2972-52-3Relevant academic research and scientific papers
Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents
Liu, Lingfeng,Kong, Chengcheng,Fumagalli, Marco,Savková, Karin,Xu, Yiwen,Huszár, Stanislav,Sammartino, José C.,Fan, Dongguang,Chiarelli, Laurent R.,Miku?ová, Katarína,Sun, Zhaogang,Qiao, Chunhua
, (2020)
Decaprenylphosphoryl-β-D-ribose 2′-oxidoreductase (DprE1) is a promising drug target for the development of novel anti-tubercular agents, and inhibitors of DprE1 are being investigated extensively. Among them, the 1,3-benzothiazinone compounds such as BTZ
Substituted pyrimidine compound, pharmaceutical composition thereof and application of compound
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Paragraph 0196-0201, (2021/01/24)
The invention relates to a substituted pyrimidine compound, a pharmaceutical composition thereof and application of the compound. The substituted pyrimidine compound has excellent inhibitory activityon mutant EGFR and mutant HER2, and has excellent pharma
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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Paragraph 001035, (2021/02/19)
This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators.
Substituted pyrazolopyrimidine TAM inhibitor and application thereof
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Paragraph 0270; 0277-0279, (2021/05/08)
The invention relates to the technical field of medicines, in particular to a substituted pyrazolopyrimidine TAM inhibitor compound and pharmaceutically acceptable salt, ester or stereoisomer thereof, a pharmaceutical composition containing the compound,
JNK inhibitor as well as pharmaceutical composition and application thereof
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Paragraph 0406-0409; 0428-0431, (2021/03/31)
The invention provides a compound represented by a formula (I), racemates, stereoisomers, tautomers, isotope markers, solvates, polymorphic substances, nitrogen oxides, or pharmaceutically acceptablesalts thereof, and application as a JNK inhibitor. The invention also provides a preparation method of the compound shown in the formula (I), a pharmaceutical composition containing the compound shownin the formula (I), and application of the compound shown in the formula (I) to preparation of a medicine, and the medicine is used for treating diseases which can be treated by inhibiting the activity of JNK.
Nitrogen-containing heterocyclic compound, pharmaceutical composition and application thereof
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Paragraph 0098; 0100-0102, (2020/03/06)
The invention provides a nitrogen-containing heterocyclic compound shown as general formula (I) in the specification or a pharmaceutically acceptable salt, solvate, active metabolite, polymorph, isotope label or isomer thereof, and further provides a phar
Method for synthesizing 2,4-dichloro-5-pyrimidineformyl chloride
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Paragraph 0018-0032, (2019/11/13)
The invention provides a method for synthesizing 2,4-dichloro-5-pyrimidineformyl chloride. The method comprises the synthesis steps: taking uracil-5-formic acid, phosphorous oxychloride and phosphoruspentachloride, performing mixing, performing heating for a reflux reaction, performing cooling after completion of the reflux reaction, evaporating excessive phosphorus oxychloride, and performing reduced pressure distillation so as to obtain the pure product. The commercially-available uracil-5-formic acid is adopted as a raw material, and 2,4-dichloro-5-pyrimidineformyl chloride is generated through one step of chlorination; the starting materials of the reaction have commercial supply of a large amount, and are cheap and easily available, and auxiliary materials can be recycled, so that the cost is reduced significantly, pollution of toxic substances to the environment in the production process is avoided, and the safety during the operation is improved at the same time; and the yieldis improved greatly, the time is shortened effectively, the operation is simple, and the post-treatment process is simplified.
SYNTHESIS OF CERDULATINIB
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Paragraph 0101, (2019/11/19)
The present disclosure provides processes for the preparation of cerdulatinib, which is of formula (I): Formula (I) or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.
PYRAZOLOPYRIMIDINE DERIVATIVES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR USE IN PREVENTING OR TREATING CANCER, AUTOIMMUNE DISEASE AND BRAIN DISEASE CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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Paragraph 469-472, (2018/12/02)
The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.
Atorvastatin that non-preparation method
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, (2017/07/01)
The invention relates to a preparation method of avanafil and a new compound provided in a preparation process. According to the method, 5-uracil carboxylic acid or an ester thereof is taken as the raw material, and the avanafil meeting the clinical requirements can be synthesized at a relatively cost; besides, the preparation method is simple and convenient to operate, mild in reaction conditions, high in yield, low in cost, environmentally friendly and suitable for industrial large-scale production of the avanafil.
