127116-19-2Relevant academic research and scientific papers
Synthesis of N-pyrimidin[1,3,4]oxadiazoles and N-pyrimidin[1,3,4]-thiadiazoles from 1,3,4-oxadiazol-2-amines and 1,3,4-thiadiazol-2-amines via Pd-catalyzed heteroarylamination
Yan, Longjia,Deng, Minggao,Chen, Anchao,Li, Yongliang,Zhang, Wanzheng,Du, Zhi-yun,Dong, Chang-zhi,Meunier, Bernard,Chen, Huixiong
supporting information, p. 1359 - 1362 (2019/04/25)
An efficient and practical procedure was developed to prepare various N-pyrimidin[1,3,4]oxadiazole and thiadiazole scaffolds using a Buchwald-type coupling. The products of this reaction are otherwise difficult to access and could be used as building bloc
Diazole derivative as well as preparation method and application thereof
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Paragraph 0066-0068, (2019/12/02)
The invention belongs to the technical field of medicines, and particularly relates to a diazole derivative as well as a preparation method and application thereof. The invention provides a diazole derivative. The structural formula of the diazole derivative is shown as a formula (I); the diazole derivative is novel in structure, has good water solubility, has a strong inhibition effect on tyrosine kinase and tumor cells, can be used as a tyrosine kinase inhibitor, and has a good application prospect in preparation of antitumor drugs.
Synthesis method of dasatinib intermediate
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Paragraph 0025; 0028; 0029; 0030; 0031, (2017/05/16)
The invention discloses a synthesis method of a dasatinib intermediate. The method comprises the following steps: taking 2-methyl-4-amino-6-chloropyridine and bi(2-chloroethyl)amine to react to generate 2-methyl-6-chloro-pyridine-4-yl piperazine; and taking the 2-methyl-6-chloro-pyridine-4-yl piperazine and 2-ethylene chlorohydrin to react to generate 2-[4-(2-methyl-6-chloro-pyridine-4-yl)piperazine-1-yl]ethanol. The method disclosed by the invention has the advantages of simplicity and easiness of obtaining raw materials, simplicity in operation, high product yield, high purity and easiness of industrial production.
Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors
Francini, Cinzia Maria,Fallacara, Anna Lucia,Artusi, Roberto,Mennuni, Laura,Calgani, Alessia,Angelucci, Adriano,Schenone, Silvia,Botta, Maurizio
, p. 2027 - 2041 (2015/12/23)
Src family kinases (SFKs) are a family of non-receptor tyrosine kinases (TKs) implicated in the regulation of many cellular processes. The aberrant activity of these TKs has been associated with the growth and progression of cancer. In particular, c-Src i
HETEROCYCLIC COMPOUND
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Paragraph 0605, (2015/01/18)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
SYNTHESIS PROCESS OF DASATINIB AND INTERMEDIATE THEREOF
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Paragraph 0138; 0139, (2013/03/26)
Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.
SYNTHESIS PROCESS OF DASATINIB AND INTERMEDIATE THEREOF
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Page/Page column 16, (2013/02/27)
Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.
THIAZOLE INHIBITORS TARGETING RESISTANT AND KINASE MUTATIONS
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Page/Page column 36, (2010/11/27)
A compound is provided, having the general structure (A): wherein A is an aryl or heteroaryl group, Y is a hydrophobic linking moiety, and L is a substitutent. The compound (A) can be used for treatment of various angiogenic-associated or hematologic disorders, such as myeloproliferative disorders in patients who do not respond to kinase-inhibition therapy that comprises administering currently used medications.
PYRIMIDINE COMPOUNDS AND METHODS OF USE
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Page/Page column 108, (2010/11/24)
The invention provides pyrimidine compounds having formula (A): The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, and various other specific receptor and non-receptor kinases.
Benzotriazine inhibitors of kinases
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Page/Page column 78, (2008/06/13)
The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
