbonyl methyl amino) acetoxy methyl) pyridine-2-yl] carbamate-1-ethyl chloride. The method is as below: first reacting 2-(N-methyl amino)-3- hydroxymethyl pyridine with Boc-sarcosine at low temperature; and reacting with 1-chloroethyl chloroformate. The invention has the advantages of mild reaction condition and simple process and high purity of products, and meets the basic requirements of industrial enlargement production.
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Paragraph 0033; 0034
(2017/01/26)
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- N-substituted carbamoyloxyalkyl-azolium derivatives
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N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.
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Page/Page column 21-22; 36
(2010/02/09)
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- Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
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A highly potent water soluble triazole antifungal prodrug, RO0098557 (1), has been identified from its parent, the novel antifungal agent RO0094815 (2). The prodrug includes a triazolium salt linked to an aminocarboxyl moiety, which undergoes enzymatic activation followed by spontaneous chemical degradation to release 2. Prodrug 1 showed high chemical stability and water solubility and exhibited strong antifungal activity against systemic candidiasis and aspergillosis as well as pulmonary aspergillosis in rats.
- Ohwada, Jun,Tsukazaki, Masao,Hayase, Tadakatsu,Oikawa, Nobuhiro,Isshiki, Yoshiaki,Fukuda, Hiroshi,Mizuguchi, Eisaku,Sakaitani, Masahiro,Shiratori, Yasuhiko,Yamazaki, Toshikazu,Ichihara, Shigeyasu,Umeda, Isao,Shimma, Nobuo
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p. 191 - 196
(2007/10/03)
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