1400686-74-9

Upstream product

• 1400689-72-6 4-((1R,3S)-3-amino-2,2,3-trimethylcyclopentylamino)-6-bromopyrrolo[1,2-b]-pyridazine-3-carboxamide 
• 1993-03-9 o-fluorophenylboronic acid 
• 1400580-11-1 6-bromo-4-chloropyrrolo[1,2-b]pyridazine-3-carboxamide 
• 1400580-14-4 6-bromo-4-chloropyrrolo[1,2-b]pyridazine-3-carbonitrile 
• 1400580-13-3 6-bromo-4-hydroxypyrrolo[1,2-b]pyridazine-3-carbonitrile 

Relevant academic research and scientific papers

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors

A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 while maintaining good selectivity against JAK2 and Tyk2. Translation to in vivo efficacy was observed in a murine model of chronic inflammation. X-ray co-crystal structure determination confirmed the presumed inhibitor binding orientation in JAK3. Efforts to reduce hERG channel inhibition will be described.

PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES

Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.