952194-68-2

Upstream product

• 53666-60-7 N¹,N¹-dimethyl-4-chloro-m-phenylenediamine 
• 50817-44-2 N-(4-chloro-3-nitrophenyl)-N,N-dimethylamine 
• 952194-66-0 N-(2-chloro-5-dimethylamino-phenyl)-3,4-dimethoxy-benzenesulfonamide 
• 952194-67-1 [(2-chloro-5-dimethylamino-phenyl)-(3,4-dimethoxy-benzenesulfonyl)-amino]-acetic acid tert-butyl ester 

Relevant academic research and scientific papers

NOVEL SULFONAMIDE COMPOUNDS

The invention relates to novel sulfonamide compounds and their use as orexin receptor antagonists.

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists

A series of dual OX1R/OX2R orexin antagonists was prepared based on a N-glycine-sulfonamide core. SAR studies of a screening hit led to compounds with low nanomolar affinity for both receptors and good oral bioavailability. One of these compounds, 47, has demonstrated in vivo activity in rats following oral administration.

NOVEL SULFONAMIDE COMPOUNDS

The invention relates to sulfonamide compounds of formula (I), where A, B, R3 and R4 are as defined in the claims, and their use as orexin receptor antagonists in the prevention and treatment of eating and drinking disorders, all types of sleep disorders, all kinds of cognitive dysfunctions in the healthy population and psychiatric and neurologic disorders. Formula (I).