- Raltitrexed pharmaceutical composition and preparation method thereof
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The invention relates to a raltitrexed pharmaceutical composition which is high in safety and a preparation method thereof. The raltitrexed pharmaceutical composition comprises raltitrexed and thiophene related substances, wherein the content of the thiophene related substances is not higher than 0.3%. The raltitrexed pharmaceutical composition is good in safety, effectiveness and stability and can relieve the blood toxicity of the raltitrexed to a certain degree.
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- Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists
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A novel series of 2-(phenoxyaryl)-3-urea derivatives were designed, synthesized, and biologically evaluated for their anti-thrombotic activity. Most of compounds exhibited good inhibition against P2Y1 receptor. Among them, three compounds 11, 12, and 13 demonstrated good P2Y1 receptor antagonistic potency in vitro (IC50 = 0.62 μM, 0.82 μM, and 0.21 μM, respectively). In antiplatelet aggregation study, four compounds 2, 3, 9, and 13 showed good antiplatelet activity. The possible binding modes of compounds with P2Y1 receptor were also explored by molecular docking simulation. The docking studies demonstrated that compound 13 interacted well with Phe119 through hydrophobic interaction and modestly improved the P2Y1 receptor antagonistic activity, making it justifiable for further investigation.
- Peng, Jingjing,Zhao, Lifen,Wang, Lanlan,Chen, Hui,Qiu, Yunguang,Wang, Jiang,Yang, Huaiyu,Liu, Jun,Liu, Hong
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p. 302 - 310
(2018/09/18)
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- Improved modular synthesis of thieno[3,2-b]pyrroles and thieno[2,3-b]pyrroles
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A convenient modular synthesis for the construction of densely functionalized thieno[3,2-b]pyrroles, allosteric inhibitors of the Hepatitis C virus NS5B polymerase, is described. The route allows the introduction of substituents in positions 4, 5, and 6 o
- Malancona, Savina,Hernando, Josè I. Martin,Attenni, Barbara,Ontoria, Jesus M.,Narjes, Frank
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supporting information; experimental part
p. 1625 - 1628
(2009/06/18)
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- Novel acyl hydrazino thiophene derivatives, process for preparing them, their use as medicinal products, pharmaceutical compositions and novel use
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The invention concerns novel compounds of formula (I), process for making, pharmaceutical compositions and methods of treating diseases associated with abnormal physiological behavior in the secretion and/or the activity of cysteine proteases especially c
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Page/Page column 20
(2010/02/12)
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- THIENOPYRROLES AS ANTIVIRAL AGENTS
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The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
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Page/Page column 50
(2008/06/13)
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- Hypolipidemic and antiatherosclerotic novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs
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This disclosure described novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.
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