10216. Mitratapide

Nomenclature

CAS number: 179602-65-4
4-[4-[4-[4-[[(2S,4R)-2-(4-Chlorophenyl)-2-[[(4-methyl-4H-1,2,4-triazol-3-yl)thio]methyl]-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-[(1R)-1-methylpropyl]-3H-1,2,4-triazol-3-one; R-103757; Yarvitan (Janssen Animal Health).
C36H41ClN8O4S; mol wt 717.28.
C 60.28%, H 5.76%, Cl 4.94%, N 15.62%, O 8.92%, S 4.47%.

Description and references

Microsomal triglyceride transfer protein inhibitor; blocks the assembly and release of lipoprotein particles into the bloodstream. Prepn: J. Heeres et al., WO 9613499; eidem, US 5521186 (both 1996 to Janssen). Development of a bioavailable formulation: G. Verreck et al., J. Pharm. Sci. 93, 1217 (2004) DOI PubMed.

Chemical structure

Properties

mp 157°. pKa 4.1. Soly in water (mg/ml): <0.0005 (neutral pH); in 0.1 N HCl: 0.42. Log P (octanol/water): >5.

Therapeutic Category (Veterinary)

Canine antiobesity agent.