1360552-08-4

Upstream product

• 402960-38-7 5-(4,4,5,5-tetramethyl[1,3,2]dioxaborolan-2-yl)pyrimidin-2-ylamine 
• 1360551-90-1 (R)-2-(4-bromo-phenyl)-2-cyclopropylpropionitrile 
• 6952-89-2 (4-bromophenyl)(cyclopropyl)methanone 
• 1360551-88-7 2-(4-bromo-phenyl)-2-cyclopropylpropionitrile 
• 56041-75-9 1-(4-bromophenyl)-1-cyclopropylethan-1-ol 

Downstream Products

• 1360552-61-9 2-{2-[4-(3-{(R)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-ethyl}-isoindole-1,3-dione 
• 1360549-37-6 5-(4-{(R)-1-cyclopropyl-1-[5-(1H-pyrazol-4-yl)-[1,2,4]oxadiazol-3-yl]ethyl}phenyl)pyrimidin-2-ylamine 
• 1360550-04-4 2-[4-(3-{(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl}-1,2,4-oxadiazol-5-yl)-1H-pyrazol-1-yl]-N,N-dimethylacetamide 
• 1360550-70-4 5-[4-((R)-1-cyclopropyl-1-{5-[1-(2-dimethylaminoethyl)-1H-pyrazol-4-yl]-[1,2,4]oxadiazol-3-yl}-ethyl)phenyl]pyrimidin-2-ylamine 
• 1360550-78-2 5-[4-((R)-1-{5-[1-(2-aminoethyl)-1H-pyrazol-4-yl]-[1,2,4]oxadiazol-3-yl}-1-cyclopropylethyl)phenyl]pyrimidin-2-ylamine 

Relevant academic research and scientific papers

Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: Discovery of 2-[4-(3-{(R)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]- N, N -dimethyl-acetamide (BI 665915)

The synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds that demonstrated excellent FLAP binding potency (IC50 4 synthesis in human whole blood (IC50 4 production.

OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION FOR COMBINATION THERAPY

The present invention relates to combination therapy using compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein and an additional pharmaceutically active agent. The invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations in the treatment of various diseases and disorders.

OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.