660406-84-8Relevant academic research and scientific papers
CONDENSED-RING PYRIMIDYLAMINO DERIVATIVE, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF
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Paragraph 0225; 0226, (2018/03/25)
Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b' to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.
SUBSTITUTED PYRAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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Paragraph 0251, (2017/05/27)
There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin and/or kallikrein, which compounds include substituted pyrazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which diseases or disorders are amenable to treatment or prevention by the inhibition of thrombin and/or kallikrein.
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)
Patel, Snahel,Harris, Seth F.,Gibbons, Paul,Deshmukh, Gauri,Gustafson, Amy,Kellar, Terry,Lin, Han,Liu, Xingrong,Liu, Yanzhou,Liu, Yichin,Ma, Changyou,Scearce-Levie, Kimberly,Ghosh, Arundhati Sengupta,Shin, Young G.,Solanoy, Hilda,Wang, Jian,Wang, Bei,Yin, Jianping,Siu, Michael,Lewcock, Joseph W.
, p. 8182 - 8199 (2015/11/09)
Recent data suggest that inhibition of dual leucine zipper kinase (DLK, MAP3K12) has therapeutic potential for treatment of a number of indications ranging from acute neuronal injury to chronic neurodegenerative disease. Thus, high demand exists for selective small molecule DLK inhibitors with favorable drug-like properties and good CNS penetration. Herein we describe a shape-based scaffold hopping approach to convert pyrimidine 1 to a pyrazole core with improved physicochemical properties. We also present the first crystal structures of DLK. By utilizing a combination of property and structure-based design, we identified inhibitor 11, a potent, selective, and brain-penetrant inhibitor of DLK with activity in an in vivo nerve injury model.
3-SUBSTITUTED PYRAZOLES AND USE AS DLK INHIBITORS
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Page/Page column 153, (2014/08/06)
The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. (I) In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach - Part 1
Dwyer, Michael P.,Paruch, Kamil,Labroli, Marc,Alvarez, Carmen,Keertikar, Kerry M.,Poker, Cory,Rossman, Randall,Fischmann, Thierry O.,Duca, Jose S.,Madison, Vincent,Parry, David,Davis, Nicole,Seghezzi, Wolfgang,Wiswell, Derek,Guzi, Timothy J.
scheme or table, p. 471 - 474 (2011/02/26)
The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a] pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such as compound 17r. In the Letter, the further utility of the pyrazolo[1,5-a]pyrimidine template fo
