1160848-89-4

Upstream product

• 1160848-88-3 4-hydroxy-5-iodo-6-methylnicotinamide 
• 1073160-08-3 4-hydroxy-6-methylnicotinamide 
• 67367-33-3 4-hydroxy-6-methylnicotinic acid 
• 1160848-88-3 5-iodo-6-methyl-4-oxo-1,4-dihydropyridine-3-carboxamide 

Downstream Products

• 1436405-39-8 4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-6-methyl-5-vinylnicotinonitrile 
• 1436405-41-2 4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-6-methyl-5-(2-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)furan-2-yl)vinyl)nicotinonitrile 
• 1436405-38-7 4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-5-iodo-6-methylnicotinonitrile 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors

36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure-activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an IC50 value of 45 nM to EGFR kinase. Several compounds of other series also show IC50 values 1 μM for EGFR and 5 μM for A-549 and HL60 cells growth inhibition.

INDOLE-SUBSTITUTED 3-CYANOPYRIDINES AS KINASE INHIBITORS

Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is -O-, -N(R3)-, -S-, -S(O)- or -S(O)2-; R2 is a C1-4 alkyl group or -CF3; and R1, R3, R4 and p are as defined herein; wherein the compounds are useful as kinase inhibitors. Also disclosed are pharmaceutical compositions containing, and intermediate compounds and methods for making the compounds of formula (I) and their pharmaceutically acceptable salts; and methods of using the foregoing to treat inflammatory and autoimmune diseases such as asthma, colitis, multiple sclerosis, psoriasis, arthritis, rheumatoid arthritis, inflammatory bowel disease, and joint inflammation.

5-ALKYL/ALKENYL-3-CYANOPYRIDINES AS KINASE INHIBITORS

Described herein are compounds of formula I: wherein G is and pharmaceutically acceptable salts thereof, wherein J, X, R1, R2, R11, R12' and p are as defined herein. Also provided herein are methods of making the compounds of formula I, and methods of using these compounds for inhibiting or treating a pathological condition or disorder linked to or mediated by a protein kinase in a mammal.