1027785-06-3

Upstream product

• 1204435-57-3 6-amino-5-(phenylethynyl)-3-pyridinecarbonitrile 
• 850429-51-5 6-amino-5-bromonicotinic acid ethyl ester 
• 536-74-3 phenylacetylene 
• 180340-70-9 methyl 6-amino-5-bromopyridine-3-carboxylate 
• 1027785-04-1 ethyl 6-amino-5-(phenylethynyl)nicotinate 

Downstream Products

• 1027785-48-3 methyl 3-(2-phenyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamido)benzoate 
• 1027785-07-4 (2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)methanol 
• 1616385-54-6 N-(4,5-dimethyl-1H-pyrazol-3-yl)-2-phenyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide 

Relevant academic research and scientific papers

Identification of lead small molecule inhibitors of glycogen synthase kinase-3 beta using a fragment-linking strategy

Glycogen synthase kinase-3 beta (GSK3β) kinase serves as a promising therapeutic target for the treatment of various human diseases, such as diabetes, obesity, and Alzheimer's disease. In this study, we report lead GSK3β inhibitors identified using a fragment-linking strategy. Through the systematic exploration, a six-atom chain unit bearing the rigid double bond was found to be a suitable linker connecting two fragments, which enables favorable contacts with backbone groups of residues in the pockets. As a consequence, potent GSK3β inhibitor 9i was found with IC50values of 19 nM. The binding mode analysis indicates that the activities of the inhibitors appear to be achieved by the establishment of multiple hydrogen bonds and hydrophobic interactions in the ATP-binding site of GSK3β. The good biochemical potencies and structural uniqueness of the inhibitors support consideration in the further study to optimize the biological activity.

COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR

Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.

Microwave-assisted synthesis of indole- and azaindole-derivatives in water via cycloisomerization of 2-alkynylanilines and alkynylpyridinamines promoted by amines or catalytic amounts of neutral or basic salts

An efficient methodology is described and exploited for the preparation of differently substituted indoles and azaindoles via microwave-assisted cycloisomerization in water of 2-alkynylanilines and alkynylpyridinamines, which is promoted by catalytic amounts of neutral or basic salts or by stoichiometric weak organic bases. Good to high yields in the cyclization can be achieved for a variety of 2-amino(hetero)aryl alkynes. Reactions are run without any added metal catalyst. A comparison with the cycloisomerization conducted under conventional heating is also described. An efficient methodology is described for the preparation of differently substituted 1H-indoles and 1H-azaindoles via microwave-assisted cycloisomerization in water of 2-alkynylanilines and alkynylpyridinamines, promoted by catalytic amounts of neutral or basic salts or by weak organic bases.

NOVEL KINASE INHIBITORS

The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1 and IGFR-1, thereby making them usefu