385425-17-2

Upstream product

• 385425-15-0 1-(2-oxopiperidin-1-yl)-4-iodobenzene 
• 540-37-4 p-aminoiodobenzene 
• 385425-14-9 1-(4-iodophenyl)-4-(2,2,2-trifluoroacetyl)-piperidine-2,3-dione 
• 17672-26-3 3-cyanophenyl hydrazine 
• 4509-90-4 5-bromovaleroyl chloride 
• 536759-87-2 1-(4-iodophenyl)-3-(4-morpholinyl)-4-(trifluoroacetyl)-5,6-dihydro-2(1H)-pyridinone 
• 473927-69-4 1-(4-iodo-phenyl)-3-morpholin-4-yl-5,6-dihydro-1H-pyridin-2-one 
• 545445-10-1 3,3-dichloro-1-(4-iodophenyl)-piperidin-2-one 

Downstream Products

• 915306-36-4 3-[6-(2'-formyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl]-benzonitrile 
• 503613-07-8 3-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydropyrazolo[3,4-c]pyridin-1-yl}benzamide 
• 503612-98-4 N-methoxy-3-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzamidine 
• 503612-97-3 N-hydroxy-3-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydropyrazolo[3,4-c]pyridin-1-yl}benzamidine 
• 1217070-64-8 C₂₆H₂₂F₃N₇O 
• 915306-22-8 3-[6-(2'-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl]-benzonitrile 

Relevant academic research and scientific papers

Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties

The bicyclic dihydropyrazolopyridinone scaffold allowed for incorporation of multiple P1 moieties with subnanomolar binding affinities for blood coagulation factor Xa. The compound 3-[6-(2′-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoro-methyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-l-yl]-benzamide 6d shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability. Compound 6d was selected for further pre-clinical evaluations.

Heteroaryl- phenyl heterobicyclic factor Xa inhibitors

The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.