- Preparation method of sulfadoxine
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The invention provides a preparation method of sulfadoxine. The method is a preparation method of sulfadimethoxine, and the sulfadimethoxine product is prepared by directly taking 4-chloro-5, 6-dimethoxypyrimidine and sodium sulfanilamide as raw materials through a condensation reaction. The method is simple in process, free of special requirements on equipment, simple and convenient to operate, good in product quality and suitable for industrial production.
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Paragraph 0030-0032
(2021/03/11)
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- Phenyl substituted 4-hydroxypyridazin-3(2 H)-ones and 5-hydroxypyrimidin-4(3 H)-ones: Inhibitors of influenza a endonuclease
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Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Our earlier studies identified a series of 5- and 6-phenyl substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza endonuclease. These agents identified as bimetal chelating ligands binding to the active site of the enzyme. In the present study, several aza analogues of these phenyl substituted 3-hydroxypyridin-2(1H)-one compounds were synthesized and evaluated for their ability to inhibit the endonuclease activity. In contrast to the 4-aza analogue of 6-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one, the 5-aza analogue (5-hydroxy-2-(4-fluorophenyl)pyrimidin-4(3H)-one) did exhibit significant activity as an endonuclease inhibitor. The 6-aza analogue of 5-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one (6-(4-fluorophenyl)-4-hydroxypyridazin-3(2H)-one) also retained modest activity as an inhibitor. Several varied 6-phenyl-4-hydroxypyridazin-3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones were synthesized and evaluated as endonuclease inhibitors. The SAR observed for these aza analogues are consistent with those previously observed with various phenyl substituted 3-hydroxypyridin-2(1H)-ones.
- Sagong, Hye Yeon,Bauman, Joseph D.,Patel, Disha,Das, Kalyan,Arnold, Eddy,Lavoie, Edmond J.
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p. 8086 - 8098
(2014/12/10)
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- THERAPEUTIC HYDROXYPYRIDINONES, HYDROXYPYRIMIDINONES AND HYDROXYPYRIDAZINONES
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The invention provides compounds of formula (I): and salts and prodrugs thereof wherein R4, X1 and X2 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts and methods for their use in therapy. The compounds have useful antiviral properties.
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Page/Page column 62
(2014/04/03)
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- INDOL DERIVATIVES USEFUL FOR THE TREATMENT OF MIGRAINE, COMPOSITION AND UTILIZATION
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Indole derivatives having the Formula (I) wherein R1 is H, alkyl or acyl group; R2 is H, halogen or alkyl, hydroxy, alkoxy; ciano, carboxamide, carboxyl, alkoxicarbonyl, phenyl, phenyloxy or a group -(CH2)n-R6, (n=1-3), and R6 is a group ciano, nitro, phenyl, carboxyl, -CO2R7; -CONR7R8; -SO2NR7R8; -COR7; -SO2R7, R7 and R8 being H or alkyl; R7 and R8, together with N, can form a cycle of 4-7 links; R3, R4 and R5 are H, halogen or a group alkyl, phenyl, substituted phenyl, hydroxy, alcoxy, phenyloxy or benziloxy; NR11R12 is H or a group ciano, nitro, carboxyl, alcoxycarbonyl, carboxamido or a group R3; A is an alkyliden group -(CH2)-m, (m = 1-5), or alkenyl group; B is a piperazinoring (a), aminopyrrolidinoring (b); pyrrolidinamino ring (c); piperidinoring (d) or ethylendiamino -NR9-CH2-CH2-NR10-, R9 and R10 being H or an alkyl group. The compounds are useful for the treatment of migraine.
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