280118-23-2

Usage

Uses

Used in Pharmaceutical Industry:
BMS-740808 is used as a therapeutic agent for the treatment of neurological and psychiatric disorders such as schizophrenia, attention deficit hyperactivity disorder (ADHD), and cognitive deficits associated with aging. Its antagonistic action on the histamine H3 receptor helps in modulating the affected pathways and improving cognitive function and attention.
Used in Obesity Treatment:
BMS-740808 is used as a potential treatment for obesity due to its involvement in the regulation of appetite and metabolism through the histamine H3 receptor. Further research is needed to explore its therapeutic potential in managing obesity and related metabolic disorders.

Upstream product

• 161886-21-1 2-fluoro-5-hydrazinobenzonitrile 
• 540-37-4 p-aminoiodobenzene 
• 53312-81-5 3-cyano-4-fluoroaniline 
• 4509-90-4 5-bromovaleroyl chloride 
• 543745-12-6 1-(3-Cyano-4-fluoro)phenyl-3-trifluoromethyl-6-[4-(2-formyl)phenyl]phenyl-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one 
• 543745-11-5 1-(3-cyano-4-fluoro)phenyl-3-trifluoromethyl-6-(4-iodo)phenyl-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one 
• 385425-14-9 1-(4-iodophenyl)-4-(2,2,2-trifluoroacetyl)-piperidine-2,3-dione 
• 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 
• 385425-15-0 1-(2-oxopiperidin-1-yl)-4-iodobenzene 
• 546-88-3 acetylhydroxamic acid 

Relevant academic research and scientific papers

1-[3-Aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa

Attempts to further optimize the pyrazole factor Xa inhibitors centered on masking the aryl aniline P4 moiety. Scaffold optimization resulted in the identification of a novel bicyclic pyrazolo-pyridinone scaffold which retained fXa potency. The novel bicyclic scaffold preserved all binding interactions observed with the monocyclic counterpart and importantly the carboxamido moiety was integrated within the scaffold making it less susceptible to hydrolysis. These efforts led to the identification of 1-[3-aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one 6f (BMS-740808), a highly potent (fXa Ki = 30 pM) with a rapid onset of inhibition (2.7 × 107 M-1 s-1) in vitro, selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model, and orally bioavailable inhibitor of blood coagulation factor Xa.