- Synthesis method of 6-chloro-3-alkyl uracil
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The invention relates to a synthesis method of 6-chloro-3-alkyl uracil, which is characterized by comprising the following steps: by using malonic acid and N-alkyl urea as raw materials, carrying outthe cyclization reaction to generate alkyl tripyrimidone; and then carrying out chlorination on the alkyl tripyrimidone to generate the 6-chloro-3-alkyl uracil. Compared with an existing method, the method is mild in reaction and low in cost, high-cost and high-risk raw materials such as high-toxicity and high-boiling phosphorus oxychloride are not used, and industrial large-scale production is facilitated; meanwhile, the chemical purity obtained by the method is high, the yield is good, and the economic benefit is good.
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Paragraph 0053-0054
(2019/12/02)
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- Barbiturate and thiobarbiturate compounds for use in cancer therapy
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Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.
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Page/Page column 56
(2018/02/28)
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- HETEROCYCLYLMETHYL-THIENOURACILE AS ANTAGONISTS OF THE ADENOSINE-A2B-RECEPTOR
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The present application relates to novel thieno[2,3-d]pyrimidine-2,4-dione (“thienouracil”) derivatives bearing a particular type of (azaheterocyclyl)methyl substituent, to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of pulmonary and cardiovascular disorders and of cancer.
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Paragraph 1240
(2018/03/25)
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- CYCLIC THIENOURACILCARBOXAMIDES AND USE THEREOF
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The present application relates to novel 2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxam ide derivatives ("thienouracil"-carboxamides), to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases and to their use for the preparation of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of pulmonary and cardiovascular disorders.
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Paragraph 0250
(2016/10/08)
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- COMPOUNDS FOR USE IN CANCER THERAPY
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Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxor-ubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds
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Page/Page column 57
(2013/03/26)
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- Microwave-assisted synthesis of 3-aryl-pyrimido[5,4-e][1,2,4]triazine-5, 7(1H,6H)-dione libraries: Derivatives of toxoflavin
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The parallel synthesis of a library of toxoflavin derivatives is described. The microwave-assisted approach involves the de novo generation of the heterocyclic scaffold and allows for facile introduction of a variety of fragments.
- Todorovic, Nick,Giacomelli, Andrew,Hassell, John A.,Frampton, Christopher S.,Capretta, Alfredo
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experimental part
p. 6037 - 6040
(2010/11/21)
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- Synthesis of Paraxanthine Analogs (1,7-Disubstituted Xanthines) and Other Xanthines Unsubstituted at the 3-Position: Structure-Activity Relationships at Adenosine Receptors
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Synthetic procedures for the preparation of various 3-unsubstituted xanthines, including paraxanthine analogs (1,7-disubstituted xanthines) and 1,8-disubstituted xanthines, were developed.Sylylation of 1-substituted xanthines followed by alkylation at the 7-position provides a facile route to paraxanthine analogs.Regioselective alkylation of tris(trimethylsilyl)-6-aminouracil provides 3-substituted 6-aminouracils, which are converted to 1,8-disubstituted xanthines by standard procedures.The ring closure of 3-substituted 5-cyclopentanecarboxamido- and 5-(benzoylamino)-6-aminouracils requires drastic reaction conditions.Affinity for brain A1 and A2 adenosine receptors was determined in binding assays for these and other xanthines with substituents in 1-, 3-, 7-, 8-, and 9-positions.Substitution at the 1-position was necessary for high affinity at adenosine receptors. 1,3-Disubstituted xanthines generally had higher affinity than 1,7-disubstituted xanthines. 1,8-Disubstituted xanthines had high affinity for adenosine receptors; some were highly selective for A1 receptors.
- Mueller, Christa E.,Shi, Dan,Manning, Malcolm,Daly, John W.
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p. 3341 - 3349
(2007/10/02)
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