55899-29-1Relevant academic research and scientific papers
Pyrimidine-4 (3H)-ketone heterocyclic compound, preparation method thereof and application of pyrimidine-4 (3H)-ketone heterocyclic compound in medicine
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Paragraph 0183-0185; 0186-0190, (2021/07/21)
The invention relates to pyrimidine-4 (3H)-ketone heterocyclic compounds suitable for inhibiting or regulating SHP2, a preparation method of the pyrimidine-4 (3H)-ketone heterocyclic compounds and application of the pyrimidine-4 (3H)-ketone heterocyclic compounds in medicine. Specifically, the invention relates to a compound as shown in a general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, a method for treating and/or preventing related diseases mediated by SHP2, especially cancers by using the compound or the pharmaceutically acceptable salt thereof, and a preparation method of the compound or the pharmaceutically acceptable salt thereof. The invention also relates to application of the compound or the pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof in preparation of drugs for treating and/or preventing SHP2-mediated related diseases. Wherein each substituent in the general formula (I) is as defined in the specification.
Divergent and Regioselective Synthesis of Pyrazolo[1,5- a]pyridines and Imidazo[1,5- a]pyridines
Mennie, Katrina M.,Reutershan, Michael H.,White, Catherine,Adams, Bruce,Becker, Bridget,Deng, James,Katz, Jason D.,Lablue, Elisabeth,Margrey, Kaila,Saurí, Josep
, p. 4694 - 4698 (2021/06/28)
Nitrogenous heterocycles are ubiquitous in pharmaceuticals and drug-like compounds; however, regioselective synthesis has proved challenging. Herein we report our efforts to develop a regioselective method for the synthesis of pyrazolo[1,5-a]pyridines and the serendipitous discovery of a protocol for the regioselective formation of imidazo[1,5-a]pyridines. Together, these transformations allow for the rapid and selective formation of two important heterocyclic motifs from a common intermediate.
In Situ Preparation and Consumption of O -Mesitylsulfonylhydroxylamine (MSH) in Continuous Flow for the Amination of Pyridines
Brocklehurst, Cara E.,Koch, Guido,Rothe-P?llet, Stephanie,La Vecchia, Luigi
supporting information, p. 1636 - 1640 (2017/08/11)
The paper demonstrates a safe method in which highly unstable O -mesitylsulfonylhydroxylamine (MSH) can be prepared and consumed in continuous flow. MSH was prepared in situ and used for the flow amination of a range of pyridines, which were subsequently transformed into useful pyrazolopyridine building blocks.
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
Kendall, Jackie D.,O'Connor, Patrick D.,Marshall, Andrew J.,Frédérick, Rapha?l,Marshall, Elaine S.,Lill, Claire L.,Lee, Woo-Jeong,Kolekar, Sharada,Chao, Mindy,Malik, Alisha,Yu, Shuqiao,Chaussade, Claire,Buchanan, Christina,Rewcastle, Gordon W.,Baguley, Bruce C.,Flanagan, Jack U.,Jamieson, Stephen M.F.,Denny, William A.,Shepherd, Peter R.
experimental part, p. 69 - 85 (2012/03/08)
We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model.
