1057393-44-8Relevant articles and documents
Metal free [4+1] and [5+1] annulation reactions to prepare heterocycles using DMF and its derivatives as one-carbon source
Liu, Lingfeng,Qiao, Chunhua,Shen, Bei,Xu, Yiwen
supporting information, (2020/04/01)
1,2,4-Triazolo[3,4-a]pyridines and related heterocycles and substituted triazines were commonly discovered scaffolds in a variety of pharmaceutical and agrochemical agents. Herein, we report a highly efficient and practical method using DMF and its derivative for the [4+1] and [5+1] annulation reactions to prepare these heterocycles. This metal free reaction takes advantages of shelf stable DMF as solvent and carbon donor, imidazole chloride as a catalyst, the mild reaction condition tolerates a broad substrate range and substitutes. The prepared 3-unsubstituted 1,2,4-triazolo[3,4-a]pyridine and derivatives allow further introduction of a variety of functional group1 at 3-position.
HISTONE DEMETHYLASE INHIBITORS
-
Paragraph 0146; 0148; 0185; 186, (2017/11/06)
The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.
OXAZOLIDINONE COMPOUNDS AND DERIVATIVES THEREOF
-
Paragraph 0187-0188, (2013/09/26)
Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors
Aiguadé, Josep,Balagué, Cristina,Carranco, Inés,Caturla, Francisco,Domínguez, María,Eastwood, Paul,Esteve, Cristina,González, Jacob,Lumeras, Wenceslao,Orellana, Adelina,Preciado, Sara,Roca, Ramón,Vidal, Laura,Vidal, Bernat
experimental part, p. 3431 - 3436 (2012/06/18)
A new class of p38α inhibitors based on a biaryl-triazolopyridine scaffold was investigated. X-ray crystallographic data of the initial lead compound cocrystallised with p38α was crucial in order to uncover a unique binding mode of the inhibitor to the hinge region via a pair of water molecules. Synthesis and SAR was directed towards the improvement of binding affinity, as well as ADME properties for this new class of p38α inhibitors and ultimately afforded compounds showing good in vivo efficacy.
CANNABINOID RECEPTOR MODULATORS
-
Page/Page column 115, (2012/09/11)
Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor.
NEW 7-PHENYL-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3(2H)-ONE DERIVATIVES
-
Page/Page column 31-32, (2011/06/16)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to processes for their preparation, to pharmaceutical compositions comprising them, and to their use in therapy.
New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
-
Page/Page column 16, (2011/06/10)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to pharmaceutical compositions comprising them, and to their use in therapy.
NEW 3-([1,2,4]TRIAZOLO[4,3-A]PYRIDIN-7-YL)BENZAMIDE DERIVATIVES
-
Page/Page column 34-35, (2008/12/07)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.