5241. Israpafant

Nomenclature

CAS number: 117279-73-9
4-(2-Chlorophenyl)-6,9-dimethyl-2-[2-[4-(2-methylpropyl)phenyl]ethyl]-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine; (±)-4-(o-chlorophenyl)-2-(p-isobutylphenethyl)-6,9-dimethyl-6H-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine; Y-24180; Pafnol (Yoshitomi).
C28H29ClN4S; mol wt 489.07.
C 68.76%, H 5.98%, Cl 7.25%, N 11.46%, S 6.56%.

Description and references

Platelet activating factor (PAF) antagonist. Prepn: T. Tahara et al., EP 268242; eidem, US 4820703 (1988, 1989 both to Yoshitomi). Pharmacology: M. Terasawa et al., Prostaglandins 40, 553 (1990). Receptor binding study: S. Takehara et al., ibid. 571. Clinical evaluation in asthma: S. Hozawa et al., Am. J. Respir. Crit. Care Med. 152, 1198 (1995).

Chemical structure

Properties

Colorless crystals from isopropyl ether, mp 129.5-131.5°. Sol in propylene glycol.

Therapeutic Category

Antiasthmatic.

Keywords

Antiasthmatic (Nonbronchodilator); Platelet Activating Factor Antagonist