1220517-76-9

Upstream product

• 90213-66-4 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine 
• 98-59-9 p-toluenesulfonyl chloride 
• 934524-10-4 2,4-dichloro-7-p-methylbenzenesulfonyl-7H-pyrrole[2,3-d]pyrimidin-4-amine 
• 89088-69-7 1-methyl-1H-imidazole-4-amine hydrochloride 
• 79578-98-6 1-methyl-1H-imidazol-4-amine 

Downstream Products

• 1220516-46-0 N₂-[1-(5-fluoropyrimidin-2-yl)ethyl]-N₄-(1-methyl-1H-imidazol-4-yl)-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine 
• 1220517-13-4 N₂-[1-(3,5-difluoropyridin-2-yl)ethyl]-N₄-(1-methyl-1H-imidazol-4-yl)-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine 

Relevant academic research and scientific papers

Discovery of 1-methyl-1 H-imidazole derivatives as potent Jak2 inhibitors

Structure based design, synthesis, and biological evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clinical candidate AZD1480 (24), optimization of the series led to the discovery of compound 19a, a potent, orally bioavailable Jak2 inhibitor. Compound 19a displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound 19a demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range.

HETEROCYCLIC JAK KINASE INHIBITORS

The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer