1380087-45-5

Upstream product

• 1380088-18-5 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-isoxazolo[5,4-c]thieno[2,3-e]azepin-6-yl)acetic acid 
• 1019115-42-4 methyl 2-bromo-4,5-dimethylthiophene-3-carboxylate 
• 43214-88-6 (3-methylisoxazol-5-yl)methyl acetate 
• 14559-13-8 methyl 4,5-dimethylthiophene-3-carboxylate 
• 1380089-34-8 (3-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isoxazol-5-yl)methyl acetate 
• 1448631-46-6 methyl 2-(5-(hydroxymethyl)-3-methylisoxazol-4-yl)-4,5-dimethylthiophene-3-carboxylate 
• 1380089-56-4 tert-butyl 2-((6S)-2,3,9-trimethyl-4-oxo-5,6-dihydro-4H-isoxazolo[5,4-c]thieno[2,3-e]azepin-6-yl)acetate 
• 1380089-74-6 tert-butyl 2-((6S)-4-chloro-2,3,9-trimethyl-6H-isoxazolo[5,4-c]thieno[2,3-e]azepin-6-yl)acetate 

Downstream Products

• 1380088-44-7 (6S)-6-((1H-imidazol-2-yl)methyl)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-isoxazolo[5,4-c]thieno[2,3-e]azepine 
• 1380089-76-8 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-isoxazolo[5,4-c]thieno[2,3-e]azepin-6-yl)ethanethioamide 

Relevant academic research and scientific papers

Discovery, design, and optimization of isoxazole azepine BET inhibitors

The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-based drug design effort lead to a novel isoxazole azepine scaffold. This scaffold showed good potency in biochemical and cellular assays and oral activity in an in vivo model of BET inhibition.

BROMODOMAIN INHIBITORS AND USES THEREOF

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.